JP2014504622A5 - - Google Patents
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- Publication number
- JP2014504622A5 JP2014504622A5 JP2013552207A JP2013552207A JP2014504622A5 JP 2014504622 A5 JP2014504622 A5 JP 2014504622A5 JP 2013552207 A JP2013552207 A JP 2013552207A JP 2013552207 A JP2013552207 A JP 2013552207A JP 2014504622 A5 JP2014504622 A5 JP 2014504622A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- nhc
- cycloalkyl
- alkynyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 61
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 20
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 18
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 18
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 5
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000000824 cytostatic agent Substances 0.000 claims 1
- 230000001085 cytostatic effect Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 0 Cc1cc(O*)cnc1 Chemical compound Cc1cc(O*)cnc1 0.000 description 3
- PYDFXCVDNUZZTC-UHFFFAOYSA-N CCCS(Nc(c(F)c1-[n](cc2-c3cncnc3)c(cc3)c2nc3N(C)C2CCN(CC(C)(C)O)CC2)ccc1F)(=O)=O Chemical compound CCCS(Nc(c(F)c1-[n](cc2-c3cncnc3)c(cc3)c2nc3N(C)C2CCN(CC(C)(C)O)CC2)ccc1F)(=O)=O PYDFXCVDNUZZTC-UHFFFAOYSA-N 0.000 description 1
- TWGNOYAGHYUFFR-UHFFFAOYSA-N Cc1cncnc1 Chemical compound Cc1cncnc1 TWGNOYAGHYUFFR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11153087.9 | 2011-02-02 | ||
| EP11153087 | 2011-02-02 | ||
| EP11181258.2 | 2011-09-14 | ||
| EP11181258 | 2011-09-14 | ||
| PCT/EP2012/051796 WO2012104388A1 (en) | 2011-02-02 | 2012-02-02 | New azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014504622A JP2014504622A (ja) | 2014-02-24 |
| JP2014504622A5 true JP2014504622A5 (enExample) | 2015-03-19 |
| JP5850952B2 JP5850952B2 (ja) | 2016-02-03 |
Family
ID=45558742
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013552207A Active JP5850952B2 (ja) | 2011-02-02 | 2012-02-02 | セリン／スレオニンキナーゼ阻害剤としての新しいアザインドリルフェニルスルホンアミド |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8889684B2 (enExample) |
| EP (1) | EP2670749B1 (enExample) |
| JP (1) | JP5850952B2 (enExample) |
| KR (1) | KR20140014149A (enExample) |
| CN (1) | CN103476773A (enExample) |
| AU (1) | AU2012213390A1 (enExample) |
| BR (1) | BR112013019714A2 (enExample) |
| CA (1) | CA2825279A1 (enExample) |
| CL (1) | CL2013002063A1 (enExample) |
| EA (1) | EA201300874A1 (enExample) |
| IL (1) | IL227399A0 (enExample) |
| MX (1) | MX2013008868A (enExample) |
| PH (1) | PH12013501618A1 (enExample) |
| UY (1) | UY33890A (enExample) |
| WO (1) | WO2012104388A1 (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20090837A1 (es) | 2007-07-02 | 2009-07-24 | Boehringer Ingelheim Int | Nuevos compuestos quimicos |
| TW201014860A (en) | 2008-09-08 | 2010-04-16 | Boehringer Ingelheim Int | New chemical compounds |
| EA201100564A1 (ru) | 2008-09-29 | 2011-12-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Антипролиферативные соединения |
| US8569316B2 (en) | 2009-02-17 | 2013-10-29 | Boehringer Ingelheim International Gmbh | Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases |
| ES2835553T3 (es) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos |
| CN102821607B (zh) | 2009-12-21 | 2014-12-17 | 萨穆梅德有限公司 | 1H-吡唑并[3，4-b]吡啶及其治疗应用 |
| WO2011117382A1 (en) | 2010-03-26 | 2011-09-29 | Boehringer Ingelheim International Gmbh | Pyridyltriazoles |
| JP5871896B2 (ja) | 2010-03-26 | 2016-03-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂ−ｒａｆキナーゼインヒビター |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| HRP20190281T1 (hr) | 2011-09-14 | 2019-05-31 | Samumed, Llc | Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| PL2770994T3 (pl) | 2012-05-04 | 2020-03-31 | Samumed, Llc | 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne |
| BR112014028424A2 (pt) | 2012-05-22 | 2018-04-24 | Univ North Carolina Chapel Hill | compostos de pirimidina para o tratamento de câncer |
| EP2909211A4 (en) | 2012-10-17 | 2016-06-22 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| EP2925752A4 (en) | 2012-11-27 | 2016-06-01 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| EP2943198B1 (en) | 2013-01-08 | 2019-07-17 | Samumed, LLC | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof |
| CA2906523A1 (en) | 2013-03-15 | 2014-09-25 | Myriad Genetics, Inc. | Genes and gene signatures for diagnosis and treatment of melanoma |
| CA2945128A1 (en) | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Mertk-specific pyrimidine compounds |
| WO2016003810A1 (en) | 2014-07-02 | 2016-01-07 | Myriad Genetics, Inc. | Genes and gene signatures for diagnosis and treatment of melanoma |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| US10239881B2 (en) | 2014-10-27 | 2019-03-26 | University Health Network | RIPK2 inhibitors and method of treating cancer with same |
| US10285982B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| WO2017023975A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10519169B2 (en) | 2015-08-03 | 2019-12-31 | Samumed, Llc | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024015A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10166218B2 (en) | 2015-08-03 | 2019-01-01 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10392383B2 (en) | 2015-08-03 | 2019-08-27 | Samumed, Llc | 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017023986A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023984A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| WO2017023987A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| WO2017023972A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10231956B2 (en) | 2015-08-03 | 2019-03-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10188634B2 (en) | 2015-08-03 | 2019-01-29 | Samumed, Llc | 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10285983B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof |
| WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017024010A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| EP3336090B1 (en) * | 2015-08-13 | 2020-07-22 | Beijing Hanmi Pharmaceutical Co., Ltd. | Irak4 inhibitor and use thereof |
| KR20180080262A (ko) | 2015-11-06 | 2018-07-11 | 사뮤메드, 엘엘씨 | 골관절염의 치료 |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| AR108325A1 (es) | 2016-04-27 | 2018-08-08 | Samumed Llc | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas |
| ES2933109T3 (es) | 2016-06-01 | 2023-02-02 | Biosplice Therapeutics Inc | Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida |
| CN110709082A (zh) | 2016-10-21 | 2020-01-17 | 萨穆梅德有限公司 | 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途 |
| KR102558716B1 (ko) | 2016-11-07 | 2023-07-21 | 사뮤메드, 엘엘씨 | 단일-투여량, 즉시-사용가능한 주사용 제제 |
| DK3689868T3 (da) | 2016-12-01 | 2024-01-02 | Arvinas Operations Inc | Tetrahydronaphthalen- og tetrahydroisoquinolinderivater som østrogenreceptordegraderende midler |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| AU2017382436C1 (en) * | 2016-12-23 | 2021-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of Rapidly Accelerated Fibrosarcoma polypeptides |
| JP7230041B2 (ja) * | 2017-10-26 | 2023-02-28 | ザイノミック・ファーマシューティカルズ・インコーポレイテッド | Ｂ－ｒａｆキナーゼ阻害物質の結晶塩 |
| IL290789B2 (en) | 2019-08-26 | 2025-09-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| CN116390916A (zh) | 2020-09-14 | 2023-07-04 | 阿尔维纳斯运营股份有限公司 | 用于靶向降解雌激素受体的化合物的结晶形式 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| CN115010574B (zh) * | 2022-06-06 | 2024-01-05 | 爱斯特（成都）生物制药股份有限公司 | 1-溴-2-氯-4-氟-2碘苯的合成方法 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
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| CN1326457A (zh) * | 1998-09-18 | 2001-12-12 | 巴斯福股份公司 | 作为激酶抑制剂的4－氨基吡咯并嘧啶 |
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| JP2013503188A (ja) * | 2009-08-28 | 2013-01-31 | アレイ バイオファーマ、インコーポレイテッド | Ｒａｆ阻害化合物およびその使用方法 |
| JP5871896B2 (ja) | 2010-03-26 | 2016-03-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂ−ｒａｆキナーゼインヒビター |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US20130023531A1 (en) | 2011-01-27 | 2013-01-24 | Boehringer Ingelheim International Gmbh | Pyrimido[5,4-d]pyrimidylamino phenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
-
2012
- 2012-01-27 US US13/359,555 patent/US8889684B2/en active Active
- 2012-02-01 UY UY0001033890A patent/UY33890A/es unknown
- 2012-02-02 EP EP12701914.9A patent/EP2670749B1/en active Active
- 2012-02-02 BR BR112013019714A patent/BR112013019714A2/pt not_active IP Right Cessation
- 2012-02-02 MX MX2013008868A patent/MX2013008868A/es not_active Application Discontinuation
- 2012-02-02 CN CN2012800157100A patent/CN103476773A/zh active Pending
- 2012-02-02 CA CA2825279A patent/CA2825279A1/en not_active Abandoned
- 2012-02-02 AU AU2012213390A patent/AU2012213390A1/en not_active Abandoned
- 2012-02-02 JP JP2013552207A patent/JP5850952B2/ja active Active
- 2012-02-02 EA EA201300874A patent/EA201300874A1/ru unknown
- 2012-02-02 WO PCT/EP2012/051796 patent/WO2012104388A1/en not_active Ceased
- 2012-02-02 PH PH1/2013/501618A patent/PH12013501618A1/en unknown
- 2012-02-02 KR KR1020137022388A patent/KR20140014149A/ko not_active Withdrawn
-
2013
- 2013-07-09 IL IL227399A patent/IL227399A0/en unknown
- 2013-07-17 CL CL2013002063A patent/CL2013002063A1/es unknown
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