RU2345077C2 - ПРОИЗВОДНЫЕ ПИРИДИНО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ СЕЛЕКТИВНЫХ ИНГИБИТОРОВ KDR И FGFR - Google Patents
ПРОИЗВОДНЫЕ ПИРИДИНО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ СЕЛЕКТИВНЫХ ИНГИБИТОРОВ KDR И FGFR Download PDFInfo
- Publication number
- RU2345077C2 RU2345077C2 RU2005122901/04A RU2005122901A RU2345077C2 RU 2345077 C2 RU2345077 C2 RU 2345077C2 RU 2005122901/04 A RU2005122901/04 A RU 2005122901/04A RU 2005122901 A RU2005122901 A RU 2005122901A RU 2345077 C2 RU2345077 C2 RU 2345077C2
- Authority
- RU
- Russia
- Prior art keywords
- phenyl
- compounds
- alkyl
- propionic acid
- formula
- Prior art date
Links
- 108091008794 FGF receptors Proteins 0.000 title claims abstract 4
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 title claims abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title abstract 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 title 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 14
- 125000001424 substituent group Chemical group 0.000 claims abstract 7
- 229910052736 halogen Inorganic materials 0.000 claims abstract 6
- 150000002367 halogens Chemical class 0.000 claims abstract 6
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 206010028980 Neoplasm Diseases 0.000 claims abstract 2
- 201000011510 cancer Diseases 0.000 claims abstract 2
- 229940079593 drug Drugs 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims abstract 2
- -1 3- (methyl 2,4-diphenylaminopyrimidin-5-yl) -2- (3,5-dimethoxyphenyl) propionic acid Chemical compound 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 3
- LDBUGKOPMCHTDP-UHFFFAOYSA-N 2-anilino-6,8-diphenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C=3C=CC=CC=3)C(=O)C(C=3C=CC=CC=3)CC2=CN=C1NC1=CC=CC=C1 LDBUGKOPMCHTDP-UHFFFAOYSA-N 0.000 claims 1
- JRQIBVOYUXEJIW-UHFFFAOYSA-N 2-anilino-6-(2,5-dimethoxyphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound COC1=CC=C(OC)C(C2C(N(C3=NC(NC=4C=CC=CC=4)=NC=C3C2)C=2C=CC=CC=2)=O)=C1 JRQIBVOYUXEJIW-UHFFFAOYSA-N 0.000 claims 1
- GIGAZROYAJXXTN-UHFFFAOYSA-N 2-anilino-6-(2,6-dichlorophenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound ClC1=CC=CC(Cl)=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 GIGAZROYAJXXTN-UHFFFAOYSA-N 0.000 claims 1
- OEMYZUFXEPIMDM-UHFFFAOYSA-N 2-anilino-6-(2-methoxyphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound COC1=CC=CC=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 OEMYZUFXEPIMDM-UHFFFAOYSA-N 0.000 claims 1
- GETIOEHNGKCANU-UHFFFAOYSA-N 2-anilino-6-(2-methylphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound CC1=CC=CC=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 GETIOEHNGKCANU-UHFFFAOYSA-N 0.000 claims 1
- QUIYHXLKXVLUBW-UHFFFAOYSA-N 2-anilino-6-(3,4-dimethoxyphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound C1=C(OC)C(OC)=CC=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 QUIYHXLKXVLUBW-UHFFFAOYSA-N 0.000 claims 1
- SSDDMPJZNWJRCN-UHFFFAOYSA-N 2-anilino-6-(3,5-dimethoxyphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound COC1=CC(OC)=CC(C2C(N(C3=NC(NC=4C=CC=CC=4)=NC=C3C2)C=2C=CC=CC=2)=O)=C1 SSDDMPJZNWJRCN-UHFFFAOYSA-N 0.000 claims 1
- HNJCPWULRKXSLE-UHFFFAOYSA-N 2-anilino-6-(4-methoxyphenyl)-8-(2-methylpropyl)-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1C1C(=O)N(CC(C)C)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 HNJCPWULRKXSLE-UHFFFAOYSA-N 0.000 claims 1
- WMRQLRVQUZGQAU-UHFFFAOYSA-N 2-anilino-6-(4-methoxyphenyl)-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 WMRQLRVQUZGQAU-UHFFFAOYSA-N 0.000 claims 1
- APFYHLDWEOGXQM-UHFFFAOYSA-N 2-anilino-6-[3,5-bis(trifluoromethyl)phenyl]-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C2C(N(C3=NC(NC=4C=CC=CC=4)=NC=C3C2)C=2C=CC=CC=2)=O)=C1 APFYHLDWEOGXQM-UHFFFAOYSA-N 0.000 claims 1
- DGBNPJFTEKXMIB-UHFFFAOYSA-N 2-anilino-8-(cyclopropylmethyl)-6-(4-methoxyphenyl)-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1C1C(=O)N(CC2CC2)C2=NC(NC=3C=CC=CC=3)=NC=C2C1 DGBNPJFTEKXMIB-UHFFFAOYSA-N 0.000 claims 1
- QEAQQVNPEOCGOV-UHFFFAOYSA-N 2-anilino-8-phenyl-6-pyridin-3-yl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C=3C=CC=CC=3)C(=O)C(C=3C=NC=CC=3)CC2=CN=C1NC1=CC=CC=C1 QEAQQVNPEOCGOV-UHFFFAOYSA-N 0.000 claims 1
- PJTGIOFFDNLJBZ-UHFFFAOYSA-N 2-anilino-8-phenyl-6-pyridin-4-yl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C=3C=CC=CC=3)C(=O)C(C=3C=CN=CC=3)CC2=CN=C1NC1=CC=CC=C1 PJTGIOFFDNLJBZ-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- DRSMPFSBTJWOFI-UHFFFAOYSA-N 6-(4-methoxyphenyl)-2-[(6-methoxypyridin-3-yl)amino]-8-phenyl-5,6-dihydropyrido[2,3-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1C1C(=O)N(C=2C=CC=CC=2)C2=NC(NC=3C=NC(OC)=CC=3)=NC=C2C1 DRSMPFSBTJWOFI-UHFFFAOYSA-N 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- 229940124639 Selective inhibitor Drugs 0.000 claims 1
- 235000001484 Trigonella foenum graecum Nutrition 0.000 claims 1
- 244000250129 Trigonella foenum graecum Species 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- COFYLUNQQJILFO-UHFFFAOYSA-N ethyl 3-(2,4-dianilinopyrimidin-5-yl)-2-(2,5-dimethoxyphenyl)propanoate Chemical compound C=1C(OC)=CC=C(OC)C=1C(C(=O)OCC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=CC=C1 COFYLUNQQJILFO-UHFFFAOYSA-N 0.000 claims 1
- JVJSOURCIHXXBR-UHFFFAOYSA-N ethyl 3-(2,4-dianilinopyrimidin-5-yl)-2-pyridin-4-ylpropanoate Chemical compound C=1C=NC=CC=1C(C(=O)OCC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=CC=C1 JVJSOURCIHXXBR-UHFFFAOYSA-N 0.000 claims 1
- 125000004494 ethyl ester group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- TVFFUJKYOVNIPR-UHFFFAOYSA-N methyl 2-(2,6-dichlorophenyl)-3-(2,4-dichloropyrimidin-5-yl)propanoate Chemical compound ClC=1C=CC=C(Cl)C=1C(C(=O)OC)CC1=CN=C(Cl)N=C1Cl TVFFUJKYOVNIPR-UHFFFAOYSA-N 0.000 claims 1
- XMWRLCCDUVRRBL-UHFFFAOYSA-N methyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-(2,4-dianilinopyrimidin-5-yl)propanoate Chemical compound C=1C(C(F)(F)F)=CC(C(F)(F)F)=CC=1C(C(=O)OC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=CC=C1 XMWRLCCDUVRRBL-UHFFFAOYSA-N 0.000 claims 1
- UHPDMTRIBIJMNL-UHFFFAOYSA-N methyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-(2,4-dichloropyrimidin-5-yl)propanoate Chemical compound C=1C(C(F)(F)F)=CC(C(F)(F)F)=CC=1C(C(=O)OC)CC1=CN=C(Cl)N=C1Cl UHPDMTRIBIJMNL-UHFFFAOYSA-N 0.000 claims 1
- IGUJOLYSXPXQGN-UHFFFAOYSA-N methyl 3-(2,4-dianilinopyrimidin-5-yl)-2-(2-methylphenyl)propanoate Chemical compound C=1C=CC=C(C)C=1C(C(=O)OC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=CC=C1 IGUJOLYSXPXQGN-UHFFFAOYSA-N 0.000 claims 1
- SDXRQYLJBJOROB-UHFFFAOYSA-N methyl 3-(2,4-dianilinopyrimidin-5-yl)-2-phenylpropanoate Chemical compound C=1C=CC=CC=1C(C(=O)OC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=CC=C1 SDXRQYLJBJOROB-UHFFFAOYSA-N 0.000 claims 1
- BNSNEYFSBZJQHZ-UHFFFAOYSA-N methyl 3-(2,4-dichloropyrimidin-5-yl)-2-(3,5-dimethoxyphenyl)propanoate Chemical compound C=1C(OC)=CC(OC)=CC=1C(C(=O)OC)CC1=CN=C(Cl)N=C1Cl BNSNEYFSBZJQHZ-UHFFFAOYSA-N 0.000 claims 1
- TUSYAGWZCITOPM-UHFFFAOYSA-N methyl 3-(2,4-dichloropyrimidin-5-yl)-2-(4-methoxyphenyl)propanoate Chemical compound C=1C=C(OC)C=CC=1C(C(=O)OC)CC1=CN=C(Cl)N=C1Cl TUSYAGWZCITOPM-UHFFFAOYSA-N 0.000 claims 1
- WAOGDYLJXXAFTE-UHFFFAOYSA-N methyl 3-(2-anilino-4-chloropyrimidin-5-yl)-2-(4-methoxyphenyl)propanoate Chemical compound C=1C=C(OC)C=CC=1C(C(=O)OC)CC(C(=N1)Cl)=CN=C1NC1=CC=CC=C1 WAOGDYLJXXAFTE-UHFFFAOYSA-N 0.000 claims 1
- AKABDZICYIWPDV-UHFFFAOYSA-N methyl 3-[4-anilino-2-[(6-methoxypyridin-3-yl)amino]pyrimidin-5-yl]-2-(4-methoxyphenyl)propanoate Chemical compound C=1C=C(OC)C=CC=1C(C(=O)OC)CC(C(=N1)NC=2C=CC=CC=2)=CN=C1NC1=CC=C(OC)N=C1 AKABDZICYIWPDV-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical class 0.000 abstract 1
- 210000002429 large intestine Anatomy 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- 210000005075 mammary gland Anatomy 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 150000003222 pyridines Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43496902P | 2002-12-20 | 2002-12-20 | |
| US60/434,969 | 2002-12-20 | ||
| US51361503P | 2003-10-23 | 2003-10-23 | |
| US60/513,615 | 2003-10-23 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2005122901A RU2005122901A (ru) | 2006-02-27 |
| RU2345077C2 true RU2345077C2 (ru) | 2009-01-27 |
Family
ID=32685355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005122901/04A RU2345077C2 (ru) | 2002-12-20 | 2003-12-11 | ПРОИЗВОДНЫЕ ПИРИДИНО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ СЕЛЕКТИВНЫХ ИНГИБИТОРОВ KDR И FGFR |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7098332B2 (enExample) |
| EP (1) | EP1581531B1 (enExample) |
| JP (1) | JP2006511563A (enExample) |
| KR (1) | KR100763298B1 (enExample) |
| AR (1) | AR042532A1 (enExample) |
| AT (1) | ATE387445T1 (enExample) |
| AU (1) | AU2003294830B2 (enExample) |
| BR (1) | BR0317480A (enExample) |
| CA (1) | CA2508951A1 (enExample) |
| DE (1) | DE60319430T2 (enExample) |
| ES (1) | ES2300639T3 (enExample) |
| MX (1) | MXPA05006437A (enExample) |
| PL (1) | PL377661A1 (enExample) |
| RU (1) | RU2345077C2 (enExample) |
| WO (1) | WO2004056822A1 (enExample) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2730503C2 (ru) * | 2015-12-17 | 2020-08-24 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Терапевтическое средство для лечения рака молочной железы |
| US11219619B2 (en) | 2018-03-28 | 2022-01-11 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| RU2809987C2 (ru) * | 2018-12-27 | 2023-12-20 | Ле Лаборатуар Сервье | Гетероциклические ингибиторы mat2a и способы применения для лечения рака |
| US12077534B2 (en) | 2018-12-27 | 2024-09-03 | Les Laboratoires Servier | Aza-heterobicyclic inhibitors of MAT2A and methods of use for treating cancer |
| US12364690B2 (en) | 2015-03-25 | 2025-07-22 | National Cancer Center | Therapeutic agent for bile duct cancer |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| IL166241A0 (en) * | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| RS53109B (sr) | 2003-07-30 | 2014-06-30 | Rigel Pharmaceuticals Inc. | Jedinjenja 2,4 pirimidindiamina za upotrebu u tretmanu ili prevenciji autoimunih bolesti |
| ES2292130T3 (es) * | 2004-05-04 | 2008-03-01 | Warner-Lambert Company Llc | Pirido(2,3-d)pirimidin-7-onas pirrolil-sustituidas y derivados de las mismas como agentes terapeuticos. |
| ES2380550T3 (es) * | 2004-11-24 | 2012-05-16 | Rigel Pharmaceuticals, Inc. | Compuestos de espiro-2,4-pirimidindiamina y sus usos |
| CA2604551A1 (en) * | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
| WO2007136465A2 (en) * | 2006-05-15 | 2007-11-29 | Irm Llc | Compositions and methods for fgf receptor kinases inhibitors |
| ATE514695T1 (de) * | 2006-09-15 | 2011-07-15 | Pfizer Prod Inc | Pyrido(2,3-d)pyrimidinonverbindungen und ihre verwendung als pi3-inhibitoren |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| US9663524B2 (en) * | 2013-03-15 | 2017-05-30 | Celgene Car Llc | Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors |
| UA120248C2 (uk) | 2013-03-15 | 2019-11-11 | Селджен Кар Ллс | Гетероарильні сполуки та їх застосування |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| EP3060563B1 (en) * | 2013-10-25 | 2018-05-02 | Novartis AG | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| MX370099B (es) | 2014-03-26 | 2019-12-02 | Astex Therapeutics Ltd | Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer. |
| MX369646B (es) | 2014-08-18 | 2019-11-15 | Eisai R&D Man Co Ltd | Sal de derivado de piridina monociclico y su cristal. |
| PL3200786T3 (pl) | 2014-10-03 | 2020-03-31 | Novartis Ag | Zastosowanie pochodnych pirydylowych o skondensowanym układzie bicyklicznym jako inhibitorów fgfr4 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| SG10201913036RA (en) | 2015-02-20 | 2020-02-27 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| US9802917B2 (en) * | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| WO2017050865A1 (en) | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| JP6898919B2 (ja) | 2015-09-23 | 2021-07-07 | ヤンセン ファーマシューティカ エヌ.ベー. | 新規化合物 |
| US11192890B2 (en) * | 2017-03-03 | 2021-12-07 | Auckland Uniservices Limited | FGFR kinase inhibitors and pharmaceutical uses |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN110914267B (zh) * | 2017-07-19 | 2022-07-12 | 江苏奥赛康药业有限公司 | 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用 |
| PL3788047T3 (pl) | 2018-05-04 | 2025-04-14 | Incyte Corporation | Stałe postacie inhibitora fgfr i sposoby ich otrzymywania |
| KR20210018264A (ko) | 2018-05-04 | 2021-02-17 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| KR20210103498A (ko) | 2018-12-10 | 2021-08-23 | 아이디어야 바이오사이언시스 인코포레이티드 | 메티오닌 아데노실트랜스퍼라제 2a 억제제로서 2-옥소퀴나졸린 유도체 |
| EP3902801A4 (en) * | 2018-12-28 | 2022-12-14 | SPV Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| CR20210670A (es) * | 2019-05-31 | 2022-02-11 | Servier Lab | Inhibidores aza-heterobicíclicos de mat2a y métodos de uso para tratar el cáncer |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7693656B2 (ja) | 2019-10-11 | 2025-06-17 | インサイト・コーポレイション | Cdk2阻害剤としての二環式アミン |
| CR20220169A (es) | 2019-10-14 | 2022-10-27 | Incyte Corp | Heterociclos bicíclicos como inhibidores de fgfr |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN112062770A (zh) * | 2020-08-21 | 2020-12-11 | 台州学院 | 一种稠环二氢吡啶酮的制备方法 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996034867A1 (en) * | 1995-05-03 | 1996-11-07 | Warner-Lambert Company | PYRIDO[2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION |
| RU2191188C2 (ru) * | 1994-11-14 | 2002-10-20 | Варнер-Ламберт Компани | Производные 6-арилпиридо[2,3-d]-пиримидины и -нафтиридины, фармацевтическая композиция, обладающая ингибирующим действием клеточной пролиферации, вызываемой протеиновой тирозинкиназой, и способ ингибирования клеточной пролиферации |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998024432A2 (en) | 1996-12-05 | 1998-06-11 | Sugen, Inc. | Use of indolinone compounds as modulators of protein kinases |
| DE69839338T2 (de) | 1997-02-05 | 2008-07-10 | Warner-Lambert Company Llc | Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation |
| CZ20011394A3 (cs) | 1998-10-23 | 2001-12-12 | F. Hoffmann-La Roche Ag | Derivát bicyklických, dusík obsahujících heterocyklických sloučenin, způsob jeho přípravy a farmaceutický prostředek, který ho obsahuje |
| CA2367867A1 (en) | 1999-03-16 | 2000-09-21 | Shell Internationale Research Maatschappij B.V. | Process for the purification of propylene oxide |
| AR030053A1 (es) | 2000-03-02 | 2003-08-13 | Smithkline Beecham Corp | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
| AU2001277032A1 (en) | 2000-08-04 | 2002-02-18 | Warner Lambert Company | 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido(2,3-d)pyrimidin-7 ones |
| JP2004505974A (ja) | 2000-08-04 | 2004-02-26 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 2−(4−ピリジル)アミノ−6−ジアルキルオキシフェニルピリド〔2,3−d〕ピリミジン−7−オン類の製造方法 |
| EP1315726A1 (en) | 2000-08-31 | 2003-06-04 | F. Hoffmann-La Roche Ag | 7- oxo pyridopyrimidines as inhibitors of cellular proliferation |
| EP1364212B1 (en) * | 2001-03-02 | 2011-02-02 | GPC Biotech AG | Three hybrid assay system |
-
2003
- 2003-12-08 US US10/731,594 patent/US7098332B2/en not_active Expired - Fee Related
- 2003-12-11 DE DE60319430T patent/DE60319430T2/de not_active Expired - Lifetime
- 2003-12-11 EP EP03785789A patent/EP1581531B1/en not_active Expired - Lifetime
- 2003-12-11 RU RU2005122901/04A patent/RU2345077C2/ru not_active IP Right Cessation
- 2003-12-11 BR BR0317480-8A patent/BR0317480A/pt not_active IP Right Cessation
- 2003-12-11 CA CA002508951A patent/CA2508951A1/en not_active Abandoned
- 2003-12-11 AT AT03785789T patent/ATE387445T1/de not_active IP Right Cessation
- 2003-12-11 AU AU2003294830A patent/AU2003294830B2/en not_active Expired - Fee Related
- 2003-12-11 PL PL377661A patent/PL377661A1/pl not_active Application Discontinuation
- 2003-12-11 MX MXPA05006437A patent/MXPA05006437A/es active IP Right Grant
- 2003-12-11 ES ES03785789T patent/ES2300639T3/es not_active Expired - Lifetime
- 2003-12-11 WO PCT/EP2003/014067 patent/WO2004056822A1/en not_active Ceased
- 2003-12-11 JP JP2004561276A patent/JP2006511563A/ja active Pending
- 2003-12-11 KR KR1020057011681A patent/KR100763298B1/ko not_active Expired - Fee Related
- 2003-12-18 AR ARP030104711A patent/AR042532A1/es unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2191188C2 (ru) * | 1994-11-14 | 2002-10-20 | Варнер-Ламберт Компани | Производные 6-арилпиридо[2,3-d]-пиримидины и -нафтиридины, фармацевтическая композиция, обладающая ингибирующим действием клеточной пролиферации, вызываемой протеиновой тирозинкиназой, и способ ингибирования клеточной пролиферации |
| WO1996034867A1 (en) * | 1995-05-03 | 1996-11-07 | Warner-Lambert Company | PYRIDO[2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12364690B2 (en) | 2015-03-25 | 2025-07-22 | National Cancer Center | Therapeutic agent for bile duct cancer |
| RU2730503C2 (ru) * | 2015-12-17 | 2020-08-24 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Терапевтическое средство для лечения рака молочной железы |
| US12414945B2 (en) | 2015-12-17 | 2025-09-16 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
| US11219619B2 (en) | 2018-03-28 | 2022-01-11 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| RU2830169C2 (ru) * | 2018-12-10 | 2024-11-14 | Айдиая Байосайенсиз, Инк. | Производные 2-оксохиназолина как ингибиторы метионин аденозилтрансферазы 2a |
| RU2809987C2 (ru) * | 2018-12-27 | 2023-12-20 | Ле Лаборатуар Сервье | Гетероциклические ингибиторы mat2a и способы применения для лечения рака |
| US12077534B2 (en) | 2018-12-27 | 2024-09-03 | Les Laboratoires Servier | Aza-heterobicyclic inhibitors of MAT2A and methods of use for treating cancer |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004056822A1 (en) | 2004-07-08 |
| ATE387445T1 (de) | 2008-03-15 |
| KR100763298B1 (ko) | 2007-10-04 |
| KR20050088202A (ko) | 2005-09-02 |
| RU2005122901A (ru) | 2006-02-27 |
| EP1581531B1 (en) | 2008-02-27 |
| AR042532A1 (es) | 2005-06-22 |
| DE60319430D1 (de) | 2008-04-10 |
| CA2508951A1 (en) | 2004-07-08 |
| BR0317480A (pt) | 2005-11-16 |
| MXPA05006437A (es) | 2005-08-19 |
| DE60319430T2 (de) | 2009-02-26 |
| JP2006511563A (ja) | 2006-04-06 |
| AU2003294830A1 (en) | 2004-07-14 |
| EP1581531A1 (en) | 2005-10-05 |
| AU2003294830B2 (en) | 2009-06-11 |
| US20040122029A1 (en) | 2004-06-24 |
| US7098332B2 (en) | 2006-08-29 |
| PL377661A1 (pl) | 2006-02-06 |
| ES2300639T3 (es) | 2008-06-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2345077C2 (ru) | ПРОИЗВОДНЫЕ ПИРИДИНО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ СЕЛЕКТИВНЫХ ИНГИБИТОРОВ KDR И FGFR | |
| RU2365588C2 (ru) | Хиназолиновые соединения | |
| RU2481346C2 (ru) | Ингибиторы фосфатидилинозитол-3-киназы | |
| RU2336275C2 (ru) | Пиримидопроизводные, характеризующиеся антипролиферативной активностью, и фармацевтическая композиция | |
| RU2375363C2 (ru) | Пирролотриазиновые производные анилина, полезные в качестве ингибиторов киназы | |
| RU2004130488A (ru) | Пиримидиновые производные | |
| RU2001107897A (ru) | Фармацевтическая композиция для лечения гепатита | |
| RU2018134981A (ru) | Конъюгаты, содержащие ингибиторы RIPK2 | |
| RU2003100504A (ru) | Органические соединения | |
| RU2003115429A (ru) | Производные имида индолилмалеиновой кислоты как ингибиторы протеинкиназы с | |
| DE60142469D1 (de) | Imidinderivate als antineoplastika | |
| RU2004132203A (ru) | Индолилмалеимидные производные | |
| NO2015020I1 (no) | Ceritinib, 5-klor-N-5-metyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oksy]fenyl-N-[2-(propan-2-sulfonyl)fenyl]pyrimidine-2,4-diamin, eller et farmasøytisk akseptabelt salt derav | |
| RU2003116061A (ru) | Тиоэфирзамещенные имидазохинолины | |
| ATE349432T1 (de) | 2-anilino-pyrimidin-derivate als cyclin-abhängige kinase hemmer | |
| JP2004525149A5 (enExample) | ||
| KR970704435A (ko) | 헤테로시클릭 화합물의 도파민-D 리간드로서의 용도(Use of Heterocyclic Compounds as Dopamines-D Ligands) | |
| KR940005566A (ko) | 퀴놀린 화합물 | |
| RU2014152790A (ru) | Пирролопиразоновые ингибиторы танкиразы | |
| RU2401267C2 (ru) | Замещенные производные бензохинолизина | |
| RU2221788C2 (ru) | Оксоциклические соединения мочевины, фармацевтическая композиция, способ лечения | |
| RU2001126725A (ru) | Гетероциклические соединения, их промежуточные продукты и ингибиторы эластазы | |
| KR20110097907A (ko) | 치유적 치료를 위한 hsp90 억제제 | |
| RU99101341A (ru) | 4-оксоциклические соединения мочевины, фармацевтическая композиция, способ лечения | |
| ATE476431T1 (de) | Piperidin- und azetidinderivate als glyt1- inhibitoren |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20101212 |