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11. 发明授权

US08309571B2 Heterobicyclic compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的异双环化合物
公开(公告)号：US08309571B2
公开(公告)日：2012-11-13
申请号：US13084622
申请日：2011-04-12
申请人： T. G. Murali Dhar , Stephen T. Wrobleski
发明人： T. G. Murali Dhar , Stephen T. Wrobleski
IPC分类号： A01N43/42 , A61K31/44 , C07D413/00
CPC分类号： C07D487/04
摘要： A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物及其对映异构体，非对映异构体和药学上可接受的盐。还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

12. 发明授权

US07381737B2 Crystalline forms and process for preparing spiro-hydantoin compounds 有权
标题翻译：结晶形式和制备螺 - 乙内酰脲化合物的方法
公开(公告)号：US07381737B2
公开(公告)日：2008-06-03
申请号：US11238427
申请日：2005-09-29
申请人： Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
发明人： Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
IPC分类号： A61K31/4188 , C07D235/00
CPC分类号： C07D487/10
摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.
摘要翻译：提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及使用它。提供某些中间体的结晶形式。

13. 发明授权

US07205324B2 Inhibitors of IMPDH enzyme 有权
标题翻译： IMPDH酶抑制剂
公开(公告)号：US07205324B2
公开(公告)日：2007-04-17
申请号：US10465427
申请日：2003-06-19
申请人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
发明人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
IPC分类号： A61K31/421 , A61K31/422 , C07D263/32 , C07D413/12
CPC分类号： C07D413/12 , C07D263/32 , C07D307/20 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.
摘要翻译：本发明公开了IMPDH（肌苷-5'-单磷酸脱氢酶）的新型抑制剂的鉴定。本文公开的化合物和药物组合物可用于治疗或预防IMPDH相关疾病，例如移植排斥反应和自身免疫性疾病。

14. 发明授权

US06777426B2 Imidazole and imidazoline derivatives and uses thereof 失效
标题翻译：咪唑和咪唑啉衍生物及其用途
公开(公告)号：US06777426B2
公开(公告)日：2004-08-17
申请号：US09933106
申请日：2001-08-20
申请人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
发明人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
IPC分类号： C07D23324
CPC分类号： C07D401/06 , C07D233/50 , C07D401/12 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及新的咪唑和咪唑啉衍生物，其是用于克隆的人α2肾上腺素能受体的选择性激动剂。本发明还涉及这些化合物用于治疗其中α2受体调节可能有用的任何疾病的用途。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

15. 发明授权

US06624184B1 Amide and diamide inhibitors of IMPDH enzyme for use in treating IMPDH-associated disorders 有权
标题翻译：用于治疗IMPDH相关疾病的IMPDH酶的酰胺和二酰胺抑制剂
公开(公告)号：US06624184B1
公开(公告)日：2003-09-23
申请号：US09427953
申请日：1999-10-27
申请人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
发明人： Henry H. Gu , T. G. Murali Dhar , Edwin J. Iwanowicz
IPC分类号： A61K31421
CPC分类号： C07D413/12 , C07D263/32 , C07D307/20 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention discloses the identification of the inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.
摘要翻译：本发明公开了IMPDH抑制剂（肌苷-5'-单磷酸脱氢酶）的鉴定。本文公开的化合物和药物组合物可用于治疗或预防IMPDH相关疾病，例如移植排斥反应和自身免疫性疾病。

16. 发明授权

US06268369B1 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines 失效
标题翻译： 5-（杂环烷基）-6-芳基 - 二氢嘧啶
公开(公告)号：US06268369B1
公开(公告)日：2001-07-31
申请号：US08836628
申请日：1997-05-16
申请人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski , Bharat Lagu , Shou Wu Miao
发明人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski , Bharat Lagu , Shou Wu Miao
IPC分类号： C07D4004
CPC分类号： C07D239/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D491/04
摘要： This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及下式的二氢嘧啶化合物：它们是人α1C受体的选择性拮抗剂。本发明还涉及这些化合物用于降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ence，心律失常以及用于治疗任何α1C受体拮抗作用的疾病有用本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

17. 发明授权

US06248747B1 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines 失效
标题翻译： 5-（杂环烷基）-6-芳基 - 二氢嘧啶
公开(公告)号：US06248747B1
公开(公告)日：2001-06-19
申请号：US09291553
申请日：1999-04-14
申请人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski
发明人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski
IPC分类号： A61K31505
CPC分类号： C07D239/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D491/04
摘要： This invention is directed to the use of dihydropyrimidine compounds, which are selective antagonists for cloned human &agr;1C receptors, for the treatment of benign prostatic hyperplasia and other diseases where antagonism of the human &agr;1C receptor is useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-identified compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为克隆的人α1C受体的选择性拮抗剂的二氢嘧啶化合物用于治疗良性前列腺增生症和其它人α1C受体拮抗作用的其它疾病的用途。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

18. 发明授权

US6046331A Imidazolones and their use in treating benign prostatic hyperplasia and other disorders 失效
标题翻译：咪唑啉酮及其在治疗良性前列腺增生等疾病中的应用
公开(公告)号：US6046331A
公开(公告)日：2000-04-04
申请号：US213078
申请日：1998-12-17
申请人： Wai C. Wong , T. G. Murali Dhar , Charles Gluchowski
发明人： Wai C. Wong , T. G. Murali Dhar , Charles Gluchowski
IPC分类号： C07D233/90 , A61K9/06 , A61K9/08 , A61K9/20 , A61K31/4178 , A61K31/438 , A61K31/454 , A61K31/4545 , A61K31/58 , A61K45/00 , A61P3/06 , A61P9/06 , A61P15/00 , A61P15/10 , A61P25/02 , A61P25/06 , A61P27/02 , A61P43/00 , C07D233/70 , C07D401/06 , C07D401/14 , C07D405/14 , C07D491/10 , C07D495/10 , C07D403/00 , A61K31/44 , A61K31/495 , C07D411/00
CPC分类号： C07D401/06 , C07D233/70 , C07D401/14 , C07D405/14 , C07D491/10
摘要： This invention is directed to imidazolones which are selective antagonists for human .alpha..sub.1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the .alpha..sub.1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为人α1a受体的选择性拮抗剂的咪唑啉酮。本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常，交感神经介导的疼痛，偏头痛以及用于治疗任何疾病的用途其中α1a受体的拮抗作用可能是有用的。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

19. 发明授权

US5866579A Imidazole and imidazoline derivatives and uses thereof 失效
标题翻译：咪唑和咪唑啉衍生物及其用途
公开(公告)号：US5866579A
公开(公告)日：1999-02-02
申请号：US834658
申请日：1997-04-11
申请人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
发明人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
IPC分类号： A61K31/415 , A61K31/47 , A61K31/505 , A61P9/12 , C07D233/48 , C07D233/50 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04
CPC分类号： C07D401/06 , C07D233/50 , C07D401/12 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及新颖的咪唑和咪唑啉衍生物，它们是用于克隆的人α2肾上腺素能受体的选择性激动剂。本发明还涉及这些化合物用于治疗其中α2受体调节可能有用的任何疾病的用途。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

20. 发明授权

US08877749B2 Spirocyclic compounds as modulators of chemokine receptor activity 有权
标题翻译：螺环化合物作为趋化因子受体活性的调节剂
公开(公告)号：US08877749B2
公开(公告)日：2014-11-04
申请号：US13500323
申请日：2010-10-06
申请人： T. G. Murali Dhar , John V. Duncia , Daniel S. Gardner , Weiwei Guo , John Hynes
发明人： T. G. Murali Dhar , John V. Duncia , Daniel S. Gardner , Weiwei Guo , John Hynes
IPC分类号： A61K31/535 , C07D413/12 , C07D471/04 , C07D405/12 , A61K31/4427 , C07D401/12
CPC分类号： C07D471/10 , A61K31/4427 , C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的趋化因子受体活性的调节剂或其立体异构体或其药学上可接受的盐。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和移植排斥反应的自身免疫病态的方法。

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