2-Hydroxy-Indan-2-Carbonitrile置于盐酸,氢氧化钾,Pd-Baso4,乙醇,Phosphorus Pentoxide,苯体系中,化学反应生成2-茚羧酸 参考文献:Perold; V. Reiche,Journal Of The South African Chemical Institute,1957,Vol. 10,P. 5,10 标题:Perold; V. Reiche,Journal Of The South African Chemical Institute,1957,Vol. 10,P. 5,10
专利号:WO-9717071-A1 优先权日:1995-11-08 标 题 :Stereoselective synthesis of endothelin receptor antagonists 发明人:MILLS ROBERT JOHN; KOWALSKI CONRAD JOHN; PING LI-JEN; GOMBATZ KERRY JOSEPH 权利人:SMITHKLINE BEECHAM CORP; MILLS ROBERT JOHN; KOWALSKI CONRAD JOHN; PING LI JEN; GOMBATZ KERRY JOSEPH 摘要:The present invention is directed to a synthetic route for preparing endothelium receptor antagonists of formulae (7B) and (7A) and to the chiral intermediates.
专利号:JP-2000507918-A 优先权日:1995-11-08 标 题:Stereoselective synthesis of endothelin receptor antagonists
专利号:EP-0915699-A1 优先权日:1995-11-08 标 题 :Stereoselective synthesis of endothelin receptor antagonists
专利号:EP-0915699-A4 优先权日:1995-11-08 标题:STEREPSELECTIVE SYNTHESIS OF ENDOTHELIN RECEPTOR ANTAGONISTS
专利号:US-7807709-B2 优先权日:2005-03-23 标题 :Organic compounds 发明人:EHRHARDT CLAUS; IRIE OSAMU; LORTHIOIS EDWIGE LILIANE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER 权利人:NOVARTIS AG 摘要:The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.