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1. 发明申请

US20130012702A1 PURIFICATION OF PROGESTERONE RECEPTOR MODULATORS 失效
公开(公告)号：US20130012702A1
公开(公告)日：2013-01-10
申请号：US13618090
申请日：2012-09-14
申请人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Anthony Francis Hadfield , Jean Louise Helom
发明人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Anthony Francis Hadfield , Jean Louise Helom
IPC分类号： C07D413/06 , C07D209/96 , C07D403/10 , C07D265/14
CPC分类号： C07D403/04 , C07D209/96 , C07D405/04 , C07D413/04
摘要： Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.

2. 发明授权

US08129524B2 Cyanopyrrole containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same 失效
标题翻译：含有环状氨基甲酸酯和硫代氨基甲酸酯联芳基的氰基吡咯及其制备方法
公开(公告)号：US08129524B2
公开(公告)日：2012-03-06
申请号：US13179730
申请日：2011-07-11
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D265/12 , C07D207/30
CPC分类号： C07D413/04 , C07D207/34
摘要： Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl) benzoicacid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.
摘要翻译：提供了含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法：Z相同或不同，为H，任选取代的C 1 -C 6烷基或CORA; RA为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基，或任选取代的C 1至C 6氨基烷基; Q相同或不同，为H，OH，NH 2，CN，卤素，任选取代的C 1至C 6烷基，任选取代的C 2至C 6烯基，任选取代的C 1至C 6炔基，任选取代的C 1至C 6烷氧基，任选取代的C 1至 C6氨基烷基或CORB; 且R B为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。包括2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基）苯甲酸甲酯，5- [4-氨基-3-（1-羟基-1-甲基 - 乙基） - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基） - 苯基 - 乙酮或其药学上可接受的盐，并提供其用途。

3. 发明授权

US07786297B2 Purified form of tanaproget 有权
标题翻译：纯化形式的tanaproget
公开(公告)号：US07786297B2
公开(公告)日：2010-08-31
申请号：US11412016
申请日：2006-04-26
申请人： Ramarao Chatlapalli , Arwinder Nagi , John Potoski , Jean Louise Helom , Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Vladimir Dragan
发明人： Ramarao Chatlapalli , Arwinder Nagi , John Potoski , Jean Louise Helom , Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Vladimir Dragan
IPC分类号： C07D265/14
CPC分类号： C07D265/14 , C07D413/04
摘要： Micronized tanaproget, purified tanaproget Form I, and micronized, purified tanaproget Form I are provided. Also provided are compositions containing one or more of the prepared tanaproget forms, methods of using one or more of the prepared tanaproget forms, and kits containing one or more of the prepared tanaproget forms.
摘要翻译：提供微粉化的钠盐瓶，纯化的tanaproget Form I和微粉化的纯化的Tanaproget Form I。还提供了含有一种或多种所制备的钛酸钠形式的组合物，使用一种或多种所制备的钛酸钠形式的方法，以及包含一种或多种所制备的钛酸钠形式的试剂盒。

4. 发明授权

US07358246B2 Thioamide derivatives as progesterone receptor modulators 失效
标题翻译：硫代酰胺衍生物作为孕酮受体调节剂
公开(公告)号：US07358246B2
公开(公告)日：2008-04-15
申请号：US11100860
申请日：2005-04-07
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D417/10 , C07D417/14 , A61K31/5415 , A61K31/547
CPC分类号： C07D413/04 , C07D403/04
摘要： Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
摘要翻译：提供了硫酰胺化合物，特别是硫代酰胺吡咯化合物及其制备方法。这些硫代酰胺化合物可用作孕激素受体调节剂，避孕和治疗孕激素相关性疾病。

5. 发明授权

US08609712B2 Purification of progesterone receptor modulators 失效
标题翻译：孕酮受体调节剂的纯化
公开(公告)号：US08609712B2
公开(公告)日：2013-12-17
申请号：US13618090
申请日：2012-09-14
申请人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Anthony Francis Hadfield , Jean Louise Helom
发明人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Anthony Francis Hadfield , Jean Louise Helom
IPC分类号： A01N43/38 , A61K31/40
CPC分类号： C07D403/04 , C07D209/96 , C07D405/04 , C07D413/04
摘要： Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.
摘要翻译：提供了纯化式I化合物的方法，其中A，B，X，Q和R 1在本文中定义。所述方法包括将式I化合物和溶剂混合; 向溶剂中加入碱; 并沉淀出纯化的式I化合物。

6. 发明申请

US20120016118A1 CYANOPYRROLE CONTAINING CYCLIC CARBAMATE AND THIOCARBAMATE BIARYLS AND METHODS FOR PREPARING THE SAME 失效
标题翻译：含有环状碳酸酯和硫代氨基甲酸酯的CYANOPYRROLE及其制备方法
公开(公告)号：US20120016118A1
公开(公告)日：2012-01-19
申请号：US13179730
申请日：2011-07-11
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D265/18 , C07D207/34
CPC分类号： C07D413/04 , C07D207/34
摘要： Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)benzoic acid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.
摘要翻译：提供了含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法：Z相同或不同，为H，任选取代的C 1 -C 6烷基或CORA; RA为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基，或任选取代的C 1至C 6氨基烷基; Q相同或不同，为H，OH，NH 2，CN，卤素，任选取代的C 1至C 6烷基，任选取代的C 2至C 6烯基，任选取代的C 1至C 6炔基，任选取代的C 1至C 6烷氧基，任选取代的C 1至 C6氨基烷基或CORB; 且R B为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。包括2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基）苯甲酸甲酯，5- [4-氨基-3-（1-羟基-1-甲基 - 乙基） - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基） - 苯基 - 乙酮或其药学上可接受的盐，并提供其用途。

7. 发明授权

US07582755B2 Cyanopyrrole-containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same 失效
标题翻译：含氰基吡咯的环状氨基甲酸酯和硫代氨基甲酸酯联芳基及其制备方法
公开(公告)号：US07582755B2
公开(公告)日：2009-09-01
申请号：US11113795
申请日：2005-04-25
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D265/12
CPC分类号： C07D413/04 , C07D207/34
摘要： Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl.Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl) benzoic acid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.
摘要翻译：提供了制备含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法。 Z相同或不同，为H，任选取代的C 1 -C 6烷基或CORA; RA为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基，或任选取代的C 1至C 6氨基烷基; Q相同或不同，为H，OH，NH 2，CN，卤素，任选取代的C 1至C 6烷基，任选取代的C 2至C 6烯基，任选取代的C 1至C 6炔基，任选取代的C 1至C 6烷氧基，任选取代的C 1至 C6氨基烷基或CORB; 且R B为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。包括2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基）苯甲酸甲酯，5- [4-氨基-3-（1-羟基-1-甲基 - 乙基） - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基） - 苯基 - 乙酮或其药学上可接受的盐，并提供其用途。

8. 发明申请

US20090143345A1 THIOAMIDE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 失效
标题翻译：己酰胺衍生物作为孕激素受体调节剂
公开(公告)号：US20090143345A1
公开(公告)日：2009-06-04
申请号：US12369789
申请日：2009-02-12
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： A61K31/536 , A61K31/5415 , C07D417/10 , A61P17/00 , A61P15/00 , A61K31/565
CPC分类号： C07D413/04 , C07D403/04
摘要： Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
摘要翻译：提供了硫酰胺化合物，特别是硫代酰胺吡咯化合物及其制备方法。这些硫代酰胺化合物可用作孕激素受体调节剂，避孕和治疗孕激素相关性疾病。

9. 发明申请

US20080319204A1 PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS 审中-公开
标题翻译：合成前列腺素受体调节剂的方法
公开(公告)号：US20080319204A1
公开(公告)日：2008-12-25
申请号：US12120959
申请日：2008-05-15
申请人： Yanzhong Wu , Karen Sutherland , John Leo Considine , Bogdan Kazimierz Wilk , Pierre Giguere , Michael MacEwan , Archana Sharma , Alexander Gontcharov
发明人： Yanzhong Wu , Karen Sutherland , John Leo Considine , Bogdan Kazimierz Wilk , Pierre Giguere , Michael MacEwan , Archana Sharma , Alexander Gontcharov
IPC分类号： C07D209/96
CPC分类号： C07D209/96 , C07D403/04
摘要： Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R1-R4, R6, and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R6X or XCH2(CH2)nX′, wherein R6 is C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X′ are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.
摘要翻译：描述了制备取代羟吲哚-2-酮的方法，具体如下，其中R1-R4，R6和n如本文所定义。所述方法包括使第一碱金属氢氧化物，四烷基铵盐，苄腈和R6X或XCH2（CH2）nX'反应，其中R6为C1至C6烷基，取代的C1至C6烷基，C3至C8环烷基，取代C3至 C8环烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环，X和X'独立地为离去基团，n为1至5; （ii）使步骤（i）的产物与至少约60℃的温度下的第二碱金属氢氧化物反应; （iii）使步骤（ii）的产物与碱金属醇盐在至少约140℃的温度下反应，形成羟吲哚-2-酮; （iv）溴化羟吲哚-2-酮; 和（v）将溴代羟吲哚-2-酮与偶联剂偶联。

10. 发明授权

US07446211B2 Coupling process for generating reactive boron-containing derivatives of N-substituted pyrrole-2-carbonitriles to produce biaryls 失效
标题翻译：用于产生N-取代的吡咯-2-碳腈的反应性含硼衍生物以产生联芳基的偶联方法
公开(公告)号：US07446211B2
公开(公告)日：2008-11-04
申请号：US11113794
申请日：2005-04-25
申请人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Jean Louise Helom
发明人： Bogdan Kazimierz Wilk , Arkadiy Zinoviy Rubezhov , Jean Louise Helom
IPC分类号： C07F5/02
CPC分类号： C07D413/04 , C07F5/025
摘要： A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.
摘要翻译：提供了含硼化合物，硼酸盐，含有吡咯甲腈的硼化合物，N-取代吡咯-2-腈含硼化合物及其衍生物的方便的制备方法。本发明还提供这些含硼化合物及其衍生物在偶联反应中的用途，以提供双芳基化合物。

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