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1. 发明申请

WO2023017400A1 METFORMIN CONJUGATES AND THERAPEUTIC USE THEREOF 审中-公开
公开(公告)号：WO2023017400A1
公开(公告)日：2023-02-16
申请号：PCT/IB2022/057370
申请日：2022-08-08
申请人： UNIVERSITA' DI PISA
发明人： CALDERONE, Vincenzo , MARTELLI, Alma , CITI, Valentina , PIRAGINE, Eugenia , TESTAI, Lara , DA SETTIMO PASSETTI, Federico , TALIANI, Sabrina , BARRESI, Elisabetta
IPC分类号： C07C323/60 , C07C327/54 , C07C329/02 , C07C331/32 , C07C335/28 , C07D277/34 , C07D339/04 , C07D339/06 , A61K31/17 , A61K31/381 , A61P3/10 , A61P9/00 , A61P35/00
摘要： Novel compounds of general Formula (I) derived from the conjugation of the native metformin drug to molecular moieties endowed with the property of releasing hydrogen sulfide are described. The compounds forming the object of the present invention are capable of exerting hypoglycaemic and anticancer pharmacological effects, as well as counteracting cardiovascular disruptions associated with diabetes and other metabolic or cancer diseases more effectively. A pharmaceutical composition comprising the compounds according to the invention in a pharmaceutically acceptable carrier, as well as in combination with optional adjuvants, stabilizers and/or preservatives, is also described.

2. 发明申请

WO0035860A3 ACYL ISOTHIOCYANATE RESINS AND THEIR USE IN SOLID-SUPPORTED SYNTHESIS OF GUANIDINES 审中-公开
标题翻译： ACYL异氰酸酯树脂及其在固体支持合成胍的应用
公开(公告)号：WO0035860A3
公开(公告)日：2000-10-26
申请号：PCT/US9929771
申请日：1999-12-15
申请人： PROCTER & GAMBLE , WILSON LAWRENCE JOSEPH
发明人： WILSON LAWRENCE JOSEPH
IPC分类号： C07D295/12 , C07C277/08 , C07C279/06 , C07C279/18 , C07C331/32 , C07D211/58 , C07D217/06 , C08F8/34 , C07C279/10 , C07C279/14 , C07C279/16 , C07C331/24
CPC分类号： C07C277/08 , C07C331/32
摘要： The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetraalkylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.
摘要翻译：本发明涉及式（I）的新型酰基异硫氰酸酯树脂及其制备方法：（a）从苯基羧基树脂开始，用任何将羧基转化为酰基卤的试剂处理树脂，然后用硫氰酸四烷基铵或其碱金属盐，以提供酰基异硫氰酸酯树脂。本发明还涉及使用酰基异硫氰酸酯树脂制备胍化合物和相关的环化化合物的方法，包括以下步骤：（b）使酰基异硫氰酸酯树脂与伯胺反应; （c）使来自步骤（b）的产物与硫活化剂和氨或伯胺或仲胺反应; （d）用强碱或中等强度酸处理来自步骤（c）的产物以从树脂上裂解产物，提供胍化合物或/和相关的环化化合物。

3. 发明申请

WO00035860A2 ACYL ISOTHIOCYANATE RESINS AND THEIR USE IN SOLID-SUPPORTED SYNTHESIS OF GUANIDINES 审中-公开
标题翻译： ACYL异硫氰酸酯树脂及其在固体支持的合成中的应用
公开(公告)号：WO00035860A2
公开(公告)日：2000-06-22
申请号：PCT/US1999/029771
申请日：1999-12-15
IPC分类号： C07D295/12 , C07C277/08 , C07C279/06 , C07C279/18 , C07C331/32 , C07D211/58 , C07D217/06 , C08F8/34 , C07C279/10 , C07C279/14 , C07C279/16 , C07C331/24
CPC分类号： C07C277/08 , C07C331/32
摘要： The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetraalkylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.
摘要翻译：本发明涉及式（I）的新型酰基异硫氰酸酯树脂及其制备方法：（a）由苯基羧基树脂开始，用任意将羧基转化为酰卤的试剂处理树脂，然后用硫氰酸四烷基铵或其碱金属盐，以提供酰基异硫氰酸酯树脂。本发明还涉及使用酰基异硫氰酸酯树脂制备胍化合物和相关环化化合物的方法，包括以下步骤：（b）使酰基异硫氰酸酯树脂与伯胺反应; （c）使来自步骤（b）的产物与硫活化剂和氨或伯胺或仲胺反应; （d）用强碱或中强酸处理步骤（c）的产物以从树脂中切割产物，提供胍化合物或/和相关的环化化合物。

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