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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (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 |
| ES2421139T3 (es) * | 2003-07-30 | 2013-08-29 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias |
| WO2005105801A1 (en) * | 2004-05-04 | 2005-11-10 | Warner-Lambert Company Llc | Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents |
| ATE540035T1 (de) | 2004-11-24 | 2012-01-15 | Rigel Pharmaceuticals Inc | Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| JP2008540436A (ja) * | 2005-05-03 | 2008-11-20 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｊａｋキナーゼインヒビターおよびそれらの使用 |
| JP2009537520A (ja) * | 2006-05-15 | 2009-10-29 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Ｆｇｆ受容体キナーゼ阻害剤のための組成物および方法 |
| CA2663401C (en) * | 2006-09-15 | 2011-07-12 | Pfizer Products Inc. | Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors |
| 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 |
| 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 |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| 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 |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| 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 |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| CN105683188B (zh) * | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| MA38393B1 (fr) * | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| BR112016022056B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico |
| US10736900B2 (en) | 2014-03-26 | 2020-08-11 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| WO2016027781A1 (ja) | 2014-08-18 | 2016-02-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 単環ピリジン誘導体の塩およびその結晶 |
| ES2756748T3 (es) | 2014-10-03 | 2020-04-27 | Novartis Ag | Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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- 2003-12-11 CA CA002508951A patent/CA2508951A1/en not_active Abandoned
- 2003-12-11 EP EP03785789A patent/EP1581531B1/en not_active Expired - Lifetime
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- 2003-12-11 BR BR0317480-8A patent/BR0317480A/pt not_active IP Right Cessation
- 2003-12-11 WO PCT/EP2003/014067 patent/WO2004056822A1/en not_active Ceased
- 2003-12-11 ES ES03785789T patent/ES2300639T3/es not_active Expired - Lifetime
- 2003-12-11 KR KR1020057011681A patent/KR100763298B1/ko not_active Expired - Fee Related
- 2003-12-11 DE DE60319430T patent/DE60319430T2/de not_active Expired - Lifetime
- 2003-12-11 JP JP2004561276A patent/JP2006511563A/ja active Pending
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| 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 |
|---|---|
| EP1581531A1 (en) | 2005-10-05 |
| WO2004056822A1 (en) | 2004-07-08 |
| JP2006511563A (ja) | 2006-04-06 |
| EP1581531B1 (en) | 2008-02-27 |
| DE60319430D1 (de) | 2008-04-10 |
| ATE387445T1 (de) | 2008-03-15 |
| US7098332B2 (en) | 2006-08-29 |
| AU2003294830B2 (en) | 2009-06-11 |
| RU2005122901A (ru) | 2006-02-27 |
| BR0317480A (pt) | 2005-11-16 |
| DE60319430T2 (de) | 2009-02-26 |
| KR100763298B1 (ko) | 2007-10-04 |
| ES2300639T3 (es) | 2008-06-16 |
| AU2003294830A1 (en) | 2004-07-14 |
| PL377661A1 (pl) | 2006-02-06 |
| MXPA05006437A (es) | 2005-08-19 |
| CA2508951A1 (en) | 2004-07-08 |
| KR20050088202A (ko) | 2005-09-02 |
| US20040122029A1 (en) | 2004-06-24 |
| AR042532A1 (es) | 2005-06-22 |
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