Any organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.
| Member | Definition | Role |
|---|
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | A pyridopyrimidine that is pyrido[2,3-d]pyrimidine which is substituted at positions 2 and 4 by (3S)-3-methylmorpholin-4-yl groups and at position 5 by a 3-(hydroxymethyl)-4-methoxyphenyl group. It is an mTOR complex 1/2 (mTORC1/2) dual inhibitor [mTOR = mammalian target of rapamycin]. | AZD-8055 |
| 1-(2-methoxyethyl)-7-thiophen-2-yl-5-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione | | 1-(2-methoxyethyl)-7-thiophen-2-yl-5-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione |
| 1-(3-ethoxypropyl)-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester | | 1-(3-ethoxypropyl)-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxylic acid ethyl ester |
| 1-(3,4-dimethylphenyl)-2,5-dioxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarbonitrile | | 1-(3,4-dimethylphenyl)-2,5-dioxo-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarbonitrile |
| 1-[(7-chloro-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-(3-fluoro-4-methylphenyl)thieno[3,2-d]pyrimidine-2,4-dione | | 1-[(7-chloro-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-(3-fluoro-4-methylphenyl)thieno[3,2-d]pyrimidine-2,4-dione |
| 1-[2-(3,4-dimethoxyphenyl)ethyl]-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | | 1-[2-(3,4-dimethoxyphenyl)ethyl]-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide |
| 1-butyl-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester | | 1-butyl-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxylic acid ethyl ester |
| 1-butyl-2,4-dioxo-7-thiophen-2-yl-5-pyrido[2,3-d]pyrimidinecarboxylic acid ethyl ester | | 1-butyl-2,4-dioxo-7-thiophen-2-yl-5-pyrido[2,3-d]pyrimidinecarboxylic acid ethyl ester |
| 1-cyclopentyl-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | | 1-cyclopentyl-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide |
| 2-(3-ethoxypropylamino)-8-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-pyrimidinecarboxamide | | 2-(3-ethoxypropylamino)-8-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-pyrimidinecarboxamide |
| 2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-pyridinecarboxylic acid propan-2-yl ester | | 2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-pyridinecarboxylic acid propan-2-yl ester |
| 2-[[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl]-oxomethyl]imino-1-(2-methylpropyl)-5-oxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxylic acid ethyl ester | | 2-[[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl]-oxomethyl]imino-1-(2-methylpropyl)-5-oxo-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxylic acid ethyl ester |
| 2-[2-furanyl(oxo)methyl]imino-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxylic acid ethyl ester | | 2-[2-furanyl(oxo)methyl]imino-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxylic acid ethyl ester |
| 2-benzoylimino-1-(2-furanylmethyl)-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester | | 2-benzoylimino-1-(2-furanylmethyl)-10-methyl-5-oxo-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxylic acid ethyl ester |
| 2-bromo-6-[1,4-dioxa-8-azaspiro[4.5]decan-8-yl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone | | 2-bromo-6-[1,4-dioxa-8-azaspiro[4.5]decan-8-yl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone |
| 2-chloro-6-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone | | 2-chloro-6-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone |
| 2-chloro-8-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone | | 2-chloro-8-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone |
| 2-imino-1-[(4-methylphenyl)methyl]-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | | 2-imino-1-[(4-methylphenyl)methyl]-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide |
| 2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | | 2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide |
| 2-imino-8-methyl-5-oxo-1-(2-oxolanylmethyl)-N-(2-phenylethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | | 2-imino-8-methyl-5-oxo-1-(2-oxolanylmethyl)-N-(2-phenylethyl)-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide |
| 2-imino-N,8-dimethyl-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | | 2-imino-N,8-dimethyl-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide |
| 2-methyl-1-cyclopropanecarboxylic acid (7-bromo-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl ester | | 2-methyl-1-cyclopropanecarboxylic acid (7-bromo-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl ester |
| 3-(3,4-dimethylphenyl)sulfonyl-2-imino-1-prop-2-enyl-5-dipyrido[1,2-e-4',3'-f]pyrimidinone | | 3-(3,4-dimethylphenyl)sulfonyl-2-imino-1-prop-2-enyl-5-dipyrido[1,2-e:4',3'-f]pyrimidinone |
| 3-(4-fluorophenyl)sulfonyl-1-(2-furanylmethyl)-2-imino-10-methyl-5-dipyrido[3,4-c-1',2'-f]pyrimidinone | | 3-(4-fluorophenyl)sulfonyl-1-(2-furanylmethyl)-2-imino-10-methyl-5-dipyrido[3,4-c:1',2'-f]pyrimidinone |
| 3-(benzenesulfonyl)-2-imino-1-(2-oxolanylmethyl)-5-dipyrido[1,2-d-3',4'-f]pyrimidinone | | 3-(benzenesulfonyl)-2-imino-1-(2-oxolanylmethyl)-5-dipyrido[1,2-d:3',4'-f]pyrimidinone |
| 3-(benzenesulfonyl)-2-imino-1-propyl-5-dipyrido[1,2-d-3',4'-f]pyrimidinone | | 3-(benzenesulfonyl)-2-imino-1-propyl-5-dipyrido[1,2-d:3',4'-f]pyrimidinone |
| 3-[(3-chlorophenyl)methyl]-5-ethoxy-1,6-dimethylpyrido[2,3-d]pyrimidine-2,4-dione | | 3-[(3-chlorophenyl)methyl]-5-ethoxy-1,6-dimethylpyrido[2,3-d]pyrimidine-2,4-dione |
| 3-[2,4-dioxo-1-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-quinazolinyl]-N-(2-furanylmethyl)propanamide | | 3-[2,4-dioxo-1-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-quinazolinyl]-N-(2-furanylmethyl)propanamide |
| 3-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]propanoic acid | | 3-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]propanoic acid |
| 3-ethyl-2-sulfanylidene-6,7,8,9-tetrahydro-1H-pyrimido[4,5-b]quinolin-4-one | | 3-ethyl-2-sulfanylidene-6,7,8,9-tetrahydro-1H-pyrimido[4,5-b]quinolin-4-one |
| 5-[[2-(diethylamino)-9-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinyl]methylidene]-1,3-diazinane-2,4,6-trione | | 5-[[2-(diethylamino)-9-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinyl]methylidene]-1,3-diazinane-2,4,6-trione |
| 5-deazaflavin | | Deazaflavin |
| 6-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]hexanoic acid | | 6-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]hexanoic acid |
| 6-propan-2-yl-2-sulfanylidene-1,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-one | | 6-propan-2-yl-2-sulfanylidene-1,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-one |
| 7-methyl-4-oxo-2-[(phenylmethyl)amino]-3-pyrido[1,2-a]pyrimidinecarboxaldehyde | | 7-methyl-4-oxo-2-[(phenylmethyl)amino]-3-pyrido[1,2-a]pyrimidinecarboxaldehyde |
| 8-(1-piperidinylsulfonyl)-6-pyrido[1,2-a]quinazolinone | | 8-(1-piperidinylsulfonyl)-6-pyrido[1,2-a]quinazolinone |
| 8-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinecarboxylic acid ethyl ester | | 8-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinecarboxylic acid ethyl ester |
| 9,10-dimethoxy-2-(2-pyridinylmethylamino)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one | | 9,10-dimethoxy-2-(2-pyridinylmethylamino)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one |
| gw2974 | | N6,N6-dimethyl-N4-[1-(phenylmethyl)-5-indazolyl]pyrido[3,4-d]pyrimidine-4,6-diamine |
| kin-193 | | 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-9-pyrido[1,2-a]pyrimidinyl]ethyl]amino]benzoic acid |
| ku 0063794 | A member of the class of pyridopyrimidines that is an mTOR inhibitor and shows anti-tumour properties. | Ku-0063794 |
| LSM-16446 | | LSM-16446 |
| LSM-16483 | | LSM-16483 |
| LSM-20487 | | LSM-20487 |
| LSM-26967 | | LSM-26967 |
| LSM-27960 | | LSM-27960 |
| LSM-28172 | | LSM-28172 |
| LSM-28559 | | LSM-28559 |
| LSM-31933 | | LSM-31933 |
| LSM-33283 | | LSM-33283 |
| ly3009120 | A member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by methylamino, 5-{[(3,3-dimethylbutyl)carbamoyl]amino}-4-fluoro-2-methylphenyl, and methyl groups at positions 2, 6 and 7, respectively. It is a potent pan RAF inhibitor which inhibits BRAF(V600E), BRAF(WT) and CRAF(WT) (IC50 = 5.8, 9.1 and 15 nM, respectively). It also inhibits RAF homo- and heterodimers and exhibits anti-cancer properties. | LY3009120 |
| N-(2-furanylmethyl)-1-[2-(2-hydroxyethoxy)ethyl]-2-imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | | N-(2-furanylmethyl)-1-[2-(2-hydroxyethoxy)ethyl]-2-imino-10-methyl-5-oxo-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide |
| N-(2-furanylmethyl)-2-imino-5-oxo-1-(2-phenylethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | | N-(2-furanylmethyl)-2-imino-5-oxo-1-(2-phenylethyl)-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide |
| N-cyclopentyl-2-imino-1-[3-(4-morpholinyl)propyl]-5-oxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide | | N-cyclopentyl-2-imino-1-[3-(4-morpholinyl)propyl]-5-oxo-3-dipyrido[1,2-d:3',4'-f]pyrimidinecarboxamide |
| N-ethyl-2-imino-10-methyl-1-[(4-methylphenyl)methyl]-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide | | N-ethyl-2-imino-10-methyl-1-[(4-methylphenyl)methyl]-5-oxo-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide |
| ocaperidone | | Ocaperidone |
| palbociclib | A member of the class of pyridopyrimidines that is 2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7-one bearing additional methyl, acetyl and cyclopentyl substituents at positions 5, 6 and 8 respectively. It is used in combination with letrozole for the treatment of metastatic breast cancer. | palbociclib |
| paliperidone | A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one |
| paliperidone palmitate | A fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one. | 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate |
| pamapimod | A member of the class of pyridopyrimidines that is 8-methylpyrido[2,3-d]pyrimidin-7(8H)-one carrying additional (1,5-dihydroxypentan-3-yl)amino and 2,4-difluorophenoxy substituents at positions 2 and 6 respectively. It is a potent inhibitor of MAPK and is used for treatment of rheumatoid arthritis. | pamapimod |
| pd 158780 | A pyridopyrimidine that is pyrido[3,4-d]pyrimidine-4,6-diamine in which the amino groups at positions 4 and 6 are substituted by a m-bromophenyl group and a methyl group, respectively. It is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity [IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4)]. It does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. | PD158780 |
| pd 166866 | A member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by an amino group at position 2, 3,5-dimethoxyphenyl group at position 6, and by a (tert-butylcarbamoyl)nitrilo group at position 7. It is a selective ATP competitive inhibitor of the human fibroblast growth factor-1 receptor (FGFR1) tyrosine kinase with an IC50 of 52.4 nM. | PD-166866 |
| pd 173074 | A member of the class of ureas that is 1-tert-butylurea in which one of the hydrogens attached to N(3) is substituted by a pyrido[2,3-d]pyrimidin-7-yl group, which is itself substituted at positions 2 and 6 by a 4-(diethylamino)butyl]amino group and a 3,5-dimethoxyphenyl group, respectively. It is a FGF/VEGF receptor tyrosine kinase inhibitor. | PD173074 |
| pd 173955 | | PD173955 |
| pemirolast | | pemirolast |
| pipemidic acid | A pyridopyrimidine that is 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid substituted at position 2 by a piperazin-1-yl group and at position 8 by an ethyl group. A synthetic broad-spectrum antibacterial, it is used for treatment of gastrointestinal, biliary, and urinary infections. | pipemidic acid |
| piromidic acid | A pyridopyrimidine that is 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid, substituted at position 2 by a pyrrolidin-1-yl group and at position 8 by an ethyl group. A synthetic antibacterial which is used for the treatment of urinary tract and intestinal infections. | piromidic acid |
| probon | | rimazolium |
| risperidone | A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | risperidone |
| sotorasib | A pyridopyrimidine that is pyrido[2,3-d]pyrimidin-2(1H)-one substituted by 4-methyl-2-(propan-2-yl)pyridin-3-yl, (2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl, fluoro and 2-fluoro-6-hydroxyphenyl groups at positions 1, 4, 6 and 7, respectively. It is approved for the treatment of patients with non-small cell lung cancer having KRAS(G12C) mutations. | sotorasib |
| ssr 69071 | | 6-methoxy-1,1-dioxo-2-[[4-oxo-9-[2-(1-piperidinyl)ethoxy]-2-pyrido[1,2-a]pyrimidinyl]oxymethyl]-4-propan-2-yl-1,2-benzothiazol-3-one |
| tgx 221 | | 9-(1-anilinoethyl)-7-methyl-2-(4-morpholinyl)-4-pyrido[1,2-a]pyrimidinone |
| trametinib | A pyridopyrimidine that is used (as its dimethyl sulfoxide addition compound) for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, and who have not received prior BRAF inhibitor treatment. | trametinib |
| trequinsin | | 9,10-dimethoxy-3-methyl-2-(2,4,6-trimethylphenyl)imino-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one |