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31. 发明授权

US4322416A 10-Alkynyl steroids 失效
标题翻译： 10-炔基类固醇
公开(公告)号：US4322416A
公开(公告)日：1982-03-30
申请号：US258214
申请日：1981-04-27
申请人： Brian W. Metcalf , J. O'Neal Johnston
发明人： Brian W. Metcalf , J. O'Neal Johnston
IPC分类号： A61K31/565 , A61P5/00 , C07J1/00 , C07J21/00 , C07J71/00 , A61K31/56
CPC分类号： C07J71/001 , C07J1/0011 , C07J1/0022 , C07J21/008
摘要： Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, when the 5,6-bond is saturated, R.sup.5 is divalent .dbd.O; R.sup.6 and R.sup.7 are each H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.2-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, and methods of using the aromatase inhibitors of the invention are also provided.
摘要翻译：提供了具有式“IMAGE”+ TR

32. 发明授权

US4267374A Derivatives of amines and amino acids 失效
标题翻译：胺和氨基酸的衍生物
公开(公告)号：US4267374A
公开(公告)日：1981-05-12
申请号：US52035
申请日：1979-06-25
申请人： Brian W. Metcalf , Michel Jung , Charles Danzin
发明人： Brian W. Metcalf , Michel Jung , Charles Danzin
IPC分类号： A61K31/205 , C07C271/06 , C07C87/24 , C07C103/28 , C07C103/44 , C07C125/06
CPC分类号： A61K31/205 , C07C271/06
摘要： Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## 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 ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.H; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.
摘要翻译：新颖的式（Ⅰ）化合物，其中A是亚甲基，亚乙基或亚乙基; R1是-C3BCH或-CH = CH2; R2是氢或COR，其中R是羟基，1至8个碳原子的直链或支链烷氧基，-NR4R5，其中R4和R5分别是氢或1-4个碳原子的直链或支链低级烷基或其中R 6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; R a是氢，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或其中R7被选定由氢，1至4个碳原子的直链或支链低级烷基，苄基和对羟基苄基; 并且Rb具有与Ra所定义的相同的含义，不同之处在于Rb不是＆lt; IMAGE＆gt;并且Ra和Rb可以相同或不同; 条件是当R 2是氢时，R 1是-C 3 H H; 当A为亚乙基时，R 2为氢; 而当Ra为亚甲基时，及其药学上可接受的盐和单独的光学异构体。

33. 发明授权

US4260823A .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：US4260823A
公开(公告)日：1981-04-07
申请号：US54167
申请日：1979-07-02
申请人： Patrick J. Casara , Michel Jung , Brian W. Metcalf
发明人： Patrick J. Casara , Michel Jung , Brian W. Metcalf
IPC分类号： C07C101/20 , C07C101/26 , C07C101/28 , C07C101/72
CPC分类号： C07C237/12
摘要： Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein 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## is hydrogen, a straight or branched lower alkyl group of 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 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R是氢，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个碳原子是直链或支链的，或者是氢，1-4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; 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; 及其药学上可接受的盐和单独的光学异构体。

34. 发明授权

US4183858A .alpha.-Vinyl tryptophanes 失效
标题翻译： α-乙烯基色氨酸
公开(公告)号：US4183858A
公开(公告)日：1980-01-15
申请号：US812113
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： C07D209/20 , C07D317/30 , C07D501/20 , A61K31/405
CPC分类号： C07D317/30 , C07D209/20
摘要： Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.
摘要翻译：下列通式的新颖化合物及其药学上可接受的盐和单独的光学异构体。该化合物可用作芳族胺脱羧酶抑制剂。

35. 发明授权

US4182891A .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：US4182891A
公开(公告)日：1980-01-08
申请号：US812067
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： A61K31/195 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/27 , A61K38/55 , A61P3/00 , A61P17/00 , A61P25/00 , A61P33/00 , A61P35/00 , A61P37/00 , C07C67/00 , C07C229/30 , C07C233/47 , C07C237/12 , C07C237/16 , C07C237/20 , C07C237/22 , C07C239/00 , C07C279/14 , C07C313/00 , C07C323/58 , C07C323/60 , C07D211/76 , C07H19/16 , C07K1/113 , C07K5/06 , C07D211/72 , C07C101/24 , C07D223/10
CPC分类号： C07H19/16 , C07D211/76
摘要： Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5' -yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or RHN(CH.sub.2).sub.n --; n is the integer 3 or 4; each 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 p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is RHN(CH.sub.2).sub.n -- and each R is hydrogen; with the provisos that when Z is .beta.-benzylthioethyl or S-(5'-desoxyadenosin-5' -yl)-S-methyl-thioethyl, R is hydrogen and R.sub.1 is hydroxy, when Z is .gamma.-guanidinopropyl, R is hydrogen and R.sub.1 is hydroxy or a straight or branched lower alkoxy group of from 1 to 8 carbon atoms, and when Z is RHN(CH.sub.2).sub.n -- both R groups are the same; and pharmaceutically acceptable salts and individual optical isomers thereof.
摘要翻译：下列通式结构的α-氨基酸的新型炔属衍生物：其中Z是β-甲硫基乙基，β-苄硫基乙基，S-（5'-脱氧腺苷-5'-基）-S-甲硫基乙基，γ-胍基丙基，或RHN（CH 2）n - n是3或4的整数; 每个R是氢，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; R1是羟基，1至8个碳原子的直链或支链烷氧基，-NR4R5，其中R4和R5各自是氢或1-4个碳原子的低级烷基，或者其中R3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; 当Z为RHN（CH 2）n - 且每个R为氢时，其内酰胺; 条件是当Z是β-苄基硫代乙基或S-（5'-脱氧腺苷-5'-基）-S-甲基 - 硫代乙基时，R是氢并且R 1是羟基，当Z是γ-胍基丙基时，R是氢和 R 1是羟基或1至8个碳原子的直链或支链低级烷氧基，当Z是RHN（CH2）n-时，两个R基都相同; 及其药学上可接受的盐和单独的光学异构体。

36. 发明授权

US08058288B2 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：US08058288B2
公开(公告)日：2011-11-15
申请号：US12817887
申请日：2010-06-17
申请人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Colin Zhang , Brian W. Metcalf , Chunhong He , Ding-Quan Qian
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Colin Zhang , Brian W. Metcalf , Chunhong He , Ding-Quan Qian
IPC分类号： A61K31/44 , A61K31/40 , A61K31/34 , C07D491/20
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。

37. 发明申请

US20110015212A1 PYRIMIDINONES AS PI3K INHIBITORS 有权
标题翻译： PYRIMIDINONES作为PI3K抑制剂
公开(公告)号：US20110015212A1
公开(公告)日：2011-01-20
申请号：US12824924
申请日：2010-06-28
申请人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： A61K31/519 , C07D473/34 , C07D495/04 , A61K31/52 , A61P19/02 , A61P9/10 , A61P19/08 , A61P17/06 , A61P29/00 , A61P35/00 , A61P1/00 , A61P21/04 , A61P35/02 , A61P11/00 , C12N9/99
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
摘要翻译：本发明提供调节磷酸肌醇3-激酶（PI3K）的活性的嘧啶酮，并且可用于治疗与PI3Ks的活性相关的疾病，包括例如炎症性疾病，基于免疫的疾病，癌症和其它疾病。

38. 发明申请

US20080255154A1 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：US20080255154A1
公开(公告)日：2008-10-16
申请号：US12136529
申请日：2008-06-10
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： A61K31/497 , C07D207/04 , A61K31/40 , A61K31/438 , A61P3/10 , A61P3/04 , C12N9/04 , C07D487/00 , C07D401/02
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1型11-β羟基类固醇脱氢酶抑制剂，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1-β羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病的表达或活性相关的各种疾病。

39. 发明授权

US5237065A 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：US5237065A
公开(公告)日：1993-08-17
申请号：US830806
申请日：1992-02-04
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： C07J3/00 , C07J31/00 , C07J73/00
CPC分类号： C07J31/003 , C07J3/005 , C07J73/005 , C07C2103/16
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.
摘要翻译：本发明的是具有8（14），7（8）或16（17）双键的4-氮杂-5-α-8（14）-17取代的 - --3-酮，任选还具有1（2 ）双键，含有这些化合物的药物组合物，以及使用这些化合物抑制类固醇5-α-还原酶的方法。

40. 发明授权

US5110939A Intermediates in the preparation of steriod 5-alpha-reductase inhibitors 失效
标题翻译：中间体制备的steriod 5-α-还原酶抑制剂
公开(公告)号：US5110939A
公开(公告)日：1992-05-05
申请号：US419563
申请日：1989-10-10
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： C07J3/00 , C07J31/00 , C07J73/00
CPC分类号： C07J31/003 , C07J3/005 , C07J73/005 , C07C2103/16
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.
摘要翻译：本发明的是具有8（14），7（8）或16（17）双键的4-氮杂-5-α-8（14）-17取代的 - --3-酮，任选还具有1（2 ）双键，含有这些化合物的药物组合物，以及使用这些化合物抑制类固醇5-α-还原酶的方法。

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