CA2933250A1 - Sgc stimulators - Google Patents
Sgc stimulators Download PDFInfo
- Publication number
- CA2933250A1 CA2933250A1 CA2933250A CA2933250A CA2933250A1 CA 2933250 A1 CA2933250 A1 CA 2933250A1 CA 2933250 A CA2933250 A CA 2933250A CA 2933250 A CA2933250 A CA 2933250A CA 2933250 A1 CA2933250 A1 CA 2933250A1
- Authority
- CA
- Canada
- Prior art keywords
- ring
- alkyl
- independently selected
- membered heteroaryl
- membered heterocyclic
- 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.)
- Abandoned
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Classifications
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| US201361914908P | 2013-12-11 | 2013-12-11 | |
| US61/914,908 | 2013-12-11 | ||
| US201462051539P | 2014-09-17 | 2014-09-17 | |
| US62/051,539 | 2014-09-17 | ||
| PCT/US2014/069537 WO2015089182A1 (en) | 2013-12-11 | 2014-12-10 | Sgc stimulators |
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| CA2933250A1 true CA2933250A1 (en) | 2015-06-18 |
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| EP (1) | EP3092231B1 (https=) |
| JP (1) | JP2016540017A (https=) |
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| US9487508B2 (en) | 2012-09-19 | 2016-11-08 | Ironwood Pharmaceuticals, Inc. | SGC stimulators |
| SI2970243T1 (sl) | 2013-03-15 | 2020-04-30 | Cyclerion Therapeutics, Inc. | SGC stimulatorji |
| US20170291889A1 (en) * | 2014-09-17 | 2017-10-12 | Ironwood Pharmaceuticals, Inc. | Pyrazole derivatives as sgc stimulators |
| EP3194386A2 (en) * | 2014-09-17 | 2017-07-26 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| US20170298055A1 (en) * | 2014-09-17 | 2017-10-19 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| AU2016371762A1 (en) | 2015-12-14 | 2018-06-21 | Cyclerion Therapeutics, Inc. | Use of sGC stimulators for the treatment of gastrointestinal sphincter dysfunction |
| CN109563077B (zh) * | 2016-07-07 | 2026-03-10 | 赛克里翁治疗有限公司 | 用于制备可溶性鸟苷酸环化酶刺激剂的新方法 |
| CR20220309A (es) | 2016-09-02 | 2022-09-16 | Cyclerion Therapeutics Inc | Estimuladores de sgc |
| US10918639B2 (en) | 2016-10-11 | 2021-02-16 | Bayer Pharma Aktiengesellschaft | Combination containing SGC stimulators and mineralocorticoid receptor antagonists |
| CA3039735A1 (en) | 2016-10-11 | 2018-04-19 | Bayer Pharma Aktiengesellschaft | Combination containing sgc activators and mineralocorticoid receptor antagonists |
| WO2018111795A2 (en) | 2016-12-13 | 2018-06-21 | Ironwood Pharmaceuticals, Inc. | Use of sgc stimulators for the treatment of esophageal motility disorders |
| CN108203396B (zh) * | 2016-12-19 | 2020-12-08 | 江西东邦药业有限公司 | 一种脑啡肽酶抑制剂的合成 |
| WO2019081456A1 (en) | 2017-10-24 | 2019-05-02 | Bayer Aktiengesellschaft | USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT |
| EP3498298A1 (en) | 2017-12-15 | 2019-06-19 | Bayer AG | The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi) |
| CA3086207A1 (en) * | 2017-12-19 | 2019-06-27 | Cyclerion Therapeutics, Inc. | Sgc stimulators |
| JP7314173B2 (ja) | 2018-04-30 | 2023-07-25 | バイエル アクチェンゲゼルシャフト | 認知障害の治療のためのｓＧＣ活性化薬及びｓＧＣ刺激薬の使用 |
| CA3100096A1 (en) | 2018-05-15 | 2019-11-21 | Bayer Aktiengesellschaft | 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization |
| EP3574905A1 (en) | 2018-05-30 | 2019-12-04 | Adverio Pharma GmbH | Method of identifying a subgroup of patients suffering from dcssc which benefits from a treatment with sgc stimulators and sgc activators in a higher degree than a control group |
| KR20210031931A (ko) | 2018-07-11 | 2021-03-23 | 사이클리온 테라퓨틱스, 인크. | 미토콘드리아 장애의 치료를 위한 sGC 자극제의 용도 |
| EP3911675A1 (en) | 2019-01-17 | 2021-11-24 | Bayer Aktiengesellschaft | Methods to determine whether a subject is suitable of being treated with an agonist of soluble guanylyl cyclase (sgc) |
| WO2022075756A1 (ko) | 2020-10-08 | 2022-04-14 | 주식회사 큐롬바이오사이언스 | 베타-라파촌을 유효성분으로 포함하는 담즙 정체성 간질환 예방 또는 치료용 약학 조성물 |
| CN117327016A (zh) * | 2023-09-12 | 2024-01-02 | 湖北泰盛化工有限公司 | 一种砜吡草唑中间体的制备方法 |
Family Cites Families (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US3995631A (en) | 1971-01-13 | 1976-12-07 | Alza Corporation | Osmotic dispenser with means for dispensing active agent responsive to osmotic gradient |
| US4203440A (en) | 1978-10-23 | 1980-05-20 | Alza Corporation | Device having variable volume chamber for dispensing useful agent |
| US4627850A (en) | 1983-11-02 | 1986-12-09 | Alza Corporation | Osmotic capsule |
| EP0192963B1 (de) | 1985-02-27 | 1988-07-20 | Werkzeugmaschinenfabrik Oerlikon-Bührle AG | Schwingungsmesseinrichtung für ein Spiralkegelradgetriebe auf einer Zahnradprüfmaschine |
| IL92966A (en) | 1989-01-12 | 1995-07-31 | Pfizer | Dispensing devices powered by hydrogel |
| US5721365A (en) | 1989-09-15 | 1998-02-24 | Us Health | N-substituted piperazine NONOates |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5324280A (en) | 1990-04-02 | 1994-06-28 | Alza Corporation | Osmotic dosage system for delivering a formulation comprising liquid carrier and drug |
| US5155137A (en) | 1990-09-20 | 1992-10-13 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Complexes of nitric oxide with polyamines |
| AU668107B2 (en) | 1991-09-24 | 1996-04-26 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | Oxygen substituted derivatives of nucleophile-nitric oxide adducts as nitric oxide donor prodrugs |
| US5814666A (en) | 1992-04-13 | 1998-09-29 | The United States As Represented By The Department Of Health And Human Services | Encapsulated and non-encapsulated nitric oxide generators used as antimicrobial agents |
| US5632981A (en) | 1992-08-24 | 1997-05-27 | The United States Of America As Represented By The Department Of Health And Human Services | Biopolymer-bound nitric oxide-releasing compositions, pharmaceutical compositions incorporating same and methods of treating biological disorders using same |
| US5910316A (en) | 1992-08-24 | 1999-06-08 | The United States Of America, As Represented By The Department Of Health And Human Services | Use of nitric oxide-releasing agents to treat impotency |
| US5691423A (en) | 1992-08-24 | 1997-11-25 | The United States Of America As Represented By The Department Of Health And Human Services | Polysaccharide-bound nitric oxide-nucleophile adducts |
| US5405919A (en) | 1992-08-24 | 1995-04-11 | The United States Of America As Represented By The Secretary Of Health And Human Services | Polymer-bound nitric oxide/nucleophile adduct compositions, pharmaceutical compositions and methods of treating biological disorders |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| AU685178B2 (en) | 1993-10-08 | 1998-01-15 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | Use of nitric oxide-releasing compounds as hypoxic cell radiation sensitizers |
| JP2928079B2 (ja) | 1994-02-14 | 1999-07-28 | 永信薬品工業股▲ふん▼有限公司 | １−（置換ベンジル）−３−（置換アリール）縮合ピラゾール類、その製造法及びその用途 |
| US5700830A (en) | 1994-11-22 | 1997-12-23 | The United States Of America As Represented By The Department Of Health And Human Services | Use of nitric oxide-releasing agents for reducing metastasis risk |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| EP0837052B1 (en) | 1995-06-21 | 2006-08-23 | Shionogi & Co., Ltd. | Bicyclic amino derivatives and pgd 2 antagonist containing the same |
| US5714511A (en) | 1995-07-31 | 1998-02-03 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Selective prevention of organ injury in sepsis and shock using selection release of nitric oxide in vulnerable organs |
| EP0945450B1 (en) | 1996-12-12 | 2005-05-11 | Shionogi & Co., Ltd. | Fused heterocyclic benzenecarboxylic acid amide derivatives and pgd2 antagonists containing the same |
| CZ297324B6 (cs) | 1996-12-13 | 2006-11-15 | Shionogi & Co., Ltd. | Benzothiofenkarboxamidové deriváty a antagonisty PGD2, které je obsahují |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| CN1332943C (zh) | 1998-07-08 | 2007-08-22 | 萨诺费－阿文蒂斯德国有限公司 | 硫取代的磺酰基氨基羧酸n－芳基酰胺,其制备方法、用途以及含有该化合物的药物制剂 |
| DE19830430A1 (de) | 1998-07-08 | 2000-01-13 | Hoechst Marion Roussel De Gmbh | Schwefelsubstituierte Sulfonylamino-carbonsäure-N-arylamide, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| GB9824310D0 (en) | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
| WO2000035419A2 (en) | 1998-12-17 | 2000-06-22 | Alza Corporation | Conversion of liquid filled gelatin capsules into controlled release systems by multiple coatings |
| US6342249B1 (en) | 1998-12-23 | 2002-01-29 | Alza Corporation | Controlled release liquid active agent formulation dosage forms |
| DE19942809A1 (de) | 1999-09-08 | 2001-03-15 | Bayer Ag | Verfahren zur Herstellung substituierter Pyrimidinderivate |
| DE19943635A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE60115411D1 (de) | 2000-04-12 | 2006-01-05 | Merck Frosst Canada & Co Kirkl | Verfahren und zusammensetzungen zur behandlung von allergischen zuständen mit pgd2 rezeptor antagonisten |
| US20010051624A1 (en) | 2000-04-12 | 2001-12-13 | Jones Thomas R. | Method and compositions for the treatment of allergic conditions using PGD2 receptor antagonists |
| US6878522B2 (en) | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
| FR2811989A1 (fr) | 2000-07-18 | 2002-01-25 | Sanofi Synthelabo | Derives de polyfluoroalkytriazole, leur preparation et leur application en therapeutique |
| AR031176A1 (es) * | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| PE20020856A1 (es) | 2001-02-13 | 2002-11-11 | Aventis Pharma Gmbh | 1,2,3,4-tetrahidronaftil aminas aciladas |
| TWI243164B (en) | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| TWI241190B (en) | 2001-02-13 | 2005-10-11 | Aventis Pharma Gmbh | 4-Fluoro-N-indan-2-yl benzamide and its use as pharmaceutical |
| PE20020870A1 (es) | 2001-02-13 | 2002-11-18 | Aventis Pharma Gmbh | 6,7,8,9-tetrahidro-5h-benzocicloheptenil aminas aciladas |
| US6511911B1 (en) | 2001-04-03 | 2003-01-28 | Advanced Micro Devices, Inc. | Metal gate stack with etch stop layer |
| EP1424325A4 (en) | 2001-09-07 | 2005-12-21 | Ono Pharmaceutical Co | INDOLE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND MEDICAMENTS CONTAINING THEM AS AN ACTIVE AGENT |
| KR20040044856A (ko) | 2001-09-07 | 2004-05-31 | 오노 야꾸힝 고교 가부시키가이샤 | 인돌 유도체 화합물 |
| SE0200411D0 (sv) | 2002-02-05 | 2002-02-05 | Astrazeneca Ab | Novel use |
| SE0200356D0 (sv) | 2002-02-05 | 2002-02-05 | Astrazeneca Ab | Novel use |
| DE10216145A1 (de) | 2002-04-12 | 2003-10-23 | Bayer Ag | Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Glaukom |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| AU2003231513A1 (en) | 2002-05-16 | 2003-12-02 | Shionogi And Co., Ltd. | Pgd2 receptor antagonist |
| EP2423190A1 (en) | 2002-05-16 | 2012-02-29 | Shionogi&Co., Ltd. | Compounds Exhibiting PGD 2 Receptor Antagonism |
| SE0201635D0 (sv) | 2002-05-30 | 2002-05-30 | Astrazeneca Ab | Novel compounds |
| TW200307542A (en) | 2002-05-30 | 2003-12-16 | Astrazeneca Ab | Novel compounds |
| SE0202241D0 (sv) | 2002-07-17 | 2002-07-17 | Astrazeneca Ab | Novel Compounds |
| AU2003277285B2 (en) | 2002-10-04 | 2007-12-13 | Millennium Pharmaceuticals, Inc. | PGD2 receptor antagonists for the treatment of inflammatory diseases |
| ZA200505523B (en) | 2002-12-20 | 2006-09-27 | Amgen Inc | Asthma and allergic inflammation modulators |
| US20050059660A1 (en) * | 2003-08-01 | 2005-03-17 | Pharmacia & Upjohn Company | Novel combination |
| EP1653926A1 (en) | 2003-08-04 | 2006-05-10 | Pfizer Products Inc. | Dosage forms providing controlled release of cholesteryl ester transfer protein inhibitors and immediate release of hmg-coa reductase inhibitors |
| US8309608B2 (en) | 2003-11-06 | 2012-11-13 | Sanofi-Aventis Deutschland Gmbh | Use of eNOS transcription enhancers in the cell therapy of ischemic heart diseases |
| US20090186896A1 (en) * | 2005-09-29 | 2009-07-23 | Bayer Healthcare Ag | PDE Inhibitors and Combinations Thereof for the Treatment of Urological Disorders |
| GB0604937D0 (en) | 2006-03-10 | 2006-04-19 | Novartis Ag | Organic compounds |
| AU2007292347A1 (en) | 2006-09-07 | 2008-03-13 | Allergan, Inc. | Heteroaromatic compounds having sphingosine-1-phosphate (S1P) receptor agonist and/or antagonist biological activity |
| DE602007008470D1 (en) | 2006-10-17 | 2010-09-23 | Bend Res Inc | Off |
| WO2008138483A1 (en) * | 2007-05-12 | 2008-11-20 | Bayer Schering Pharma Aktiengesellschaft | sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS |
| KR20100059952A (ko) | 2007-09-06 | 2010-06-04 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 사이클라제 활성제 |
| WO2009094242A1 (en) | 2008-01-24 | 2009-07-30 | Merck & Co., Inc. | Angiotensin ii receptor antagonists |
| AU2009322836B2 (en) | 2008-11-25 | 2013-04-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| CN102414194A (zh) | 2009-02-26 | 2012-04-11 | 默沙东公司 | 可溶性鸟苷酸环化酶激活剂 |
| SI2531187T1 (sl) | 2010-02-05 | 2016-01-29 | Adverio Pharma Gmbh | Stimulatorji sGC ali aktivatorji sGC sami in v kombinaciji z inhibitorji PDE5 za zdravljenje cistične fibroze |
| US9284301B2 (en) | 2010-03-25 | 2016-03-15 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| UA107112C2 (uk) | 2010-05-27 | 2014-11-25 | Мерк Шарп Енд Доме Корп. | Активатори розчинної гуанілатциклази |
| AR088020A1 (es) * | 2010-06-30 | 2014-05-07 | Ironwood Pharmaceuticals Inc | Compuestos heterociclicos como estimuladores de sgc |
| EP2590987B1 (de) | 2010-07-09 | 2016-03-09 | Bayer Intellectual Property GmbH | Annellierte 4-aminopyrimidine und ihre verwendung als stimulatoren der löslichen guanylatcyclase |
| EP2632551B1 (en) | 2010-10-28 | 2016-07-06 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| EP2637659B1 (en) * | 2010-11-09 | 2016-05-18 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| US9012651B2 (en) | 2011-03-24 | 2015-04-21 | Abbvie Inc. | TRPV3 modulators |
| KR20140050029A (ko) | 2011-07-06 | 2014-04-28 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 헤테로아릴-치환된 피라졸로피리딘 및 가용성 구아닐레이트 시클라제 자극제로서의 그의 용도 |
| CN104039784B (zh) | 2011-09-02 | 2017-08-22 | 拜耳知识产权有限责任公司 | 取代的增环嘧啶及其用途 |
| WO2013092512A1 (en) * | 2011-12-21 | 2013-06-27 | Bayer Intellectual Property Gmbh | Substituted benzylpyrazoles |
| CN106117194A (zh) | 2011-12-27 | 2016-11-16 | 铁木医药有限公司 | 可用作sgc刺激剂的2‑苄基、3‑(嘧啶‑2‑基)取代的吡唑类 |
| DE102012200349A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung |
| SI2970243T1 (sl) * | 2013-03-15 | 2020-04-30 | Cyclerion Therapeutics, Inc. | SGC stimulatorji |
| WO2014202588A1 (en) * | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
-
2014
- 2014-12-10 JP JP2016539132A patent/JP2016540017A/ja active Pending
- 2014-12-10 WO PCT/US2014/069537 patent/WO2015089182A1/en not_active Ceased
- 2014-12-10 CN CN201480074810.XA patent/CN106304835A/zh active Pending
- 2014-12-10 EP EP14824644.0A patent/EP3092231B1/en active Active
- 2014-12-10 CA CA2933250A patent/CA2933250A1/en not_active Abandoned
- 2014-12-10 EA EA201691194A patent/EA032028B1/ru not_active IP Right Cessation
- 2014-12-10 MX MX2016007522A patent/MX2016007522A/es unknown
- 2014-12-10 US US15/103,178 patent/US20160311826A1/en not_active Abandoned
-
2020
- 2020-12-15 US US17/122,542 patent/US20210214364A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016540017A (ja) | 2016-12-22 |
| US20160311826A1 (en) | 2016-10-27 |
| WO2015089182A1 (en) | 2015-06-18 |
| EA201691194A1 (ru) | 2016-12-30 |
| US20210214364A1 (en) | 2021-07-15 |
| CN106304835A (zh) | 2017-01-04 |
| EP3092231B1 (en) | 2018-06-27 |
| MX2016007522A (es) | 2017-12-15 |
| EP3092231A1 (en) | 2016-11-16 |
| EA032028B1 (ru) | 2019-03-29 |
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