Compounds > thiazoles
Page last updated: 2024-08-21

thiazoles and alpha-aminopyridine

thiazoles has been researched along with alpha-aminopyridine in 75 studies

Research

Studies (75)

TimeframeStudies, this research(%)All Research%
pre-19901 (1.33)18.7374
1990's0 (0.00)18.2507
2000's10 (13.33)29.6817
2010's49 (65.33)24.3611
2020's15 (20.00)2.80

Authors

AuthorsStudies
Hösli, E; Hösli, L; Schneider, U; Wiget, W1
Andrews, RC; Beaudet, EJ; Becherer, JD; Brodie, TA; Gaul, MD; Hamilton, G; Hoivik, DJ; Jolley, S; Kliewer, S; Laethem, R; LeCluyse, EL; Lehmann, J; McDougald, DL; Mellon-Kusibab, K; Moore, L; Novick, S; Tippin, TK; Zhao, Z1
Adell, A; Amargós-Bosch, M; Artigas, F; Bortolozzi, A; Díaz-Mataix, L; Pons, S; Serrats, J1
Balitza, AE; Bilodeau, MT; Buser-Doepner, C; Coll, KE; Fernandes, C; Gibbs, JB; Hartman, GD; Heimbrook, DC; Huckle, WR; Koester, TJ; Kohl, N; Lynch, JJ; Manley, PJ; Mao, X; McFall, RC; McLoughlin, D; Miller-Stein, CM; Rickert, KW; Rodman, LD; Sepp-Lorenzino, L; Shipman, JM; Subramanian, R; Thomas, KA; Wong, BK; Yu, S1
Cosi, C; Newman-Tancredi, A; Rollet, K; Tesori, V; Waget, A1
Barrish, JC; Bhide, RS; Borzilleri, RM; D'Arienzo, CJ; Derbin, GM; Fargnoli, J; Hunt, JT; Jeyaseelan, R; Kamath, A; Kukral, DW; Lombardo, LJ; Marathe, P; Mortillo, S; Qian, L; Tokarski, JS; Wautlet, BS; Zheng, X1
Draeger, G; Hey-Hawkins, E; Jashari, A; Mikhova, B; Popovski, E1
Binder, M; Boissin, P; Buettelmann, B; Ceccarelli, SM; Hanlon, S; Jaeschke, G; Kolczewski, S; Kupfer, E; Peters, JU; Porter, RH; Prinssen, EP; Rueher, M; Ruf, I; Schlotterbeck, G; Spooren, W; Stämpfli, A; Vieira, E1
Elzein, E; Zablocki, J1
Farde, L; Jeppsson, F; Johnson, AE; Juréus, A; Neelissen, JA; Norman, H; Sandell, J; Ström, P; Svensson, SP; Wensbo, D1
Ando, M; Ito, S; Kameda, M; Kawamoto, H; Kobayashi, K; Nakama, C; Ozaki, S; Sato, N; Suzuki, T; Tani, T; Tokita, S1
Bissantz, C; Kratzeisen, C; Malherbe, P; Marcuz, A; Roche, O; Wettstein, JG1
Boitano, S; Flynn, AN; Hoffman, J; Price, TJ; Schulz, SM; Vagner, J1
Hussar, DA2
Agrawal, R; Bednarkiewicz, Z; Czarnecka, D; Gaszewska-Żurek, E; Jankowska, E; Kawecka-Jaszcz, K; Krzemińska-Pakuła, M; Ochan Kilama, M; Parma, Z; Ponikowski, P; Sosnowski, M; Tendera, M1
Koutentis, PA; Koyioni, M; Michaelidou, SS1
Jung, SH; Ryu, WS; Sun, X; Yang, BS1
Chibale, K; Gordon, R; Paquet, T; Waterson, D; Witty, MJ1
Bazer, FW; Dorniak, P; Spencer, TE; Welsh, TH1
Andersson, J; Cselényi, Z; Eriksdotter, M; Farde, L; Forsberg, A; Freund-Levi, Y; Halldin, C; Jeppsson, F; Johnström, P; Julin, P; Juréus, A; Sandell, J; Schou, M; Svensson, S; Swahn, BM; Varnäs, K1
Albrecht-Küpper, BE; Diedrichs, N; Gupta, RC; Kohli, S; Rastogi, S; Sabbah, HN; Wang, M; Zhang, K; Zimmermann, K1
Chang, M; Hua, J; Huang, CS; Lam, PY; Lloyd, J; Pi, Z; Price, L; Rehfuss, R; Sutton, J; Wexler, RR; Wu, Q; Zheng, J1
Aicher, TD; Boyd, SA; Chicarelli, MJ; Condroski, KR; DeWolf, WE; Hinklin, RJ; Lee, PA; Lee, W; Singh, A; Thomas, L; Voegtli, WC; Williams, L1
Aoki, I; Chang, Q; Furumoto, S; Higuchi, M; Ito, H; Iwata, N; Jang, MK; Ji, B; Kudo, Y; Lee, VM; Lewis, J; Maeda, J; Maruyama, M; Masamoto, K; Okamura, N; Ono, M; Sahara, N; Saido, TC; Shimada, H; Shinotoh, H; Suhara, T; Takano, H; Takashima, A; Trojanowski, JQ; Zhang, MR1
Fan, L; Han, TT; Li, JY; Xu, W1
Antonakos, B; Cooke, VG; Danial, NN; Flemming, D; Hurov, KE; Jones, MD; Korn, JM; Ledell, J; Lehár, J; Mishina, Y; Schoumacher, M; Sellers, WR; Shao, W; Sonkin, D; Steiger, J; Stump, MD; Yan-Neale, Y1
Arban, R; Cavallini, P; Davies, CH; Davis, TG; Gray, FA; Montanari, D; Negri, M; Poffe, A; Rutter, AR; Schneck, J; Vicentini, E; Wren, PB1
Becq, F; Boinot, C; Ferru-Clément, R; Jollivet Souchet, M1
Song, SD; Tang, HF1
Abramson, V; Arteaga, CL; Balko, JM; Estrada, MV; Fox, EM; Garrett, JT; González-Angulo, AM; Kelley, MC; Kuba, MG; Mayer, IA; Meszoely, IM; Mills, GB; Red-Brewer, M; Rizzo, M; Schwarz, LJ1
Galanis, A; Levis, M1
Li, D; Lin, J; Liu, P; Wang, Z; Xu, J1
Alfieri, RR; Ardizzoni, A; Bonelli, MA; Caffarra, C; Cavazzoni, A; Cretella, D; Falco, A; Frati, C; Fumarola, C; Galetti, M; La Monica, S; Lagrasta, CA; Madeddu, D; Petronini, PG; Quaini, F; Rossetti, P; Saccani, F; Tiseo, M1
Guo, D; Heitman, LH; IJzerman, AP; Lenselink, EB; Louvel, J; Mocking, TA; Mulder-Krieger, T; Soethoudt, M1
Ågren, H; Kuang, G; Murugan, NA; Nordberg, A; Tu, Y1
Ashino, H; Bando, K; Chen, CJ; Farde, L; Higuchi, M; Ji, B; Kasahara, H; Minamizawa, T; Ono, M; Sano, H; Seki, C; Shiraishi, H; Suhara, T; Yamada, K; Zhang, MR1
Beekman, JM; de Winter-de Groot, KM; Dekkers, JF; Gogorza Gondra, RA; Janssens, HM; Kruisselbrink, E; van der Ent, CK; Vonk, AM1
Bali, V; Bebok, Z; Guroji, P; Lazrak, A; Matalon, S1
Jacobsen, EN; Kennedy, CR; Lin, S1
Liu, P; Xu, B; Zhang, C1
Albrecht-Küpper, B; Dinh, W; Gheorghiade, M; Sabbah, HN; van der Laan, M; Voors, AA1
Bonazzi, VF; Cummings, MC; Geng, X; Ju, RJ; Mahon, CE; Packer, LM; Pollock, PM; Stephenson, SA1
Hata, T; Iwasaki, H; Kato, T; Kobayashi, H; Matsuo, A; Matsushita, M; Miyagawa, N1
Furumoto, S; Gonda, K; Ibaraki, M; Ishikawa, Y; Iwata, R; Matsubara, K; Okamura, N; Oyama, S; Shidahara, M; Tashiro, M; Thomas, BA; Watabe, H; Watanuki, S; Yanai, K1
Chen, B; Kraus, D; Palasuberniam, P1
Chen, IC; Cheng, AL; Hsiao, LP; Huang, IW; Lin, CH; Lu, YS; Wei-Wu Chen, T; Yeh, LC; Yu, HC1
Park, KB; Weon, H1
Hata, T; Iwasaki, H; Kato, T; Kobayashi, H; Matsuo, A; Matsushita, M; Ohta, T2
Arkel, M; Cichero, E; Damonte, G; Fossa, P; Galietta, LJV; Liessi, N; Millo, E; Paccagnella, M; Pedemonte, N; Pesce, E; Salis, A; Tasso, B; Tomati, V1
Bear, CE; Casavola, V; Laselva, O; Molinski, S1
Arai, H; Funaki, Y; Furukawa, K; Furumoto, S; Harada, R; Hiraoka, K; Ishikawa, Y; Ishiki, A; Iwata, R; Kai, H; Kitamoto, T; Kudo, Y; Okamura, N; Sasano, H; Sato, N; Tashiro, M; Tomita, N; Totsune, T; Watanuki, S; Yanai, K1
Bormans, G; Bruffaerts, R; Dries, E; Dupont, P; Evenepoel, C; Gabel, S; Koole, M; Liuzzi, AG; Meersmans, K; Peeters, R; Pijnenburg, Y; Schaeverbeke, J; Sieben, A; Van Bouwel, K; Van Laere, K; Vandenberghe, R1
Auriemma, RS; Cappabianca, P; Cavallo, LM; Colao, A; De Martino, MC; Di Cera, M; Frio, F; Grasso, LFS; Patalano, R; Pivonello, C; Pivonello, R; Solari, D; Vitulli, F1
Arai, H; Hayashi, H; Ishiki, A; Kawakatsu, S; Kobayashi, R; Okamura, N; Otani, K1
Nai, YH; Okamura, N; Tashiro, M; Watabe, H; Watanuki, S1
Han, ES; Mortimer, J; Wen, W; Xing, Q; Yan, J; Yim, JH; Yost, SE; Yuan, Y1
Al-Horani, RA; Clemons Bankston, P1
Cooper, SL; Hill, SJ; Jörg, M; March, J; Sabbatini, AR; Scammells, PJ; Woolard, J1
Amico, G; Baroni, D; Brandas, C; Moran, O1
Fortescue, R; Janjua, S; Poole, P1
Inkielewicz-Stępniak, I; Kowalski, S; Sikorski, A; Tesmar, A1
Chang, YC; Chao, TY; Chen, SC; Chitapanarux, I; Gao, M; Jung, KH; Kim, JH; Lee, KS; Liu, CT; Lu, YS; Park, YH; Shotelersuk, K; Slader, C; Sohn, J; Tseng, LM; Valenti, R; Yang, Y1
Abdelhady, AM; Bachelot, T; Calvo, E; Fasolo, A; Forero-Torres, A; Hamilton, E; Im, YH; Lee, SC; Lu, YS; Maur, M; Nardi, L; Ruan, S; Stammberger, U; Tiedt, R; Tolaney, SM1
Clark, AS; DeMichele, A; Makhlin, I1
Jian, L; Lian, S; Liu, M; Liu, N; Wang, S; Zhang, G; Zhang, Y; Zhao, Q1
Chen, JH; Chuang, FC; Hwang, TZ; Su, YC; Wang, CC; Yeh, SA1
Ali, T; Imran, M; Li, JB; Li, S; Nadeem, H; Naz, S; Sarwar, S; Shah, FA; Tan, Z1
Benedet, A; Bunai, T; Kang, MSP; Lussier, F; Matsudaira, T; Obi, T; Ouchi, Y; Pascoal, TA; Rosa-Neto, P; Savard, M; Terada, T; Therriault, J; Tissot, C; Tsukada, H; Wang, YT1
Allegra, A; Caserta, S; Innao, V; Musolino, C; Zaccuri, AM1
Ferrera, VP; Foltin, RW; Grassetti, A; Martinez, D; Salling, MC1
Balbin, A; Cresta, S; Crystal, A; Curigliano, G; De Vita, S; Duhoux, FP; He, W; Huober, J; Jhaveri, K; Ji, Y; Juric, D; Kundamal, N; Layman, RM; Sheng, Q; Takahashi, S; Terret, C; Yap, YS1
Baroni, D; Brandas, C; Cichero, E; Ludovico, A; Millo, E; Moran, O; Parodi, A1
Arahata, Y; Bundo, M; Ikenuma, H; Ito, K; Iwata, K; Kato, T; Kimura, Y; Nakamura, A; Nihashi, T; Okamura, N; Sakurai, K; Sakurai, T; Suzuki, K; Takeda, A; Washimi, Y; Yamaoka, A; Yanai, K1

Reviews

10 review(s) available for thiazoles and alpha-aminopyridine

ArticleYear
A1 adenosine receptor agonists and their potential therapeutic applications.
    Expert opinion on investigational drugs, 2008, Volume: 17, Issue:12

    Topics: Adenosine A1 Receptor Agonists; Aminopyridines; Angina Pectoris; Animals; Anti-Arrhythmia Agents; Humans; Insulin; Pain; Receptor, Adenosine A1; Thiazoles

2008
Role of chemokines and their receptors in chronic lymphocytic leukemia: function in microenvironment and targeted therapy.
    Cancer biology & therapy, 2014, Volume: 15, Issue:1

    Topics: Aminopyridines; Antineoplastic Agents; Benzylamines; Chemokine CXCL12; Clinical Trials as Topic; Cyclams; Dasatinib; Heterocyclic Compounds; Humans; Lenalidomide; Leukemia, Lymphocytic, Chronic, B-Cell; Molecular Targeted Therapy; Morpholines; Niacinamide; Oxazines; Phenylurea Compounds; Protein Kinase Inhibitors; Purines; Pyridines; Pyrimidines; Quinazolinones; Receptors, CXCR4; Sorafenib; Thalidomide; Thiazoles; Tumor Microenvironment

2014
[Progress in PDE4 targeted therapy for inflammatory diseases].
    Zhejiang da xue xue bao. Yi xue ban = Journal of Zhejiang University. Medical sciences, 2014, Volume: 43, Issue:3

    Topics: Aminopyridines; Aminoquinolines; Arthritis; Asthma; Benzamides; Cyclopropanes; Dermatitis; Humans; Inflammation; Inflammatory Bowel Diseases; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Sulfones; Thalidomide; Thiazoles

2014
The Cation-π Interaction in Small-Molecule Catalysis.
    Angewandte Chemie (International ed. in English), 2016, 10-04, Volume: 55, Issue:41

    Topics: Aminopyridines; Catalysis; Cations; Cycloaddition Reaction; Guanidine; Hydrogen Bonding; Lewis Acids; Quantum Theory; Small Molecule Libraries; Thiazoles

2016
Partial Adenosine A1 Agonist in Heart Failure.
    Handbook of experimental pharmacology, 2017, Volume: 243

    Topics: Adenosine; Adenosine A1 Receptor Agonists; Aminopyridines; Angina Pectoris; Animals; Anti-Arrhythmia Agents; Coronary Artery Disease; Diabetes Mellitus; Dipeptides; Drug Partial Agonism; Furans; Heart; Heart Failure; Humans; Insulin Resistance; Ischemic Preconditioning, Myocardial; Lipolysis; Mitochondria, Heart; Myocardium; Oxygen Consumption; Pyridines; Renal Insufficiency; Tachycardia, Supraventricular; Thiazoles

2017
[
    BMC neurology, 2018, Aug-08, Volume: 18, Issue:1

    Topics: Aged; Aminopyridines; Aniline Compounds; Aphasia, Primary Progressive; Atrophy; Humans; Magnetic Resonance Imaging; Male; Middle Aged; Organotechnetium Compounds; Positron-Emission Tomography; Quinolines; Semantics; Temporal Lobe; Thiazoles; Tomography, Emission-Computed, Single-Photon

2018
New Small Molecule Drugs for Thrombocytopenia: Chemical, Pharmacological, and Therapeutic Use Considerations.
    International journal of molecular sciences, 2019, Jun-20, Volume: 20, Issue:12

    Topics: Aminopyridines; Animals; Cinnamates; Drug Development; Humans; Morpholines; Oxazines; Pyridines; Pyrimidines; Receptors, Thrombopoietin; Small Molecule Libraries; Syk Kinase; Thiazoles; Thiophenes; Thrombocytopenia

2019
Phosphodiesterase-4 inhibitors for chronic obstructive pulmonary disease.
    The Cochrane database of systematic reviews, 2020, 05-01, Volume: 5

    Topics: Administration, Oral; Aminopyridines; Benzamides; Cyclohexanecarboxylic Acids; Cyclopropanes; Diarrhea; Disease Progression; Forced Expiratory Volume; Humans; Middle Aged; Nitriles; Peak Expiratory Flow Rate; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Quality of Life; Randomized Controlled Trials as Topic; Thiazoles; Vital Capacity

2020
Which Is the Most Appropriate PI3K Inhibitor for Breast Cancer Patients with or without PIK3CA Status Mutant? A Systematic Review and Network Meta-Analysis.
    BioMed research international, 2020, Volume: 2020

    Topics: Aminopyridines; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Class I Phosphatidylinositol 3-Kinases; Clinical Trials as Topic; Female; Humans; Morpholines; Mutation; Network Meta-Analysis; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Progression-Free Survival; Signal Transduction; Thiazoles; Treatment Outcome

2020
Immune thrombocytopenia: options and new perspectives.
    Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis, 2021, Oct-01, Volume: 32, Issue:7

    Topics: Aminopyridines; Antibodies, Monoclonal, Humanized; COVID-19; Histocompatibility Antigens Class I; Humans; Immunosuppressive Agents; Morpholines; Protein Kinase Inhibitors; Purpura, Thrombocytopenic, Idiopathic; Pyrimidines; Receptors, Fc; Receptors, Thrombopoietin; SARS-CoV-2; Syk Kinase; Thiazoles; Thiophenes

2021

Trials

2 trial(s) available for thiazoles and alpha-aminopyridine

ArticleYear
The new oral adenosine A1 receptor agonist capadenoson in male patients with stable angina.
    Clinical research in cardiology : official journal of the German Cardiac Society, 2012, Volume: 101, Issue:7

    Topics: Adenosine A1 Receptor Agonists; Administration, Oral; Adult; Aged; Aminopyridines; Analysis of Variance; Angina, Stable; Dose-Response Relationship, Drug; Double-Blind Method; Exercise Test; Exercise Tolerance; Heart Rate; Humans; Male; Middle Aged; Poland; Receptor, Adenosine A1; Sex Factors; Thiazoles; Time Factors; Treatment Outcome

2012
LYN-activating mutations mediate antiestrogen resistance in estrogen receptor-positive breast cancer.
    The Journal of clinical investigation, 2014, Volume: 124, Issue:12

    Topics: Amino Acid Substitution; Aminopyridines; Animals; Breast Neoplasms; Dasatinib; Drug Resistance, Neoplasm; Drug Synergism; Estrogen Receptor Modulators; Female; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Humans; Mice; Mice, Nude; Morpholines; Mutation, Missense; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Phosphorylation; Protein Kinase Inhibitors; Pyrimidines; Receptors, Estrogen; src Homology Domains; src-Family Kinases; Thiazoles; Xenograft Model Antitumor Assays

2014

Other Studies

63 other study(ies) available for thiazoles and alpha-aminopyridine

ArticleYear
Evidence for the existence of histamine H1- and H2-receptors on astrocytes of cultured rat central nervous system.
    Neuroscience letters, 1984, Aug-10, Volume: 48, Issue:3

    Topics: Aminopyridines; Animals; Astrocytes; Brain Stem; Cells, Cultured; Cimetidine; Histamine; Histamine H1 Antagonists; Membrane Potentials; Pyrilamine; Rats; Receptors, Histamine; Receptors, Histamine H1; Receptors, Histamine H2; Spinal Cord; Thiazoles

1984
CYP3A induction by N-hydroxyformamide tumor necrosis factor-alpha converting enzyme/matrix metalloproteinase inhibitors use of a pregname X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans.
    Drug metabolism and disposition: the biological fate of chemicals, 2003, Volume: 31, Issue:7

    Topics: ADAM Proteins; ADAM17 Protein; Administration, Oral; Amides; Aminopyridines; Animals; Aryl Hydrocarbon Hydroxylases; Cell Culture Techniques; Cytochrome P-450 CYP3A; Dipeptides; Dose-Response Relationship, Drug; Drug Evaluation; Drug Evaluation, Preclinical; Enzyme Induction; Formamides; Hepatocytes; Humans; Male; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Metalloendopeptidases; Oxidoreductases, N-Demethylating; Pregnane X Receptor; Rats; Rats, Wistar; Receptors, Cytoplasmic and Nuclear; Receptors, Steroid; Thiazoles

2003
In vivo modulation of 5-hydroxytryptamine release in mouse prefrontal cortex by local 5-HT(2A) receptors: effect of antipsychotic drugs.
    The European journal of neuroscience, 2003, Volume: 18, Issue:5

    Topics: alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Aminopyridines; Anesthetics, Local; Animals; Antipsychotic Agents; Benzopyrans; Blotting, Western; Dizocilpine Maleate; Dose-Response Relationship, Drug; Drug Interactions; Excitatory Amino Acid Antagonists; Fluorobenzenes; Immunohistochemistry; In Situ Hybridization; Indoles; Indophenol; Male; Mice; Mice, Inbred C57BL; Microdialysis; Piperidines; Prazosin; Prefrontal Cortex; Quinoxalines; Receptor, Serotonin, 5-HT2A; Receptors, Serotonin; RNA, Messenger; Serotonin; Serotonin Antagonists; Serotonin Receptor Agonists; Tetrodotoxin; Thiazoles; Time Factors

2003
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
    Journal of medicinal chemistry, 2004, Dec-02, Volume: 47, Issue:25

    Topics: Administration, Oral; Aminopyridines; Animals; Biological Availability; Cell Line; Dogs; Electrocardiography; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; In Vitro Techniques; Lung; Macaca mulatta; Male; Mice; Microsomes, Liver; Phosphorylation; Potassium Channels, Voltage-Gated; Pyridines; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Vascular Endothelial Growth Factor; Thiazoles; Tissue Distribution; Vascular Endothelial Growth Factor Receptor-2

2004
Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation.
    Brain research, 2005, May-10, Volume: 1043, Issue:1-2

    Topics: Aminopyridines; Animals; Antipsychotic Agents; Aripiprazole; Clozapine; Corpus Striatum; Disease Models, Animal; Excitatory Amino Acid Agonists; Haloperidol; Kainic Acid; Male; Mice; Mice, Inbred C57BL; Piperazines; Piperidines; Pyridines; Quinolones; Receptor, Serotonin, 5-HT1A; Schizophrenia; Serotonin 5-HT1 Receptor Agonists; Serotonin Antagonists; Thiazoles

2005
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
    Journal of medicinal chemistry, 2006, Jun-29, Volume: 49, Issue:13

    Topics: Administration, Oral; Aminopyridines; Angiogenesis Inhibitors; Animals; Binding Sites; Cell Proliferation; Endothelial Cells; Endothelium, Vascular; Humans; In Vitro Techniques; Macaca fascicularis; Mice; Mice, Nude; Models, Molecular; Rats; Structure-Activity Relationship; Thiazoles; Umbilical Veins; Vascular Endothelial Growth Factor Receptor-2; Xenograft Model Antitumor Assays

2006
An improved synthesis of 4-chlorocoumarin-3-sulfonyl chloride and its reactions with different bidentate nucleophiles to give pyrido[1',2':2,3]- and thiazino[3',2':2,3]-1,2,4-thiadiazino[6,5-c]benzopyran-6-one 7,7-dioxides.
    Molecules (Basel, Switzerland), 2007, Aug-22, Volume: 12, Issue:8

    Topics: Aminopyridines; Anti-HIV Agents; Antineoplastic Agents; Benzopyrans; Coumarins; Sulfones; Thiazoles

2007
Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series.
    ChemMedChem, 2008, Volume: 3, Issue:1

    Topics: Allosteric Regulation; Aminopyridines; Chromatography, High Pressure Liquid; Humans; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mass Spectrometry; Microsomes, Liver; Oxidation-Reduction; Pharmaceutical Preparations; Receptor, Metabotropic Glutamate 5; Receptors, Metabotropic Glutamate; Solid Phase Extraction; Stereoisomerism; Thiazoles

2008
AZD2184: a radioligand for sensitive detection of beta-amyloid deposits.
    Journal of neurochemistry, 2009, Volume: 108, Issue:5

    Topics: Alzheimer Disease; Aminopyridines; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Aniline Compounds; Animals; Autoradiography; Benzothiazoles; Brain; Carbon Radioisotopes; Competitive Bidding; Humans; Male; Mice; Mice, Transgenic; Mutation; Plaque, Amyloid; Positron-Emission Tomography; Presenilin-1; Protein Binding; Radioligand Assay; Rats; Rats, Sprague-Dawley; Thiazoles; Tritium

2009
Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
    Bioorganic & medicinal chemistry letters, 2009, Sep-01, Volume: 19, Issue:17

    Topics: 4-Aminopyridine; Aminopyridines; Animals; Cell Line; CHO Cells; Cricetinae; Cricetulus; Humans; Positron-Emission Tomography; Receptors, Neuropeptide Y; Recombinant Proteins; Structure-Activity Relationship; Thiazoles

2009
Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-py
    Molecular pharmacology, 2010, Volume: 78, Issue:1

    Topics: Acetamides; Amino Acid Sequence; Aminopyridines; Binding Sites; Cell Line; Humans; Isoquinolines; Molecular Sequence Data; Mutagenesis, Site-Directed; Orexin Receptors; Pyrrolidines; Radioligand Assay; Receptors, G-Protein-Coupled; Receptors, Neuropeptide; Sequence Homology, Amino Acid; Sulfonamides; Thiazoles

2010
Potent agonists of the protease activated receptor 2 (PAR2).
    Journal of medicinal chemistry, 2011, Mar-10, Volume: 54, Issue:5

    Topics: Aminopyridines; Calcium; Cells, Cultured; Epithelial Cells; Humans; Oligopeptides; Peptidomimetics; Receptor, PAR-2; Signal Transduction; Structure-Activity Relationship; Thiazoles

2011
New drugs 2012 part I.
    Nursing, 2012, Volume: 42, Issue:3

    Topics: Aminopyridines; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Benzamides; Benzazepines; Benzimidazoles; Benzofurans; Ceftaroline; Cephalosporins; Cyclopropanes; Drug Approval; Drug Combinations; Humans; Imidazoles; Indoles; Isoindoles; Linagliptin; Lurasidone Hydrochloride; Macrolides; Oxadiazoles; Piperazines; Proline; Purines; Quinazolines; Thiazoles; United States; Vilazodone Hydrochloride

2012
Synthesis of [(4-chloro-5H-1,2,3-dithiazol-5-ylidene)amino]azines.
    Molecules (Basel, Switzerland), 2011, Volume: 16, Issue:11

    Topics: Aminopyridines; Chemical Phenomena; Hydrazines; Molecular Structure; Temperature; Thiazoles

2011
Topical administration of the pan-Src kinase inhibitors, dasatinib and LCB 03-0110, prevents allergic contact dermatitis in mice.
    The British journal of dermatology, 2013, Volume: 168, Issue:1

    Topics: Adjuvants, Immunologic; Administration, Cutaneous; Aminopyridines; Animals; Anti-Inflammatory Agents; Atrophy; Dasatinib; Dermatitis, Allergic Contact; Drug Evaluation; Female; Mice; Mice, Hairless; Mice, Inbred BALB C; Oxazolone; Protein Kinase Inhibitors; Pyrimidines; Skin; Thiazoles; Thiophenes

2013
Antimalarial aminothiazoles and aminopyridines from phenotypic whole-cell screening of a SoftFocus(®) library.
    Future medicinal chemistry, 2012, Volume: 4, Issue:18

    Topics: Aminopyridines; Animals; Antimalarials; Databases, Pharmaceutical; Drug Resistance; Humans; Malaria, Falciparum; Parasitic Sensitivity Tests; Plasmodium falciparum; Structure-Activity Relationship; Thiazoles

2012
Cortisol and interferon tau regulation of endometrial function and conceptus development in female sheep.
    Endocrinology, 2013, Volume: 154, Issue:2

    Topics: 11-beta-Hydroxysteroid Dehydrogenases; Aminopyridines; Animals; Cyclooxygenase 2; Embryo Implantation; Female; Fetal Development; Hydrocortisone; Interferon Type I; Meloxicam; Pregnancy; Pregnancy Proteins; Sheep, Domestic; Sulfonamides; Thiazines; Thiazoles

2013
Low background and high contrast PET imaging of amyloid-β with [11C]AZD2995 and [11C]AZD2184 in Alzheimer's disease patients.
    European journal of nuclear medicine and molecular imaging, 2013, Volume: 40, Issue:4

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Aminopyridines; Amyloid beta-Peptides; Aniline Compounds; Animals; Benzothiazoles; Benzoxazoles; Binding Sites; Brain; Carbon Radioisotopes; Case-Control Studies; Female; Humans; Magnetic Resonance Imaging; Male; Mice; Mice, Transgenic; Middle Aged; Positron-Emission Tomography; Protein Binding; Radioligand Assay; Radiopharmaceuticals; Sensitivity and Specificity; Thiazoles

2013
Chronic therapy with a partial adenosine A1-receptor agonist improves left ventricular function and remodeling in dogs with advanced heart failure.
    Circulation. Heart failure, 2013, Volume: 6, Issue:3

    Topics: Adenosine A1 Receptor Agonists; Aminopyridines; Animals; Dogs; Echocardiography, Doppler; Heart Failure; Hemodynamics; Stroke Volume; Thiazoles; Ventricular Function, Left; Ventricular Pressure; Ventricular Remodeling

2013
2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.
    Bioorganic & medicinal chemistry letters, 2013, Jul-15, Volume: 23, Issue:14

    Topics: Aminopyridines; Animals; Blood Platelets; Half-Life; Platelet Aggregation; Platelet Aggregation Inhibitors; Protein Binding; Purinergic P2Y Receptor Antagonists; Rats; Receptors, Purinergic P2Y1; Structure-Activity Relationship; Thiazoles

2013
Identification of a new class of glucokinase activators through structure-based design.
    Journal of medicinal chemistry, 2013, Oct-10, Volume: 56, Issue:19

    Topics: Allosteric Regulation; Aminopyridines; Animals; Diabetes Mellitus, Type 2; Enzyme Activators; Glucokinase; Glucose Tolerance Test; Humans; Hypoglycemic Agents; Mice; Mice, Inbred C57BL; Rats; Rats, Zucker; Structure-Activity Relationship; Thiazoles; Young Adult

2013
Imaging of tau pathology in a tauopathy mouse model and in Alzheimer patients compared to normal controls.
    Neuron, 2013, Sep-18, Volume: 79, Issue:6

    Topics: Age Factors; Aged; Alzheimer Disease; Aminopyridines; Amyloid beta-Peptides; Aniline Compounds; Animals; Autoradiography; Benzothiazoles; Brain; Brain Mapping; Calcium-Binding Proteins; Carbon Isotopes; Disease Models, Animal; DNA-Binding Proteins; Dose-Response Relationship, Drug; Female; Humans; Magnetic Resonance Imaging; Male; Mice; Mice, Inbred C57BL; Mice, Transgenic; Microfilament Proteins; Middle Aged; Mutation; Positron-Emission Tomography; Protein Structure, Secondary; tau Proteins; Tauopathies; Thiazoles

2013
Inhibiting Tankyrases sensitizes KRAS-mutant cancer cells to MEK inhibitors via FGFR2 feedback signaling.
    Cancer research, 2014, Jun-15, Volume: 74, Issue:12

    Topics: Acetamides; Aminopyridines; Aniline Compounds; Animals; Antineoplastic Combined Chemotherapy Protocols; Cell Line, Tumor; Drug Synergism; Erlotinib Hydrochloride; Feedback, Physiological; Female; Humans; MAP Kinase Kinase Kinases; Mice; Mice, Nude; Morpholines; Mutation; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Proto-Oncogene Proteins p21(ras); Pyrimidinones; Quinazolines; ras Proteins; Receptor, Fibroblast Growth Factor, Type 2; Signal Transduction; Sulfonamides; Tankyrases; Thiazoles; Xenograft Model Antitumor Assays

2014
GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species.
    The Journal of pharmacology and experimental therapeutics, 2014, Volume: 350, Issue:1

    Topics: Aminopyridines; Animals; Anti-Anxiety Agents; Behavior, Animal; Benzamides; Callithrix; Cerebral Cortex; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclopropanes; Drug Evaluation, Preclinical; Ferrets; Inflammation; Isoenzymes; Macaca fascicularis; Male; Nootropic Agents; Oxadiazoles; Phosphodiesterase 4 Inhibitors; Pica; Rats; Rolipram; Thiazoles

2014
Searching for combinations of small-molecule correctors to restore f508del-cystic fibrosis transmembrane conductance regulator function and processing.
    The Journal of pharmacology and experimental therapeutics, 2014, Volume: 350, Issue:3

    Topics: 1-Deoxynojirimycin; Aminopyridines; Benzamides; Benzodioxoles; Cell Survival; Colforsin; Cystic Fibrosis Transmembrane Conductance Regulator; Dose-Response Relationship, Drug; HeLa Cells; Humans; Thiazoles

2014
Inhibition of c-Kit by tyrosine kinase inhibitors.
    Haematologica, 2015, Volume: 100, Issue:3

    Topics: Aminopyridines; Antineoplastic Agents; Benzothiazoles; Biomarkers; Bone Marrow; Cell Line, Tumor; Clinical Trials as Topic; Dasatinib; fms-Like Tyrosine Kinase 3; Gene Expression; Hair; Hematopoietic Stem Cells; Humans; Indazoles; Leukemia, Myeloid, Acute; Niacinamide; Phenylurea Compounds; Pigmentation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-kit; Pyrimidines; Pyrroles; Sorafenib; Sulfonamides; Thiazoles

2015
An insight into antagonist binding and induced conformational dynamics of class B GPCR corticotropin-releasing factor receptor 1.
    Molecular bioSystems, 2015, Volume: 11, Issue:7

    Topics: Aminopyridines; Binding Sites; Humans; Molecular Dynamics Simulation; Protein Binding; Protein Structure, Secondary; Pyridazines; Receptors, Corticotropin-Releasing Hormone; Thermodynamics; Thiazoles

2015
Inhibition of PI3K Pathway Reduces Invasiveness and Epithelial-to-Mesenchymal Transition in Squamous Lung Cancer Cell Lines Harboring PIK3CA Gene Alterations.
    Molecular cancer therapeutics, 2015, Volume: 14, Issue:8

    Topics: Aminopyridines; Animals; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Movement; Cell Proliferation; Class I Phosphatidylinositol 3-Kinases; Disease Models, Animal; Epithelial-Mesenchymal Transition; Humans; Imidazoles; Lung Neoplasms; Morpholines; Mutation; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Quinolines; Signal Transduction; Thiazoles; Xenograft Model Antitumor Assays

2015
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
    European journal of medicinal chemistry, 2015, Aug-28, Volume: 101

    Topics: Adenosine A1 Receptor Agonists; Aminopyridines; Dose-Response Relationship, Drug; Humans; Kinetics; Models, Molecular; Molecular Structure; Receptor, Adenosine A1; Structure-Activity Relationship; Thiazoles

2015
Investigation of the Binding Profiles of AZD2184 and Thioflavin T with Amyloid-β(1-42) Fibril by Molecular Docking and Molecular Dynamics Methods.
    The journal of physical chemistry. B, 2015, Sep-03, Volume: 119, Issue:35

    Topics: Alzheimer Disease; Aminopyridines; Amyloid beta-Peptides; Benzothiazoles; Drug Design; Elasticity; Fluorescent Dyes; Molecular Docking Simulation; Molecular Dynamics Simulation; Molecular Structure; Peptide Fragments; Positron-Emission Tomography; Protein Binding; Radiopharmaceuticals; Static Electricity; Thiazoles

2015
Distinct binding of amyloid imaging ligands to unique amyloid-β deposited in the presubiculum of Alzheimer's disease.
    Journal of neurochemistry, 2015, Volume: 135, Issue:5

    Topics: Alzheimer Disease; Aminopyridines; Amyloidogenic Proteins; Aniline Compounds; Autoradiography; Benzothiazoles; Humans; Imidazoles; In Vitro Techniques; Parahippocampal Gyrus; Plaque, Amyloid; Positron-Emission Tomography; Pyridines; Radiopharmaceuticals; Receptors, GABA; Thiazoles; Tomography, Emission-Computed, Single-Photon

2015
Optimal correction of distinct CFTR folding mutants in rectal cystic fibrosis organoids.
    The European respiratory journal, 2016, Volume: 48, Issue:2

    Topics: Aminopyridines; Benzodioxoles; Biopsy; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; Genotype; Homozygote; Humans; Mutation; Organoids; Protein Folding; Protein Transport; Rectum; Thiazoles; Treatment Outcome

2016
Mechanistic Approaches to Improve Correction of the Most Common Disease-Causing Mutation in Cystic Fibrosis.
    PloS one, 2016, Volume: 11, Issue:5

    Topics: Aminophenols; Aminopyridines; Benzamides; Benzodioxoles; Cell Line; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; Endoplasmic Reticulum; Gene Expression Regulation; Half-Life; HEK293 Cells; Humans; Mutation; Quinolones; Thiazoles

2016
Addition of the p110α inhibitor BYL719 overcomes targeted therapy resistance in cells from Her2-positive-PTEN-loss breast cancer.
    Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine, 2016, Volume: 37, Issue:11

    Topics: Aminopyridines; Animals; Antibodies; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Cell Survival; Female; Humans; Lapatinib; Mice; Morpholines; ortho-Aminobenzoates; Phosphoinositide-3 Kinase Inhibitors; Phosphorylation; PTEN Phosphohydrolase; Pyrimidinones; Quinazolines; Receptor, ErbB-2; Thiazoles; Xenograft Model Antitumor Assays

2016
PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2
    Molecular cancer therapeutics, 2017, Volume: 16, Issue:4

    Topics: Aminopyridines; Animals; Antineoplastic Combined Chemotherapy Protocols; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Synergism; Endometrial Neoplasms; Female; Gene Expression Regulation, Neoplastic; Humans; Indazoles; Mice; Morpholines; Mutation; Phenylurea Compounds; Phosphoinositide-3 Kinase Inhibitors; Pyrimidines; Receptor, Fibroblast Growth Factor, Type 2; Sulfonamides; Thiazoles; Xenograft Model Antitumor Assays

2017
JTE-852, a novel spleen tyrosine kinase inhibitor, blocks mediator secretion from mast cells with immunoglobulin E crosslinking.
    European journal of pharmacology, 2017, Apr-15, Volume: 801

    Topics: Aminopyridines; Animals; Cell Line, Tumor; Immunoglobulin E; Intracellular Space; Mast Cells; Passive Cutaneous Anaphylaxis; Protein Kinase Inhibitors; Rats; Rats, Sprague-Dawley; Syk Kinase; Thiazoles

2017
A comparison of five partial volume correction methods for Tau and Amyloid PET imaging with [
    Annals of nuclear medicine, 2017, Volume: 31, Issue:7

    Topics: Aged, 80 and over; Aminopyridines; Amyloid; Aniline Compounds; Benzothiazoles; Female; Humans; Image Processing, Computer-Assisted; Male; Positron-Emission Tomography; Quinolines; tau Proteins; Thiazoles

2017
Targeting Phosphatidylinositol 3-Kinase Signaling Pathway for Therapeutic Enhancement of Vascular-Targeted Photodynamic Therapy.
    Molecular cancer therapeutics, 2017, Volume: 16, Issue:11

    Topics: Aminopyridines; Animals; Apoptosis; Cell Line, Tumor; Cell Proliferation; Combined Modality Therapy; Endothelial Cells; Humans; Imidazoles; Mice; Morpholines; Myeloid Cell Leukemia Sequence 1 Protein; Neoplasm Recurrence, Local; Neoplasms; Neovascularization, Pathologic; Oxidative Stress; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Photochemotherapy; Porphyrins; Protein Kinase Inhibitors; Quinolines; Signal Transduction; Thiazoles; Verteporfin; Xenograft Model Antitumor Assays

2017
Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen.
    Scientific reports, 2017, 08-29, Volume: 7, Issue:1

    Topics: Aminopyridines; Antineoplastic Agents, Hormonal; Apoptosis; Cell Line, Tumor; Drug Resistance, Neoplasm; Drug Synergism; Estrogen Receptor alpha; Female; Humans; Morpholines; Mutation; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Phosphorylation; Proto-Oncogene Proteins c-akt; Receptors, Estrogen; Signal Transduction; Tamoxifen; Thiazoles

2017
Orexin receptors mediate long-term depression of excitatory synaptic transmission in the spinal cord dorsal horn.
    Neuroscience letters, 2017, Nov-01, Volume: 660

    Topics: Aminopyridines; Animals; Electric Stimulation; Excitatory Postsynaptic Potentials; Female; Long-Term Synaptic Depression; Male; Orexin Receptor Antagonists; Orexin Receptors; Pyrrolidines; Rats, Sprague-Dawley; Receptors, N-Methyl-D-Aspartate; Spinal Cord Dorsal Horn; Sulfonamides; Thiazoles

2017
JTE-852, a novel spleen tyrosine kinase inhibitor, blocks immunoglobulin G-mediated cellular responses and autoimmune reactions in vivo.
    Life sciences, 2017, Dec-15, Volume: 191

    Topics: Aminopyridines; Animals; Arthritis, Experimental; Autoimmune Diseases; Autoimmunity; Cells, Cultured; Disease Models, Animal; Female; Humans; Immunoglobulin G; Male; Mast Cells; Monocytes; Passive Cutaneous Anaphylaxis; Protein Kinase Inhibitors; Rats; Rats, Inbred Lew; Rats, Sprague-Dawley; Rats, Wistar; Syk Kinase; Thiazoles

2017
Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.
    European journal of medicinal chemistry, 2018, Jan-20, Volume: 144

    Topics: Aminopyridines; Benzodioxoles; Cell Line; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; Humans; Mutation; Quantitative Structure-Activity Relationship; Thiazoles

2018
JTE-852, a novel spleen tyrosine kinase inhibitor, blocks antigen-induced allergic reactions in rats.
    The Journal of veterinary medical science, 2018, Mar-24, Volume: 80, Issue:3

    Topics: Airway Obstruction; Aminopyridines; Animals; Antigens; Cytokines; Disease Models, Animal; Hypersensitivity; Male; Mast Cells; Nasal Mucosa; Protein-Tyrosine Kinases; Rats; Rats, Inbred BN; Respiratory Hypersensitivity; Sneezing; Spleen; Thiazoles

2018
Correctors of the Major Cystic Fibrosis Mutant Interact through Membrane-Spanning Domains.
    Molecular pharmacology, 2018, Volume: 93, Issue:6

    Topics: Aminopyridines; Benzamides; Benzodioxoles; Cell Line; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; HEK293 Cells; Humans; Mutation; Phenylalanine; Protein Structure, Tertiary; Thiazoles

2018
Neuroimaging-pathological correlations of [
    Acta neuropathologica communications, 2018, 06-29, Volume: 6, Issue:1

    Topics: Aged; Aged, 80 and over; Aminopyridines; Aniline Compounds; Astrocytes; Autopsy; Autoradiography; Correlation of Data; Female; Globus Pallidus; Humans; Magnetic Resonance Imaging; Male; Mesencephalon; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Nerve Tissue Proteins; Picolinic Acids; Positron-Emission Tomography; Quinolines; Supranuclear Palsy, Progressive; tau Proteins; Thiazoles

2018
Single-word comprehension deficits in the nonfluent variant of primary progressive aphasia.
    Alzheimer's research & therapy, 2018, 07-18, Volume: 10, Issue:1

    Topics: Aged; Aged, 80 and over; Aminopyridines; Amyloid beta-Peptides; Aniline Compounds; Aphasia, Primary Progressive; Brain; Cognition Disorders; Comprehension; Female; Humans; Magnetic Resonance Imaging; Male; Middle Aged; Neuropsychological Tests; Positron-Emission Tomography; Quinolines; Thiazoles; Tomography Scanners, X-Ray Computed; Vocabulary

2018
Effect of combined treatment with a pan-PI3K inhibitor or an isoform-specific PI3K inhibitor and everolimus on cell proliferation in GH-secreting pituitary tumour in an experimental setting.
    Endocrine, 2018, Volume: 62, Issue:3

    Topics: Aminopyridines; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cell Survival; Enzyme Inhibitors; Everolimus; Morpholines; Phosphoinositide-3 Kinase Inhibitors; Pituitary Neoplasms; Rats; Signal Transduction; Thiazoles

2018
Investigation of the quantitative accuracy of low-dose amyloid and tau PET imaging.
    Radiological physics and technology, 2018, Volume: 11, Issue:4

    Topics: Aged; Algorithms; Alzheimer Disease; Aminopyridines; Amyloid; Aniline Compounds; Artifacts; Benzothiazoles; Brain; Case-Control Studies; Female; Humans; Image Processing, Computer-Assisted; Male; Movement; Positron-Emission Tomography; Quinolines; Radiation Dosage; tau Proteins; Thiazoles; Young Adult

2018
Combination therapy with BYL719 and LEE011 is synergistic and causes a greater suppression of p-S6 in triple negative breast cancer.
    Scientific reports, 2019, 05-17, Volume: 9, Issue:1

    Topics: Aminopyridines; Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Cell Line, Tumor; Cell Survival; Class I Phosphatidylinositol 3-Kinases; Cyclin-Dependent Kinase 4; Cyclin-Dependent Kinase 6; Drug Synergism; Enzyme Inhibitors; Female; Humans; Mice; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Purines; Retinoblastoma Protein; Ribosomal Protein S6 Kinases; Signal Transduction; Thiazoles; TOR Serine-Threonine Kinases; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays

2019
The effect of two selective A
    British journal of pharmacology, 2020, Volume: 177, Issue:2

    Topics: Adenosine; Adenosine A1 Receptor Agonists; Adenosine A2 Receptor Agonists; Aminopyridines; Animals; Cardiovascular System; Consciousness; Drug Partial Agonism; Heart Rate; Hemodynamics; Ligands; Male; Rats, Sprague-Dawley; Receptor, Adenosine A1; Receptor, Adenosine A2A; Receptor, Adenosine A2B; Regional Blood Flow; Thiazoles; Thiophenes

2020
New Drugs 2019, part 4.
    Nursing, 2019, Volume: 49, Issue:11

    Topics: Aminopyridines; Cinnamates; Drug Approval; Factor Xa; Humans; Macrolides; Morpholines; Oligonucleotides; Oxazines; Pyridines; Pyrimidines; Recombinant Proteins; RNA, Small Interfering; Sisomicin; Tetracyclines; Thiazoles; Thiophenes; United States; United States Food and Drug Administration

2019
Unravelling the Regions of Mutant F508del-CFTR More Susceptible to the Action of Four Cystic Fibrosis Correctors.
    International journal of molecular sciences, 2019, Nov-01, Volume: 20, Issue:21

    Topics: Aminopyridines; Benzamides; Benzodioxoles; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; Gene Expression Regulation; HEK293 Cells; Humans; Indoles; Mutant Proteins; Mutation; Quinazolines; Thiazoles

2019
Oxidovanadium(IV) Complex Disrupts Mitochondrial Membrane Potential and Induces Apoptosis in Pancreatic Cancer Cells.
    Anti-cancer agents in medicinal chemistry, 2021, Volume: 21, Issue:1

    Topics: Aminopyridines; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Coordination Complexes; Drug Screening Assays, Antitumor; Humans; Ligands; Membrane Potential, Mitochondrial; Oxidative Stress; Pancreas; Pancreatic Neoplasms; Structure-Activity Relationship; Tetrazolium Salts; Thiazoles; Vanadium

2021
A Phase Ib Study of Alpelisib or Buparlisib Combined with Tamoxifen Plus Goserelin in Premenopausal Women with HR-Positive HER2-Negative Advanced Breast Cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2021, 01-15, Volume: 27, Issue:2

    Topics: Aminopyridines; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cyclin-Dependent Kinase 4; Female; Goserelin; Humans; Morpholines; Phosphatidylinositol 3-Kinases; Receptor, ErbB-2; Tamoxifen; Thiazoles

2021
Phase Ib Study of Ribociclib plus Fulvestrant and Ribociclib plus Fulvestrant plus PI3K Inhibitor (Alpelisib or Buparlisib) for HR
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2021, 01-15, Volume: 27, Issue:2

    Topics: Aminopyridines; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cyclin-Dependent Kinase 4; Female; Fulvestrant; Humans; Morpholines; Phosphatidylinositol 3-Kinases; Purines; Receptors, Estrogen; Thiazoles

2021
Setting the Pick: Can PI3K Inhibitors Circumvent CDK4/6 Inhibitor Resistance?
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2021, 01-15, Volume: 27, Issue:2

    Topics: Aminopyridines; Breast Neoplasms; Cyclin-Dependent Kinase 4; Cyclin-Dependent Kinase 6; Female; Goserelin; Humans; Morpholines; Phosphatidylinositol 3-Kinases; Tamoxifen; Thiazoles

2021
PI3k inhibitors (BKM120 and BYL719) as radiosensitizers for head and neck squamous cell carcinoma during radiotherapy.
    PloS one, 2021, Volume: 16, Issue:1

    Topics: Aminopyridines; Carcinoma, Squamous Cell; Cell Line, Tumor; Head and Neck Neoplasms; Humans; Morpholines; Neoplasm Proteins; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Radiation-Sensitizing Agents; Thiazoles

2021
Amino Acid Conjugates of Aminothiazole and Aminopyridine as Potential Anticancer Agents: Synthesis, Molecular Docking and in vitro Evaluation.
    Drug design, development and therapy, 2021, Volume: 15

    Topics: Amino Acids; Aminopyridines; Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Molecular Docking Simulation; Molecular Structure; Picrates; Thiazoles; Tumor Cells, Cultured

2021
Mitochondrial complex I abnormalities is associated with tau and clinical symptoms in mild Alzheimer's disease.
    Molecular neurodegeneration, 2021, 04-26, Volume: 16, Issue:1

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Aminopyridines; Aniline Compounds; Benzothiazoles; Brain Chemistry; Carbon Radioisotopes; Electron Transport Complex I; Entorhinal Cortex; Female; Fluorine Radioisotopes; Humans; Magnetic Resonance Imaging; Male; Mental Status and Dementia Tests; Middle Aged; Neuroimaging; Positron-Emission Tomography; Pyridazines; Pyridines; Radiopharmaceuticals; Severity of Illness Index; Symptom Assessment; tau Proteins; Thiazoles

2021
Negative allosteric modulation of metabotropic glutamate receptor 5 attenuates alcohol self-administration in baboons.
    Pharmacology, biochemistry, and behavior, 2021, Volume: 208

    Topics: Alcoholism; Allosteric Regulation; Aminopyridines; Animals; Ethanol; Female; Glutamic Acid; Humans; Papio; Picolinic Acids; Pyridines; Receptor, Metabotropic Glutamate 5; Self Administration; Thiazoles

2021
A Phase I Study of LSZ102, an Oral Selective Estrogen Receptor Degrader, with or without Ribociclib or Alpelisib, in Patients with Estrogen Receptor-Positive Breast Cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2021, 11-01, Volume: 27, Issue:21

    Topics: Adult; Aminopyridines; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Female; Humans; Purines; Receptors, Estrogen; Thiazoles; Thiophenes

2021
NBD2 Is Required for the Rescue of Mutant F508del CFTR by a Thiazole-Based Molecule: A Class II Corrector for the Multi-Drug Therapy of Cystic Fibrosis.
    Biomolecules, 2021, 09-28, Volume: 11, Issue:10

    Topics: Aminopyridines; Benzodioxoles; Cell Membrane; Cystic Fibrosis; Cystic Fibrosis Transmembrane Conductance Regulator; Epithelial Cells; Gene Expression Regulation; HEK293 Cells; Humans; Mutant Proteins; Phenylalanine; Thiazoles

2021
Patterns of Distribution of 18F-THK5351 Positron Emission Tomography in Alzheimer's Disease Continuum.
    Journal of Alzheimer's disease : JAD, 2022, Volume: 85, Issue:1

    Topics: Aged; Alzheimer Disease; Aminopyridines; Amnesia; Aniline Compounds; Brain; Cognitive Dysfunction; Disease Progression; Female; Fluorodeoxyglucose F18; Humans; Magnetic Resonance Imaging; Male; Middle Aged; Neuropsychological Tests; Positron-Emission Tomography; Quinolines; Radiopharmaceuticals; Severity of Illness Index; tau Proteins; Thiazoles

2022