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91. 发明授权

US08962613B2 P2X4 receptor antagonist 有权
标题翻译： P2X4受体拮抗剂
公开(公告)号：US08962613B2
公开(公告)日：2015-02-24
申请号：US13807387
申请日：2011-07-13
申请人： Shogo Sakuma , Masahiko Arai , Kunio Kobayashi , Yoshikazu Watanabe , Toshiyasu Imai , Kazuhide Inoue
发明人： Shogo Sakuma , Masahiko Arai , Kunio Kobayashi , Yoshikazu Watanabe , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： C07D243/12 , C07D403/10 , A61K31/551 , A61P25/04 , C07D243/10 , C07D401/10 , C07D409/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D491/056 , C07D401/04 , C07D403/04 , C07D243/24 , C07D487/04
CPC分类号： C07D243/10 , C07D243/12 , C07D243/24 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D409/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/056
摘要： A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.
摘要翻译：使用具有下式（III）的二氮杂衍生物或其药理学上可接受的盐作为P2X4受体拮抗剂：其中R21和R22各自为氢，C1-8烷基等; R 23为氢，C 1-8烷基等; R 24和R 25各自为氢，C 1-8烷基等; R 26是氢，C 1-8烷基，卤素原子，羟基，硝基，氰基，任选具有一个或多个取代基的苯基，或任选具有一个或多个取代基的杂环基等; p为0或1。

92. 发明授权

US08049006B2 7-membered ring compound and method of production and pharmaceutical application thereof 失效
公开(公告)号：US08049006B2
公开(公告)日：2011-11-01
申请号：US12302646
申请日：2007-05-30
申请人： Tsuyoshi Muto , Taisaku Tanaka , Hiroshi Maruoka , Seiichi Imajo , Yoshiaki Tomimori , Koji Sato , Tsutomu Yagi
发明人： Tsuyoshi Muto , Taisaku Tanaka , Hiroshi Maruoka , Seiichi Imajo , Yoshiaki Tomimori , Koji Sato , Tsutomu Yagi
IPC分类号： C07D243/08
CPC分类号： C07D243/08 , C07D243/10 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12
摘要： A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.

93. 发明授权

US07709470B2 11-phenyl-dibenzodiazepine derivatives as RXR-antagonists 失效
标题翻译： 11-苯基 - 二苯并二氮杂衍生物作为RXR-拮抗剂
公开(公告)号：US07709470B2
公开(公告)日：2010-05-04
申请号：US10550776
申请日：2004-04-08
申请人： Junichi Sakaki , Kazuhide Konishi , Masashi Kishida , Masaaki Kimura , Hidefumi Uchiyama , Hironobu Mitani
发明人： Junichi Sakaki , Kazuhide Konishi , Masashi Kishida , Masaaki Kimura , Hidefumi Uchiyama , Hironobu Mitani
IPC分类号： A61P3/00 , A61K31/551 , C07D243/38
CPC分类号： C07D243/38 , C07D243/10
摘要： The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with RXR-antagonism, in particular selected from diabetes, complication of diabetes such as retinopathy, nephropathy, neuropathy, and hyperlipidemia, obesity, dyslipidemia, and osteoporosis.
摘要翻译：本发明涉及显示RXR拮抗剂功效的新型苯并二氮杂类化合物，用于延缓进展，预防或治疗与RXR拮抗作用有关的病症或疾病，特别是选自糖尿病，糖尿病并发症如视网膜病，肾病，神经病，和高脂血症，肥胖，血脂异常和骨质疏松症。

94. 发明申请

US20090253683A1 7-MEMBERED RING COMPOUND AND METHOD OF PRODUCTION AND PHARMACEUTICAL APPLICATION THEREOF 失效
标题翻译： 7-会员环化合物及其生产方法和药物应用
公开(公告)号：US20090253683A1
公开(公告)日：2009-10-08
申请号：US12302646
申请日：2007-05-30
申请人： Tsuyoshi Muto , Taisaku Tanaka , Hiroshi Maruoka , Seiichi Imajo , Yoshiaki Tomimori , Koji Sato , Tsutomu Yagi
发明人： Tsuyoshi Muto , Taisaku Tanaka , Hiroshi Maruoka , Seiichi Imajo , Yoshiaki Tomimori , Koji Sato , Tsutomu Yagi
IPC分类号： A61K31/551 , C07D243/08 , A61P9/00 , A61P27/00 , A61P17/00
CPC分类号： C07D243/08 , C07D243/10 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12
摘要： A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
摘要翻译：具有式（I）的7元杂环化合物或其盐或其具有糜酶抑制作用的溶剂化物并且可用于预防或治疗涉及糜酶的各种疾病：其制备方法，以及可用于预防或治疗其中涉及胃促胰酶的药物组合物，包括具有式（I）的化合物或其药学上可接受的盐或溶剂合物。

95. 发明申请

US20070258905A1 Contrast Agents Endowed with High Relaxivity for Use in Magnetic Resonance Imaging (Mri) Which Contain a Chelating Moiety with Polyhydroxylated Substituents 有权
标题翻译：具有高松弛度的对比剂用于磁共振成像（Mri），其含有多羟基化取代基的螯合物
公开(公告)号：US20070258905A1
公开(公告)日：2007-11-08
申请号：US11630605
申请日：2005-06-28
申请人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
发明人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
IPC分类号： A61B5/055 , C07C211/00 , C07D211/00 , C07D243/00 , C07D243/08 , C07D255/04 , C07D315/00 , C07F9/02 , G01N24/08
CPC分类号： C07H15/26 , A61K49/085 , A61K49/124 , C07C237/08 , C07D243/08 , C07D243/10 , C07F9/3808 , C07F9/4006 , C07F9/5728 , C07H17/02
摘要： The present invention relates to a new class of paramagnetic ion-based contrast agents of molecular weight lower than 3.5 kDa that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents and that are further characterized by a higher relaxivity.
摘要翻译：本发明涉及分子量低于3.5kDa的新型顺磁离子型造影剂，其显示类似于通常使用的T1-一般血管外试剂的药代动力学特征，并且其进一步特征在于较高的弛豫度。

96. 发明申请

US20070173494A1 Diaza heterocyclic sulfonamide derivatives and their uses 有权
标题翻译：二氮杂环磺酰胺衍生物及其用途
公开(公告)号：US20070173494A1
公开(公告)日：2007-07-26
申请号：US11637932
申请日：2006-12-13
申请人： Jay Powers , Xuelei Yan , Daqing Sun , Hua Tu
发明人： Jay Powers , Xuelei Yan , Daqing Sun , Hua Tu
IPC分类号： A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/506 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D295/26 , C07D213/74 , C07D241/04 , C07D243/08 , C07D243/10 , C07D401/04 , C07D403/06
摘要： Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R7, R8, R9, R10, R11, R12, R13, X, Y1, Y2, m, and n are set forth in the description.
摘要翻译：式I的二氮杂杂环磺酰胺衍生物具有治疗效用，特别是治疗糖尿病，肥胖症及相关病症和病症：其中R 7，R 8，R SUP R 9，R 10，R 11，R 12，R 13，X，Y ^{1，Y 2，m和n在说明书中列出。}

97. 发明申请

US20070072847A1 Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions 有权
标题翻译：选择的CGRP拮抗剂，其制备方法及其作为药物组合物的用途
公开(公告)号：US20070072847A1
公开(公告)日：2007-03-29
申请号：US11533096
申请日：2006-09-19
申请人： Stephan Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Marco Santagostino , Fabio Paleari , Henri Doods , Kirsten Arndt , Gerhard Schaenzle
发明人： Stephan Mueller , Klaus Rudolf , Philipp Lustenberger , Dirk Stenkamp , Marco Santagostino , Fabio Paleari , Henri Doods , Kirsten Arndt , Gerhard Schaenzle
IPC分类号： A61K31/5513 , A61K31/517 , A61K31/454 , C07D403/04
CPC分类号： C07D243/10 , C07D249/12 , C07D401/12 , C07D403/12
摘要： The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译：本发明涉及通式I的CGRP拮抗剂，其中R 1，R 2，R 3和R 4， / SUP>如权利要求1中所定义，互变异构体，异构体，非对映异构体，对映异构体，其水合物，其混合物及其盐及其盐的水合物，特别是其生理上可接受的盐与无机或有机酸或碱，以及其中一个或多个氢原子被氘代替的通式I化合物，其含有这些化合物的药物组合物，其用途和制备方法。

98. 发明授权

US07153850B2 Lactam compounds and pharmaceutical use thereof 有权
公开(公告)号：US07153850B2
公开(公告)日：2006-12-26
申请号：US10449774
申请日：2003-06-02
申请人： Yukio Iino , Takao Ikenoue , Nobuo Kondo , Hiroyuki Matsueda , Toshihiro Hatanaka , Ryusuke Hirama , Yoko Masuzawa , Fumio Ohta , Akiyo Yamazaki , Seiji Niwa , Takashi Yamamoto
发明人： Yukio Iino , Takao Ikenoue , Nobuo Kondo , Hiroyuki Matsueda , Toshihiro Hatanaka , Ryusuke Hirama , Yoko Masuzawa , Fumio Ohta , Akiyo Yamazaki , Seiji Niwa , Takashi Yamamoto
IPC分类号： C07D487/04 , C07D498/04 , C07D513/04 , A61K31/5517 , A61P3/10
CPC分类号： C07D487/04 , A61K31/5517 , A61K31/554 , C07D243/10 , C07D513/04
摘要： An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.

99. 发明申请

US20060276456A1 Biphenyl vasopressin agonists 失效
公开(公告)号：US20060276456A1
公开(公告)日：2006-12-07
申请号：US11502982
申请日：2006-08-11
申请人： Kevin Memoli , Amedeo Failli , Thomas Caggiano , Jay Shumsky , Eugene Trybulski , John Dusza
发明人： Kevin Memoli , Amedeo Failli , Thomas Caggiano , Jay Shumsky , Eugene Trybulski , John Dusza
IPC分类号： A61K31/551 , C07D487/02
CPC分类号： C07D243/10 , C07D243/38 , C07D401/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04
摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

100. 发明申请

US20060205696A1 [[2-(Amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives for the treatment of pain 失效
标题翻译： [[2-（氨基-3,4-二氧代-1-环丁烯-1-基）氨基]烷基] - 酸衍生物，用于治疗疼痛
公开(公告)号：US20060205696A1
公开(公告)日：2006-09-14
申请号：US11433737
申请日：2006-05-12
申请人： Michael Brandt , Margaret Zaleska , John Moyer
发明人： Michael Brandt , Margaret Zaleska , John Moyer
IPC分类号： A61K31/663 , A61K31/4245 , A61K31/41 , A61K31/195 , A61K31/215
CPC分类号： C07D243/10 , A61K31/122 , A61K31/198 , A61K31/4245 , A61K31/551 , A61K31/662 , A61K45/06
摘要： This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are —CH2C—H2—, —CH2C(R6)(R7)CH2— or —CH2C(R8)(R9)—C(R10)(R11)CH2—, where R6, R8 and R10 are, independently, H, alkyl or hydroxyl and R7, R9 and R11 are, independently, H or alkyl; A is alkylene or alkenylene; X is CO2R3, P(O)(OR4)(OR5), 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl in which R3, R4 and R5 are, independently, H or alkyl, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions for treating pain containing a pain treating effective amount of the compound of formula (I).
摘要翻译：本发明提供一种治疗哺乳动物疼痛的方法，包括向需要这种治疗的哺乳动物施用疼痛治疗有效量的式（I）化合物：其中R 1是H，烷基或苯基烷基; R 2是H，烷基，烯基或苯基烷基; 或R 1和R 2一起作为Z是-CH 2 CH 2 - ， - CH＆lt; SUB （R 6）（R 7）CH 2 - 或-CH 2 CH 2 C（R 8）（R 9） - （R 10） - （R 11）其中R 6，R 8和R 10独立地为H，烷基或羟基，R 1，R 2， R 9，R 9和R 11独立地是H或烷基; A是亚烷基或亚烯基; X是CO 2 R 3，P（O）（OR 4）（OR 5），3， 5-二氧代-1,2,4-恶二唑烷-2-基或其中R 3，R 4和R 5的5-四唑基，独立地是H或烷基，或其药学上可接受的盐。本发明还提供用于治疗疼痛的药物组合物，其含有疼痛治疗有效量的式（I）化合物。

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