UA80571C2 - Quinolinyl-pyrrolopyrazoles - Google Patents
Quinolinyl-pyrrolopyrazoles Download PDFInfo
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- UA80571C2 UA80571C2 UAA200504767A UA2005004767A UA80571C2 UA 80571 C2 UA80571 C2 UA 80571C2 UA A200504767 A UAA200504767 A UA A200504767A UA 2005004767 A UA2005004767 A UA 2005004767A UA 80571 C2 UA80571 C2 UA 80571C2
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| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| US7405299B2 (en) * | 2002-11-27 | 2008-07-29 | Eli Lilly And Company | Compounds as pharmaceutical agents |
| CA2616196C (en) * | 2005-07-22 | 2012-08-21 | Eli Lilly And Company | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
| WO2007039151A1 (en) * | 2005-09-28 | 2007-04-12 | Universität Zürich | Blockers of transforming growth factor beta and its receptors for the treatment of infectious diseases |
| CN101553254A (zh) | 2006-10-03 | 2009-10-07 | 建新公司 | TGF-β拮抗物治疗具有罹患支气管肺发育不良风险的婴儿的用途 |
| EP2527345B1 (en) * | 2006-10-16 | 2015-12-16 | Thesan Pharmaceuticals, Inc. | Therapeutic pyrazolyl thienopyridines |
| CN103140474A (zh) | 2010-07-02 | 2013-06-05 | 吉里德科学公司 | 治疗aids的萘-2-基乙酸衍生物 |
| EP2588455B1 (en) | 2010-07-02 | 2018-04-04 | Gilead Sciences, Inc. | 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| MX2013012266A (es) | 2011-04-21 | 2013-11-22 | Gilead Sciences Inc | Compuestos de benzotiazol y su uso farmaceutico. |
| WO2013014262A1 (en) | 2011-07-27 | 2013-01-31 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating myhre syndrome |
| US9468612B2 (en) | 2011-10-26 | 2016-10-18 | Seattle Children's Hospital | Cysteamine in the treatment of fibrotic disease |
| US9782452B2 (en) | 2011-11-22 | 2017-10-10 | Cornell University | Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling |
| US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
| US9376392B2 (en) | 2012-01-04 | 2016-06-28 | Gilead Sciences, Inc. | 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS |
| ES2571479T3 (es) | 2012-04-20 | 2016-05-25 | Gilead Sciences Inc | Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH |
| CN105007939B (zh) | 2012-10-05 | 2018-10-19 | 卡德门企业有限公司 | 人抗vegfr-2/kdr抗体 |
| EP2917365B1 (en) | 2012-11-12 | 2020-03-11 | Institució Catalana de Recerca i Estudis Avançats | Methods and kits for the prognosis of colorectal cancer |
| JO3336B1 (ar) | 2014-10-07 | 2019-03-13 | Lilly Co Eli | مركبات أمينو بيريديلوكسي بيرازول |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| WO2016123573A1 (en) | 2015-01-30 | 2016-08-04 | President And Fellows Of Harvard College | Peritumoral and intratumoral materials for cancer therapy |
| EP3277673B1 (en) | 2015-04-01 | 2022-05-04 | Rigel Pharmaceuticals, Inc. | Tgf-beta inhibitors |
| US10450318B2 (en) | 2015-12-15 | 2019-10-22 | Bristol-Myers Squibb Company | CXCR4 receptor antagonists |
| US10604528B2 (en) | 2016-07-07 | 2020-03-31 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Galunisertib crystalline form, preparation method thereof and use thereof |
| WO2018165979A1 (zh) * | 2017-03-17 | 2018-09-20 | 杭州领业医药科技有限公司 | 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的晶型及其制备方法和药物组合物 |
| WO2018170724A1 (zh) * | 2017-03-21 | 2018-09-27 | 杭州领业医药科技有限公司 | 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的共晶，其制备方法和药物组合物 |
| WO2019042383A1 (zh) * | 2017-08-31 | 2019-03-07 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| WO2019105082A1 (zh) * | 2017-11-30 | 2019-06-06 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| WO2019137027A1 (zh) * | 2018-01-12 | 2019-07-18 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| EP3827010B1 (en) | 2018-07-23 | 2025-08-27 | Brise Pharmaceuticals Co., Ltd. | Bisphosphonate drug conjugates |
| SG11202103457PA (en) | 2018-12-27 | 2021-05-28 | Nexys Therapeutics Inc | (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| CN113557236B (zh) * | 2019-06-10 | 2022-05-10 | 中国科学院广州生物医药与健康研究院 | 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物 |
| CN115052663B (zh) | 2020-01-08 | 2026-06-09 | 辛瑟斯治疗股份有限公司 | Alk5抑制剂缀合物及其用途 |
| JP7842690B2 (ja) | 2020-02-19 | 2026-04-08 | ナミ セラピューティクス， インコーポレイテッド | がんの処置において有用なＴＦＧβアンタゴニストプロドラッグを含有する製剤化および／または共製剤化リポソーム組成物ならびにその方法 |
| WO2024258967A1 (en) | 2023-06-13 | 2024-12-19 | Synthis Therapeutics, Inc. | Anti-cd5 antibodies and their uses |
| GB202309553D0 (en) | 2023-06-24 | 2023-08-09 | Ucl Business Ltd | Compostions and uses thereof |
Family Cites Families (4)
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| US5356897A (en) * | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| ATE267830T1 (de) * | 1999-08-27 | 2004-06-15 | Abbott Lab | Als cox-hemmer verwendbare sulfonylphenylpyrazol- verbindungen |
| SI1397364T1 (sl) * | 2001-05-24 | 2007-12-31 | Lilly Co Eli | Novi pirolni derivati kot farmacevtske uäśinkovine |
| EP1567528A1 (en) | 2002-11-21 | 2005-08-31 | Eli Lilly And Company | Mixed lineage kinase modulators |
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2003
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