MXPA02008535A - Inhibidores de 5-alquilpirido (2.3-d) pirimidinas tirosina quinasa. - Google Patents

Inhibidores de 5-alquilpirido (2.3-d) pirimidinas tirosina quinasa.

Info

Publication number: MXPA02008535A
Authority: MX; Mexico
Prior art keywords: compound; methyl; pyrido; pyrimidin; cyclopentyl
Prior art date: 2000-03-06

Application number

MXPA02008535A

Other languages

English (en)

Spanish (es)

Inventor

Ellen Myra Dobrusin

Original Assignee

Warner Lambert Co

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-03-06

Filing date

2001-01-29

Publication date

2002-12-13

2001-01-29 Application filed by Warner Lambert Co filed Critical Warner Lambert Co

2002-12-13 Publication of MXPA02008535A publication Critical patent/MXPA02008535A/es

Links

150000003230 pyrimidines Chemical class 0.000 title 1
229940121358 tyrosine kinase inhibitor Drugs 0.000 title 1
239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
150000001875 compounds Chemical class 0.000 claims abstract description 419
125000000217 alkyl group Chemical group 0.000 claims abstract description 91
229910052736 halogen Inorganic materials 0.000 claims abstract description 52
150000002367 halogens Chemical class 0.000 claims abstract description 52
125000003545 alkoxy group Chemical group 0.000 claims abstract description 48
229910052739 hydrogen Inorganic materials 0.000 claims abstract description 44
239000001257 hydrogen Substances 0.000 claims abstract description 41
125000003118 aryl group Chemical group 0.000 claims abstract description 38
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 34
150000002431 hydrogen Chemical group 0.000 claims abstract description 33
150000002825 nitriles Chemical class 0.000 claims abstract description 22
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 21
206010028980 Neoplasm Diseases 0.000 claims abstract description 18
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 16
125000003342 alkenyl group Chemical group 0.000 claims abstract description 15
201000011510 cancer Diseases 0.000 claims abstract description 14
125000000304 alkynyl group Chemical group 0.000 claims abstract description 13
125000001188 haloalkyl group Chemical group 0.000 claims abstract description 12
102000003903 Cyclin-dependent kinases Human genes 0.000 claims abstract description 10
108090000266 Cyclin-dependent kinases Proteins 0.000 claims abstract description 10
125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 10
208000037803 restenosis Diseases 0.000 claims abstract description 9
230000002062 proliferating effect Effects 0.000 claims abstract description 8
101100295741 Gallus gallus COR4 gene Proteins 0.000 claims abstract description 7
201000001320 Atherosclerosis Diseases 0.000 claims abstract description 6
239000003102 growth factor Substances 0.000 claims abstract description 6
230000001404 mediated effect Effects 0.000 claims abstract description 6
108091000080 Phosphotransferase Proteins 0.000 claims abstract description 5
102000020233 phosphotransferase Human genes 0.000 claims abstract description 5
-1 trifluoromethylalkyl Chemical group 0.000 claims description 296
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 75
229910052757 nitrogen Chemical group 0.000 claims description 49
125000002837 carbocyclic group Chemical group 0.000 claims description 46
229910052717 sulfur Inorganic materials 0.000 claims description 42
229910052760 oxygen Inorganic materials 0.000 claims description 39
125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 32
125000004356 hydroxy functional group Chemical group O* 0.000 claims description 32
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 31
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 27
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 27
125000001072 heteroaryl group Chemical group 0.000 claims description 27
239000001301 oxygen Substances 0.000 claims description 27
125000004663 dialkyl amino group Chemical group 0.000 claims description 26
125000005842 heteroatom Chemical group 0.000 claims description 26
239000011593 sulfur Chemical group 0.000 claims description 26
125000004448 alkyl carbonyl group Chemical group 0.000 claims description 23
229960001171 acetohydroxamic acid Drugs 0.000 claims description 22
238000000034 method Methods 0.000 claims description 22
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 20
125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 18
125000002768 hydroxyalkyl group Chemical group 0.000 claims description 18
150000003839 salts Chemical class 0.000 claims description 18
239000002253 acid Substances 0.000 claims description 17
150000001408 amides Chemical class 0.000 claims description 17
125000004103 aminoalkyl group Chemical group 0.000 claims description 17
150000002148 esters Chemical class 0.000 claims description 14
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 14
RRUDCFGSUDOHDG-UHFFFAOYSA-N acetohydroxamic acid Chemical compound CC(O)=NO RRUDCFGSUDOHDG-UHFFFAOYSA-N 0.000 claims description 12
239000000651 prodrug Substances 0.000 claims description 12
229940002612 prodrug Drugs 0.000 claims description 12
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 11
LNUFLCYMSVYYNW-ZPJMAFJPSA-N [(2r,3r,4s,5r,6r)-2-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[[(3s,5s,8r,9s,10s,13r,14s,17r)-10,13-dimethyl-17-[(2r)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl]oxy]-4,5-disulfo Chemical compound O([C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1C[C@@H]2CC[C@H]3[C@@H]4CC[C@@H]([C@]4(CC[C@@H]3[C@@]2(C)CC1)C)[C@H](C)CCCC(C)C)[C@H]1O[C@H](COS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@H](OS(O)(=O)=O)[C@H]1OS(O)(=O)=O LNUFLCYMSVYYNW-ZPJMAFJPSA-N 0.000 claims description 11
201000010099 disease Diseases 0.000 claims description 10
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 9
125000005843 halogen group Chemical group 0.000 claims description 9
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 9
JJFFJESALPMDFO-UHFFFAOYSA-N O1CCN(CC1)CCCC1CCN(CC1)C1=CC=C(C=C1)NC=1N=CC2=C(N=1)NC(C=C2)=O Chemical compound O1CCN(CC1)CCCC1CCN(CC1)C1=CC=C(C=C1)NC=1N=CC2=C(N=1)NC(C=C2)=O JJFFJESALPMDFO-UHFFFAOYSA-N 0.000 claims description 8
150000001450 anions Chemical class 0.000 claims description 8
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 8
230000002401 inhibitory effect Effects 0.000 claims description 8
DIDKOYSHJAGQQS-UHFFFAOYSA-N 8-cyclohexyl-5-methyl-2-(4-piperazin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(=CC=3)N3CCNCC3)=NC=C2C(C)=CC(=O)N1C1CCCCC1 DIDKOYSHJAGQQS-UHFFFAOYSA-N 0.000 claims description 7
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims description 7
125000003710 aryl alkyl group Chemical group 0.000 claims description 7
125000005936 piperidyl group Chemical group 0.000 claims description 7
230000035755 proliferation Effects 0.000 claims description 7
ASGMFNBUXDJWJJ-JLCFBVMHSA-N (1R,3R)-3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethylcyclopentane-1-carboxamide Chemical compound BrC1=NN(C2=NC(=NC=C21)N[C@H]1C[C@@](CC1)(C(=O)NC)C)C1=CC=C(C=C1)C=1SC(=NN=1)C ASGMFNBUXDJWJJ-JLCFBVMHSA-N 0.000 claims description 6
VVCMGAUPZIKYTH-VGHSCWAPSA-N 2-acetyloxybenzoic acid;[(2s,3r)-4-(dimethylamino)-3-methyl-1,2-diphenylbutan-2-yl] propanoate;1,3,7-trimethylpurine-2,6-dione Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O.CN1C(=O)N(C)C(=O)C2=C1N=CN2C.C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 VVCMGAUPZIKYTH-VGHSCWAPSA-N 0.000 claims description 6
VYQVLIJXHSKRIZ-UHFFFAOYSA-N 4-amino-8-cyclopentyl-2-(2,3-dimethyl-1H-indol-5-yl)-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound Cc1[nH]c2ccc(cc2c1C)-c1nc(N)c2c(C)cc(=O)n(C3CCCC3)c2n1 VYQVLIJXHSKRIZ-UHFFFAOYSA-N 0.000 claims description 6
LDWPCANEKZCUQT-UHFFFAOYSA-N 8-cyclopentyl-2-[4-(1,4-diazepan-1-yl)anilino]-5-methylpyrido[2,3-d]pyrimidin-7-one;hydrochloride Chemical compound Cl.C12=NC(NC=3C=CC(=CC=3)N3CCNCCC3)=NC=C2C(C)=CC(=O)N1C1CCCC1 LDWPCANEKZCUQT-UHFFFAOYSA-N 0.000 claims description 6
RMNWLVFFWRBNQK-UHFFFAOYSA-N 8-cyclopentyl-5-methyl-2-(4-piperidin-1-ylanilino)pyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(=CC=3)N3CCCCC3)=NC=C2C(C)=CC(=O)N1C1CCCC1 RMNWLVFFWRBNQK-UHFFFAOYSA-N 0.000 claims description 6
125000004183 alkoxy alkyl group Chemical group 0.000 claims description 6
125000004181 carboxyalkyl group Chemical group 0.000 claims description 6
229940125904 compound 1 Drugs 0.000 claims description 6
125000004446 heteroarylalkyl group Chemical group 0.000 claims description 6
125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
ATLXXIXQFJFKSW-UHFFFAOYSA-N 2-amino-8h-pyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(=O)NC2=NC(N)=NC=C21 ATLXXIXQFJFKSW-UHFFFAOYSA-N 0.000 claims description 5
ZNVKRQSAAFJHSX-UHFFFAOYSA-N 4-amino-8-cyclopentyl-2-(1H-indazol-5-yl)-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound Cc1cc(=O)n(C2CCCC2)c2nc(nc(N)c12)-c1ccc2[nH]ncc2c1 ZNVKRQSAAFJHSX-UHFFFAOYSA-N 0.000 claims description 5
OQSUTVNZWPPSCU-UHFFFAOYSA-N 8-cyclopentyl-2-(4-piperazin-1-ylanilino)-5-propylpyrido[2,3-d]pyrimidin-7-one;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C12=NC(NC=3C=CC(=CC=3)N3CCNCC3)=NC=C2C(CCC)=CC(=O)N1C1CCCC1 OQSUTVNZWPPSCU-UHFFFAOYSA-N 0.000 claims description 5
KROKICGNSBBBTA-UHFFFAOYSA-N 8-cyclopentyl-5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(C)=CC(=O)N2C3CCCC3)C2=N1 KROKICGNSBBBTA-UHFFFAOYSA-N 0.000 claims description 5
102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 5
108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 5
229910052799 carbon Inorganic materials 0.000 claims description 5
230000004663 cell proliferation Effects 0.000 claims description 5
239000003085 diluting agent Substances 0.000 claims description 5
208000035475 disorder Diseases 0.000 claims description 5
GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 claims description 4
QCNGGERJGDWDQD-UHFFFAOYSA-N 2-(3-chloro-4-morpholin-4-ylanilino)-8-cyclopentyl-6-fluoro-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=C(Cl)C(N4CCOCC4)=CC=3)=NC=C2C(C)=C(F)C(=O)N1C1CCCC1 QCNGGERJGDWDQD-UHFFFAOYSA-N 0.000 claims description 4
HBKSAUJHTFQTMK-UHFFFAOYSA-N 2-(3-chloro-4-piperazin-1-ylanilino)-8-cyclopentyl-6-fluoro-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=C(Cl)C(N4CCNCC4)=CC=3)=NC=C2C(C)=C(F)C(=O)N1C1CCCC1 HBKSAUJHTFQTMK-UHFFFAOYSA-N 0.000 claims description 4
FQTDEBGLGLWEQA-UHFFFAOYSA-N 2-(9h-carbazol-3-ylamino)-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=C4C5=CC=CC=C5NC4=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 FQTDEBGLGLWEQA-UHFFFAOYSA-N 0.000 claims description 4
QMZVCQKRIINZTA-UHFFFAOYSA-N 2-[4-(3-aminopyrrolidin-1-yl)anilino]-6-bromo-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(=CC=3)N3CC(N)CC3)=NC=C2C(C)=C(Br)C(=O)N1C1CCCC1 QMZVCQKRIINZTA-UHFFFAOYSA-N 0.000 claims description 4
BUWGSASRFPMSRO-UHFFFAOYSA-N 2-[4-[(8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]phenoxy]-n-(2h-tetrazol-5-yl)acetamide Chemical compound C12=NC(NC=3C=CC(OCC(=O)NC4=NNN=N4)=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 BUWGSASRFPMSRO-UHFFFAOYSA-N 0.000 claims description 4
LCSNHEQSAWBZRW-UHFFFAOYSA-N 3-[[4-[(8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]phenyl]methyl]-2h-1,2,4-oxadiazol-5-one Chemical compound C12=NC(NC=3C=CC(CC=4NOC(=O)N=4)=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 LCSNHEQSAWBZRW-UHFFFAOYSA-N 0.000 claims description 4
MABISOYNQBKDCJ-UHFFFAOYSA-N 4-[(8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]benzoic acid Chemical compound C12=NC(NC=3C=CC(=CC=3)C(O)=O)=NC=C2C(C)=CC(=O)N1C1CCCC1 MABISOYNQBKDCJ-UHFFFAOYSA-N 0.000 claims description 4
MQMVVICIZXNENP-UHFFFAOYSA-N 8-cyclopentyl-2-(1h-indol-5-ylamino)-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=C4C=CNC4=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 MQMVVICIZXNENP-UHFFFAOYSA-N 0.000 claims description 4
HPCNYSQWPMYYEH-UHFFFAOYSA-N 8-cyclopentyl-5-methyl-2-[4-(2h-triazol-4-ylsulfanylmethyl)anilino]pyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(CSC4=NNN=C4)=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 HPCNYSQWPMYYEH-UHFFFAOYSA-N 0.000 claims description 4
XDIGYIOQAKKGOG-UHFFFAOYSA-N 8-cyclopentyl-6-fluoro-5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(C)=C(F)C(=O)N2C3CCCC3)C2=N1 XDIGYIOQAKKGOG-UHFFFAOYSA-N 0.000 claims description 4
241000124008 Mammalia Species 0.000 claims description 4
ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 claims description 4
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
229940125797 compound 12 Drugs 0.000 claims description 4
229940127573 compound 38 Drugs 0.000 claims description 4
PIDFDZJZLOTZTM-KHVQSSSXSA-N ombitasvir Chemical compound COC(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)NC1=CC=C([C@H]2N([C@@H](CC2)C=2C=CC(NC(=O)[C@H]3N(CCC3)C(=O)[C@@H](NC(=O)OC)C(C)C)=CC=2)C=2C=CC(=CC=2)C(C)(C)C)C=C1 PIDFDZJZLOTZTM-KHVQSSSXSA-N 0.000 claims description 4
125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims description 4
239000008194 pharmaceutical composition Substances 0.000 claims description 4
239000000546 pharmaceutical excipient Substances 0.000 claims description 4
OKJVIDWCJPJGJP-UHFFFAOYSA-N 2-(3-chloro-4-piperazin-1-ylanilino)-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C12=NC(NC=3C=C(Cl)C(N4CCNCC4)=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 OKJVIDWCJPJGJP-UHFFFAOYSA-N 0.000 claims description 3
MUEXYYGLGBJONZ-UHFFFAOYSA-N 2-[4-(4-acetyl-3,3-dimethylpiperazin-1-yl)anilino]-8-cyclopentyl-6-fluoro-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1C(C)(C)N(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(C)=C(F)C(=O)N2C3CCCC3)C2=N1 MUEXYYGLGBJONZ-UHFFFAOYSA-N 0.000 claims description 3
VEMYILRVAQWCCT-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-8-cyclopentyl-6-fluoro-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(C)=C(F)C(=O)N2C3CCCC3)C2=N1 VEMYILRVAQWCCT-UHFFFAOYSA-N 0.000 claims description 3
125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
BRLUAHNVJPJLRS-UHFFFAOYSA-N 5-ethyl-2-(4-piperazin-1-ylanilino)-8-propan-2-ylpyrido[2,3-d]pyrimidin-7-one Chemical compound N=1C=C2C(CC)=CC(=O)N(C(C)C)C2=NC=1NC(C=C1)=CC=C1N1CCNCC1 BRLUAHNVJPJLRS-UHFFFAOYSA-N 0.000 claims description 3
GTMYJLACTBZULS-UHFFFAOYSA-N 5-ethyl-2-(4-piperazin-1-ylanilino)-8-propan-2-ylpyrido[2,3-d]pyrimidin-7-one;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.N=1C=C2C(CC)=CC(=O)N(C(C)C)C2=NC=1NC(C=C1)=CC=C1N1CCNCC1 GTMYJLACTBZULS-UHFFFAOYSA-N 0.000 claims description 3
RACNDJAQNJWRIL-UHFFFAOYSA-N 8-cyclohexyl-6-fluoro-5-methyl-2-[4-[4-(3-morpholin-4-ylpropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(=CC=3)N3CCC(CCCN4CCOCC4)CC3)=NC=C2C(C)=C(F)C(=O)N1C1CCCCC1 RACNDJAQNJWRIL-UHFFFAOYSA-N 0.000 claims description 3
APNAVIIJIKHXNQ-UHFFFAOYSA-N 8-cyclopentyl-2-[(2,3-dimethyl-1h-indol-5-yl)amino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1=C2C(C)=C(C)NC2=CC=C1NC(N=C12)=NC=C1C(C)=CC(=O)N2C1CCCC1 APNAVIIJIKHXNQ-UHFFFAOYSA-N 0.000 claims description 3
KOHCENFNOCYUTH-UHFFFAOYSA-N 8-cyclopentyl-2-[4-(2-hydroxyethyl)anilino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(CCO)=CC=3)=NC=C2C(C)=CC(=O)N1C1CCCC1 KOHCENFNOCYUTH-UHFFFAOYSA-N 0.000 claims description 3
NTGNTTDNUQRUSW-UHFFFAOYSA-N 8-cyclopentyl-2-[4-(2-methoxyethoxy)anilino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(OCCOC)=CC=C1NC1=NC=C(C(C)=CC(=O)N2C3CCCC3)C2=N1 NTGNTTDNUQRUSW-UHFFFAOYSA-N 0.000 claims description 3
FSADLTOIDQVCAJ-UHFFFAOYSA-N 8-cyclopentyl-2-[4-(3-hydroxypyrrolidin-1-yl)anilino]-5-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C12=NC(NC=3C=CC(=CC=3)N3CC(O)CC3)=NC=C2C(C)=CC(=O)N1C1CCCC1 FSADLTOIDQVCAJ-UHFFFAOYSA-N 0.000 claims description 3
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201000004681 Psoriasis Diseases 0.000 claims description 3
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Dermatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

MXPA02008535A 2000-03-06 2001-01-29 Inhibidores de 5-alquilpirido (2.3-d) pirimidinas tirosina quinasa. MXPA02008535A (es)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US18712400P	2000-03-06	2000-03-06
PCT/US2001/002657 WO2001070741A1 (en)	2000-03-06	2001-01-29	5-alkylpyrido[2,3-d]pyrimidines tyrosine kinase inhibitors

Publications (1)

Publication Number	Publication Date
MXPA02008535A true MXPA02008535A (es)	2002-12-13

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ID=22687699

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
MXPA02008535A MXPA02008535A (es)	2000-03-06	2001-01-29	Inhibidores de 5-alquilpirido (2.3-d) pirimidinas tirosina quinasa.

Country Status (36)

Country	Link
EP (1)	EP1268476A1 (et)
JP (1)	JP2003528101A (et)
KR (1)	KR20020075805A (et)
CN (1)	CN1422268A (et)
AP (1)	AP2002002643A0 (et)
AR (1)	AR034119A1 (et)
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CO5280200A1 (es)	2003-05-30
KR20020075805A (ko)	2002-10-05
BG107161A (en)	2003-06-30
ZA200207110B (en)	2003-12-04
AU2001233028A1 (en)	2001-10-03
DZ3308A1 (fr)	2001-09-27
YU66502A (sh)	2005-09-19
IS6524A (is)	2002-08-23
PE20011177A1 (es)	2001-11-23
CA2401368A1 (en)	2001-09-27
NO20024235D0 (no)	2002-09-05
PL358271A1 (en)	2004-08-09
SK12472002A3 (sk)	2003-04-01
NZ520962A (en)	2003-09-26
IL151480A0 (en)	2003-04-10
SV2001000338A (es)	2001-11-30
BR0109056A (pt)	2003-06-03
CZ20022929A3 (cs)	2003-02-12
AR034119A1 (es)	2004-02-04
PA8513201A1 (es)	2003-06-30
HUP0300136A2 (en)	2003-05-28
GT200100037A (es)	2002-03-04
NO20024235L (no)	2002-11-05
MA26881A1 (fr)	2004-12-20
CR6736A (es)	2004-03-10
EA200200802A1 (ru)	2003-02-27
AP2002002643A0 (en)	2002-12-31
WO2001070741A1 (en)	2001-09-27
JP2003528101A (ja)	2003-09-24
OA12227A (en)	2004-03-18
HN2001000040A (es)	2001-09-06
CN1422268A (zh)	2003-06-04
HRP20020798A2 (en)	2004-02-29
EP1268476A1 (en)	2003-01-02
EE200200506A (et)	2004-02-16

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AU2003237009A1 (en)	2003-09-18	2-(pyridin-2-ylamino)-pyrido[2,3d]pyrimidin-7-ones
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WO2005082903A1 (en)	2005-09-09	2-(pyridin-3-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
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KR20170023872A (ko)	2017-03-06	특정한 단백질 키나아제 억제제
TWI464170B (zh)	2014-12-11	５-酮基-５，８-二氫吡啶并［２，３-ｄ］嘧啶衍生物，其製備及其治療用途
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