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1. 发明授权

US08173682B2 Substituted pyridones as inhibitors of poly(ADP-ribose) polymerase (PARP) 有权
标题翻译：取代的吡啶酮作为聚（ADP-核糖）聚合酶（PARP）的抑制剂
公开(公告)号：US08173682B2
公开(公告)日：2012-05-08
申请号：US11535127
申请日：2006-09-26
申请人： Philip M. Weintraub , Paul R. Eastwood , Shujaath Mehdi , David W. Stefany , Kwon Yon Musick , Neil Moorcroft , Sungtaek Lim , John Z. Jiang , Hartmut Rutten , Stefan Peukert , Uwe Schwahn
发明人： Philip M. Weintraub , Paul R. Eastwood , Shujaath Mehdi , David W. Stefany , Kwon Yon Musick , Neil Moorcroft , Sungtaek Lim , John Z. Jiang , Hartmut Rutten , Stefan Peukert , Uwe Schwahn
IPC分类号： A61K31/4436 , C07D401/14
CPC分类号： C07D213/64 , C07D217/24 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14
摘要： The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
摘要翻译：本发明涉及一系列式I的2,3,5-取代吡啶酮衍生物：其中R，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及制备这些化合物的方法。本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病系统和心血管疾病。

2. 发明授权

US07169925B2 Indole derivatives as interleukin-4 gene expression inhibitors 失效
标题翻译：吲哚衍生物作为白细胞介素-4基因表达抑制剂
公开(公告)号：US07169925B2
公开(公告)日：2007-01-30
申请号：US10421511
申请日：2003-04-23
申请人： Gregory H. Merriman , Philip M. Weintraub , Jeffrey S. Sabol , Ramalinga M. Dharanipragada , Nicholas J. Hrib , John G. Jurcak , Alexandre Gross , Brian Whiteley , Kwon Yon Musick , Joseph T. Klein
发明人： Gregory H. Merriman , Philip M. Weintraub , Jeffrey S. Sabol , Ramalinga M. Dharanipragada , Nicholas J. Hrib , John G. Jurcak , Alexandre Gross , Brian Whiteley , Kwon Yon Musick , Joseph T. Klein
IPC分类号： C07D403/12 , C07D401/00
CPC分类号： A61K31/381 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
摘要翻译：本发明公开了一种用于治疗过敏，哮喘，鼻炎，皮炎，B细胞淋巴瘤，肿瘤和与细菌，鼻病毒或呼吸道合胞病毒（RSV）感染相关的疾病的新一类吲哚衍生物。现在已经发现，本发明的化合物能够调节T辅助细胞Th1 / Th2，从而能够抑制白细胞介素-4（IL-4）信号，IL-4释放或IL的转录 -4生产。

3. 发明授权

US5120840A 4-amino-4-ene-steroids and their use as 5.alpha.-reductase inhibitors 失效
标题翻译： 4-氨基-4-烯类固醇及其作为5α-还原酶抑制剂的用途
公开(公告)号：US5120840A
公开(公告)日：1992-06-09
申请号：US720900
申请日：1991-07-02
申请人： Philip M. Weintraub , Joseph P. Burkhart , Thomas R. Blohm
发明人： Philip M. Weintraub , Joseph P. Burkhart , Thomas R. Blohm
IPC分类号： C07J41/00
CPC分类号： C07J41/0011 , C07J41/0005 , C07J41/0027
摘要： The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.The present application is a continuation-in-part of application Ser. No. 561,041, filed Aug. 1, 1990 and application Ser. No. 671,555, filed Mar. 19, 1991.
摘要翻译：本发明涉及可用作5α-还原酶抑制剂的4-氨基-DTA4-类固醇。通过合适的4-叠氮基类固醇与三苯基膦在含水惰性溶剂中加热反应来制备化合物。本申请是应用程序Ser的部分继续申请。 1990年8月1日提交的第561,041号申请， 1991年3月19日提交的第671,555号。

4. 发明授权

US5990328A Process for the preparation of 4-amino-.DELTA.4-3-ketosteroids via 4-nitro-.DELTA.4-3-ketosteroids 失效
标题翻译：通过4-硝基-DTTA 4-3-酮类固醇制备4-氨基-TATA 4-3-酮类固醇的方法
公开(公告)号：US5990328A
公开(公告)日：1999-11-23
申请号：US256353
申请日：1999-02-24
申请人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Gary Alan Flynn , Timothy Thomas Curran , Chi-Hsin Richard King
发明人： Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates , Gary Alan Flynn , Timothy Thomas Curran , Chi-Hsin Richard King
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
摘要翻译：本发明提供了4-硝基-DTTA 4-3-酮类固醇，它们用作类固醇C17-20裂合酶和5α-还原酶抑制剂，以及制备下式化合物的新方法：包括：a）使起始化合物与有效量的强碱在升高或合适的温度下反应足以产生相应的热力学二烯醇化物的时间，然后加入中性硝化剂以生产4-硝基甾类; 接着; b）使4-硝基甾类与合适的还原剂反应。

5. 发明授权

US5218110A 4-amino-.DELTA..sup.4 -steroids and their use as 5.alpha.-reductase inhibitors 失效
标题翻译： 4-氨基-TATA4-类固醇，它们用作5α-还原酶抑制剂
公开(公告)号：US5218110A
公开(公告)日：1993-06-08
申请号：US855368
申请日：1992-03-20
申请人： Philip M. Weintraub
发明人： Philip M. Weintraub
IPC分类号： C07J41/00 , C07J71/00
CPC分类号： C07J41/0011 , C07J41/0005 , C07J41/0027 , C07J71/001
摘要： The present invention relates to 4-azido-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.
摘要翻译：本发明涉及可用作5α-还原酶抑制剂的4-叠氮基-TATA 4-类固醇。通过合适的4-叠氮基类固醇与三苯基膦在含水惰性溶剂中加热反应来制备化合物。

6. 发明授权

US06365597B1 4-aza steroids 失效
标题翻译： 4-氮杂类固醇
公开(公告)号：US06365597B1
公开(公告)日：2002-04-02
申请号：US08798258
申请日：1997-02-11
申请人： James R. Pribish , Cynthia A. Gates , Philip M. Weintraub
发明人： James R. Pribish , Cynthia A. Gates , Philip M. Weintraub
IPC分类号： A61K3144
CPC分类号： A61K31/568 , C07D221/18
摘要： The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formula:
摘要翻译：本发明涉及4-氮杂-17β-（环丙氧基） - 雄甾-5α-雄甾烷-3-酮，4-氮杂-17β-（环丙基氨基） - 雄甾-4-烯-3-酮及相关化合物，这些化合物，以及C17-20裂解酶，5α-还原酶和C17alpha-羟化酶的抑制以及这些化合物在治疗雄激素和雌激素介导的疾病中的应用，包括良性前列腺增生，雄激素介导的前列腺癌，雌激素介导乳腺癌和DHT介导的疾病如痤疮。与皮质醇过度合成有关的疾病，例如库欣综合征，也包括在内。雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。本发明的化合物具有以下通式：

7. 发明授权

US5869475A Certain 3-ketosteroids used to inhibit steroid 5.alpha.-reductase 失效
标题翻译：某些3-酮类固醇用于抑制类固醇5α-还原酶
公开(公告)号：US5869475A
公开(公告)日：1999-02-09
申请号：US970843
申请日：1997-11-14
申请人： Timothy Thomas Curran , Chi-Hsin Richard King , Gary Alan Flynn , Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates
发明人： Timothy Thomas Curran , Chi-Hsin Richard King , Gary Alan Flynn , Philip M. Weintraub , Michael R. Angelastro , Cynthia A. Gates
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The invention discloses 3-ketosteroids of the following formula used to inhibit steroid 5.alpha.-reductase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropoxy, acetylthioalkane, cyclopylamino, 2-2-dimethyldioxolan-4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkanethiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1-6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1-8 alkyl;R.sub.8 is C.sub.1-8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; and with the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
摘要翻译：本发明公开了用于抑制类固醇5α-还原酶的下式的3-酮甾烷：其中R是OH，C 1 -C 6烷酰基，C 1 -C 6烷酰氧基，C 1 -C 4链烷醇，COCH 2 OH，CO 2 H，CONR 7 R 8，环丙氧基，乙酰硫基烷烃，环氨基，2-2-二甲基二氧戊环-4-基，1,2-二羟乙基和C 1-4链烷硫醇; R1是氢，羟基或C1-6烷基; R1和R2一起可以表示= O，即与17碳双键结合的氧; R2，R3和R4各自独立地为氢或C1-6烷基; R5和R6各自独立地为氢或OH; R5和R6一起可以表示= O，即与11碳双键结合的氧; R7是氢或C1-8烷基; R8是C1-8烷基; 并且条件是当R是OH时，则R1是氢; 并且条件是当R5是OH时，则R6是氢。

8. 发明授权

US5189032A 4-amino-.DELTA..sup.4,6 -steroids and their use as 5.alpha.-reductase inhibitors 失效
标题翻译： 4-氨基-DTA4-4-类固醇，它们用作5α-还原酶抑制剂
公开(公告)号：US5189032A
公开(公告)日：1993-02-23
申请号：US855372
申请日：1992-03-20
申请人： Philip M. Weintraub
发明人： Philip M. Weintraub
IPC分类号： C07J41/00 , C07J71/00
CPC分类号： C07J41/0011 , C07J41/0005 , C07J71/001
摘要： The present invention relates to 4-amino-.DELTA..sup.4,6 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence of a strong acid such as sulfuric acid at about 100.degree. C.
摘要翻译：本发明涉及可用作5α-还原酶抑制剂的4-氨基-DTA4-4-类固醇。通过在约100℃的强酸例如硫酸存在下，在惰性溶剂中，通过适当的4,5-环氧类固醇与叠氮化钠的反应制备化合物。

9. 发明授权

US06413951B2 20-fluoro-17(20)-vinyl steroids 失效
标题翻译： 20-氟-17（20） - 乙烯基类固醇
公开(公告)号：US06413951B2
公开(公告)日：2002-07-02
申请号：US09886818
申请日：2001-06-21
申请人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K3156
CPC分类号： C07J13/007
摘要： The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formulae:
摘要翻译：本发明涉及20和xgr-氟孕烷-4,17（20） - 二烯-21-蓖麻油酸乙酯，20＆xgr-氟-3β-羟基孕烯-5,17（20） - 二烯-21-酸（20） - 二烯-3-酮，20和xgr-氟孕烷-5,17（20） - 二烯-3β，21-二醇及相关化合物，并与掺入这些化合物的组合物以及C17,20裂解酶，5α-还原酶和C17-羟化酶的抑制，以及这些化合物在治疗雄激素和雌激素介导或依赖性疾病（包括良性前列腺增生症，前列腺癌）中的用途，乳腺癌和DHT介导的疾病如痤疮和多毛症。还包括治疗与过度合成皮质醇有关的疾病，例如库欣综合征。雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。本发明化合物具有以下通式：

10. 发明授权

US5750744A Process for the preparation of 4-amino- 4-3-ketosteroids via 4-nitro- 4-3-ketosteroids 失效
标题翻译：通过4-硝基-4- 3-酮类固醇制备4-氨基-4- 3-酮类固醇的方法
公开(公告)号：US5750744A
公开(公告)日：1998-05-12
申请号：US737031
申请日：1997-02-11
申请人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Gary Alan Flynn , Chi-Hsin Richard King , Timothy Thomas Curran
发明人： Philip M. Weintraub , Cynthia A. Gates , Michael R. Angelastro , Gary Alan Flynn , Chi-Hsin Richard King , Timothy Thomas Curran
IPC分类号： A61K31/56 , A61P37/04 , C07J41/00 , C07J1/00
CPC分类号： C07J41/0005 , C07J41/0011 , C07J41/0066
摘要： The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitro-steroid; and then; b) reacting the 4-nitrosteroid with a suitable reducing agent.
摘要翻译： PCT No.PCT / US95 / 04399 Sec。 371日期1997年2月11日 102（e）1997年2月11日PCT PCT 1995年4月11日PCT公布。公开号WO95 / 29932 日期：1995年11月9日本发明提供4-硝基-D3TA 4-3-酮类固醇，它们用作类固醇C17-20裂合酶和5α-还原酶抑制剂，以及制备下式化合物的新方法： I顺序地包括：a）在升高的或合适的温度下使式Ⅰ的起始化合物与有效量的强碱反应足以产生相应的热力学二烯醇化物的时间，然后加入中性硝化剂以产生4-硝基类固醇; 接着; b）使4-硝基甾类与合适的还原剂反应。

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