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11. 发明授权

US5260309A 4,5,6,11-tetrahydrobenzo [6,7] cycloocta [1,2-b]thiophen-6,11-imines and 6,11-dihydrobenzo [6,7] cycloocta [1,2-b] thiophen-6,11-imines 失效
标题翻译： 4,5,6,11-四氢苯并[6,7]环辛[1,2-b]噻吩-6,11-亚胺和6,11-二氢苯并[6,7]环辛[1,2-b] 6,11-亚胺
公开(公告)号：US5260309A
公开(公告)日：1993-11-09
申请号：US828892
申请日：1992-01-29
申请人： Ralph P. Robinson
发明人： Ralph P. Robinson
IPC分类号： C07D495/18 , C07D513/22 , A61K31/38
CPC分类号： C07D495/18
摘要： The present invention relates to compounds of the formula ##STR1## wherein the broken line represents a saturated or an olefinic bond, R.sup.1 and R.sup.4 are each hydrogen or C.sub.1 to C.sub.6 alkyl, and R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 to C.sub.6 alkyl, halogen, C.sub.1 to C.sub.6 alkoxy or C.sub.1 to C.sub.6 alkylthio, and pharmaceutically acceptable salts thereof, pharmaceutical compounds containing the same, methods of preparing the foregoing compounds, and to novel intermediates in the preparation of the foregoing compounds. These compounds are useful as agents in the prevention of neuronal damage in the brain following cerebral ischemia and during the progression of Alzheimer's disease and also as anticonvulsants.
摘要翻译： PCT No.PCT / US89 / 02387第 371日期1992年1月29日 102（e）日期1992年1月29日PCT提交1989年6月1日PCT公布。 WO90 / 15060 PCT出版物 1990年12月13日。本发明涉及下式化合物：其中虚线代表饱和或烯键，R 1和R 4各自为氢或C 1至C 6烷基，R 2和R 3各自为氢 C 1〜C 6烷基，卤素，C 1〜C 6烷氧基或C 1〜C 6烷硫基，及其药学上可接受的盐，含有该化合物的药物组合物，制备上述化合物的方法，以及制备上述化合物的新中间体。这些化合物可用作预防脑缺血后和阿尔茨海默氏病进程期间脑内神经元损伤以及作为抗惊厥药的药剂。

12. 发明授权

US5994351A Arylsulfonylamino hydroxamic acid derivatives 失效
公开(公告)号：US5994351A
公开(公告)日：1999-11-30
申请号：US122920
申请日：1998-07-27
申请人： Ralph P. Robinson , James P. Rizzi
发明人： Ralph P. Robinson , James P. Rizzi
IPC分类号： A61P19/02 , A61P35/00 , C07C311/29 , C07D213/40 , C07D295/13 , C07D295/15 , C07D295/185 , A61K31/495 , A61K31/535 , C07D295/192
CPC分类号： C07D213/40 , C07C311/29 , C07D295/13 , C07D295/15 , C07D295/185
摘要： A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.

13. 发明授权

US5607959A Oxindole 1-[N-(alkoxycarbonyl) ] carboxamides and 1-(N-carboxamido) carboxamides as antiinflammatory agents 失效
标题翻译：羟吲哚1- [N-（烷氧基羰基）]甲酰胺和1-（N-甲酰氨基）甲酰胺作为抗炎剂
公开(公告)号：US5607959A
公开(公告)日：1997-03-04
申请号：US495509
申请日：1995-07-21
申请人： Ralph P. Robinson
发明人： Ralph P. Robinson
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/34 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14
CPC分类号： C07D405/06 , C07D409/06 , C07D409/14
摘要： Compounds of formula (I) where R.sup.1 is thienyl, phenyl or furyl, X and Y are halogen or hydrogen and Q is alkoxy or amino are useful as analgesic and antiinflamatory agents. ##STR1##
摘要翻译： PCT No.PCT / US93 / 11792 Sec。 371日期1995年7月21日 102（e）日期1995年7月21日PCT提交1993年12月10日PCT公布。公开号WO94 / 18194 日期：1994年8月18日，其中R 1是噻吩基，苯基或呋喃基，X和Y的式（I）化合物是卤素或氢，Q是烷氧基或氨基可用作止痛剂和抗炎剂。（一）

14. 发明授权

US5270331A Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides 失效
标题翻译：抗炎3-酰基-2-羟基吲哚-1-甲酰胺的前药
公开(公告)号：US5270331A
公开(公告)日：1993-12-14
申请号：US009188
申请日：1993-01-26
申请人： Wayne E. Barth , Kelvin Cooper , Edward F. Kleinman , Lawrence A. Reiter , Ralph P. Robinson
发明人： Wayne E. Barth , Kelvin Cooper , Edward F. Kleinman , Lawrence A. Reiter , Ralph P. Robinson
IPC分类号： A61K31/40 , A61K31/404 , A61K31/4433 , A61K31/445 , A61K31/465 , A61K31/535 , A61K31/55 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/04 , C07D405/00 , C07D409/06 , C07D409/14 , C07F7/18 , C07D403/06
CPC分类号： C07D409/06 , C07D409/14 , C07F7/1856
摘要： Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.
摘要翻译：其中R10，R11，R12和R13为氢，烷基或卤素，R为亚烷基氧基烷酰基，亚甲基氧代烯酰基或烯酰基的抗炎和镇痛羟吲哚前药。

15. 发明公开

US20240174637A1 DEGRADERS OF GRK2 AND USES THEREOF 审中-公开
公开(公告)号：US20240174637A1
公开(公告)日：2024-05-30
申请号：US18273755
申请日：2022-01-21
申请人： Grazia PIIZZI , Eugene L., Piatnitski CHEKLER , Jonathan Barry HUROV , Alexandra LANTERMANN , Kiley Marie COUTO , Hua XU , Sourav SARKAR , Bruce Allen LEFKER , Ralph P. ROBINSON , Volodymyr KYSIL , Sonata Therapeutics, Inc.
发明人： Grazia Piizzi , Eugene L. Piatnitski Chekler , Jonathan Barry Hurov , Alexandra Lantermann , Kiley Marie Couto , Hua Xu , Sourav Sarkar , Bruce Allen Lefker , Ralph P. Robinson , Volodymyr Kysil
IPC分类号： C07D401/14 , C07D405/14 , C07D417/14
CPC分类号： C07D401/14 , C07D405/14 , C07D417/14
摘要： Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are degraders of GRK2 proteins and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting the activity of GRK2 and/or degrading a GRK2 protein in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.

16. 发明授权

US07553877B2 Modulators of the glucocorticoid receptor 有权
标题翻译：糖皮质激素受体的调节剂
公开(公告)号：US07553877B2
公开(公告)日：2009-06-30
申请号：US11457323
申请日：2006-07-13
申请人： Yves A. Chantigny , Edward F. Kleinman , Ralph P. Robinson
发明人： Yves A. Chantigny , Edward F. Kleinman , Ralph P. Robinson
IPC分类号： A61K31/56 , A61K31/015
CPC分类号： C07D213/30 , C07C35/42 , C07C39/17 , C07C39/23 , C07C39/42 , C07C43/23 , C07C49/747 , C07C49/755 , C07C49/83 , C07C59/72 , C07C69/712 , C07C205/57 , C07C215/64 , C07C235/20 , C07C255/13 , C07C255/29 , C07C255/53 , C07C271/52 , C07C2603/26 , C07D213/40 , C07D257/04 , C07D271/06 , C07D277/24 , C07D295/088 , C07D295/185 , C07D413/06 , C07D413/12
摘要： The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1—R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
摘要翻译：本发明提供下式的化合物其中A为下式，X，Y，n，R 1 -R 25如说明书中所述，其为糖皮质激素受体的调节剂，因此可用于治疗需要糖皮质激素受体激动剂治疗。糖皮质激素受体调节剂可用于治疗某些炎性疾病。

17. 发明授权

US07468378B2 Substituted quinoline compounds 失效
标题翻译：取代喹啉化合物
公开(公告)号：US07468378B2
公开(公告)日：2008-12-23
申请号：US11049852
申请日：2005-02-03
申请人： Peter Bertinato , Michel A. Couturier , Ernest S. Hamanaka , Marcus D. Ewing , Ralph P. Robinson , Derek L. Tickner
发明人： Peter Bertinato , Michel A. Couturier , Ernest S. Hamanaka , Marcus D. Ewing , Ralph P. Robinson , Derek L. Tickner
IPC分类号： A61K31/44 , C07D275/04
CPC分类号： C07D215/48 , C07D401/12
摘要： This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1—R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.
摘要翻译：本发明涉及式（I）的MTP / Apo-B分泌抑制剂，其中R1-R7，X1，m和n如说明书中所定义，以及包含该化合物的药物组合物，以及该化合物的使用方法和组合物。本发明的化合物可用于治疗肥胖症和相关疾病，病症或病症。

18. 发明授权

US07393958B2 Triamide-substituted heterobicyclic compounds 失效
公开(公告)号：US07393958B2
公开(公告)日：2008-07-01
申请号：US11554351
申请日：2006-10-30
申请人： Peter Bertinato , Michel A. Couturier , Ernest S. Hamanaka , Marcus D. Ewing , Ralph P. Robinson , Derek L. Tickner
发明人： Peter Bertinato , Michel A. Couturier , Ernest S. Hamanaka , Marcus D. Ewing , Ralph P. Robinson , Derek L. Tickner
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D215/48 , C07D401/12
摘要： This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

19. 发明授权

US06380219B1 Arylsulfonylamino hydroxamic acid derivatives 失效
标题翻译：芳基磺酰氨基异羟肟酸衍生物
公开(公告)号：US06380219B1
公开(公告)日：2002-04-30
申请号：US09635186
申请日：2000-08-08
申请人： Ralph P. Robinson , James P. Rizzi
发明人： Ralph P. Robinson , James P. Rizzi
IPC分类号： A61K314468
CPC分类号： C07D213/40 , C07C311/29 , C07D295/13 , C07D295/15 , C07D295/185
摘要： A compound of the formula wherein n, X, R3, R4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
摘要翻译：化合物n，X，R 3，R 4和Ar如上所定义，可用于治疗选自关节炎，癌症，组织溃疡，再狭窄，牙周病，大疱性表皮松解症，巩膜炎等的病症以基质金属蛋白酶活性为特征的疾病，艾滋病，败血症，败血性休克和涉及TNF产生的其他疾病。

20. 发明授权

US06852719B2 Glucocorticoid receptor modulators 失效
标题翻译：糖皮质激素受体调节剂
公开(公告)号：US06852719B2
公开(公告)日：2005-02-08
申请号：US10012274
申请日：2001-10-26
申请人： Kevin K. Liu , Bradley P. Morgan , Ralph P. Robinson
发明人： Kevin K. Liu , Bradley P. Morgan , Ralph P. Robinson
IPC分类号： A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , A61P3/04 , A61P3/10 , A61P25/00 , A61P25/22 , A61P25/24 , A61P29/00 , C07D271/06 , C07D413/04 , C07D413/06
CPC分类号： C07D271/06 , C07D413/04 , C07D413/06
摘要： The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds
摘要翻译：本发明提供式I的非类固醇化合物，包括其前体药物和药学上可接受的盐，其是类固醇受体的特异性调节剂（例如激动剂，部分激动剂和拮抗剂），特别是糖皮质激素受体。本发明还提供含有这些化合物的药物组合物和使用这些化合物治疗需要糖皮质激素受体激动剂或拮抗剂治疗的动物的方法。糖皮质激素受体调节剂可用于治疗如下所述的疾病，例如肥胖，糖尿病，炎症等。本发明还提供了制备这些化合物的方法

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