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1. 发明授权

US06936606B2 Cyanoamido-containing heterocyclic compounds useful as reversible inhibitors of cysteine proteases 有权
标题翻译：可用作半胱氨酸蛋白酶的可逆抑制剂的含氰酰氨基的杂环化合物
公开(公告)号：US06936606B2
公开(公告)日：2005-08-30
申请号：US10256512
申请日：2002-09-27
申请人： Younes Bekkali , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young , Eugene R. Hickey , Weimin Liu , Usha R. Patel
发明人： Younes Bekkali , Denice Mary Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young , Eugene R. Hickey , Weimin Liu , Usha R. Patel
IPC分类号： C07D295/12 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/428 , A61K31/517 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P5/14 , A61P9/10 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07C257/20 , C07C269/06 , C07C271/20 , C07C271/64 , C07C319/20 , C07C323/41 , C07C323/60 , C07D211/22 , C07D213/30 , C07D213/57 , C07D239/80 , C07D263/32 , C07D265/24 , C07D275/06 , C07D277/30 , C07D295/14 , C07D295/215 , C07D307/12 , C07D307/54 , C07D309/08 , C07D309/12 , C07D333/24 , C07D401/04 , C07D401/06 , C07D239/95 , C07D401/12
CPC分类号： C07D295/215 , C07C271/64 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07D213/57 , C07D263/32 , C07D277/30 , C07D307/54 , C07D333/24
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds
摘要翻译：公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R 1，R 2，R 2 R 3，R 4，R 5，R 6，R 8，R SUB， > 9＆gt;和X在本文中定义。该化合物可用于治疗自身免疫性疾病和其他疾病。还公开了制备这些新化合物的方法

2. 发明授权

US06858623B2 Compounds useful as reversible inhibitors of cysteine proteases 有权
标题翻译：可用作半胱氨酸蛋白酶的可逆抑制剂的化合物
公开(公告)号：US06858623B2
公开(公告)日：2005-02-22
申请号：US10448698
申请日：2003-05-29
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31/40 , A61K31/4468 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5365 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K31/55 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P19/10 , A61P21/04 , A61P25/28 , A61P29/00 , A61P31/00 , A61P37/00 , A61P37/06 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08 , A61K31/445 , A61K31/404 , A61K31/428 , A61K31/4523 , A61K31/536 , C07D223/06 , C07D239/80 , C07D263/54 , C07D265/28 , C07D277/62 , C07D451/02
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译：公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R 2，R 3，R 4，R 5，R 6，R 7，R 8，Het和X如本文所定义。该化合物可用于治疗自身免疫性疾病和其他疾病。还公开了制备这些新化合物的方法。

3. 发明授权

US06787540B2 Compounds useful as reversible inhibitors of cysteine proteases 有权
标题翻译：可用作半胱氨酸蛋白酶的可逆抑制剂的化合物
公开(公告)号：US06787540B2
公开(公告)日：2004-09-07
申请号：US10261994
申请日：2002-10-01
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31535
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译：公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R2，R3，R4，R5，R6，R7，R8，Het和X如本文所定义。该化合物可用于治疗自身免疫性疾病和其他疾病。还公开了制备这些新化合物的方法。

4. 发明授权

US06525052B2 Compounds useful as reversible inhibitors of cysteine proteases 有权
标题翻译：可用作半胱氨酸蛋白酶的可逆抑制剂的化合物
公开(公告)号：US06525052B2
公开(公告)日：2003-02-25
申请号：US09808439
申请日：2001-03-14
申请人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
发明人： Younes Bekkali , Eugene R. Hickey , Weimin Liu , Usha R. Patel , Denice M. Spero , Sanxing Sun , David S. Thomson , Yancey D. Ward , Erick R. R. Young
IPC分类号： A61K31335
CPC分类号： C07D401/12 , C04B35/632 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/66 , C07D309/14 , C07D335/02 , C07D401/04 , C07D403/06 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D455/02 , C07D487/08
摘要： Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
摘要翻译：公开了式（Ia）和（Ib）的新型组织蛋白酶S，K，F，L和B可逆抑制性化合物，其中R2，R3，R4，R5，R6，R7，R8，Het和X如本文所定义。该化合物可用于治疗自身免疫性疾病和其他疾病。还公开了制备这些新化合物的方法。

5. 发明授权

US06313117B1 Succinate derivative compounds useful as cysteine protease inhibitors 有权
标题翻译：可用作半胱氨酸蛋白酶抑制剂的琥珀酸衍生物化合物
公开(公告)号：US06313117B1
公开(公告)日：2001-11-06
申请号：US09627869
申请日：2000-07-28
申请人： Younes Bekkali , Rajashehar Betageri , Michel Jose Emmanuel , Eugene Richard Hickey , Weimin Liu , Usha R. Patel , Denice Mary Spero , David S. Thomson , Yancey David Ward , Erick Richard Roush Young , Sanxing Sun
发明人： Younes Bekkali , Rajashehar Betageri , Michel Jose Emmanuel , Eugene Richard Hickey , Weimin Liu , Usha R. Patel , Denice Mary Spero , David S. Thomson , Yancey David Ward , Erick Richard Roush Young , Sanxing Sun
IPC分类号： A61K315355
CPC分类号： C07D295/185 , C07B2200/07 , C07C255/31 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2602/20 , C07D207/16 , C07D211/66 , C07D403/06 , C07D405/04 , C07D409/06
摘要： Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
摘要翻译：公开了式（I）/（Ia）的新型琥珀酸酯衍生物化合物：其中R1，R2，R3，R4，R5，R6，R7，X和A如本文所定义。该化合物可用作半胱氨酸蛋白酶的抑制剂。还公开了使用方法和制备这些化合物的方法。

6. 发明授权

US06982263B2 Nitriles useful as reversible inhibitors of cysteine proteases 有权
标题翻译：用作半胱氨酸蛋白酶的可逆抑制剂的腈
公开(公告)号：US06982263B2
公开(公告)日：2006-01-03
申请号：US10163015
申请日：2002-06-04
申请人： Eugene R. Hickey , Younes Bekkali , Usha R. Patel , Denice Mary Spero , David S. Thomson , Erick Richard Roush Young
发明人： Eugene R. Hickey , Younes Bekkali , Usha R. Patel , Denice Mary Spero , David S. Thomson , Erick Richard Roush Young
IPC分类号： C07D207/16 , C07D211/66 , C07D217/56 , C07D223/12 , C07D413/12
CPC分类号： C07D213/84 , C07B2200/07 , C07C255/29 , C07C271/12 , C07C271/28 , C07C271/30 , C07C271/34 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/28 , C07C2602/50 , C07D207/16 , C07D295/185 , C07D295/205 , C07D295/215
摘要： Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
摘要翻译：公开了本文进一步定义的式（I）的新型腈化合物，该化合物可用作半胱氨酸蛋白酶如组织蛋白酶K，S，F，L和B的可逆抑制剂。这些化合物可用于治疗由这些化合物加重的疾病和病理状况蛋白酶，例如但不限于骨质疏松症，类风湿性关节炎，多发性硬化症，哮喘和其它自身免疫性疾病，阿尔茨海默氏病，动脉粥样硬化。还公开了制备这些新化合物的方法。

7. 发明授权

US08741897B2 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 有权
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US08741897B2
公开(公告)日：2014-06-03
申请号：US10947420
申请日：2004-09-22
申请人： Younes Bekkali , Rajashekhar Betageri , Michel J. Emmanuel , Abdelhakim Hammach , Christian Hanke Justus Joachim Harcken , Thomas Martin Kirrane, Jr. , Daniel Kuzmich , Thomas Wai-Ho Lee , Pingrong Liu , Usha R. Patel , John Robert Proudfoot , Hossein Razavi , Doris Riether , Hidenori Takahashi , David S. Thomson , Ji Wang , Renee Zindell
发明人： Younes Bekkali , Rajashekhar Betageri , Michel J. Emmanuel , Abdelhakim Hammach , Christian Hanke Justus Joachim Harcken , Thomas Martin Kirrane, Jr. , Daniel Kuzmich , Thomas Wai-Ho Lee , Pingrong Liu , Usha R. Patel , John Robert Proudfoot , Hossein Razavi , Doris Riether , Hidenori Takahashi , David S. Thomson , Ji Wang , Renee Zindell
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/4355 , A61K31/5025 , A61P25/28 , A61P9/00 , A61P35/00 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61K31/4406 , A61K31/497 , A61K31/506 , A61K31/4184 , A61K31/404 , A61K31/416 , A61K31/47
CPC分类号： C07D213/75 , A61K31/4745 , A61K31/52 , C07D209/08 , C07D209/12 , C07D213/30 , C07D215/14 , C07D231/12 , C07D231/56 , C07D237/20 , C07D239/42 , C07D307/79 , C07D319/06 , C07D319/08 , C07D333/56 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：式（IA），（IB），（IC）和（ID）的化合物，其中R 1，R 2，R 3，R 4，R 5和R 6如本文中对于式（IA），（IB），和（ID），或互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

8. 发明授权

US06660732B2 Compounds useful as anti-inflammatory agents 有权
公开(公告)号：US06660732B2
公开(公告)日：2003-12-09
申请号：US09962709
申请日：2001-09-25
申请人： Rajashehar Betageri , Steffen Breitfelder , Pier F. Cirillo , Thomas A. Gilmore , Eugene R. Hickey , Thomas M. Kirrane , Monica H. Moriak , Neil Moss , Usha R. Patel , John R. Proudfoot , John R. Regan , Rajiv Sharma , Sanxing Sun , Alan D. Swinamer , Hidenori Takahashi
发明人： Rajashehar Betageri , Steffen Breitfelder , Pier F. Cirillo , Thomas A. Gilmore , Eugene R. Hickey , Thomas M. Kirrane , Monica H. Moriak , Neil Moss , Usha R. Patel , John R. Proudfoot , John R. Regan , Rajiv Sharma , Sanxing Sun , Alan D. Swinamer , Hidenori Takahashi
IPC分类号： A61K315377
CPC分类号： C07D213/74 , C07D213/38 , C07D213/76 , C07D231/38 , C07D307/12 , C07D307/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D493/08 , C07D495/08
摘要： Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

9. 发明授权

US06506747B1 Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents 有权
标题翻译：取代的1-（4-氨基苯基）吡唑及其作为抗炎剂的用途
公开(公告)号：US06506747B1
公开(公告)日：2003-01-14
申请号：US09324933
申请日：1999-06-03
申请人： Rajashekhar Betageri , Charles L. Cywin , Karl Hargrave , Mary Ann Hoermann , Thomas M. Kirrane , Thomas M. Parks , Usha R. Patel , John R. Proudfoot , Rajiv Sharma , Sanxing Sun , Xiao-Jun Wang
发明人： Rajashekhar Betageri , Charles L. Cywin , Karl Hargrave , Mary Ann Hoermann , Thomas M. Kirrane , Thomas M. Parks , Usha R. Patel , John R. Proudfoot , Rajiv Sharma , Sanxing Sun , Xiao-Jun Wang
IPC分类号： A61K31535
CPC分类号： C07D401/04 , C07D231/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D495/04
摘要： 1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.
摘要翻译：公开和描述了在吡唑环的3位和5位和苯环4位的氨基上任意取代的1-（4-氨基苯基）吡唑，其中吡唑抑制T中的IL-2产生淋巴细胞

10. 发明授权

US4942234A Isothiazolone 1,1-dioxide derivatives with psychotropic activity 失效
标题翻译：异噻唑酮1,1-二氧化物衍生物具有精神活性
公开(公告)号：US4942234A
公开(公告)日：1990-07-17
申请号：US316888
申请日：1989-02-28
申请人： Magid A. Abou-Gharbia , Guy A. Schiehser , Usha R. Patel
发明人： Magid A. Abou-Gharbia , Guy A. Schiehser , Usha R. Patel
IPC分类号： C07D417/06 , C07D513/18
CPC分类号： C07D417/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译：公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，低级烷基，芳基或卤素，或者R 1和R 2一起表示 + TR 其中虚线表示可选的双键; R 3，R 4和R 5各自独立地为氢，低级烷基，芳基或卤素; R6是2-吡啶基，2-吡嗪基，2-喹啉基，2-喹喔啉基或由低级烷基，低级烷氧基，三氟甲基，氰基，硝基或卤素取代的任何前述R 6部分; 或其中R 7为苯基，2-吡啶基，2-嘧啶基，3-哒嗪基或2-吡嗪基或由低级烷基，低级烷氧基，卤素，氰基，三氟甲基或硝基取代的前述R7部分中的任一个。 Z是低级亚烷基，亚乙烯基，O或NH; m为1-5; n为0-4; p为1-4; q是1-2; 及其药学上可接受的盐，以及它们作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。

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