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71. 发明授权

US5783582A Piperidines and hexahydro-1H-azepines spiro substituted at the 4-position promote release of growth hormone 失效
标题翻译：在4-位上被螺环取代的哌啶和六氢-1H-吖庚因促进生长激素的释放
公开(公告)号：US5783582A
公开(公告)日：1998-07-21
申请号：US776041
申请日：1997-01-16
申请人： Liangquin Guo , Arthur Patchett , Lihu Yang
发明人： Liangquin Guo , Arthur Patchett , Lihu Yang
IPC分类号： C07D471/10 , A01N43/42 , A61K31/44 , C07D211/00
CPC分类号： C07D471/10
摘要： Di and trisubstituted Piperidines, pyrrolidines and hexahydro-1H-azepines which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible mea products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di- and trisubstituted piperidines and pyrrolidines as the active ingredient thereof are also disclosed.
摘要翻译： PCT No.PCT / US95 / 08854 Sec。 371日期1997年1月16日 102（e）日期1997年1月16日PCT提交1995年7月17日PCT公布。公开号WO96 / 02530 日期1996年2月1日Di和促进人和动物中生长激素释放的三取代哌啶，吡咯烷和六氢-1H-吖庚因。这种性质可以用于促进食用动物的生长，使食用食品的生产更有效，并且在人类中，以治疗生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童和治疗由生长激素的合成代谢作用改善的医疗状况。还公开了含有这种二取代和三取代的哌啶和吡咯烷作为其活性成分的生长激素释放组合物。

72. 发明授权

US5767118A 4-Heterocyclic peperidines promote release of growth hormone 失效
标题翻译： 4-杂环peperidines促进生长激素的释放
公开(公告)号：US5767118A
公开(公告)日：1998-06-16
申请号：US329357
申请日：1994-10-26
申请人： Ravi Nargund , Arthur A. Patchett , Lihu Yang
发明人： Ravi Nargund , Arthur A. Patchett , Lihu Yang
IPC分类号： A23K1/16 , A61K31/66 , A61K38/00 , A61K38/04 , A61K38/27 , A61P3/04 , A61P5/00 , A61P17/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D413/14 , C07K5/06 , A61K31/535 , A01N43/40 , A01N43/54 , A61K31/54 , C07D211/36 , C07D211/68 , C07D401/00 , C07D409/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14
摘要： The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, A, R.sup.3 and the dashed line are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及鉴定为以下结构式的4-杂环取代的哌啶的某些新化合物：其中R1，R4，R5，A，R3和虚线如本文所定义。这些化合物促进人和动物中生长激素的释放。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有这些化合物作为其活性成分的生长激素释放组合物。

73. 发明授权

US5663171A Acyclic compounds promote release of growth hormone 失效
标题翻译：无环化合物促进生长激素的释放
公开(公告)号：US5663171A
公开(公告)日：1997-09-02
申请号：US398247
申请日：1995-03-03
申请人： Meng Hsin Chen , Gregori J. Morriello , Ravi Nargund , Arthur A. Patchett , Lihu Yang
发明人： Meng Hsin Chen , Gregori J. Morriello , Ravi Nargund , Arthur A. Patchett , Lihu Yang
IPC分类号： C07D403/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/435 , A61K38/00 , A61P3/00 , A61P37/00 , A61P43/00 , C07D209/20 , C07D401/12 , C07D471/04 , C07K5/02 , C07K5/06 , C07K5/083 , C07D413/14 , A61K31/405 , A61K31/535 , C07D413/12 , A61K21/455
CPC分类号： C07D401/12 , C07D209/20 , C07D471/04 , C07K5/0202 , C07K5/06026 , C07K5/0806 , A61K38/00
摘要： The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及以下通式结构式的某些化合物：其中R1，R1a，R2a，R3，R3a，R4，R5，R6，A，W和n如本文所定义。这些化合物促进人和动物中生长激素的释放。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有这些化合物作为其活性成分的生长激素释放组合物。

74. 发明授权

US5622973A Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates 失效
标题翻译：用取代的哌啶，吡咯烷和六氢-1H-吖庚因与双膦酸盐组合治疗骨质疏松症
公开(公告)号：US5622973A
公开(公告)日：1997-04-22
申请号：US464982
申请日：1995-06-05
申请人： Gregori J. Morriello , Arthur A. Patchett , Lihu Yang
发明人： Gregori J. Morriello , Arthur A. Patchett , Lihu Yang
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/083 , A61K31/445 , A61K31/41 , A61K31/425 , A61K31/505
CPC分类号： C07K5/06139 , C07K5/0202 , C07K5/06034 , C07K5/0808 , A61K38/00
摘要： The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A, X, Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及鉴定为二 - 和三 - 取代的哌啶，吡咯烷和六氢-1H-吖庚因的一些新化合物，其通式为：其中R1，R4，R5，A，X，Y和 n如本文所定义。这些化合物促进人和动物中生长激素的释放。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有这种二取代和三取代的哌啶，吡咯烷酮和六氢-1H-吖庚因作为其活性成分的生长激素释放组合物。

75. 发明授权

US5492916A Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
标题翻译：二取代和三取代的哌啶，吡咯烷和六氢-1H-吖庚因促进生长激素的释放
公开(公告)号：US5492916A
公开(公告)日：1996-02-20
申请号：US323988
申请日：1994-10-17
申请人： Gregori J. Morriello , Arthur A. Patchett , Lihu Yang
发明人： Gregori J. Morriello , Arthur A. Patchett , Lihu Yang
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/083 , A61K31/445 , C07D209/04 , C07D401/06
CPC分类号： C07K5/06139 , C07K5/0202 , C07K5/06034 , C07K5/0808 , A61K38/00
摘要： The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及鉴定为二 - 和三 - 取代的哌啶，吡咯烷和六氢-1H-吖庚因的一些新化合物，其通式为：其中R1，R4，R5，A，X，Y和 n如本文所定义。这些化合物促进人和动物中生长激素的释放。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。还公开了含有这种二取代和三取代的哌啶，吡咯烷酮和六氢-1H-吖庚因作为其活性成分的生长激素释放组合物。

76. 发明申请

US20130316398A1 EFFICIENT PRODUCTION OF HETEROLOGOUS PROTEINS USING MANNOSYL TRANSFERASE INHIBITORS 有权
标题翻译：使用芒硝转移酶抑制剂有效生产异位蛋白
公开(公告)号：US20130316398A1
公开(公告)日：2013-11-28
申请号：US13588022
申请日：2012-08-17
申请人： RANJIT DESAI , Lihu Yang
发明人： RANJIT DESAI , Lihu Yang
IPC分类号： C12P21/00 , C07D277/36
CPC分类号： C12P21/005 , C07D277/36 , C12P21/02
摘要： Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
摘要翻译：描述了用于生产具有降低量的O-连接糖基化的蛋白质组合物的化合物和方法。该方法包括在某些亚苄基噻唑烷二酮类Pmt介导的O-连接糖基化抑制剂存在下培养的细胞中产生蛋白质。

77. 发明授权

US08309325B2 Efficient production of heterologous proteins using mannosyl transferase inhibitors 有权
标题翻译：使用甘露糖基转移酶抑制剂有效生产异源蛋白
公开(公告)号：US08309325B2
公开(公告)日：2012-11-13
申请号：US12993716
申请日：2009-05-18
申请人： Ranjit Desai , Lihu Yang
发明人： Ranjit Desai , Lihu Yang
IPC分类号： C12P21/02 , C07D277/36
CPC分类号： C12P21/005 , C07D277/36 , C12P21/02
摘要： Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
摘要翻译：描述了用于生产具有降低量的O-连接糖基化的蛋白质组合物的化合物和方法。该方法包括在某些亚苄基噻唑烷二酮类Pmt介导的O-连接糖基化抑制剂存在下培养的细胞中产生蛋白质。

78. 发明授权

US08138197B2 Spirochromanon derivatives 有权
标题翻译：螺二色素衍生物
公开(公告)号：US08138197B2
公开(公告)日：2012-03-20
申请号：US12518466
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
IPC分类号： A61K31/438 , C07D221/20
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[ 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-a]吡啶，其具有Ar 2，并且任选具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a）-Q 2 -R b的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或次甲基; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

79. 发明申请

US20110201615A1 TRIAZOLE BETA CARBOLINE DERIVATIVES AS ANTI-DIABETIC AGENTS 审中-公开
标题翻译：三唑衍生物作为抗糖尿病药物
公开(公告)号：US20110201615A1
公开(公告)日：2011-08-18
申请号：US13125319
申请日：2009-10-19
申请人： Liangqin Guo , Jian Liu , Ravi P. Nargund , Alexander Pasternak , Lihu Yang , Zhixiong Ye
发明人： Liangqin Guo , Jian Liu , Ravi P. Nargund , Alexander Pasternak , Lihu Yang , Zhixiong Ye
IPC分类号： A61K31/501 , C07D471/04 , A61K31/437 , C07D401/14 , A61K31/506 , A61P3/00 , A61P9/12
CPC分类号： C07D471/04
摘要： Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
摘要翻译：结构式（I）的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖，脂质障碍和高血压。这些化合物也可用于治疗抑郁症和焦虑症。

80. 发明授权

US07700772B2 Amino heterocyclic modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的氨基杂环调节剂
公开(公告)号：US07700772B2
公开(公告)日：2010-04-20
申请号：US10589406
申请日：2005-02-08
申请人： Lihu Yang , Alexander Pasternak , Sander G. Mills
发明人： Lihu Yang , Alexander Pasternak , Sander G. Mills
IPC分类号： C07D401/04 , C07D407/04 , A61K31/445 , A61K31/438
CPC分类号： C07D307/24 , C07D207/16 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要： Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：式I和式II化合物（其中n，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R15，R16，R17，R18，R19，R24，R25，R26， R28，R29，R30，R33，R34，R35，R36，R37，R38，A，j，k，m，n，X，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫性病态如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

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