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91. 发明授权

US07897785B2 1,3-Diiodohydantoin compound and production method thereof 有权
标题翻译： 1,3-二碘乙内酰脲化合物及其制备方法
公开(公告)号：US07897785B2
公开(公告)日：2011-03-01
申请号：US11991285
申请日：2006-08-30
申请人： Kazuhisa Inoue , Yukihiko Hanamura , Takaaki Miyazawa
发明人： Kazuhisa Inoue , Yukihiko Hanamura , Takaaki Miyazawa
IPC分类号： C07D233/00
CPC分类号： C07D233/82
摘要： The present invention provides a means which can inhibit release of I2 in production or storage of 1,3-diiodohydantoin compound, and thereby solve decrease in purity of the compound and various problems caused by I2.The present invention provides a production method for 1,3-diiodohydantoin compound comprising a step to prepare a wet body containing a 1,3-diiodohydantoin compound, and (1) a step to dry the wet body by contacting the wet body with heated gas or (2) a step to lyophilize the wet body, a storage method for 1,3-diiodohydantoin compound comprising a step to store a 1,3-diiodohydantoin compound under a temperature condition of 15° C. or lower, and a 1,3-diiodohydantoin compound wherein content of released I2 is 1% by mass or less.
摘要翻译：本发明提供了可以抑制1,3-二碘乙内酰脲化合物的生产或储存中I2的释放，从而解决化合物的纯度下降和I2引起的各种问题的方法。本发明提供一种1,3-二碘海因组合物的制造方法，其包括制备含有1,3-二碘乙内酰脲化合物的湿体的工序，（1）通过使湿体与加热气体接触来干燥湿体的工序或（2）冻干湿体的步骤，一种1,3-二碘海内因组合物的储存方法，包括在15℃或更低的温度条件下存放1,3-二碘乙内酰脲化合物的步骤，其中释放的I2的含量为1质量％以下的3-二碘乙内酰脲化合物。

92. 发明授权

US07858653B2 2-imidazoles 失效
标题翻译： 2-咪唑
公开(公告)号：US07858653B2
公开(公告)日：2010-12-28
申请号：US11950446
申请日：2007-12-05
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A01N43/50 , C07D233/00
CPC分类号： C07D233/88 , C07D233/64
摘要： The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine. The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, processes for making the compound, and a composition comprising such a compound.
摘要翻译：本发明涉及式I化合物，其中X是-CH 2 - 或-NH-; Y是-CH（低级烷氧基） - ， - CH（低级烷基） - ， - O - ， - S - ， - S（O） - ， - S（O）并且Ar是苯基或萘基，该环任选地被一个或两个选自卤素，低级烷氧基，低级烷基和被卤素取代的低级烷基的取代基取代; 或其药学上可接受的酸加成盐; 条件是当X是-NH-时，Y是-CH（低级烷基） - 或-CH 2 - ; 另外的条件是该化合物不是2-苯乙基-1H-咪唑盐酸盐，2-（3,4-二氯 - 苯氧基甲基）-1H-咪唑盐酸盐，2-（2-氯 - 苯氧基甲基）-1H-咪唑盐酸盐， 2-（2,3-二氯 - 苯氧基甲基）-1H-咪唑，苄基 - （1H-咪唑-2-基） - 胺，（4-氯 - 苄基） - （1H-咪唑-2-基） - 胺，或（2-氯 - 苄基） - （1H-咪唑-2-基） - 胺。本发明还涉及这种化合物的药学上可接受的酸加成盐，制备该化合物的方法和包含这种化合物的组合物。

93. 发明授权

US07820673B2 Urea derivative, process for producing the same, and use 失效
标题翻译：尿素衍生物，其制造方法及用途
公开(公告)号：US07820673B2
公开(公告)日：2010-10-26
申请号：US10583046
申请日：2004-12-15
申请人： Keiji Kubo , Yasuhiro Imaeda
发明人： Keiji Kubo , Yasuhiro Imaeda
IPC分类号： A61K31/4188 , A61K31/496 , C07D233/00 , C07D403/14
CPC分类号： A61K31/454 , A61K31/427 , A61K31/4545 , A61K31/496 , A61K31/5377 , C07D417/06
摘要： The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis. The derivative is represented by Formula (I): wherein Cy is an aromatic hydrocarbon group which may be substituted or an aromatic heterocyclic group which may be substituted; R1 is a hydrogen atom or a hydrocarbon group which may be substituted; V is —C(O)—, —S(O)—, or —S(O)2—; W is —N(R2)—, —O—, or a bond (wherein R2 is a hydrogen atom or a hydrocarbon group which may be substituted); X is alkylene which may be substituted; Y is —C(O)—, —S(O)—, or —S(O)2—; Z is a bond, a chain hydrocarbon group which may be substituted, or —N═; ring A is a non-aromatic nitrogen-containing heterocyclic ring which may be substituted; ring B is a nitrogen-containing heterocyclic ring which may be substituted; and [Chemical formula 2] , are each independently a single bond or a double bond; provided that R1 may be bonded to R2 to form a non-aromatic nitrogen-containing heterocyclic ring and that R2 may be bonded to a substituent of X to form a non-aromatic nitrogen-containing heterocyclic ring which may be substituted.
摘要翻译：本发明提供可用作血栓形成治疗剂的尿素衍生物或其盐。该衍生物由式（I）表示：其中Cy是可被取代的芳族烃基或可被取代的芳族杂环基; R1是氢原子或可被取代的烃基; V是-C（O） - ， - S（O） - 或-S（O）2 - ; W是-N（R 2） - ，-O-或键（其中R 2是氢原子或可被取代的烃基）; X是可被取代的亚烷基; Y是-C（O） - ， - S（O） - 或-S（O）2 - ; Z是一个键，可以被取代的链烃基，或-N =; 环A是可以被取代的非芳香族含氮杂环; 环B是可以被取代的含氮杂环; 和[化学式2]各自独立地为单键或双键; 条件是R 1可以与R 2结合以形成非芳族含氮杂环，并且R 2可以与X的取代基键合，以形成可被取代的非芳香族含氮杂环。

94. 发明申请

US20100222358A1 OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES 有权
标题翻译： OCTAHYDRO-PYRROLO [3,4-B]吡咯烷酮衍生物
公开(公告)号：US20100222358A1
公开(公告)日：2010-09-02
申请号：US12715660
申请日：2010-03-02
申请人： Marlon D. Cowart , Chen Zhao , Minghua Sun , Lawrence A. Black , Guo Zhu Zheng , Robert J. Gregg , Geoff G.Z. Zhang , Ahmad Y. Sheikh , Xiaochun Lou , Rodger F. Henry , David M. Barnes , Lawrence Kolaczkowski , Anthony R. Haight , Sou-Jen Chang , Steven J. Wittenberger , Michael G. Fickes
发明人： Marlon D. Cowart , Chen Zhao , Minghua Sun , Lawrence A. Black , Guo Zhu Zheng , Robert J. Gregg , Geoff G.Z. Zhang , Ahmad Y. Sheikh , Xiaochun Lou , Rodger F. Henry , David M. Barnes , Lawrence Kolaczkowski , Anthony R. Haight , Sou-Jen Chang , Steven J. Wittenberger , Michael G. Fickes
IPC分类号： A61K31/501 , A61K31/407 , C07D487/04 , A61K31/47 , C07D215/00 , A61K31/4439 , C07D401/14 , A61K31/428 , C07D417/14 , A61K31/4164 , C07D233/00 , C07D403/14 , A61K31/506 , A61K31/497 , A61P3/04 , A61P5/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/08 , A61P1/02
CPC分类号： C07D487/04
摘要： Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
摘要翻译：八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。

95. 发明授权

US07713975B1 3,6-substituted imidazol[1,2-b]pyridazine analogs for treating allergic and inflammatory diseases 有权
标题翻译： 3,6-取代咪唑并[1,2-b]哒嗪类似物用于治疗过敏性和炎性疾病
公开(公告)号：US07713975B1
公开(公告)日：2010-05-11
申请号：US11330590
申请日：2006-01-12
申请人： Mark R. Hellberg , Steven T. Miller , Andrew Rusinko
发明人： Mark R. Hellberg , Steven T. Miller , Andrew Rusinko
IPC分类号： A61K31/50 , A61K31/501 , C07D237/26 , C07D487/00 , C07D235/00 , C07D233/00
CPC分类号： A61K31/5025 , C07D473/04 , C07D487/04 , Y02A50/411
摘要： Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.
摘要翻译：用于治疗过敏性或炎性疾病或其它Syk介导的疾病或Syk介导的病症的方法，其特征在于施用含有治疗有效量的3,6-取代的咪唑并[1,2-b]哒嗪化合物的组合物。

96. 发明授权

US07674899B2 Dimeric azacyclic compounds and their use 失效
标题翻译：二甲基氮杂化合物及其用途
公开(公告)号：US07674899B2
公开(公告)日：2010-03-09
申请号：US10586838
申请日：2005-02-01
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B Timmermann
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B Timmermann
IPC分类号： C07D487/00 , C07D243/00 , C07D241/04 , C07D295/00 , C07D233/00 , C07D233/02
摘要： This invention relates to novel azacyclic derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新型的氮杂环十二烷衍生物及其作为药物的用途。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

97. 发明授权

US07662844B2 Naphthylene derivatives as cytochrome P450 inhibitors 失效
标题翻译：萘衍生物作为细胞色素P450抑制剂
公开(公告)号：US07662844B2
公开(公告)日：2010-02-16
申请号：US10889520
申请日：2004-07-12
申请人： Vanessa Smith , Anthony Nigro , Mark Mulvihill , Cara Cesario , Patricia Anne Beck , Arlindo L. Castelhano
发明人： Vanessa Smith , Anthony Nigro , Mark Mulvihill , Cara Cesario , Patricia Anne Beck , Arlindo L. Castelhano
IPC分类号： A61K31/50 , A61K31/415 , C07D231/00 , C07D233/00
CPC分类号： C07D233/64
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
摘要翻译：其中n1，n2，n3，n4，G1，Q1，Z3，R1，R2，R3，R4a，R4b，R5a和R5b在本文中定义的式和其药学上可接受的盐的化合物抑制细胞色素P450RAI酶，可用于治疗和/或预防响应于类视黄醇和天然存在的视黄酸的治疗的各种疾病和病症。

98. 发明授权

US07642279B2 Atipamezole hydrochloride crystallization method 有权
标题翻译：盐酸阿替美唑结晶法
公开(公告)号：US07642279B2
公开(公告)日：2010-01-05
申请号：US11913776
申请日：2006-06-16
申请人： Seppo Parhi , Arto Karjalainen
发明人： Seppo Parhi , Arto Karjalainen
IPC分类号： A01N43/50 , C07D233/00
CPC分类号： C07D233/64
摘要： A method of isolating atipamezole hydrocloride as a crystalline salt is provided.
摘要翻译：提供了一种分离作为结晶盐的阿替美唑氢氯化物的方法。

99. 发明授权

US07622491B2 Modulators of PPAR and methods of their preparation 失效
标题翻译： PPAR的调节剂及其制备方法
公开(公告)号：US07622491B2
公开(公告)日：2009-11-24
申请号：US11202963
申请日：2005-08-11
申请人： Yan Zhu , Jingyuan Ma , Peng Cheng , Zuchun Zhao , Francine M. Gregoire , Vera A. Rakhmanova
发明人： Yan Zhu , Jingyuan Ma , Peng Cheng , Zuchun Zhao , Francine M. Gregoire , Vera A. Rakhmanova
IPC分类号： A61K31/40 , A61K31/415 , C07D207/00 , C07D231/00 , C07D233/00
CPC分类号： C07D263/57 , C07D249/06 , C07D249/20 , C07D403/12 , C07D409/10
摘要： The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.
摘要翻译：本发明涉及由式（I）表示的某些新型化合物及其药学上可接受的盐，溶剂合物，水合物和前药。本发明还涉及制备和使用这些化合物和含有这些化合物的药物组合物的方法，以治疗或控制由PPAR介导的许多疾病，例如葡萄糖代谢，脂质代谢和胰岛素分泌，特别是2型糖尿病，高胰岛素血症，高脂血症高尿酸血症，高胆固醇血症，动脉粥样硬化，心血管疾病的一个或多个危险因素，X综合征，高甘油三酯血症，高血糖症，肥胖症和进食障碍。

100. 发明授权

US07598389B2 Silylated carboxamides 有权
标题翻译：甲硅烷基化甲酰胺
公开(公告)号：US07598389B2
公开(公告)日：2009-10-06
申请号：US10579033
申请日：2004-11-06
申请人： Ralf Dunkel , Hans-Ludwig Elbe , Benoit Hartmann , Alexander Klausener , Jörg Nico Greul , Ulrike Wachendorff-Neumann , Peter Dahmen , Karl-Heinz Kuck
发明人： Ralf Dunkel , Hans-Ludwig Elbe , Benoit Hartmann , Alexander Klausener , Jörg Nico Greul , Ulrike Wachendorff-Neumann , Peter Dahmen , Karl-Heinz Kuck
IPC分类号： C07D231/00 , C07D233/00 , C07D235/00 , C07D249/00 , C07D261/00 , C07D263/00 , C07D271/00 , C07D273/00 , C07D275/00 , C07D277/00 , C07D283/00 , C07D291/00 , C07D293/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D498/00 , C07D513/00 , C07D515/00 , C07D517/00 , C07F5/02 , C07F7/02
CPC分类号： C07F7/081
摘要： Novel silylated carboxamides of the formula (I) in which R, L, R1, R3, R3, R4 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms.
摘要翻译：式（I）的新型甲硅烷基化甲酰胺其中R，L，R 1，R 3，R 3，R 4和A如说明书中所定义，多种制备这些化合物的方法及其用于防治有害微生物的方法。

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