CN102753548B - 作为syk抑制剂的稠合的杂芳族吡咯烷酮 - Google Patents
作为syk抑制剂的稠合的杂芳族吡咯烷酮 Download PDFInfo
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- CN102753548B CN102753548B CN201080063801.2A CN201080063801A CN102753548B CN 102753548 B CN102753548 B CN 102753548B CN 201080063801 A CN201080063801 A CN 201080063801A CN 102753548 B CN102753548 B CN 102753548B
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- Prior art keywords
- pyrrolo
- pyridin
- fluoro
- methyl
- aminocyclohexylamino
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- 0 CC(CCC1=N)*C[C@]1Nc1nc(CNC2=O)c2c(C2=CC*(C=C3)C3=C=CC(C)N2)n1 Chemical compound CC(CCC1=N)*C[C@]1Nc1nc(CNC2=O)c2c(C2=CC*(C=C3)C3=C=CC(C)N2)n1 0.000 description 6
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N C1CCNCCC1 Chemical compound C1CCNCCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 description 1
- ORFPWEPWRPUBLL-GFCCVEGCSA-N CC(C)C[C@H](C(NC)=O)Nc(nc(-c1c[n](C)nc1)c1c2CNC1=O)c2F Chemical compound CC(C)C[C@H](C(NC)=O)Nc(nc(-c1c[n](C)nc1)c1c2CNC1=O)c2F ORFPWEPWRPUBLL-GFCCVEGCSA-N 0.000 description 1
- UJXGDCSKTYHOHE-GJZGRUSLSA-N CC(C)C[n]1ncc(-c2nc(NC[C@H]3[C@@H](C)CCCC3)nc(CN3)c2C3=O)c1 Chemical compound CC(C)C[n]1ncc(-c2nc(NC[C@H]3[C@@H](C)CCCC3)nc(CN3)c2C3=O)c1 UJXGDCSKTYHOHE-GJZGRUSLSA-N 0.000 description 1
- OMANDRNISYELRU-YGPZHTELSA-N CC(CCC1)C2(CC2)[C@@H]1OC Chemical compound CC(CCC1)C2(CC2)[C@@H]1OC OMANDRNISYELRU-YGPZHTELSA-N 0.000 description 1
- CWDUXGINCDZFAQ-UHFFFAOYSA-N CCOC(CC(CN(C(c1ccccc11)=O)C1=O)=O)=O Chemical compound CCOC(CC(CN(C(c1ccccc11)=O)C1=O)=O)=O CWDUXGINCDZFAQ-UHFFFAOYSA-N 0.000 description 1
- VFYIMFKQSSVIKO-GFCCVEGCSA-N CCOC[C@@H](CNc(nc(c1c2CNC1=O)Nc1cc(C)ccc1)c2F)N Chemical compound CCOC[C@@H](CNc(nc(c1c2CNC1=O)Nc1cc(C)ccc1)c2F)N VFYIMFKQSSVIKO-GFCCVEGCSA-N 0.000 description 1
- DRKGKGJFMZTSNZ-UHFFFAOYSA-N COC(c(c(C#N)c1)c(Nc2cc([nH]nc3)c3cc2)nc1Cl)=O Chemical compound COC(c(c(C#N)c1)c(Nc2cc([nH]nc3)c3cc2)nc1Cl)=O DRKGKGJFMZTSNZ-UHFFFAOYSA-N 0.000 description 1
- FUTNTFGNWKWROW-KBPLZSHQSA-N CS(O[C@@H]1C2(CC2)CCCC1)=O Chemical compound CS(O[C@@H]1C2(CC2)CCCC1)=O FUTNTFGNWKWROW-KBPLZSHQSA-N 0.000 description 1
- JELYNPYRWQHLLZ-XHDPSFHLSA-N C[C@@H](CCCC1)[C@@H]1Nc(nc(-c1c[n](C2CC2)nc1)c1c2CNC1=O)c2F Chemical compound C[C@@H](CCCC1)[C@@H]1Nc(nc(-c1c[n](C2CC2)nc1)c1c2CNC1=O)c2F JELYNPYRWQHLLZ-XHDPSFHLSA-N 0.000 description 1
- MJHOMTRKVMKCNE-NEPJUHHUSA-N C[n]1ncc(-c(c2c3CNC2=O)nc(N[C@@H](CCCC2)[C@@H]2N)c3F)c1 Chemical compound C[n]1ncc(-c(c2c3CNC2=O)nc(N[C@@H](CCCC2)[C@@H]2N)c3F)c1 MJHOMTRKVMKCNE-NEPJUHHUSA-N 0.000 description 1
- OPDRSBKBDWZHLE-UHFFFAOYSA-N Cc1cc(Nc(nc(NCCN)nc2CN3)c2C3=O)ccc1 Chemical compound Cc1cc(Nc(nc(NCCN)nc2CN3)c2C3=O)ccc1 OPDRSBKBDWZHLE-UHFFFAOYSA-N 0.000 description 1
- YIGCYDBPDPMTIR-DLBZAZTESA-N Cc1cc(Nc2c(C=O)c(CNC)nc(N[C@H](CCCC3)[C@H]3N)n2)ccc1 Chemical compound Cc1cc(Nc2c(C=O)c(CNC)nc(N[C@H](CCCC3)[C@H]3N)n2)ccc1 YIGCYDBPDPMTIR-DLBZAZTESA-N 0.000 description 1
- PAABVLWGZSJDEP-UHFFFAOYSA-N Cc1cc(Nc2nc(C#N)nc(C#N)c2C(OC)=O)ccc1 Chemical compound Cc1cc(Nc2nc(C#N)nc(C#N)c2C(OC)=O)ccc1 PAABVLWGZSJDEP-UHFFFAOYSA-N 0.000 description 1
- YJPFXOMSUYUCKG-UHFFFAOYSA-N OC(c(c1c(nc2Cl)Cl)c2F)OC1=O Chemical compound OC(c(c1c(nc2Cl)Cl)c2F)OC1=O YJPFXOMSUYUCKG-UHFFFAOYSA-N 0.000 description 1
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- 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
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Applications Claiming Priority (5)
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| US38696410P | 2010-09-27 | 2010-09-27 | |
| US61/386,964 | 2010-09-27 | ||
| PCT/US2010/061146 WO2011079051A1 (en) | 2009-12-23 | 2010-12-17 | Fused heteroaromatic pyrrolidinones as syk inhibitors |
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| CN102753548A CN102753548A (zh) | 2012-10-24 |
| CN102753548B true CN102753548B (zh) | 2015-03-11 |
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Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG181857A1 (en) | 2009-12-23 | 2012-07-30 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| RU2610840C2 (ru) * | 2011-03-28 | 2017-02-16 | Ф. Хоффманн-Ля Рош Аг | Тиазолопиримидины |
| EP2723739B1 (en) * | 2011-06-22 | 2016-08-24 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
| EP2900639B1 (en) * | 2012-09-27 | 2017-08-16 | Portola Pharmaceuticals, Inc. | Bicyclic dihydropyridone kinase inhibitors |
| EP2900243A4 (en) | 2012-09-27 | 2016-04-13 | Portola Pharm Inc | BICYCLIC OXA LACTAM KINASE HEMMER |
| KR102229478B1 (ko) | 2012-11-01 | 2021-03-18 | 인피니티 파마슈티칼스, 인코포레이티드 | Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료 |
| US20160024051A1 (en) | 2013-03-15 | 2016-01-28 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| RU2019134551A (ru) | 2013-05-30 | 2019-11-22 | Инфинити Фармасьютикалз, Инк. | Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы |
| CA2919479C (en) * | 2013-07-31 | 2017-08-22 | Gilead Sciences, Inc. | Syk inhibitors |
| US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| PL3052485T3 (pl) | 2013-10-04 | 2022-02-28 | Infinity Pharmaceuticals, Inc. | Związki heterocykliczne i ich zastosowania |
| WO2015061204A1 (en) | 2013-10-21 | 2015-04-30 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| TWI735853B (zh) | 2013-12-23 | 2021-08-11 | 美商克洛諾斯生技有限公司 | 脾酪胺酸激酶抑制劑 |
| AU2015222865B2 (en) * | 2014-02-28 | 2019-06-20 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
| CA2943075C (en) | 2014-03-19 | 2023-02-28 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| WO2015149130A1 (en) * | 2014-04-01 | 2015-10-08 | The University Of Queensland | Immunological reagents and uses therefor |
| WO2015160986A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP3134439B1 (en) * | 2014-04-21 | 2018-12-26 | Millennium Pharmaceuticals, Inc. | Anti-psyk antibody molecules and use of same for syk-targeted therapy |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2016090285A1 (en) | 2014-12-05 | 2016-06-09 | Array Biopharma Inc. | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
| EP3677582B1 (en) * | 2014-12-18 | 2023-01-25 | Calithera Biosciences Inc. | Solid state forms of fused heteroaromatic pyrrolidinones |
| ES2930585T3 (es) * | 2015-02-27 | 2022-12-19 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
| WO2017040757A1 (en) | 2015-09-02 | 2017-03-09 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| NZ740616A (en) | 2015-09-14 | 2023-05-26 | Infinity Pharmaceuticals Inc | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| GB201604970D0 (en) | 2016-03-23 | 2016-05-04 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| WO2017205801A1 (en) | 2016-05-27 | 2017-11-30 | Takeda Pharmaceutical Company Limited | Combination of immunotherapy agents and spleen tyrosine kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| PE20190971A1 (es) | 2016-06-13 | 2019-07-09 | Glaxosmithkline Ip Dev Ltd | Compuestos quimicos |
| IL263680B2 (en) | 2016-06-24 | 2025-10-01 | Infinity Pharmaceuticals Inc | PI3K inhibitors for use in combination with a second therapeutic agent for the treatment, management or prevention of cancer |
| EP3484466A1 (en) | 2016-07-13 | 2019-05-22 | Takeda Pharmaceutical Company Limited | Combination of spleen tyrosine kinase inhibitors and other therapeutic agents |
| TW201822764A (zh) | 2016-09-14 | 2018-07-01 | 美商基利科學股份有限公司 | Syk抑制劑 |
| WO2018053190A1 (en) | 2016-09-14 | 2018-03-22 | Gilead Sciences, Inc. | Syk inhibitors |
| WO2018195471A1 (en) | 2017-04-21 | 2018-10-25 | Gilead Sciences, Inc. | Syk inhibitors in combination with hypomethylating agents |
| US11091460B2 (en) * | 2017-06-14 | 2021-08-17 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Syk inhibitor and use method therefor |
| TWI782056B (zh) * | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
| EP3689871B1 (en) * | 2017-09-28 | 2021-09-29 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | 4,6,7-trisubstituted 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative and use |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| BR112020007679A2 (pt) * | 2017-10-19 | 2020-10-20 | Bayer Animal Health Gmbh | uso de pirrolidonas heteroaromáticas fundidas para tratamento e prevenção de doenças em animais. |
| WO2019088039A1 (en) | 2017-10-30 | 2019-05-09 | Takeda Pharmaceutical Company Limited | Treatment of acute myeloid leukemia |
| WO2020073945A1 (zh) * | 2018-10-10 | 2020-04-16 | 江苏豪森药业集团有限公司 | 双环类衍生物抑制剂、其制备方法和应用 |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| EP3909583A4 (en) | 2019-01-11 | 2022-08-17 | Shionogi & Co., Ltd | DIHYDROPYRAZOLOPYRAZINONE DERIVATIVES WITH MGAT2 INHIBITORY ACTIVITY |
| CN113950479A (zh) * | 2019-02-22 | 2022-01-18 | 克洛诺斯生物股份有限公司 | 作为syk抑制剂的缩合吡嗪的固体形式 |
| EP3851438A4 (en) * | 2019-03-18 | 2021-11-10 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd | BTK INHIBITOR, PHARMACEUTICALLY ACCEPTABLE SALT, POLYMORPHIC AND APPLICATION OF THE SAME |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN116096369B (zh) * | 2020-09-01 | 2025-09-16 | 上海海雁医药科技有限公司 | 布鲁顿酪氨酸激酶抑制剂的多晶型物及其制备方法和应用 |
| WO2022127753A1 (zh) * | 2020-12-18 | 2022-06-23 | 山东轩竹医药科技有限公司 | 稠环类AhR抑制剂 |
| US20240174662A1 (en) * | 2021-02-01 | 2024-05-30 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| JP2024506909A (ja) | 2021-02-12 | 2024-02-15 | ニンバス サターン, インコーポレイテッド | Hpk1アンタゴニスト及びその使用 |
| JP2024509192A (ja) | 2021-03-05 | 2024-02-29 | ニンバス サターン, インコーポレイテッド | Hpk1アンタゴニスト及びその使用 |
| JP2024513011A (ja) | 2021-03-29 | 2024-03-21 | ニンバス サターン, インコーポレイテッド | Hpk1アンタゴニスト及びその使用 |
| MX2024005434A (es) * | 2021-11-04 | 2024-05-21 | Redx Pharma Plc | Inhibidores de ddr1 y ddr2 para el tratamiento de cancer y enfermedades fibroticas. |
| CN114907992B (zh) | 2022-05-18 | 2023-06-16 | 塔里木大学 | 拮抗植物病原菌的菌株c11及其应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001009134A1 (en) * | 1999-07-30 | 2001-02-08 | Novartis Ag | Purine derivatives inhibitors of tyrosine protein kinase syk |
| CN1697830A (zh) * | 2002-03-15 | 2005-11-16 | 诺瓦提斯公司 | 嘧啶衍生物 |
| WO2007070872A1 (en) * | 2005-12-15 | 2007-06-21 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
| EP1880993A1 (en) * | 2005-04-19 | 2008-01-23 | Kyowa Hakko Kogyo Co., Ltd. | Nitrogen-containing heterocyclic compound |
Family Cites Families (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63107966A (ja) | 1986-05-22 | 1988-05-12 | Fujisawa Pharmaceut Co Ltd | ピリミジン誘導体 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5272158A (en) | 1991-10-29 | 1993-12-21 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| US5238950A (en) | 1991-12-17 | 1993-08-24 | Schering Corporation | Inhibitors of platelet-derived growth factor |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| ATE401312T1 (de) | 1997-12-15 | 2008-08-15 | Astellas Pharma Inc | Pyrimidin-5-carboxamid-derivate |
| AU2095099A (en) | 1997-12-23 | 1999-07-12 | Alcon Laboratories, Inc. | Phthalimide-piperidine, -pyrrolidine and -azepine derivatives, their preparationand their use as muscarinic receptor (ant-)agonists |
| WO2000075113A1 (en) | 1999-06-09 | 2000-12-14 | Yamanouchi Pharmaceutical Co., Ltd. | Novel heterocyclic carboxamide derivatives |
| FR2796946A1 (fr) | 1999-07-30 | 2001-02-02 | Aventis Pharma Sa | Nouveaux derives 8-carbonyl chromanes, leur preparation et leur utilisation en therapeutique |
| HK1048439A1 (zh) | 1999-12-16 | 2003-04-04 | Alcon, Inc. | 用於治疗视神经及视网膜损伤之腺激酶抑制剂 |
| WO2001049688A1 (en) | 2000-01-07 | 2001-07-12 | Universitaire Instelling Antwerpen | Purine derivatives, process for their preparation and use thereof |
| AU2001232271A1 (en) | 2000-02-14 | 2001-08-20 | Japan Tobacco Inc. | Preventives/remedies for postoperative stress |
| JP2001302667A (ja) | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| US7105667B2 (en) | 2001-05-01 | 2006-09-12 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
| PE20030008A1 (es) | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | Inhibidores duales de pde 7 y pde 4 |
| GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| WO2003009852A1 (en) | 2001-07-24 | 2003-02-06 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US20030158195A1 (en) | 2001-12-21 | 2003-08-21 | Cywin Charles L. | 1,6 naphthyridines useful as inhibitors of SYK kinase |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| US7304071B2 (en) | 2002-08-14 | 2007-12-04 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
| WO2004037814A1 (en) | 2002-10-25 | 2004-05-06 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| JP2006508107A (ja) | 2002-11-05 | 2006-03-09 | バーテックス ファーマシューティカルズ インコーポレイテッド | Jakおよび他のプロテインキナーゼのインヒビターとして有用な化合物 |
| US20040235834A1 (en) | 2003-03-25 | 2004-11-25 | Farmer Luc J. | Thiazoles useful as inhibitors of protein kinases |
| KR20050122220A (ko) | 2003-03-25 | 2005-12-28 | 다케다 샌디에고, 인코포레이티드 | 디펩티딜 펩티다제 억제제 |
| ATE396731T1 (de) | 2003-03-25 | 2008-06-15 | Vertex Pharma | Thiazole zur verwendung als inhibitoren von protein-kinasen |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| US7320992B2 (en) | 2003-08-25 | 2008-01-22 | Amgen Inc. | Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use |
| US20050182061A1 (en) | 2003-10-02 | 2005-08-18 | Jeremy Green | Phthalimide compounds useful as protein kinase inhibitors |
| BRPI0416692A (pt) * | 2003-11-19 | 2007-01-30 | Array Biopharma Inc | inibidores heterocìclicos de mek e métodos de emprego destes |
| WO2005056524A2 (en) | 2003-12-09 | 2005-06-23 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| US8057815B2 (en) | 2004-04-19 | 2011-11-15 | Portola Pharmaceuticals, Inc. | Methods of treatment with Syk inhibitors |
| WO2006028833A1 (en) | 2004-09-01 | 2006-03-16 | Rigel Pharmaceuticals, Inc. | Synthesis of 2,4-pyrimidinediamine compounds |
| DK1814878T3 (da) | 2004-11-24 | 2012-05-07 | Rigel Pharmaceuticals Inc | Spiro-2, 4-pyrimidindiamin-forbindelser og anvendelser deraf |
| US20060128710A1 (en) | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| BRPI0608934A2 (pt) | 2005-04-06 | 2010-02-17 | Irm Llc | compostos e composições contendo diarilamina, e seu uso como moduladores de receptores nucleares de hormÈnios esteróides |
| WO2006129100A1 (en) | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| CA2608476A1 (en) | 2005-06-28 | 2007-01-04 | Bausch & Lomb Incorporated | Preparations comprising arylazine substituted with a carbonylic moiety to increase the activity of gelatinase a in ocular cells |
| AR056191A1 (es) | 2005-08-23 | 2007-09-26 | Idenix Phatmaceuticals Inc | Anillo de nucleosidos de siete miembros como inhibidores de la replica viral, metodos para su sintesis, composiciones farmaceuticas que los contienen y su uso en el tratamiento de infecciones con virus de la familia flaviviridae |
| WO2007023382A2 (en) | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
| EA200800664A1 (ru) * | 2005-10-13 | 2009-02-27 | Глаксо Груп Лимитед | Производные пирролопиримидина в качестве ингибиторов syk |
| US20070117775A1 (en) | 2005-10-31 | 2007-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and Methods For Treating Inflammatory Disorders |
| EP2537849A3 (en) | 2006-01-17 | 2013-04-03 | Vertex Pharmaceuticals, Inc. | Azaindoles useful as inhibitors of janus kinases |
| CL2007002617A1 (es) | 2006-09-11 | 2008-05-16 | Sanofi Aventis | Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto. |
| EP2108642A1 (en) | 2006-10-17 | 2009-10-14 | Kyowa Hakko Kirin Co., Ltd. | Jak inhibitor |
| KR20140104060A (ko) | 2006-10-19 | 2014-08-27 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도 |
| WO2008057402A2 (en) | 2006-11-02 | 2008-05-15 | Cytovia, Inc. | N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof |
| US8163902B2 (en) | 2006-11-21 | 2012-04-24 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| US20100298557A1 (en) | 2006-12-28 | 2010-11-25 | Taisho Pharmaceutical Co., Ltd | Pyrazolopyrimidine compound |
| CN101605792A (zh) * | 2007-02-09 | 2009-12-16 | 阿斯利康(瑞典)有限公司 | 氮杂-异吲哚酮和它们作为亲代谢性谷氨酸受体增效剂-613的用途 |
| WO2008118332A2 (en) | 2007-03-23 | 2008-10-02 | Schering Corporation | Hydrazido-peptides as inhibitors of hcv ns3-protease |
| WO2008151184A1 (en) | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US7705004B2 (en) | 2007-08-17 | 2010-04-27 | Portola Pharmaceuticals, Inc. | Protein kinase inhibitors |
| JP2009067729A (ja) | 2007-09-14 | 2009-04-02 | Kyowa Hakko Kirin Co Ltd | Hsp90ファミリー蛋白質阻害剤 |
| EP2217239A2 (en) | 2007-11-07 | 2010-08-18 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
| EP2234986A2 (en) | 2007-12-20 | 2010-10-06 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
| TW200938542A (en) * | 2008-02-01 | 2009-09-16 | Irm Llc | Compounds and compositions as kinase inhibitors |
| US20090221612A1 (en) | 2008-02-13 | 2009-09-03 | Mitchell Scott A | Certain substituted amides, method of making, and method of use thereof |
| AU2009215430B2 (en) | 2008-02-22 | 2015-02-12 | Rigel Pharmaceuticals, Inc. | Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis |
| US8436005B2 (en) | 2008-04-03 | 2013-05-07 | Abbott Laboratories | Macrocyclic pyrimidine derivatives |
| KR20100132550A (ko) | 2008-04-16 | 2010-12-17 | 포톨라 파마슈티컬스, 인코포레이티드 | syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드 |
| CA2723205C (en) | 2008-04-16 | 2017-03-14 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| KR20110031318A (ko) | 2008-06-13 | 2011-03-25 | 노파르티스 아게 | Ia 심부전 및 암 치료에 유용한 단백질 키나제 d 억제제로서의 2,4'-비피리디닐 화합물 |
| WO2010015518A2 (de) | 2008-08-05 | 2010-02-11 | Boehringer Ingelheim Interntional Gmbh | 4-dimethylamino-phenyl-substituierte naphthyridine und ihre verwendung als arzneimittel |
| WO2010015520A1 (de) | 2008-08-05 | 2010-02-11 | Boehringer Ingelheim International Gmbh | Substituierte naphthyridine und ihre verwendung als arzneimittel |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶,其組合物及使用其之治療方法 |
| WO2010068258A1 (en) | 2008-12-08 | 2010-06-17 | Cgi Pharmaceuticals, Inc. | Imidazopyrazine syk inhibitors |
| WO2010146133A1 (en) | 2009-06-18 | 2010-12-23 | Cellzome Limited | Heterocyclylaminopyrimidines as kinase inhibitors |
| US8759366B2 (en) | 2009-12-17 | 2014-06-24 | Merck Sharp & Dohme Corp. | Aminopyrimidines as SYK inhibitors |
| US8735417B2 (en) | 2009-12-17 | 2014-05-27 | Merck Sharp & Dohme Corp. | Aminopyrimidines as Syk inhibitors |
| SG181857A1 (en) * | 2009-12-23 | 2012-07-30 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| GB201007203D0 (en) | 2010-04-29 | 2010-06-16 | Glaxo Group Ltd | Novel compounds |
| EP2723739B1 (en) | 2011-06-22 | 2016-08-24 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
-
2010
- 2010-12-17 SG SG2012045936A patent/SG181857A1/en unknown
- 2010-12-17 MA MA35044A patent/MA33909B1/fr unknown
- 2010-12-17 EA EA201290555A patent/EA021568B1/ru unknown
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001009134A1 (en) * | 1999-07-30 | 2001-02-08 | Novartis Ag | Purine derivatives inhibitors of tyrosine protein kinase syk |
| CN1697830A (zh) * | 2002-03-15 | 2005-11-16 | 诺瓦提斯公司 | 嘧啶衍生物 |
| EP1880993A1 (en) * | 2005-04-19 | 2008-01-23 | Kyowa Hakko Kogyo Co., Ltd. | Nitrogen-containing heterocyclic compound |
| WO2007070872A1 (en) * | 2005-12-15 | 2007-06-21 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
Non-Patent Citations (1)
| Title |
|---|
| Synthetic studies on novel Syk inhibitors. Part 1:Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives;H. Hisamichi et al.;《Bioorganic & Medicinal Chemistry》;20051231;第13卷;4936–4951 * |
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