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1. 发明申请

US20090221633A1 INHIBITORS OF AKT (PROTEIN KINASE B) 失效
标题翻译： AKT抑制剂（蛋白激酶B）
公开(公告)号：US20090221633A1
公开(公告)日：2009-09-03
申请号：US12300358
申请日：2007-06-12
申请人： Sajan Joseph , Renhua Li , Michael Ray Myers , Aktham Aburub , Jenny Pingqi Dai , Christopher Randall Schmid
发明人： Sajan Joseph , Renhua Li , Michael Ray Myers , Aktham Aburub , Jenny Pingqi Dai , Christopher Randall Schmid
IPC分类号： A61K31/472 , C07D217/00 , A61P35/00
CPC分类号： C07D217/02
摘要： 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds.
摘要翻译： 4- [5-（2-氨基 - 乙磺酰基） - 异喹啉-7-基] - 苯酚或其药学上可接受的盐或化合物或其盐的水合物作为抗肿瘤和/或抗病毒剂的Akt抑制剂作为包含这些化合物的组合物和使用这些化合物的方法。

2. 发明授权

US07304062B2 Peroxisome proliferator activated receptor alpha agonists 失效
标题翻译：过氧化物酶体增殖物激活受体α激动剂
公开(公告)号：US07304062B2
公开(公告)日：2007-12-04
申请号：US10415673
申请日：2001-11-09
申请人： Samuel James Dominianni , Garret Jay Etgen , Richard Duane Johnston , Nathan Bryan Mantlo , Daniel Ray Mayhugh , Ashraf Saeed , Richard Craig Thompson , Xiaodong Wang , Christopher Randall Schmid , Yanping Xu
发明人： Samuel James Dominianni , Garret Jay Etgen , Richard Duane Johnston , Nathan Bryan Mantlo , Daniel Ray Mayhugh , Ashraf Saeed , Richard Craig Thompson , Xiaodong Wang , Christopher Randall Schmid , Yanping Xu
IPC分类号： A61K31/5377 , A61K31/4709 , A61K31/4196 , C07D413/06 , C07D249/12 , C07D215/12
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基的取代或未取代的基团，烷基，芳基-C 0-2 - - 烷基，杂芳基-C 0-2-2 - 烷基，C 3 -C 6环烷基芳基-C 0-2-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 3烷基的取代或未取代的基团， C 6环烷基和杂芳基。 X是连接子的一个碳原子可以被O，NH或S取代的C 2 -C 5亚烷基连接基，Y是C，O，S，NH 或单一债券。此外，E是（CH 2 SO 2）n COOH，其中n是0,1,2或3，或C（R 3）（R 4）A，其中A是酸性官能团如羧基，羧酰胺取代或未取代的磺酰胺，或取代或未取代的四唑。 R 3是H，饱和或不饱和的C 1 -C 5烷基，C 1 -C 5烷氧基。另外，R 4是H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 3烷基， 5个烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4结合形成C 3 -C 4环烷基。

3. 发明授权

US6018056A Intermediates and processes for preparing benzo (b) thiophenes 失效
标题翻译：制备苯并（b）噻吩的中间体和方法
公开(公告)号：US6018056A
公开(公告)日：2000-01-25
申请号：US69278
申请日：1998-04-29
申请人： Christopher Randall Schmid , Jerry Wayne Misner
发明人： Christopher Randall Schmid , Jerry Wayne Misner
IPC分类号： C07D333/56 , C07D333/64 , C07D333/68 , C07D327/00 , C07D333/52
CPC分类号： C07D333/64 , C07D333/56 , C07D333/68
摘要： The instant invention provides processes for preparing compounds of formula IV, V, and IX, having the structures provided hereinbelow: ##STR1## These compounds are useful intermediates in the further preparation of benzo[b] thiophenes.
摘要翻译：本发明提供制备式IV，V和IX化合物的方法，其具有以下提供的结构：这些化合物是进一步制备苯并[b]噻吩的有用中间体。

4. 发明授权

US07998977B2 Inhibitors of AKT (protein kinase B) 失效
标题翻译： AKT抑制剂（蛋白激酶B）
公开(公告)号：US07998977B2
公开(公告)日：2011-08-16
申请号：US12300358
申请日：2007-06-12
申请人： Sajan Joseph , Renhua Li , Michael Ray Myers , Aktham Aburub , Jenny Pingqi Dai , Christopher Randall Schmid
发明人： Sajan Joseph , Renhua Li , Michael Ray Myers , Aktham Aburub , Jenny Pingqi Dai , Christopher Randall Schmid
IPC分类号： A01N43/42 , A61K31/47 , C07D217/00
CPC分类号： C07D217/02
摘要： 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds.
摘要翻译： 4- [5-（2-氨基 - 乙磺酰基） - 异喹啉-7-基] - 苯酚或其药学上可接受的盐或化合物或其盐的水合物作为抗肿瘤和/或抗病毒剂的Akt抑制剂作为包含这些化合物的组合物和使用这些化合物的方法。

5. 发明授权

US5962475A Substituted benzo(B)thiophene compounds having activity as selective estrogen receptor modulators 失效
标题翻译：具有作为选择性雌激素受体调节剂活性的取代的苯并（B）噻吩化合物
公开(公告)号：US5962475A
公开(公告)日：1999-10-05
申请号：US956802
申请日：1997-10-23
申请人： Christopher Randall Schmid , James Patrick Sluka , Kristin Sue Marron
发明人： Christopher Randall Schmid , James Patrick Sluka , Kristin Sue Marron
IPC分类号： A61K31/38 , A61K31/381 , A61P3/02 , A61P19/10 , A61P43/00 , C07D333/56 , A61K31/445 , C07D409/04 , C07D417/04
CPC分类号： C07D333/56
摘要： The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH.sub.2 ; Y is --CH.sub.2 --, --NH--, --NMe--, --S--, --SO.sub.2 --; and R.sup.3 and R.sup.4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring.The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).
摘要翻译：本发明提供具有下式的氮，硫或碳连接的碱性侧链的化合物，其中R 1和R 2独立地是氢，卤素，羟基，烷氧基，烷基羰基氧基，烷氧基羰基，烷氧基羰基氧基，芳基羰基氧基，芳氧基羰基氧基或烷基磺酰氧基; O-SO 2 - （C 1 -C 6烷基），氯，氟或溴; W是CHOH，C（O）或CH 2; Y是-CH 2 - ， - NH - ， - Me - ， - S - ， - SO 2 - ; 并且R 3和R 4独立地是氢，烷基，烷基羰基，烷基氨基 - 羰基或芳基羰基，或与它们所连接的氮一起形成1-吡咯烷基，1-哌啶基或5-或6-元酰亚胺或环状酰胺环。本发明还提供含有任选含有雌激素或孕激素的化合物的药物组合物，以及这些化合物单独或与雌激素或孕激素组合用于治疗骨质疏松症，主动脉平滑肌细胞增殖（特别是再狭窄）和雌激素的用途依赖性癌症（特别是乳腺癌）。

6. 发明申请

US20090062358A1 PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS 审中-公开
标题翻译： PEROXISOME PROLIFERATOR ACTIVED RECEPTOR ALPHA AGONISTS
公开(公告)号：US20090062358A1
公开(公告)日：2009-03-05
申请号：US11828446
申请日：2007-07-26
申请人： Ivan Collado Cano , Samuel James Dominianni , Garret Jay Etgen, JR. , Cristina Garcia-Paredes , Richard Duane Johnston , Michael Edward Letourneau , Nathan Bryan Mantlo , Michael John Martinelli , Daniel Ray Mayhugh , Ashraf Saeed , Richard Craig Thompson , Xiaodong Wang , David Scott Coffey , Christopher Randall Schmid , Jeffrey Thomas Vicenzi , Yanping Xu
发明人： Ivan Collado Cano , Samuel James Dominianni , Garret Jay Etgen, JR. , Cristina Garcia-Paredes , Richard Duane Johnston , Michael Edward Letourneau , Nathan Bryan Mantlo , Michael John Martinelli , Daniel Ray Mayhugh , Ashraf Saeed , Richard Craig Thompson , Xiaodong Wang , David Scott Coffey , Christopher Randall Schmid , Jeffrey Thomas Vicenzi , Yanping Xu
IPC分类号： A61K31/4196 , C07D249/12 , C07D405/02
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0 - C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团如羧基，甲酰胺取代或未取代的磺酰胺，或取代或未取代的未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。

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