JP2013507425A5 - - Google Patents
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- Publication number
- JP2013507425A5 JP2013507425A5 JP2012533621A JP2012533621A JP2013507425A5 JP 2013507425 A5 JP2013507425 A5 JP 2013507425A5 JP 2012533621 A JP2012533621 A JP 2012533621A JP 2012533621 A JP2012533621 A JP 2012533621A JP 2013507425 A5 JP2013507425 A5 JP 2013507425A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- group
- alkoxy
- heterocycle
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 51
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
- -1 —OH Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000005199 aryl carbonyloxy group Chemical group 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 238000006482 condensation reaction Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 0 Cc(c1c2C)n[n](*)c1nc(*)c2O* Chemical compound Cc(c1c2C)n[n](*)c1nc(*)c2O* 0.000 description 2
- RRFNWGMAKPDEEH-UHFFFAOYSA-N CCOC(c(c(-c(cc1)ccc1OC)c12)c(-c3ccccc3)nc1[nH]nc2N)=O Chemical compound CCOC(c(c(-c(cc1)ccc1OC)c12)c(-c3ccccc3)nc1[nH]nc2N)=O RRFNWGMAKPDEEH-UHFFFAOYSA-N 0.000 description 1
- LISFGXYHGCXVNX-UHFFFAOYSA-N CCOC(c(c(-c1c[nH]c2c1cccc2)c12)c(-c3ccccc3)nc1NNC2(C)N)=O Chemical compound CCOC(c(c(-c1c[nH]c2c1cccc2)c12)c(-c3ccccc3)nc1NNC2(C)N)=O LISFGXYHGCXVNX-UHFFFAOYSA-N 0.000 description 1
- PUMDULYJJANIOC-UHFFFAOYSA-N N#Cc(c(-c(cc1)ccc1Cl)c12)c(-c3ccccc3)nc1[nH]nc2-c(cc1)ccc1Cl Chemical compound N#Cc(c(-c(cc1)ccc1Cl)c12)c(-c3ccccc3)nc1[nH]nc2-c(cc1)ccc1Cl PUMDULYJJANIOC-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0957140 | 2009-10-13 | ||
| FR0957140A FR2951172B1 (fr) | 2009-10-13 | 2009-10-13 | Derives pyrazolopyridines en tant qu'agent anticancereux |
| US25428509P | 2009-10-23 | 2009-10-23 | |
| US61/254,285 | 2009-10-23 | ||
| PCT/EP2010/065346 WO2011045344A1 (en) | 2009-10-13 | 2010-10-13 | Pyrazolopyridine derivatives as anticancer agent |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013507425A JP2013507425A (ja) | 2013-03-04 |
| JP2013507425A5 true JP2013507425A5 (https=) | 2013-11-07 |
| JP5833010B2 JP5833010B2 (ja) | 2015-12-16 |
Family
ID=42112290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533621A Expired - Fee Related JP5833010B2 (ja) | 2009-10-13 | 2010-10-13 | 抗癌剤としてのピラゾロピリジン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8889711B2 (https=) |
| EP (1) | EP2488519B1 (https=) |
| JP (1) | JP5833010B2 (https=) |
| FR (1) | FR2951172B1 (https=) |
| WO (1) | WO2011045344A1 (https=) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| DE102011105469A1 (de) * | 2011-06-24 | 2012-12-27 | Merck Patent Gmbh | 7-Azaindolderivate |
| WO2013045413A1 (en) * | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US10138235B2 (en) | 2011-12-14 | 2018-11-27 | Sanofi | Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof |
| FR2984325A1 (fr) * | 2011-12-14 | 2013-06-21 | Sanofi Sa | Derives de pyrazolopyridine, leur procede de preparation et leur application en therapeutique |
| FR2985257B1 (fr) * | 2011-12-28 | 2014-02-14 | Sanofi Sa | Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique |
| CN103214470A (zh) * | 2012-01-18 | 2013-07-24 | 杨更亮 | 酮类与吲哚衍生物反应合成的新型抗癌化合物 |
| WO2013167403A1 (en) * | 2012-05-09 | 2013-11-14 | Sanofi | Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors |
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori fgfr |
| HK1207375A1 (en) | 2012-06-14 | 2016-01-29 | Daiichi Sankyo Company, Limited | Piperidinylpyrazolopyridine derivative |
| EP2867236B1 (en) | 2012-06-29 | 2017-06-14 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 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 |
| US9045477B2 (en) | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US9776996B2 (en) | 2013-03-15 | 2017-10-03 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| EP3083618B1 (en) | 2013-12-17 | 2018-02-21 | Pfizer Inc | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
| WO2016012896A1 (en) | 2014-07-24 | 2016-01-28 | Pfizer Inc. | Pyrazolopyrimidine compounds |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016115272A1 (en) | 2015-01-13 | 2016-07-21 | Vanderbilt University | Benzothiazole and benzisothiazole-substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TWI712601B (zh) | 2015-02-20 | 2020-12-11 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| WO2016205460A1 (en) * | 2015-06-16 | 2016-12-22 | Nantbioscience, Inc. | Polycyclic derivatives targeting ral gtpases and their therapeutical applications |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| RU2722149C1 (ru) | 2015-09-14 | 2020-05-27 | Пфайзер Инк. | Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2 |
| KR102482673B1 (ko) * | 2016-07-05 | 2022-12-30 | 광저우 맥시노벨 파마수티컬스 씨오., 엘티디. | 방향족 아세틸렌 또는 방향족 에틸렌계 화합물, 그의 중간체, 제조 방법, 약물 조성물 및 용도 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| AR111473A1 (es) * | 2017-04-19 | 2019-07-17 | Sumitomo Chemical Co | Método para la preparación de compuesto de piridina |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| AU2018312349A1 (en) | 2017-08-01 | 2020-02-06 | Theravance Biopharma R&D Ip, Llc | Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors |
| CN109988144B (zh) | 2017-12-29 | 2024-07-05 | 广州再极医药科技有限公司 | 芳香乙烯或芳香乙基类衍生物、其制备方法、中间体、药物组合物及应用 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物 |
| AU2019262579B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Salts of an FGFR inhibitor |
| HRP20241288T1 (hr) | 2018-05-04 | 2024-12-06 | Incyte Corporation | Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| CN113498352A (zh) | 2019-01-23 | 2021-10-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| JP7832891B2 (ja) | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤の誘導体 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TW202246259A (zh) * | 2021-01-29 | 2022-12-01 | 瑞士商赫孚孟拉羅股份公司 | 吡唑醯胺衍生物 |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN119968359A (zh) * | 2022-09-29 | 2025-05-09 | 英矽智能科技知识产权有限公司 | Tead抑制剂及其使用方法 |
| WO2025190406A1 (en) * | 2024-03-15 | 2025-09-18 | Insilico Medicine Ip Limited | Tead inhibitor combinations and uses thereof |
| WO2025209524A1 (en) * | 2024-04-03 | 2025-10-09 | Insilico Medicine Ip Limited | Crystalline tead inhibitor and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE84533T1 (de) * | 1985-12-13 | 1993-01-15 | American Cyanamid Co | Neue kondensierte pyridinverbindungen, zwischenverbindungen fuer die herstellung und ihre verwendung als herbizide wirkstoffe. |
| US4822799A (en) * | 1988-01-27 | 1989-04-18 | Sandoz Pharm. Corp. | Pyrazolopyridine analogs of mevalonolactone and derivatives thereof useful for inhibiting cholesterol biosynthesis in mammals |
| WO2003068773A1 (en) * | 2002-02-12 | 2003-08-21 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| AU2003250539A1 (en) | 2002-08-07 | 2004-02-25 | Mitsubishi Pharma Corporation | Dihydropyrazolopyridine compounds |
| US20040142978A1 (en) * | 2002-12-12 | 2004-07-22 | Pharmacia Corporation | Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase-2 |
| US7468376B2 (en) * | 2003-02-27 | 2008-12-23 | Palau Pharma, S.A. | Pyrazolopyridine derivates |
| EP1648455A4 (en) * | 2003-07-23 | 2009-03-04 | Exelixis Inc | MODULATORS OF ALK PROTEIN (ANAPLASTIC LYMPHOMA KINASE) AND METHODS OF USE |
| DE602005011286D1 (en) * | 2004-07-05 | 2009-01-08 | Astellas Pharma Inc | Pyrazolopyridinderivate |
| KR101011958B1 (ko) * | 2005-08-25 | 2011-01-31 | 에프. 호프만-라 로슈 아게 | ｐ38 ＭＡＰ 키나아제 저해제로서의 융합형 피라졸 |
| WO2009006580A1 (en) * | 2007-07-05 | 2009-01-08 | Cv Therapeutics, Inc. | Optionally condensed dihydropyridine, dihydropyrimidine and dihydropyrane derivatives acting as late sodium channel blockers |
| US20100113415A1 (en) * | 2008-05-29 | 2010-05-06 | Rajapakse Hemaka A | Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer |
-
2009
- 2009-10-13 FR FR0957140A patent/FR2951172B1/fr not_active Expired - Fee Related
-
2010
- 2010-10-13 US US13/500,757 patent/US8889711B2/en not_active Expired - Fee Related
- 2010-10-13 WO PCT/EP2010/065346 patent/WO2011045344A1/en not_active Ceased
- 2010-10-13 EP EP10770774.7A patent/EP2488519B1/en not_active Not-in-force
- 2010-10-13 JP JP2012533621A patent/JP5833010B2/ja not_active Expired - Fee Related
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