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11. 发明授权

US07122705B2 Method for preparing 3-cyclopentyloxy-4-methoxybenzaldehyde 有权
标题翻译： 3-环戊氧基-4-甲氧基苯甲醛的制备方法
公开(公告)号：US07122705B2
公开(公告)日：2006-10-17
申请号：US11100862
申请日：2005-04-07
申请人： Bogdan Kazimierz Wilk , Nalukui Mwisiya , Jean Louise Helom
发明人： Bogdan Kazimierz Wilk , Nalukui Mwisiya , Jean Louise Helom
IPC分类号： C07C45/71
CPC分类号： C07C47/575 , C07C41/26 , C07C45/71 , C07C2601/08 , C07C43/253
摘要： Processes for coupling phenol and cycloalkyls including combining an optionally substituted phenol, a cycloalkyl substituted with a leaving group, carbonate salt, tetrahydrofuran, and an optional phase transfer agent are provided. Also provided are processes for preparing 3-cyclopentyloxy-4-methoxybenzaldehyde by combining 3-hydroxy-4-methoxybenzaldehyde, a cyclopentyl compound, a carbonate salt, a solvent, and an optional phase transfer agent.
摘要翻译：提供了将苯酚和环烷基偶合的方法，包括将任选取代的苯酚，被离去基团取代的环烷基，碳酸盐，四氢呋喃和任选的相转移剂组合。还提供了通过3-羟基-4-甲氧基苯甲醛，环戊基化合物，碳酸盐，溶剂和任选的相转移剂组合制备3-环戊氧基-4-甲氧基苯甲醛的方法。

12. 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。

13. 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。

14. 发明申请

US20090306371A1 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：US20090306371A1
公开(公告)日：2009-12-10
申请号：US12508679
申请日：2009-07-24
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D207/337 , C07D265/36 , C07D265/18
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。

15. 发明授权

US07511071B2 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：US07511071B2
公开(公告)日：2009-03-31
申请号：US12044287
申请日：2008-03-07
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。

16. 发明授权

US08168672B2 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：US08168672B2
公开(公告)日：2012-05-01
申请号：US12698472
申请日：2010-02-02
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： A61K31/40 , C07D411/00
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。

17. 发明申请

US20100197645A1 Thioamide Derivatives as Progesterone Receptor Modulators 失效
标题翻译：硫代酰胺衍生物作为孕激素受体调节剂
公开(公告)号：US20100197645A1
公开(公告)日：2010-08-05
申请号：US12698472
申请日：2010-02-02
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： A61K31/565 , A61K31/536 , A61K31/404 , A61K31/567 , A61K31/566 , A61P35/00 , A61P15/18 , A61P5/00 , A61P5/26
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。

18. 发明授权

US07595338B2 Process for preparing 3,3-disubstituted oxindoles and thio-oxindoles 失效
标题翻译：制备3,3-二取代羟吲哚和硫代羟吲哚的方法
公开(公告)号：US07595338B2
公开(公告)日：2009-09-29
申请号：US11413159
申请日：2006-04-27
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/34 , C07C233/11 , C07C233/58 , C07C253/30 , C07C255/35 , C07C2601/02 , C07C2601/14 , C07C2602/42 , C07D209/96 , C07D213/61 , C07D241/44 , C07D333/64 , C07D333/66 , C07D403/04 , C07D471/04 , C07C255/46 , C07C255/47
摘要： Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile. Also provided are methods for preparing iminobenzo[b]thiophene and benzo[b]thiophenone compounds.
摘要翻译：提供了制备羟吲哚和硫代羟吲哚化合物的方法，该化合物可用作有用的药物化合物的前体。具体提供的是制备5-吡咯-3,3-羟基吲哚化合物和5-（7-氟-3,3-二甲基-2-氧代-2,3-二氢-1H-吲哚-5-基）-1 - 甲基-1H-吡咯-2-甲腈。还提供了制备亚氨基苯并[b]噻吩和苯并[b]噻吩酮化合物的方法。

19. 发明授权

US07384953B2 Purification of rapamycin 失效
标题翻译：雷帕霉素的纯化
公开(公告)号：US07384953B2
公开(公告)日：2008-06-10
申请号：US11359294
申请日：2006-02-22
申请人： Chia-Cheng Shaw , Warren Chew , Bogdan Kazimierz Wilk
发明人： Chia-Cheng Shaw , Warren Chew , Bogdan Kazimierz Wilk
IPC分类号： C07D498/18 , A61K31/435
CPC分类号： C07D498/18
摘要： Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.
摘要翻译：描述了纯化的雷帕霉素和用于获得纯化的雷帕霉素的化学方法。

20. 发明授权

US07381856B2 Carbon-carbon cross coupling catalyzed by transition metals on solid supports 失效
标题翻译：碳 - 碳交叉耦合由固体载体上的过渡金属催化
公开(公告)号：US07381856B2
公开(公告)日：2008-06-03
申请号：US10994598
申请日：2004-11-22
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07C1/26 , C07C1/30
CPC分类号： C07D265/18 , B01J23/44 , B01J23/58 , B01J23/628 , B01J23/755 , B01J23/78 , B01J27/053 , B01J27/232 , B01J31/0202 , B01J31/1805 , B01J31/24 , B01J2231/4211 , B01J2531/824 , B01J2531/847 , B01J2531/90 , C07B37/04
摘要： The present invention provides methods of coupling carbon-containing compounds using a transition metal or transition metal complex on a solid support. The solid support can include alkaline earth metal salts, including carbonate and sulfate salts. The transition metals can include palladium or nickel metal. The method can include combining two carbon containing compounds and a transition metal or transition metal complex on a solid support in the presence of a solvent, desirably an alcohol.
摘要翻译：本发明提供了使用过渡金属或过渡金属配合物在固体载体上偶合含碳化合物的方法。固体载体可以包括碱土金属盐，包括碳酸盐和硫酸盐。过渡金属可以包括钯或镍金属。该方法可以包括在溶剂（优选为醇）的存在下将两种含碳化合物和过渡金属或过渡金属络合物结合在固体载体上。

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