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1. 发明授权

US07678813B2 Azadecalin Glucocorticoid receptor modulators 有权
标题翻译：阿奇达林糖皮质激素受体调节剂
公开(公告)号：US07678813B2
公开(公告)日：2010-03-16
申请号：US10596998
申请日：2005-01-10
申请人： Robin D. Clark , Nicholas C. Ray , Paul Blaney , Christopher Hurley , Hazel Hunt , David Clark , Karen Williams
发明人： Robin D. Clark , Nicholas C. Ray , Paul Blaney , Christopher Hurley , Hazel Hunt , David Clark , Karen Williams
IPC分类号： A61K31/47 , C07D217/02 , C07D417/12
CPC分类号： C07D217/04 , C07D217/02 , C07D217/06 , C07D217/08 , C07D401/10 , C07D401/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/10 , C07D513/04 , C07D513/06
摘要： The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译：本发明提供了一类新颖的氮杂环丁烷化合物和使用该化合物作为糖皮质激素受体调节剂的方法。

2. 发明授权

US5192770A Serotonergic alpha-oxoacetamides 失效
标题翻译： SEROTONERGIC ALPHA-OXOACETAMIDES
公开(公告)号：US5192770A
公开(公告)日：1993-03-09
申请号：US624028
申请日：1990-12-07
申请人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
发明人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
IPC分类号： A61K31/435 , A61K31/46 , A61P1/00 , A61P1/08 , A61P9/00 , A61P25/00 , A61P25/04 , C07D451/04 , C07D451/08 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08 , C07D487/08
摘要： .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

3. 发明授权

US4957914A 1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
标题翻译： 1,9-链烷基-2,3,4,5-四氢-1H-3-苯并氮杂
公开(公告)号：US4957914A
公开(公告)日：1990-09-18
申请号：US231818
申请日：1988-08-12
申请人： Robin D. Clark , Jacob Berger , Klaus K. Weinhardt
发明人： Robin D. Clark , Jacob Berger , Klaus K. Weinhardt
IPC分类号： C07D223/14 , C07D223/32
CPC分类号： C07D223/32 , C07D223/14
摘要： 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
摘要翻译： 1,9-烷基桥-2,3,4,5-四氢-1H-3-苯并吖庚因及其衍生物，即式I化合物：其中：R选自由氢，氰基，低级烷基，低级烯基和芳烷基组成的基团; R 1，R 2和R 3各自独立地选自：氢，羟基，卤素，三氟甲基，硝基，酰氨基，低级烷氧基，低级烷基和低级烷硫基; Y是具有2至4个碳原子的低级亚烷基; 和其药学上可接受的盐可用作CNS剂，例如作为抗抑郁药，抗焦虑药和抗高血压药，和/或作为其前体。

4. 发明授权

US4956365A Decahydro-8H-isoquino(2,1-g)(1,6)naphthyridine derivatives and related compounds 失效
标题翻译：十氢-8H-异喹啉（2,1-g）（1,6）萘啶衍生物和相关化合物
公开(公告)号：US4956365A
公开(公告)日：1990-09-11
申请号：US257372
申请日：1988-10-12
申请人： Robin D. Clark , Andrew T. Kilpatrick , Michael Spedding
发明人： Robin D. Clark , Andrew T. Kilpatrick , Michael Spedding
IPC分类号： C07D471/14 , C07D491/22
CPC分类号： C07D471/14
摘要： Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;W is oxygen or sulfur; andZ is --R.sup.1, --OR.sup.2 or --NR.sup.3 R.sup.4, whereinR.sup.1 is lower alkyl, lower haloalkyl, cycloalkyl, optionally substituted phenyl or phenyl lower alkyl, or heteroaryl;R.sup.2 is lower alkyl, optionally substituted phenyl or phenyl lower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --(CH.sub.2).sub.m, --N(R.sup.5)-- or oxygen, in which m is an integer of 0-2 and R.sup.5 is hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers.
摘要翻译：（1）和（2）的化合物：其中：X和Y独立地是氢，羟基，低级烷基，低级烷氧基或卤素，或X和Y一起是亚甲二氧基或亚乙基-1,2-二氧基; W是氧或硫; 且Z为-R1，-OR2或-NR3R4，其中R1为低级烷基，低级卤代烷基，环烷基，任选取代的苯基或苯基低级烷基或杂芳基; R2是低级烷基，任意取代的苯基或苯基低级烷基; R3和R4独立地是氢，烷基，任选取代的苯基或苯基低级烷基; 或者R 3和R 4与它们所连接的氮一起代表下式的杂环：其中A是 - （CH 2）m，-N（R 5） - 或氧，其中m是整数0 -2和R5是氢或低级烷基; 或其药学上可接受的盐可用作α2-受体阻滞剂。

5. 发明授权

US4542027A Laidlomycin phenylcarbamate 失效
标题翻译：苯基氨基甲酸铵
公开(公告)号：US4542027A
公开(公告)日：1985-09-17
申请号：US582691
申请日：1984-02-23
申请人： Robin D. Clark
发明人： Robin D. Clark
IPC分类号： C07D493/10 , A23K20/195 , C07H19/01 , A61K31/35 , C07D309/10
CPC分类号： C07H19/01 , A23K20/195
摘要： A compound represented by the formula ##STR1## wherein R.sup.1 is an alkali metal cation or hydrogen and which useful for increasing the feed efficiency of ruminants and for treating coccidiosis in domestic animals, especially chickens.
摘要翻译：由式 + TR 表示的化合物，其中R1是碱金属阳离子或氢，并且其可用于提高反刍动物的饲料效率和用于在家畜，特别是鸡中治疗球虫病。

6. 发明授权

US4353901A 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones 失效
标题翻译： 9-（1,4-苯并二恶烷-2-基烷基和羟烷基）-1-氧杂-4,9-二氮杂螺[5.5]十一烷-3-酮
公开(公告)号：US4353901A
公开(公告)日：1982-10-12
申请号：US312447
申请日：1981-10-19
申请人： Robin D. Clark
发明人： Robin D. Clark
IPC分类号： C07D498/10 , A61K31/535
CPC分类号： C07D498/10 , Y10S514/821 , Y10S514/826
摘要： Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula: ##STR1## wherein:R.sup.1 is ##STR2##R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms;X is hydrogen, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms or halo;m is 1 or 2; andn is 1, 2 or 3; andthe pharmaceutically acceptable acid addition salts thereof.
摘要翻译：用于预防和/或治疗高血压，充血性心力衰竭，心律失常，偏头痛，血管痉挛症和哮喘的化合物由下式表示：（I）

7. 发明授权

US4332804A 9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones 失效
标题翻译： 9- [2-（3-吲哚基）乙基] -1-氧杂-4,9-二氮杂螺[5.5]十一烷-3-酮
公开(公告)号：US4332804A
公开(公告)日：1982-06-01
申请号：US246459
申请日：1981-03-23
申请人： Robin D. Clark
发明人： Robin D. Clark
IPC分类号： A61K31/535 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/12 , A61P11/00 , A61P43/00 , C07D211/48 , C07D498/10 , A61K27/00
CPC分类号： C07D211/48 , Y10S514/821 , Y10S514/826
摘要： Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen or lower alkyl of one to four carbon atoms; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl of one to four carbon atoms or lower alkoxy of one to four carbon atoms; andthe pharmaceutically acceptable acid addition salts thereof.
摘要翻译：用于预防和/或治疗高血压，充血性心力衰竭，心律失常，偏头痛，血管痉挛症和哮喘的化合物由式（I）表示，其中：R，R 1，R 2，R 3和R 4独立地为氢或1-4个碳原子的低级烷基; R5和R6独立地是氢，1-4个碳原子的低级烷基或1-4个碳原子的低级烷氧基; 及其药学上可接受的酸加成盐。

8. 发明申请

US20110166110A1 Fused Ring Azadecalin Glucocorticoid Receptor Modulators 审中-公开
标题翻译：融合环Azadecalin糖皮质激素受体调节剂
公开(公告)号：US20110166110A1
公开(公告)日：2011-07-07
申请号：US13046529
申请日：2011-03-11
申请人： Robin D. Clark , Nicholas C. Ray , Paul M. Blaney , Christopher A. Hurley , Karen Williams
发明人： Robin D. Clark , Nicholas C. Ray , Paul M. Blaney , Christopher A. Hurley , Karen Williams
IPC分类号： A61K31/655 , A61K31/437 , A61K31/5377 , A61K31/538 , A61K31/397 , A61K31/496 , A61K31/519 , A61P25/00 , A61P31/00 , A61P27/06 , A61P29/00 , A61P19/00 , A61P37/08
CPC分类号： C07D471/04
摘要： The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译：本发明提供了一类新颖的稠环氮杂环丁烷化合物和使用该化合物作为糖皮质激素受体调节剂的方法。

9. 发明授权

US07576076B2 Modified pyrimidine glucocorticoid receptor modulators 有权
标题翻译：改性嘧啶糖皮质激素受体调节剂
公开(公告)号：US07576076B2
公开(公告)日：2009-08-18
申请号：US11174096
申请日：2005-06-29
申请人： Robin D. Clark , Nicolas C. Ray , Karen Williams , Peter H. Crackett , Gwen Hickin , David A. Clark
发明人： Robin D. Clark , Nicolas C. Ray , Karen Williams , Peter H. Crackett , Gwen Hickin , David A. Clark
IPC分类号： A01N43/62 , A61K31/50 , A61K31/497 , A61K31/501 , A61K31/505 , C07D403/00 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D243/08
CPC分类号： C07D239/545 , A61K31/506 , A61K31/513 , A61K31/551 , C07D401/04 , C07D403/04
摘要： The present invention provides a compound having the formula: wherein, n and m are 1; X1 and X2 are O; R1 is a member selected from unsubstituted phenyl and substituted phenyl; R2 is a member selected from hydrogen, —CN, —OR2A, -L2A—C(O)R2B, -L2B—S(O)2R2C; R3 is a member selected from unsubstituted benzyl and substituted benzyl; R4 is a member selected from hydrogen and substituted or unsubstituted alkyl, wherein if R4 is methyl, then -L1-R1 is not benzyl or —C(O)—O—CH2—CH3; and L1 is a bond; and compositions and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译：本发明提供具有下式的化合物：其中n和m为1; X1和X2为O; R1是选自未取代的苯基和取代的苯基的成员; R2是选自氢，-CN，-OR2A，-L2A-C（O）R2B，-L2B-S（O）2R2C; R3是选自未取代的苄基和取代的苄基的成员; R4是选自氢和取代或未取代的烷基的成员，其中如果R 4是甲基，则-L 1 -R 1不是苄基或-C（O）-O-CH 2 -CH 3; 而L1是一个键; 以及使用该化合物作为糖皮质激素受体调节剂的组合物和方法。

10. 发明授权

US5527918A Processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl) biphenyl-4-ylmethyl]-1H-indole-3-carboxylic acid 失效
标题翻译：制备1-丁基-2- [2' - （2H-四唑-5-基）联苯-4-基甲基] -1H-吲哚-3-羧酸的方法
公开(公告)号：US5527918A
公开(公告)日：1996-06-18
申请号：US440040
申请日：1995-05-12
申请人： Robin D. Clark , Lawrence E. Fisher , Lee A. Flippin , Michael G. Martin , Stephen R. Stabler
发明人： Robin D. Clark , Lawrence E. Fisher , Lee A. Flippin , Michael G. Martin , Stephen R. Stabler
IPC分类号： A61K31/41 , A61P43/00 , C07D257/04 , C07D403/10 , C07D257/02
CPC分类号： C07D403/10
摘要： The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrasol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxylic acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrasolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.
摘要翻译：本发明涉及制备1-丁基-2- [2' - （2H-四酚-5-基）联苯-4-基甲基] -1H-吲哚-3-羧酸的方法和用于这些方法的中间体。本发明还涉及一种使含有受保护的2H-四唑基的化合物脱保护的方法，该方法包括在硫醇存在下使被保护的化合物与路易斯酸反应。

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