JP2013510886A5 - - Google Patents
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- Publication number
- JP2013510886A5 JP2013510886A5 JP2012539076A JP2012539076A JP2013510886A5 JP 2013510886 A5 JP2013510886 A5 JP 2013510886A5 JP 2012539076 A JP2012539076 A JP 2012539076A JP 2012539076 A JP2012539076 A JP 2012539076A JP 2013510886 A5 JP2013510886 A5 JP 2013510886A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- membered
- alkyl
- heteroaryl
- 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.)
- Pending
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- 0 Cc(cc1)ccc1-c1c(C=C(C(*)=O)C#N)[n](CCCO)c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(C=C(C(*)=O)C#N)[n](CCCO)c2ncnc(N)c12 0.000 description 23
- IEUOMYJAIZIKES-SFQUDFHCSA-N CC(C)(C)OC(/C(/C#N)=C/c([n](CCCO)c1ncnc(N)c11)c1-c1ccc(C)cc1)=O Chemical compound CC(C)(C)OC(/C(/C#N)=C/c([n](CCCO)c1ncnc(N)c11)c1-c1ccc(C)cc1)=O IEUOMYJAIZIKES-SFQUDFHCSA-N 0.000 description 2
- POTINGKLYOETSI-GZTJUZNOSA-N CC(C)NC(/C(/C#N)=C/c([n](CCCO)c1ncnc(N)c11)c1-c1ccc(C)cc1)=O Chemical compound CC(C)NC(/C(/C#N)=C/c([n](CCCO)c1ncnc(N)c11)c1-c1ccc(C)cc1)=O POTINGKLYOETSI-GZTJUZNOSA-N 0.000 description 2
- JOMCSJCBXRQYAV-LFIBNONCSA-N Cc(cc1)ccc1-c1c(/C=C(/C(N(C)C)=O)\C#N)[n](CCCO)c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(N(C)C)=O)\C#N)[n](CCCO)c2ncnc(N)c12 JOMCSJCBXRQYAV-LFIBNONCSA-N 0.000 description 2
- HZDYACZJZXFGHS-IZZDOVSWSA-N Cc(cc1)ccc1-c1c(/C=C(/C(N)=O)\C#N)[nH]c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(N)=O)\C#N)[nH]c2ncnc(N)c12 HZDYACZJZXFGHS-IZZDOVSWSA-N 0.000 description 2
- VGLWJTYWGAMQMT-KGENOOAVSA-N Cc(cc1)ccc1-c1c(/C=C(/C(NCc2ccccc2)=O)\C#N)[n](CCCO)c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(NCc2ccccc2)=O)\C#N)[n](CCCO)c2ncnc(N)c12 VGLWJTYWGAMQMT-KGENOOAVSA-N 0.000 description 2
- WBFCJGMKBZKZGZ-LMDBJESCSA-N CC(/C(/C1c2ccc(C)cc2)=C(/N)\N=C/N)N(CCCO)C1/C=C(/C(N(C)C)=O)\C#N Chemical compound CC(/C(/C1c2ccc(C)cc2)=C(/N)\N=C/N)N(CCCO)C1/C=C(/C(N(C)C)=O)\C#N WBFCJGMKBZKZGZ-LMDBJESCSA-N 0.000 description 1
- HZAGRSYBGQOSAL-UHFFFAOYSA-N CC(C)(CO)NC(C(CC(C(C12)c3ccc(C)cc3)N(CCCO)C1=NC=NC2N)C#N)O Chemical compound CC(C)(CO)NC(C(CC(C(C12)c3ccc(C)cc3)N(CCCO)C1=NC=NC2N)C#N)O HZAGRSYBGQOSAL-UHFFFAOYSA-N 0.000 description 1
- FEXBDPWFEBCULC-UHFFFAOYSA-N CC(C)(CO)NC(C(CC(C1c2ccc(C)cc2)N(CCCN=O)c2c1c(N)ncn2)C#N)=O Chemical compound CC(C)(CO)NC(C(CC(C1c2ccc(C)cc2)N(CCCN=O)c2c1c(N)ncn2)C#N)=O FEXBDPWFEBCULC-UHFFFAOYSA-N 0.000 description 1
- YMXATSAAJOJKBG-UHFFFAOYSA-N CC(C)NC(C(CC(C(CCCO)c1ncnc(NI)c11)=C1c1ccc(C)cc1)C#N)=O Chemical compound CC(C)NC(C(CC(C(CCCO)c1ncnc(NI)c11)=C1c1ccc(C)cc1)C#N)=O YMXATSAAJOJKBG-UHFFFAOYSA-N 0.000 description 1
- SMIILXFTIIRXRQ-CXUHLZMHSA-N CC(CC1)=CC=C1C(C12)=C(/C=C(/C(N(C3)CC3O)=O)\C#N)N(CCCO)C1=NC=NC2N Chemical compound CC(CC1)=CC=C1C(C12)=C(/C=C(/C(N(C3)CC3O)=O)\C#N)N(CCCO)C1=NC=NC2N SMIILXFTIIRXRQ-CXUHLZMHSA-N 0.000 description 1
- LTHLMMFCXLSESC-UHFFFAOYSA-O CC(c1c(CC=CCN)[n](CCCO)c(C=C(C(NC(C)(C)C)=O)C#N)c1-c1ccc(C)cc1)[NH3+] Chemical compound CC(c1c(CC=CCN)[n](CCCO)c(C=C(C(NC(C)(C)C)=O)C#N)c1-c1ccc(C)cc1)[NH3+] LTHLMMFCXLSESC-UHFFFAOYSA-O 0.000 description 1
- HUNVXONHJJSTOV-QGOAFFKASA-N Cc(cc1)ccc1-c1c(/C=C(/C(N2CCCC2)=O)\C#N)[n](CCCO)c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(N2CCCC2)=O)\C#N)[n](CCCO)c2ncnc(N)c12 HUNVXONHJJSTOV-QGOAFFKASA-N 0.000 description 1
- VDXFOORUKRSIGC-KPKJPENVSA-N Cc(cc1)ccc1-c1c(/C=C(/C(OC)=O)\C#N)[nH]c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(OC)=O)\C#N)[nH]c2ncnc(N)c12 VDXFOORUKRSIGC-KPKJPENVSA-N 0.000 description 1
- GDXHZXJALWQIPQ-XNTDXEJSSA-N Cc(cc1)ccc1-c1c(/C=C(/C(OC)=O)\C#N)[n](CCCO)c2ncnc(N)c12 Chemical compound Cc(cc1)ccc1-c1c(/C=C(/C(OC)=O)\C#N)[n](CCCO)c2ncnc(N)c12 GDXHZXJALWQIPQ-XNTDXEJSSA-N 0.000 description 1
- TXFGPVZJJSMQLS-SFQUDFHCSA-N Cc(cc1)ccc1C1=C(/C=C(/C(N2CCC2)=O)\C#N)N(CCCO)C2=NCNC(N)=C12 Chemical compound Cc(cc1)ccc1C1=C(/C=C(/C(N2CCC2)=O)\C#N)N(CCCO)C2=NCNC(N)=C12 TXFGPVZJJSMQLS-SFQUDFHCSA-N 0.000 description 1
- UKTOQAKGZCUTCX-XQNSMLJCSA-N NC(/C(/C#[N]c(cc1)ccc1-c1c(/C=C(/C(N2CCCC2)=O)\C#N)[n](CCCO)c2ncnc(N)c12)=C/c1nc2c(N)ncnc2[n]1CCCO)=O Chemical compound NC(/C(/C#[N]c(cc1)ccc1-c1c(/C=C(/C(N2CCCC2)=O)\C#N)[n](CCCO)c2ncnc(N)c12)=C/c1nc2c(N)ncnc2[n]1CCCO)=O UKTOQAKGZCUTCX-XQNSMLJCSA-N 0.000 description 1
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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2013510886A JP2013510886A (ja) | 2013-03-28 |
| JP2013510886A5 true JP2013510886A5 (https=) | 2014-01-09 |
Family
ID=43992477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539076A Pending JP2013510886A (ja) | 2009-11-16 | 2010-11-16 | キナーゼ阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US20130035325A1 (https=) |
| EP (1) | EP2558099A4 (https=) |
| JP (1) | JP2013510886A (https=) |
| CN (1) | CN102711765A (https=) |
| AU (1) | AU2010319964A1 (https=) |
| BR (1) | BR112012011528A2 (https=) |
| CA (1) | CA2781056A1 (https=) |
| MX (1) | MX2012005678A (https=) |
| WO (1) | WO2011060440A2 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2012158795A1 (en) | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| WO2013191965A1 (en) | 2012-06-18 | 2013-12-27 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| US9573958B2 (en) | 2012-08-31 | 2017-02-21 | Principia Biopharma, Inc. | Benzimidazole derivatives as ITK inhibitors |
| SI2892900T1 (en) | 2012-09-10 | 2018-01-31 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
| 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 |
| CN112353806A (zh) | 2014-02-21 | 2021-02-12 | 普林斯匹亚生物制药公司 | Btk抑制剂的盐和固体形式 |
| CN106573001B (zh) * | 2014-07-07 | 2019-01-29 | 江苏恒瑞医药股份有限公司 | 作为蛋白激酶抑制剂的氨基哒嗪酮化合物 |
| SG11201704808VA (en) | 2014-12-18 | 2017-07-28 | Principia Biopharma Inc | Treatment of pemphigus |
| WO2016210165A1 (en) | 2015-06-24 | 2016-12-29 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| RU2728827C2 (ru) * | 2016-01-05 | 2020-07-31 | Цзянсу Хэнжуй Медицин Ко., Лтд. | Кристаллическая форма ингибитора тирозинкиназы брутона и способ её получения |
| 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 |
| CN115054586B (zh) | 2016-06-29 | 2024-08-02 | 普林斯匹亚生物制药公司 | 改性的释放制剂 |
| AU2017362350B2 (en) | 2016-11-18 | 2021-12-23 | Cystic Fibrosis Foundation | Pyrrolopyrimidines as CFTR potentiators |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| US20210106584A1 (en) | 2019-10-14 | 2021-04-15 | Principia Biopharma Inc. | Methods for treating immune thrombocytopenia by administering (r)-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 |
| US11814390B2 (en) | 2020-01-22 | 2023-11-14 | Principia Biopharma Inc. | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN111205232B (zh) * | 2020-02-26 | 2022-07-01 | 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 |
| 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) |
| CN116410228B (zh) * | 2023-05-04 | 2025-10-31 | 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 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JP2594486B2 (ja) | 1991-01-15 | 1997-03-26 | アルコン ラボラトリーズ インコーポレイテッド | 局所的眼薬組成物 |
| 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 |
| US5792771A (en) * | 1992-11-13 | 1998-08-11 | Sugen, Inc. | Quinazoline compounds and compositions thereof for the treatment of disease |
| GB9226855D0 (en) * | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
| WO1995024190A2 (en) * | 1994-03-07 | 1995-09-14 | Sugen, Inc. | Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof |
| GB9406137D0 (en) * | 1994-03-28 | 1994-05-18 | Erba Carlo Spa | N-substituted beta-aryl- and betaheteroaryl-alpha-cyanoacrylamide derivatives and process for their preparation |
| GB9412719D0 (en) * | 1994-06-24 | 1994-08-17 | Erba Carlo Spa | Substituted azaindolylidene compounds and process for their preparation |
| US6331555B1 (en) * | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
| WO1999043673A1 (en) * | 1998-02-26 | 1999-09-02 | Zenyaku Kogyo Kabushiki Kaisha | 1-azaindolizine derivatives |
| WO2005011812A1 (en) * | 2003-08-01 | 2005-02-10 | Chugai Seiyaku Kabushiki Kaisha | Cyanoamide compounds useful as malonyl-coa decarboxylase inhibithors |
| US7807719B2 (en) * | 2004-09-14 | 2010-10-05 | Chaim Roifman | Compounds useful for modulating abnormal cell proliferation |
| JP5222561B2 (ja) * | 2005-10-07 | 2013-06-26 | キッセイ薬品工業株式会社 | 含窒素芳香族複素環化合物およびそれを含有する医薬組成物 |
| RU2456265C2 (ru) * | 2006-03-31 | 2012-07-20 | Дзе Борд Оф Риджентс Оф Дзе Юниверсити Оф Техас Систем | Биологически доступная для перорального применения кофейная кислота, относящаяся к противоопухолевым лекарственным средствам |
| US7645748B2 (en) | 2006-04-03 | 2010-01-12 | Forbes Medi-Tech Inc. | Sterol/stanol phosphorylnitroderivatives and use thereof |
| US20100292229A1 (en) * | 2006-06-30 | 2010-11-18 | The Board Of Regents Of The University Of Texas System | Tryphostin-analogs for the treatment of cell proliferative diseases |
| US8268809B2 (en) * | 2006-09-05 | 2012-09-18 | Emory University | Kinase inhibitors for preventing or treating pathogen infection and method of use thereof |
| US20100113520A1 (en) | 2008-11-05 | 2010-05-06 | Principia Biopharma, Inc. | Kinase knockdown via electrophilically enhanced inhibitors |
| US20120028981A1 (en) | 2008-11-05 | 2012-02-02 | Principia Biopharma Inc. | Kinase Knockdown Via Electrophilically Enhanced Inhibitors |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
-
2010
- 2010-11-16 US US13/510,272 patent/US20130035325A1/en not_active Abandoned
- 2010-11-16 JP JP2012539076A patent/JP2013510886A/ja active Pending
- 2010-11-16 AU AU2010319964A patent/AU2010319964A1/en not_active Abandoned
- 2010-11-16 WO PCT/US2010/056890 patent/WO2011060440A2/en not_active Ceased
- 2010-11-16 BR BR112012011528A patent/BR112012011528A2/pt not_active IP Right Cessation
- 2010-11-16 EP EP10830919.6A patent/EP2558099A4/en not_active Withdrawn
- 2010-11-16 MX MX2012005678A patent/MX2012005678A/es not_active Application Discontinuation
- 2010-11-16 CA CA2781056A patent/CA2781056A1/en not_active Abandoned
- 2010-11-16 CN CN2010800615701A patent/CN102711765A/zh active Pending
-
2014
- 2014-08-18 US US14/462,158 patent/US9505766B2/en active Active
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