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51. 发明授权

US08288417B2 N-substituted piperidines and their use as pharmaceuticals 有权
标题翻译： N-取代的哌啶及其作为药物的用途
公开(公告)号：US08288417B2
公开(公告)日：2012-10-16
申请号：US13279700
申请日：2011-10-24
申请人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
发明人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
IPC分类号： A61K31/4523 , C07D211/00
CPC分类号： C07D401/14 , C07D211/60 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-和bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

52. 发明申请

US20120040964A1 N-SUBSTITUTED PIPERIDINES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N-取代的哌嗪及其作为药物的用途
公开(公告)号：US20120040964A1
公开(公告)日：2012-02-16
申请号：US13279700
申请日：2011-10-24
申请人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
发明人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
IPC分类号： A61K31/445 , C07D401/12 , A61K31/4545 , C07D409/12 , A61K31/4535 , C07D405/12 , A61K31/4525 , A61K31/4709 , C07D403/04 , A61K31/497 , A61K31/506 , A61K31/501 , A61K31/55 , A61P3/04 , A61P3/10 , A61P3/08 , A61P5/48 , A61P9/12 , A61P3/06 , A61P25/28 , A61P25/24 , A61P27/06 , A61P9/00 , A61P19/10 , A61P29/00 , A61P13/12 , A61P9/04 , A61P9/10 , A61P7/02 , A61P3/00 , C07D211/60
CPC分类号： C07D401/14 , C07D211/60 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

53. 发明授权

US08071624B2 N-substituted piperidines and their use as pharmaceuticals 有权
标题翻译： N-取代的哌啶及其作为药物的用途
公开(公告)号：US08071624B2
公开(公告)日：2011-12-06
申请号：US11159448
申请日：2005-06-23
申请人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
发明人： Wenqing Yao , Meizhong Xu , Colin Zhang , Yanlong Li , Jincong Zhuo , Brian W. Metcalf
IPC分类号： A61K31/4523 , C07D211/00
CPC分类号： C07D401/14 , C07D211/60 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

54. 发明申请

US20100256114A1 Amido Compounds And Their Use As Pharmaceuticals 有权
标题翻译：酰胺化合物及其作为药物的用途
公开(公告)号：US20100256114A1
公开(公告)日：2010-10-07
申请号：US12817887
申请日：2010-06-17
申请人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
IPC分类号： A61K31/55 , C07D207/12 , A61K31/40 , C07D211/06 , A61K31/445 , A61K31/47 , C07D401/02 , A61K31/4439 , C07D403/02 , A61K31/497 , C07D217/00 , C07D209/44 , A61K31/4035 , C07D209/96 , A61K31/407 , C07D277/00 , A61K31/426 , C07D263/00 , A61K31/421 , C07D213/02 , A61K31/465 , C07D451/02 , A61K31/46 , C07D265/04 , A61K31/535 , C07D223/02 , C07D223/14 , A61P9/00 , A61P3/06 , A61P3/10
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

55. 发明授权

US5032586A 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase 失效
标题翻译： 7-酮或羟基3,5-二烯类固醇作为类固醇5-α还原酶的抑制剂
公开(公告)号：US5032586A
公开(公告)日：1991-07-16
申请号：US398192
申请日：1989-08-24
申请人： Brian W. Metcalf , Dennis A. Holt , Mark A. Levy
发明人： Brian W. Metcalf , Dennis A. Holt , Mark A. Levy
IPC分类号： A61K31/56 , A61P13/02 , A61P15/00 , A61P17/00 , A61P43/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J31/00 , C07J41/00 , C07J73/00
CPC分类号： C07J7/004 , C07J13/005 , C07J13/007 , C07J3/005 , C07J31/006 , C07J41/0005 , C07J41/0066 , C07J73/005 , C07J9/00 , C07J9/005
摘要： Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.

56. 发明授权

US4888336A Steroid 5-alpha-reductase inhibitors 失效
标题翻译：类固醇5-α-还原酶抑制剂
公开(公告)号：US4888336A
公开(公告)日：1989-12-19
申请号：US7539
申请日：1987-07-28
申请人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
发明人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
IPC分类号： A61K31/58 , C07J3/00 , C07J31/00 , C07J73/00
CPC分类号： C07J31/003 , C07J3/005 , C07J73/005 , C07C2103/16 , Y10S514/859
摘要： Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.

57. 发明授权

US4524076A Novel .gamma.-aminobutyric acid transaminase inhibitors 失效
标题翻译：新型γ-氨基丁酸转氨酶抑制剂
公开(公告)号：US4524076A
公开(公告)日：1985-06-18
申请号：US663250
申请日：1984-10-22
申请人： Brian W. Metcalf , Bruce J. Lippert
发明人： Brian W. Metcalf , Bruce J. Lippert
IPC分类号： A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P25/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C271/22 , C07D307/24 , C07D307/30 , C07D333/36 , C07D333/38 , C07F7/10 , C07F7/18 , C07D307/89
CPC分类号： C07F7/1804 , C07D307/24 , C07D307/30 , C07D333/38 , C07F7/10 , C07F7/1836 , C07F7/1856
摘要： This application relates to 4-amino-4,5-dihydro-2-furancarboxylic acid, and esters thereof, useful as .gamma.-aminobutyric acid transaminase inhibitors.
摘要翻译：本申请涉及可用作γ-氨基丁酸转氨酶抑制剂的4-氨基-4,5-二氢-2-呋喃羧酸及其酯。

58. 发明授权

US4293548A 18-Substituted pregn-4-ene-3,20-diones 失效
标题翻译： 18-取代的怀孕4-烯-3,20-二酮
公开(公告)号：US4293548A
公开(公告)日：1981-10-06
申请号：US183534
申请日：1980-09-02
申请人： Brian W. Metcalf , J. O'Neal Johnston
发明人： Brian W. Metcalf , J. O'Neal Johnston
IPC分类号： A61K31/57 , A61P3/06 , A61P5/38 , A61P7/10 , C07J5/00 , C07J7/00 , C07J21/00 , C07J43/00 , A61K31/56
CPC分类号： C07J7/002 , C07J21/006 , C07J43/003 , C07J5/0015
摘要： Progesterone derivatives having a vinylidene or a 1-alkynyl substituent at the 18-position and further optionally hydroxylated at the 11-position and the 21-position are described herein. Compounds having both an ethynyl substituent and a hydroxy substituent at the 18-position are also described herein. The compounds are useful as aldosterone inhibitors.
摘要翻译：本文描述了在18位具有亚乙烯基或1-炔基取代基并进一步任选在11位和21位羟基化的孕酮衍生物。本文还描述了在18位具有乙炔基取代基和羟基取代基的化合物。该化合物可用作醛固酮抑制剂。

59. 发明授权

US4190586A .alpha.-Acetylenic derivatives of .alpha.-amino acids 失效
标题翻译： α-氨基酸的α-乙酸衍生物
公开(公告)号：US4190586A
公开(公告)日：1980-02-26
申请号：US947940
申请日：1978-10-02
申请人： Brian W. Metcalf , Michel Jung
发明人： Brian W. Metcalf , Michel Jung
IPC分类号： C07F7/08 , C07D207/26 , C07D211/76
CPC分类号： C07F7/0818 , Y10S514/96 , Y10S514/962
摘要： Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein n is an integer of from 1 to 3; R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and the lactams thereof when n is 2 or 3; and pharmaceutically acceptable salts and individual optical isomers thereof.
摘要翻译：具有以下一般结构的α-氨基酸的新型炔属衍生物：其中n为1至3的整数; R是氢，烷基羰基，其中烷基部分具有1至4个碳原子，并且是直链或支链的烷氧基羰基，其中烷氧基部分具有1至4个碳原子并且是直链或支链的，或者其中R2是氢， 1至4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; 每个R 1相同，为羟基，具有1至8个碳原子的直链或支链烷氧基，-NR 3 R 4，其中R 3和R 4各自为氢或1至4个碳原子的低级烷基并且可以相同或不同的，或其中R5是氢，1-4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; 当n为2或3时，其内酰胺; 及其药学上可接受的盐和单独的光学异构体。

60. 发明授权

US4088668A Acetylene derivatives 失效
标题翻译：乙炔衍生物
公开(公告)号：US4088668A
公开(公告)日：1978-05-09
申请号：US812068
申请日：1977-07-01
申请人： Brian W. Metcalf , Michel Jung
发明人： Brian W. Metcalf , Michel Jung
IPC分类号： A61K31/695 , A61P9/12 , A61P25/24 , A61P25/26 , C07F7/08 , C07F7/12 , C07F7/10
CPC分类号： C07F7/0812 , C07F7/0818
摘要： Novel compounds of the following general formula are useful pharmacologic agents and are useful as intermediates for the preparation of pharmacologically useful compounds. ##STR1## wherein R.sub.1 is a straight or branched lower alkyl group having from 1 to 4 carbon atoms, R.sub.2 is trialkylmethyl, phenyl, 1-adamantanyl or 2-furyl; R.sub.3 is methoxy or ethoxy; and acid addition salts thereof.
摘要翻译：以下通式的新型化合物是有用的药理学试剂，可用作制备药理学有用化合物的中间体。其中R1是具有1-4个碳原子的直链或支链低级烷基，R2是三烷基甲基，苯基，1-金刚烷基或2-呋喃基; R3是甲氧基或乙氧基; 及其酸加成盐。

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