JP6721521B2 - ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体 - Google Patents
ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体 Download PDFInfo
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- JP6721521B2 JP6721521B2 JP2016572754A JP2016572754A JP6721521B2 JP 6721521 B2 JP6721521 B2 JP 6721521B2 JP 2016572754 A JP2016572754 A JP 2016572754A JP 2016572754 A JP2016572754 A JP 2016572754A JP 6721521 B2 JP6721521 B2 JP 6721521B2
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- amino
- methyl
- phenyl
- pyrazolo
- mmol
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- GWMDCERRKJAJGA-UHFFFAOYSA-N CC(C)C1C[N](C)(C)CCCC1 Chemical compound CC(C)C1C[N](C)(C)CCCC1 GWMDCERRKJAJGA-UHFFFAOYSA-N 0.000 description 1
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- YTTQOMVXHXPZGL-HXUWFJFHSA-N Cc1c(C(NCc(cc2)ccc2-c2n[n]([C@H](CCC3)CN3C(C=C)=O)c3ncnc(N)c23)=O)c(F)ccc1 Chemical compound Cc1c(C(NCc(cc2)ccc2-c2n[n]([C@H](CCC3)CN3C(C=C)=O)c3ncnc(N)c23)=O)c(F)ccc1 YTTQOMVXHXPZGL-HXUWFJFHSA-N 0.000 description 1
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- AVGRLHLHTFUIFX-ZHACJKMWSA-N S/N=C(\CCC1)/c2cc1ccc2 Chemical compound S/N=C(\CCC1)/c2cc1ccc2 AVGRLHLHTFUIFX-ZHACJKMWSA-N 0.000 description 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N c1ccccc1 Chemical compound c1ccccc1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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| PCT/GB2015/051719 WO2015189620A1 (en) | 2014-06-11 | 2015-06-11 | Pyrazolopyrimidine derivatives useful as inhibitors of bruton's tyrosine kinase |
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| CN114685516A (zh) * | 2015-09-16 | 2022-07-01 | 洛克索肿瘤学股份有限公司 | 用于治疗癌症的作为btk抑制剂的吡唑并嘧啶衍生物 |
| PT3390395T (pt) | 2015-12-16 | 2020-11-03 | Loxo Oncology Inc | Compostos úteis como inibidores de quinase |
| US9630968B1 (en) | 2015-12-23 | 2017-04-25 | Arqule, Inc. | Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof |
| PH12018501390B1 (en) * | 2015-12-23 | 2022-06-10 | Arqule Inc | Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof |
| IL260691B (en) * | 2016-01-21 | 2022-07-01 | Zibo Biopolar Changsheng Pharmaceutical Co Ltd | Bruton's tyrosine kinase inhibitors |
| KR102327917B1 (ko) * | 2016-07-07 | 2021-11-17 | 주식회사 대웅제약 | 신규한 4-아미노피라졸로[3,4-d]피리미디닐아자바이사이클로 유도체 및 이를 포함하는 약학 조성물 |
| BR112019003504A2 (pt) | 2016-08-24 | 2019-05-21 | Arqule, Inc. | compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos |
| WO2019130229A1 (en) * | 2017-12-28 | 2019-07-04 | Mylan Laboratories Ltd | Methods and intermediates for preparing rucaparib |
| US20220362357A1 (en) | 2018-08-31 | 2022-11-17 | Stichting Radboud Universitair Medisch Centrum | Synergistic Combinations of Amino Acid Depletion Agent Sensitizers (AADAS) and Amino Acid Depletion Agents (AADA), and Therapeutic Methods of Use Thereof |
| EP4069689A4 (en) * | 2019-12-04 | 2023-12-20 | Henan Zhiwei Biomedicine Co., Ltd. | SUBSTITUTED IMIDAZOLECARBOXAMIDE AS BRUTON TYROSINKINASE INHIBITORS |
| JP7011638B2 (ja) * | 2019-12-16 | 2022-02-10 | アークル インコーポレイテッド | テトラヒドロピラニルアミノ-ピロロピリミジノンおよびその使用の方法 |
| CN113214265B (zh) * | 2020-01-21 | 2023-07-07 | 江苏先声药业有限公司 | 嘧啶并五元环类化合物 |
| RU2747991C1 (ru) * | 2020-02-18 | 2021-05-18 | Аркьюл, Инк. | Тетрагидропиранил амино-пирролопиримидинон и способы его применения |
| EP4118086A1 (en) * | 2020-03-12 | 2023-01-18 | Fochon Biosciences, Ltd. | Compounds useful as kinase inhibitors |
| CN114075190A (zh) * | 2020-08-20 | 2022-02-22 | 北京诺诚健华医药科技有限公司 | 杂环类btk抑制剂 |
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| TR200201505T2 (tr) | 1999-09-17 | 2003-01-21 | Abbott Gmbh & Co.Kg | Terapötik maddeler olarak pirazolopirimidinler |
| US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| US20030225098A1 (en) | 2002-03-21 | 2003-12-04 | Hirst Gavin C. | Kinase inhibitors |
| SG166093A1 (en) * | 2006-09-22 | 2010-11-29 | Pharmacyclics Inc | Inhibitors of brutonæs tyrosine kinase |
| US8987233B2 (en) | 2006-11-03 | 2015-03-24 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| CN101674834B (zh) * | 2007-03-28 | 2013-06-12 | 环状药物公司 | 布鲁顿氏酪氨酸激酶(Bruton's tyrosine kinase)抑制剂 |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NZ624345A (en) | 2008-06-27 | 2016-07-29 | Celgene Avilomics Res Inc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| CA2730930C (en) * | 2008-07-16 | 2015-01-13 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| JP5385382B2 (ja) | 2008-07-24 | 2014-01-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | プロテインキナーゼ阻害剤としての3,4−ジアリールピラゾール |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| US7741330B1 (en) * | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| NZ717373A (en) | 2010-06-03 | 2017-11-24 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| AU2012255759C1 (en) | 2011-05-17 | 2025-10-23 | Principia Biopharma, Inc. | Kinase inhibitors |
| KR102027598B1 (ko) | 2011-05-17 | 2019-10-01 | 프린시피아 바이오파마, 인코퍼레이티드 | 타이로신 키나아제 저해제 |
| MX2014000518A (es) * | 2011-07-13 | 2014-05-30 | Pharmacyclics Inc | Inhibidores de la tirosina quinasa de bruton. |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| US8377946B1 (en) * | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| EP2861599B1 (en) | 2012-06-18 | 2019-12-18 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment of cancer and autoimmune diseases |
| WO2014022569A1 (en) | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
| KR101668574B1 (ko) | 2012-11-02 | 2016-10-24 | 화이자 인코포레이티드 | 브루톤 티로신 키나제 억제제 |
| CN103848810A (zh) | 2012-11-30 | 2014-06-11 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| GB201309085D0 (en) * | 2013-05-20 | 2013-07-03 | Redx Pharma Ltd | Compounds |
| US9951056B2 (en) | 2013-09-30 | 2018-04-24 | Beijing Innocare Pharma Tech Co., Ltd. | Substituted nicotinamide inhibitors of BTK and their preparation and use in the treatment of cancer, inflammation and autoimmune disease |
| US9637486B2 (en) | 2013-12-20 | 2017-05-02 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| ES2841248T3 (es) | 2014-02-21 | 2021-07-07 | Principia Biopharma Inc | Sales y forma sólida de un inhibidor de BTK |
| GB201404987D0 (en) | 2014-03-20 | 2014-05-07 | Redx Pharma Ltd | Compounds |
| CN105085474B (zh) | 2014-05-07 | 2018-05-18 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
| GB201410430D0 (en) | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| CN114685516A (zh) | 2015-09-16 | 2022-07-01 | 洛克索肿瘤学股份有限公司 | 用于治疗癌症的作为btk抑制剂的吡唑并嘧啶衍生物 |
| PT3390395T (pt) | 2015-12-16 | 2020-11-03 | Loxo Oncology Inc | Compostos úteis como inibidores de quinase |
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