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1. 发明授权

US07915420B2 Aryl piperidine amides 有权
标题翻译：芳基哌啶酰胺
公开(公告)号：US07915420B2
公开(公告)日：2011-03-29
申请号：US11780133
申请日：2007-07-19
申请人： Charles Q. Huang , Timothy W. Lovenberg , Alejandro Santillán, Jr. , Liu Y. Tang , Ronald L. Wolin
发明人： Charles Q. Huang , Timothy W. Lovenberg , Alejandro Santillán, Jr. , Liu Y. Tang , Ronald L. Wolin
IPC分类号： A61K31/4535 , C07D211/04 , C07D409/02
CPC分类号： C07D295/192 , C07C237/30 , C07D211/46 , C07D333/20 , C07D333/38
摘要： The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.
摘要翻译：本发明提供了用于调节，治疗或预防：抗焦虑障碍的新型GlyT2抑制化合物; 需要治疗受损哺乳动物神经组织的病症; 适用于通过施用神经营养因子治疗的病症; 神经障碍或肥胖; 肥胖相关疾病。

2. 发明授权

US07071200B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 有权
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：US07071200B2
公开(公告)日：2006-07-04
申请号：US10885511
申请日：2004-07-06
申请人： Yun-Fei Zhu , Collin Regan , Jaimie K. Rueter , Zhiqiang Guo , Yongsheng Chen , Charles Q. Huang
发明人： Yun-Fei Zhu , Collin Regan , Jaimie K. Rueter , Zhiqiang Guo , Yongsheng Chen , Charles Q. Huang
IPC分类号： C07D239/54 , A61K31/513
CPC分类号： C07D239/54 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有以下结构：其中R 1a，R 1b，R 2a，R 2b， R 3，R 4，R 5，R 6，R 7和R 7， X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

3. 发明授权

US07056927B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 有权
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：US07056927B2
公开(公告)日：2006-06-06
申请号：US10885491
申请日：2004-07-06
申请人： Zhiqiang Guo , Yongsheng Chen , Dongpei Wu , Chen Chen , Warren Wade , Wesley J. Dwight , Charles Q. Huang , Fabio C. Tucci
发明人： Zhiqiang Guo , Yongsheng Chen , Dongpei Wu , Chen Chen , Warren Wade , Wesley J. Dwight , Charles Q. Huang , Fabio C. Tucci
IPC分类号： C07D239/54 , A61K31/513
CPC分类号： C07D239/54 , C07D239/52 , C07D403/12 , C07D405/04
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有以下结构：其中R 1a，R 1b，R 1c，R 2a， R 2b，R 3，R 4，R 5，R 6和R 6，和 X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

4. 发明授权

US06514982B1 CRF receptor antagonists and methods relating thereto 有权
公开(公告)号：US06514982B1
公开(公告)日：2003-02-04
申请号：US09439840
申请日：1999-11-12
申请人： Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
发明人： Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
IPC分类号： C07D48704
CPC分类号： C07D471/16 , C07D487/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same

5. 发明授权

US6133276A Compounds and methods for increasing endogenous levels of corticotropin-releasing factor 失效
标题翻译：增加促肾上腺皮质激素释放因子内源性水平的化合物和方法
公开(公告)号：US6133276A
公开(公告)日：2000-10-17
申请号：US222374
申请日：1998-12-29
申请人： Jeffrey P. Whitten , James R. McCarthy , Zhengyu Liu , Charles Q. Huang , Philip E. Erickson , Dominic P. Behan
发明人： Jeffrey P. Whitten , James R. McCarthy , Zhengyu Liu , Charles Q. Huang , Philip E. Erickson , Dominic P. Behan
IPC分类号： A61K31/00 , A61K31/35 , A61K31/352 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/505 , A61K31/513 , A61P5/00 , A61P43/00 , C07D239/62 , C07D239/66 , C07D311/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/08 , C07D487/04 , A61K31/515
CPC分类号： C07D409/14 , C07D239/62 , C07D239/66 , C07D311/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/08 , C07D487/04
摘要： Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain are disclosed. Such ligand inhibitors cause release of CRF from the CRF/CRF-bind protein complex. Administration of the ligand inhibitors provide improvement in learning and memory, result in decreased food intake and/or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease.
摘要翻译：公开了用于增加脑中游离促皮质激素释放因子（CRF）水平的配体抑制剂。这种配体抑制剂引起CRF / CRF结合蛋白复合物的CRF释放。配体抑制剂的施用提供了学习和记忆的改善，导致食物摄取减少和/或提供与脑中低水平CRF相关疾病，特别是阿尔茨海默氏病的治疗。

6. 发明授权

US08504620B2 Dynamic subject information generation in message services of distributed object systems 失效
公开(公告)号：US08504620B2
公开(公告)日：2013-08-06
申请号：US11652075
申请日：2007-01-11
申请人： Yueh-Shian Chi , Parris C M Hawkins , Charles Q. Huang
发明人： Yueh-Shian Chi , Parris C M Hawkins , Charles Q. Huang
IPC分类号： G06F15/16 , G06F19/00 , H01L21/00
CPC分类号： H04L67/42 , G05B2219/33149 , H04L67/02 , H04L67/10
摘要： A system, method and medium of sending messages in a distributed data processing network is described, and contemplates receiving a message that includes subject information that is generated based on one or more pre-selected portions as the message is generated. A message delivery system in a client-server environment is also described. The message delivery system includes a server configured to receive a message that includes subject information that is generated based on one or more pre-selected portions as the message is created and configured to forward the message based on the subject information.

7. 发明授权

US07229995B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 有权
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：US07229995B2
公开(公告)日：2007-06-12
申请号：US11264702
申请日：2005-11-01
申请人： Charles Q. Huang , Chen Chen , Yongsheng Chen , Zhiqiang Guo , Warren Wade , Martin Rowbottom , Jaimie K. Rueter
发明人： Charles Q. Huang , Chen Chen , Yongsheng Chen , Zhiqiang Guo , Warren Wade , Martin Rowbottom , Jaimie K. Rueter
IPC分类号： C07D239/54 , A61K31/513
CPC分类号： C07D239/54 , C07D403/12
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有如下结构：其中n，R 1a，R 1b，R 1c，R 2a， R 2，R 3，R 3，R 4，R 5，R 6， >和X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

8. 发明授权

US06613777B1 CRF antagonistic pyrazolo[4,3-b]pyridines 有权
标题翻译： CRF拮抗性吡唑并[4,3-b]吡啶
公开(公告)号：US06613777B1
公开(公告)日：2003-09-02
申请号：US09623634
申请日：2001-02-20
申请人： Chen Chen , Keith M. Wilcoxen , Charles Q. Huang , Mustapha Hadduch , James R. McCarthy
发明人： Chen Chen , Keith M. Wilcoxen , Charles Q. Huang , Mustapha Hadduch , James R. McCarthy
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR5R6, OR6 or SR6; R2 is C1-6alkyl, C1-6alkyloxy, or C1-6alkylthio; R3 is Ar1 or Het1; R4 is hydrogen or C1-6alkyl; R5 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, mono- or di(C1-6alkyl)amino-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar2C1-6alkyl, Ar2oxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, tetrahydrofuranylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, or C1-6alkylcarbonylC1-6alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl, morpholinyl, or thiomorpholinyl group, optionally substituted with 1 or 2 substituents each independently selected from C1-6alkyl or C1-6alkyloxyC1-6alkyl; and and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括其立体异构体及其药学上可接受的酸加成盐形式的化合物，其中R 1是C 1-6烷基，NR 5 R 6，OR 6或SR 6; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R4是氢或C1-6烷基; R5是氢，C1-8烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基，单或二（C1-6烷基）氨基C1- C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基，单或二（C 3-6环烷基）甲基，Ar 2 C 1-6烷基，Ar 2氧基C 1-6烷基，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，四氢呋喃基甲基，C 1-6烷硫基C 1-6烷基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基或C 1-6烷基羰基C 1-6烷基; 或者R 5和R 6与它们所连接的氮原子一起形成吡咯烷基，哌啶基，高哌啶基，吗啉基或硫代吗啉基，任选地被1或2个独立地选自C 1-6烷基或C 1-6烷氧基C 1-6烷基的取代基取代 ; 并且Ar 1和Ar 2各自为任选取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

9. 发明授权

US07276610B2 Aryl piperidine amides 有权
标题翻译：芳基哌啶酰胺
公开(公告)号：US07276610B2
公开(公告)日：2007-10-02
申请号：US10919734
申请日：2004-08-17
申请人： Charles Q. Huang , Timothy W. Lovenberg , Alejandro Santillán, Jr. , Liu Y. Tang , Ronald L. Wolin
发明人： Charles Q. Huang , Timothy W. Lovenberg , Alejandro Santillán, Jr. , Liu Y. Tang , Ronald L. Wolin
IPC分类号： C07D211/60 , C07D207/04 , C07D223/02 , C07D265/30 , C07D295/02 , A61K31/445
CPC分类号： C07D295/192 , C07C237/30 , C07D211/46 , C07D333/20 , C07D333/38
摘要： The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.
摘要翻译：本发明提供了用于调节，治疗或预防：抗焦虑障碍的新型GlyT2抑制化合物; 需要治疗受损哺乳动物神经组织的病症; 适用于通过施用神经营养因子治疗的病症; 神经障碍或肥胖; 肥胖相关疾病。

10. 发明授权

US07329669B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 有权
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：US07329669B2
公开(公告)日：2008-02-12
申请号：US11446583
申请日：2006-06-02
申请人： Yun-Fei Zhu , Collin Regan , Jaimie K Rueter , Zhiqiang Guo , Yongsheng Chen , Charles Q Huang
发明人： Yun-Fei Zhu , Collin Regan , Jaimie K Rueter , Zhiqiang Guo , Yongsheng Chen , Charles Q Huang
IPC分类号： A61K31/513 , C07D239/54
CPC分类号： C07D239/54 , C07D401/06
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有以下结构：其中R 1a，R 1b，R 2a，R 2b， R 3，R 4，R 5，R 6，R 7和R 7， X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

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