CN102711765A - 激酶抑制剂 - Google Patents
激酶抑制剂 Download PDFInfo
- Publication number
- CN102711765A CN102711765A CN2010800615701A CN201080061570A CN102711765A CN 102711765 A CN102711765 A CN 102711765A CN 2010800615701 A CN2010800615701 A CN 2010800615701A CN 201080061570 A CN201080061570 A CN 201080061570A CN 102711765 A CN102711765 A CN 102711765A
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- Prior art keywords
- substituted
- unsubstituted
- heteroaryl
- aryl
- alkyl
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- 0 *C(CC#C)C#N Chemical compound *C(CC#C)C#N 0.000 description 8
- LOAHXFVORLJMML-UHFFFAOYSA-N CC(C)NC(CC#N)=O Chemical compound CC(C)NC(CC#N)=O LOAHXFVORLJMML-UHFFFAOYSA-N 0.000 description 1
- WBFGVBDZRKEGJV-GZTJUZNOSA-N Cc(cc1)ccc1-c1c(/C=C(/C(OC)=C)\C#N)[n](CCCN=O)c2c1c(N)ncn2 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(OC)=C)\C#N)[n](CCCN=O)c2c1c(N)ncn2 WBFGVBDZRKEGJV-GZTJUZNOSA-N 0.000 description 1
- UESBCFATMDLSBR-UHFFFAOYSA-N Cc(cc1)ccc1S([n]1c(nccc2)c2c(-c2ccc(C=O)cc2)c1)(=O)=O Chemical compound Cc(cc1)ccc1S([n]1c(nccc2)c2c(-c2ccc(C=O)cc2)c1)(=O)=O UESBCFATMDLSBR-UHFFFAOYSA-N 0.000 description 1
- NDJOLIOBEZICFO-UHFFFAOYSA-N Cc(cc1)ccc1S([n]1c2ncccc2c(Br)c1)(=O)=O Chemical compound Cc(cc1)ccc1S([n]1c2ncccc2c(Br)c1)(=O)=O NDJOLIOBEZICFO-UHFFFAOYSA-N 0.000 description 1
- JBFRGXRQXZOZTA-UHFFFAOYSA-N N#CCC(NCCO)=O Chemical compound N#CCC(NCCO)=O JBFRGXRQXZOZTA-UHFFFAOYSA-N 0.000 description 1
- VVDLREIJMXMLEQ-PXLXIMEGSA-N Nc1c(c(-c(cc2)ccc2Oc2ccccc2)c[n]2-c3cccc(/C=C(/C(NCCO)=O)\C#N)c3)c2ncn1 Chemical compound Nc1c(c(-c(cc2)ccc2Oc2ccccc2)c[n]2-c3cccc(/C=C(/C(NCCO)=O)\C#N)c3)c2ncn1 VVDLREIJMXMLEQ-PXLXIMEGSA-N 0.000 description 1
- WKBFACKTVNZRFV-UHFFFAOYSA-N Nc1c(c(-c(cc2)ccc2Oc2ccccc2)c[n]2-c3cccc(C=O)c3)c2ncn1 Chemical compound Nc1c(c(-c(cc2)ccc2Oc2ccccc2)c[n]2-c3cccc(C=O)c3)c2ncn1 WKBFACKTVNZRFV-UHFFFAOYSA-N 0.000 description 1
- CHVYTAZCPUAVJF-UHFFFAOYSA-N O=Cc(cc12)ccc1[nH]nc2-c1cccnc1 Chemical compound O=Cc(cc12)ccc1[nH]nc2-c1cccnc1 CHVYTAZCPUAVJF-UHFFFAOYSA-N 0.000 description 1
- PREGCWJEJHWTLX-UHFFFAOYSA-N O=Cc1ccc(B2CC2)cc1 Chemical compound O=Cc1ccc(B2CC2)cc1 PREGCWJEJHWTLX-UHFFFAOYSA-N 0.000 description 1
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/416—2,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Communicable Diseases (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
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- AIDS & HIV (AREA)
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26169609P | 2009-11-16 | 2009-11-16 | |
| US61/261,696 | 2009-11-16 | ||
| US33027110P | 2010-04-30 | 2010-04-30 | |
| US61/330,271 | 2010-04-30 | ||
| PCT/US2010/056890 WO2011060440A2 (en) | 2009-11-16 | 2010-11-16 | Kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102711765A true CN102711765A (zh) | 2012-10-03 |
Family
ID=43992477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800615701A Pending CN102711765A (zh) | 2009-11-16 | 2010-11-16 | 激酶抑制剂 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US20130035325A1 (enExample) |
| EP (1) | EP2558099A4 (enExample) |
| JP (1) | JP2013510886A (enExample) |
| CN (1) | CN102711765A (enExample) |
| AU (1) | AU2010319964A1 (enExample) |
| BR (1) | BR112012011528A2 (enExample) |
| CA (1) | CA2781056A1 (enExample) |
| MX (1) | MX2012005678A (enExample) |
| WO (1) | WO2011060440A2 (enExample) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106939002A (zh) * | 2016-01-05 | 2017-07-11 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| WO2017118277A1 (zh) * | 2016-01-05 | 2017-07-13 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| CN111205232A (zh) * | 2020-02-26 | 2020-05-29 | 浙江天宇药业股份有限公司 | 一种替格瑞洛中间体的合成方法 |
| CN116284135A (zh) * | 2023-05-04 | 2023-06-23 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒核苷类化合物的制备方法及其应用 |
| CN116332996A (zh) * | 2023-05-04 | 2023-06-27 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒化合物及其制备方法和应用 |
| CN116410228A (zh) * | 2023-05-04 | 2023-07-11 | 南京颐媛生物医学研究院有限公司 | 一种抗冠状病毒核苷类化合物的制备方法及其应用 |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| ES2770550T3 (es) * | 2011-05-17 | 2020-07-02 | Univ California | Inhibidores de quinasa |
| PL2710005T3 (pl) | 2011-05-17 | 2017-07-31 | Principia Biopharma Inc. | Inhibitory kinazy tyrozynowej |
| AU2013277582B2 (en) | 2012-06-18 | 2017-11-30 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| WO2014036016A1 (en) | 2012-08-31 | 2014-03-06 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| WO2014093230A2 (en) | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| KR20220027271A (ko) | 2014-02-21 | 2022-03-07 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| JP6409116B2 (ja) | 2014-07-07 | 2018-10-17 | チャンスー ヘンルイ メディシン カンパニー,リミテッド | プロテインキナーゼ阻害剤としてのアミノピリダジノン化合物 |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| WO2018005849A1 (en) | 2016-06-29 | 2018-01-04 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| JOP20180094A1 (ar) | 2017-10-18 | 2019-04-18 | Hk Inno N Corp | مركب حلقي غير متجانس كمثبط بروتين كيناز |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| TWI877239B (zh) | 2019-10-14 | 2025-03-21 | 美商普林斯匹亞生物製藥公司 | 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法 |
| BR112022014149A2 (pt) | 2020-01-22 | 2022-09-27 | Principia Biopharma Inc | Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenóxi-fenil)-1h-pirazolo[3,4-d]pirimidina-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrila |
| WO2022251597A1 (en) | 2021-05-28 | 2022-12-01 | Verge Analytics, Inc. | Methods of treating neurological disorders with modulators of ribosomal protein s6 kinase alpha-1 (rsk1) and ribosomal protein s6 kinase alpha-3 (rsk2) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995024190A2 (en) * | 1994-03-07 | 1995-09-14 | Sugen, Inc. | Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof |
| US20070232668A1 (en) * | 2006-03-31 | 2007-10-04 | The Board Of Regents Of The University Of Texas System | Orally Bioavailable Caffeic Acid Related Anticancer Drugs |
| WO2008005954A2 (en) * | 2006-06-30 | 2008-01-10 | The Board Of Regents Of The University Of Texas System | Tryphostin-analogs for the treatment of cell proliferative diseases |
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| US4444770A (en) * | 1980-05-29 | 1984-04-24 | Bayer Aktiengesellschaft | New imidazoazole-alkenoic acid amide compounds, intermediate products for their production, their production, and their medicinal use |
| DE3216416A1 (de) * | 1982-05-03 | 1983-11-03 | Bayer Ag, 5090 Leverkusen | Heteroarylthiovinyl-verbindungen, ein verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| DE3502264A1 (de) * | 1985-01-24 | 1986-07-24 | Bayer Ag, 5090 Leverkusen | Imidazoalkensaeurederivate, ein verfahren zu ihrer herstellung und ihre verwendung fuer die herstellung pharmazeutischer wirkstoffe |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| US5112833A (en) * | 1988-12-26 | 1992-05-12 | Zenyaku Kogyo Kabushiki Kaisha | 1-azaindolizine derivatives, synthetic intermediates thereof and antiallergic agents containing 1-azaindolizine derivatives |
| GB9004483D0 (en) * | 1990-02-28 | 1990-04-25 | Erba Carlo Spa | New aryl-and heteroarylethenylene derivatives and process for their preparation |
| ATE141502T1 (de) | 1991-01-15 | 1996-09-15 | Alcon Lab Inc | Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| JPH05301838A (ja) * | 1991-10-15 | 1993-11-16 | Mitsubishi Kasei Corp | スチレン誘導体 |
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- 2010-11-16 MX MX2012005678A patent/MX2012005678A/es not_active Application Discontinuation
- 2010-11-16 BR BR112012011528A patent/BR112012011528A2/pt not_active IP Right Cessation
- 2010-11-16 CA CA2781056A patent/CA2781056A1/en not_active Abandoned
- 2010-11-16 CN CN2010800615701A patent/CN102711765A/zh active Pending
- 2010-11-16 WO PCT/US2010/056890 patent/WO2011060440A2/en not_active Ceased
- 2010-11-16 JP JP2012539076A patent/JP2013510886A/ja active Pending
- 2010-11-16 EP EP10830919.6A patent/EP2558099A4/en not_active Withdrawn
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Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106939002A (zh) * | 2016-01-05 | 2017-07-11 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| WO2017118277A1 (zh) * | 2016-01-05 | 2017-07-13 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| CN107406453A (zh) * | 2016-01-05 | 2017-11-28 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| CN106939002B (zh) * | 2016-01-05 | 2019-09-24 | 江苏恒瑞医药股份有限公司 | 一种btk激酶抑制剂的结晶形式及其制备方法 |
| US10626116B2 (en) | 2016-01-05 | 2020-04-21 | Jiangsu Hengrui Medicine Co., Ltd. | Crystalline form of BTK kinase inhibitor and preparation method thereof |
| CN111205232A (zh) * | 2020-02-26 | 2020-05-29 | 浙江天宇药业股份有限公司 | 一种替格瑞洛中间体的合成方法 |
| CN116284135A (zh) * | 2023-05-04 | 2023-06-23 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒核苷类化合物的制备方法及其应用 |
| CN116332996A (zh) * | 2023-05-04 | 2023-06-27 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒化合物及其制备方法和应用 |
| CN116410228A (zh) * | 2023-05-04 | 2023-07-11 | 南京颐媛生物医学研究院有限公司 | 一种抗冠状病毒核苷类化合物的制备方法及其应用 |
| CN116284135B (zh) * | 2023-05-04 | 2025-03-21 | 南京颐媛生物医学研究院有限公司 | 抗冠状病毒核苷类化合物的制备方法及其应用 |
| CN116332996B (zh) * | 2023-05-04 | 2025-04-01 | 南京颐媛生物医学研究院有限公司 | L-呋喃核糖型抗冠状病毒化合物及其制备方法和应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010319964A2 (en) | 2012-08-02 |
| AU2010319964A1 (en) | 2012-06-07 |
| EP2558099A2 (en) | 2013-02-20 |
| US20150045343A1 (en) | 2015-02-12 |
| MX2012005678A (es) | 2012-09-07 |
| US9505766B2 (en) | 2016-11-29 |
| US20130035325A1 (en) | 2013-02-07 |
| EP2558099A4 (en) | 2013-07-17 |
| WO2011060440A2 (en) | 2011-05-19 |
| BR112012011528A2 (pt) | 2019-09-24 |
| JP2013510886A (ja) | 2013-03-28 |
| CA2781056A1 (en) | 2011-05-19 |
| WO2011060440A3 (en) | 2011-11-03 |
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