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91. 发明授权

US08895589B2 Pyridinyl amides as P2X3 and P2X2/3 inhibitors 有权
标题翻译：吡啶基酰胺作为P2X3和P2X2 / 3抑制剂
公开(公告)号：US08895589B2
公开(公告)日：2014-11-25
申请号：US13592625
申请日：2012-08-23
申请人： Chris Allen Broka , Ronald Charles Hawley
发明人： Chris Allen Broka , Ronald Charles Hawley
IPC分类号： A61K31/4418 , C07D213/24 , C07D405/14 , C07D417/12 , C07D307/68 , C07D265/30 , C07D403/12 , C07D261/18 , C07D213/56 , C07D263/34 , C07D213/61 , C07D277/56 , C07C237/42 , C07D333/38 , C07D213/81 , C07D241/24 , C07C237/32 , C07D241/12 , C07D309/08 , C07D231/14 , C07D285/06 , C07D295/125 , C07D401/12
CPC分类号： C07D241/12 , C07C237/32 , C07C237/42 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/56 , C07D213/61 , C07D213/81 , C07D231/14 , C07D241/24 , C07D261/18 , C07D263/34 , C07D265/30 , C07D277/56 , C07D285/06 , C07D295/125 , C07D307/68 , C07D309/08 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/14 , C07D417/12
摘要： Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
摘要翻译：式I化合物或其药学上可接受的盐，其中R 1为任选取代的苯基或任选取代的吡啶基，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如本文所定义。还公开了使用该化合物治疗与P2X3和/或P2X2 / 3受体拮抗剂相关疾病的方法和制备该化合物的方法。

92. 发明授权

US08889878B2 Haloalky-substituted amides as insecticides and acaricides 有权
标题翻译：卤代取代的酰胺作为杀虫剂和杀螨剂
公开(公告)号：US08889878B2
公开(公告)日：2014-11-18
申请号：US12913251
申请日：2010-10-27
申请人： Markus Heil , Eike Kevin Heilmann , Alexander Sudau , Tobias Kapferer , Friedrich August Mühlthau , Peter Jeschke , Arnd Voerste , Ulrich Görgens , Klaus Raming , Ulrich Ebbinghaus-Kintscher , Mark Drewes , Martin Adamczewski , Angela Becker
发明人： Markus Heil , Eike Kevin Heilmann , Alexander Sudau , Tobias Kapferer , Friedrich August Mühlthau , Peter Jeschke , Arnd Voerste , Ulrich Görgens , Klaus Raming , Ulrich Ebbinghaus-Kintscher , Mark Drewes , Martin Adamczewski , Angela Becker
IPC分类号： A01N43/40 , C07D211/70 , A01N43/653 , C07D331/04 , C07C281/02 , C07C233/83 , C07C237/20 , A01N37/18 , A01N37/30 , C07C317/32 , A01N43/38 , C07C311/14 , C07C237/22 , C07D213/82 , A01N43/16 , C07C323/41 , A01N43/58 , C07D209/42 , A01N43/56 , C07C233/66 , A01N43/12 , C07D401/12 , A01N43/08 , C07C255/57 , C07D405/12 , C07C255/24 , A01N43/10 , A01N43/60 , C07D249/08 , A01N41/06 , C07D409/12 , C07D213/40 , A01N43/02 , C07C233/13 , A01N43/54 , A01N43/82 , A01N43/50 , C07D307/85 , C07D213/56 , C07C233/65 , C07C233/74 , C07D271/06 , A01N37/34
CPC分类号： C07D307/85 , A01N37/18 , A01N37/30 , A01N37/34 , A01N41/06 , A01N43/02 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/16 , A01N43/38 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/82 , C07C233/13 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/83 , C07C237/20 , C07C237/22 , C07C255/24 , C07C255/57 , C07C281/02 , C07C311/14 , C07C317/32 , C07C323/41 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D209/42 , C07D213/40 , C07D213/56 , C07D213/82 , C07D249/08 , C07D271/06 , C07D331/04 , C07D401/12 , C07D405/12 , C07D409/12 , A01N25/006
摘要： The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
摘要翻译：本发明涉及通式（I）的卤素取代的酰胺衍生物，其中R1至R6，Q1至Q8，A，V，W，X，Y，n和m各自如说明书所述定义，涉及其制备方法及其作为杀虫剂和杀螨剂的用途。

93. 发明授权

US08889678B2 Acyl guanidine derivatives modulating the hedgehog protein signaling pathway 有权
标题翻译：酰基胍衍生物调节刺猬蛋白信号通路
公开(公告)号：US08889678B2
公开(公告)日：2014-11-18
申请号：US13386782
申请日：2010-07-19
申请人： Martial Ruat , Hélène Faure , Elisabeth Traiffort , Hermine Roudaut , André Mann , Angèle Schoenfelder , Maurizio Taddei , Fabrizio Manetti , Antonio Solinas
发明人： Martial Ruat , Hélène Faure , Elisabeth Traiffort , Hermine Roudaut , André Mann , Angèle Schoenfelder , Maurizio Taddei , Fabrizio Manetti , Antonio Solinas
IPC分类号： C07D295/00 , C07D213/02 , C07D513/02 , C07D209/04 , C07D317/44 , C07D307/02 , C07C239/00 , A61K31/5377 , A61K31/44 , A61K31/429 , A61K31/404 , A61K31/357 , A61K31/34 , A61K31/16 , C07D209/08 , A61K31/155 , C07D317/68 , C07D213/56 , C07C279/22 , C07D513/04 , C07D307/68 , C07D209/14 , C07D295/155 , C07D213/81
CPC分类号： C07C279/22 , A61K31/155 , C07C2601/14 , C07D209/08 , C07D209/14 , C07D213/56 , C07D213/81 , C07D295/155 , C07D307/68 , C07D317/68 , C07D513/04
摘要： The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
摘要翻译：本发明涉及调节用作药物的刺猬蛋白信号传导途径的酰基胍衍生物，特别是涉及治疗涉及与刺猬蛋白信号传导途径失调相关的组织功能障碍的疾病，以及包含其的药物组合物。本发明还涉及新颖的酰基胍衍生物。

94. 发明授权

US08883826B2 Alkynyl derivatives as modulators of metabotropic glutamate receptors 有权
标题翻译：炔基衍生物作为代谢型谷氨酸受体的调节剂
公开(公告)号：US08883826B2
公开(公告)日：2014-11-11
申请号：US13332364
申请日：2011-12-20
申请人： Anne-Sophie Bessis , Christelle Bolea , Beatrice Bonnet , Mark Epping-Jordan , Nicolas Poirier , Sonia-Maria Poli , Jean-Philippe Rocher , Yves Thollon
发明人： Anne-Sophie Bessis , Christelle Bolea , Beatrice Bonnet , Mark Epping-Jordan , Nicolas Poirier , Sonia-Maria Poli , Jean-Philippe Rocher , Yves Thollon
IPC分类号： A61K31/4439 , A61K31/4188 , A61K31/427 , A61K31/56 , C07D233/56 , C07D239/26 , C07D413/06 , C07D403/06 , C07D213/56 , C07D263/56 , C07D215/06 , C07D471/04 , C07D401/06 , C07D417/06 , C07D277/22
CPC分类号： C07D471/04 , C07D213/56 , C07D215/06 , C07D233/56 , C07D239/26 , C07D263/56 , C07D277/22 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to novel compounds of formula I wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译：本发明涉及新的式I化合物，其中W，n，X和W'在说明书中定义; 发明化合物是代谢型谷氨酸受体的调节剂 - 亚型5（“mGluR5”），其可用于治疗中枢神经系统疾病以及由mGluR5受体调节的其它病症。

95. 发明申请

US20140323390A1 COMPOUNDS AND COMPOSITIONS AS TLR2 AGONISTS 有权
标题翻译：化合物和组合物作为TLR2激动剂
公开(公告)号：US20140323390A1
公开(公告)日：2014-10-30
申请号：US14326957
申请日：2014-07-09
申请人： Tom Yao-Hsiang WU , Yefen Zou , Timothy Z. Hoffman , Jianfeng Pan
发明人： Tom Yao-Hsiang WU , Yefen Zou , Timothy Z. Hoffman , Jianfeng Pan
IPC分类号： C07C323/60 , C07D213/56 , C07K5/00 , C07F9/38
CPC分类号： C07C323/60 , C07C2601/02 , C07D213/56 , C07F9/3808 , C07K5/00
摘要： The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
摘要翻译：本发明提供了一类新颖的化合物，免疫原性组合物和包含这些化合物的药物组合物和使用这些化合物治疗或预防与Toll样受体2相关的疾病或病症的方法。一方面，该化合物可用作增强的佐剂疫苗的有效性。

96. 发明申请

US20140296249A1 4-PHENYLPIPERAZINE DERIVATIVES WITH FUNCTIONALIZED LINKERS AS DOPAMINE D3 RECEPTOR SELECTIVE LIGANDS AND METHODS OF USE 审中-公开
标题翻译：具有功能性连接子的4-苯基哌嗪衍生物作为DOPAMINE D3受体选择性配体和使用方法
公开(公告)号：US20140296249A1
公开(公告)日：2014-10-02
申请号：US14266076
申请日：2014-04-30
申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Serv , THE UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE AT FORT WORTH
发明人： Amy Hauck Newman , Peter Grundt , George C. Cyriac , Robert Luedtke , Jianjing Cao
IPC分类号： C07D307/85 , G01N33/566 , C07D209/42 , C07D213/56 , C07D295/13
CPC分类号： C07D307/85 , C07D209/42 , C07D209/48 , C07D213/56 , C07D213/64 , C07D213/81 , C07D213/89 , C07D295/092 , C07D295/096 , C07D295/13 , C07D295/145 , C07D333/70 , G01N33/566
摘要： Dopamine D3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH, OAc, and cis or trans-cyclopropyl groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.
摘要翻译：已知多巴胺D3受体拮抗剂和部分激动剂调节可卡因和其他滥用物质诱导的增强和寻求药物作用。通过将功能性引入4-苯基哌嗪类配体的丁酰胺连接链中，实现了改善的D3受体亲和力和选择性以及水溶性。公开了一系列连接链衍生物，其中诸如OH，OAc和顺式或反式 - 环丙基的官能团已被引入连接链。通常，这些修饰在D3受体上具有良好的耐受性，并且相对于D2和D4受体实现高选择性。

97. 发明申请

US20140155439A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20140155439A1
公开(公告)日：2014-06-05
申请号：US14175072
申请日：2014-02-07
申请人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
发明人： Alastair David Graham Donald , David Festus Charles Moffat , Andrew James Belfield , Carl Leslie North , Stewart Andrew Wayne Jones
IPC分类号： C07D213/56 , C07C237/20
CPC分类号： C07C237/20 , C07C259/06 , C07C2601/08 , C07D213/56 , C07D213/58
摘要： Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C═O)—, —S(═O)2—, —C(C═O)O—, —C(C═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O)2NR— wherein R′ is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(C═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
摘要翻译：式（I）化合物抑制HDAC活性：其中A，B和D独立地表示= CH-或= N-; W是-CH = CH-或-CH 2 CH 2 - ; R1是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R2和R3选自天然或非天然α氨基酸的侧链，条件是R2和R3都不是氢，或者R2和R3与它们所连接的碳一起形成3-6 元环饱和环烷基或杂环基环; Y是键，-C（= O） - ， - S（= O）2 - ， - C（C = O）O-，-C（C = O）NR' - ， - -NR'，-C（= NH）NR'或-S（= O）2 NR-，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价基团，其中n，n，p，Q，Alk1和Alk2如权利要求中所定义; X1表示键; -C（= O）; 或-S（= O）2 - ; -NR 4 C（= O） - ， - C（C = O）NR 4 - ，-NR 4 C（= O）NR 5 - ，-NR 4 S（= O）2 - 或-S（= O）2 NR 4 - 独立地是氢或任选取代的C 1 -C 6烷基; z为0或1。

98. 发明申请

US20140128408A1 HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME 有权
标题翻译： HDAC抑制剂和使用其的治疗方法
公开(公告)号：US20140128408A1
公开(公告)日：2014-05-08
申请号：US13985760
申请日：2012-01-31
申请人： Alan Kozikowski , Jay H. Kalin , Kyle V. Butier , Joel Bergman , Wayne W. Hancock
发明人： Alan Kozikowski , Jay H. Kalin , Kyle V. Butier , Joel Bergman , Wayne W. Hancock
IPC分类号： C07C229/52 , A61K31/404 , A61K51/04 , A61K45/06 , C07D473/00 , A61K31/52 , C07D209/14 , A61K31/496 , C07D235/06 , A61K31/4184 , C07D207/323 , A61K31/402 , C07D231/12 , A61K31/415 , C07D213/56 , A61K31/4409 , A61K31/24 , C07C259/10 , A61K31/166 , C07D209/08
CPC分类号： C07C229/52 , A61K45/06 , A61K49/0002 , A61K51/04 , A61K51/0446 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07C259/10 , C07C2601/08 , C07D207/08 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/18 , C07D209/20 , C07D213/56 , C07D231/12 , C07D235/06 , C07D473/00
摘要： Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
摘要翻译：公开了组蛋白脱乙酰酶抑制剂（HDACI）和包含其的组合物。治疗疾病和病症的方法，其中HDAC的抑制提供益处，如癌症，神经变性疾病，周围神经病，神经病，外伤性脑损伤，中风，高血压，疟疾，自身免疫疾病，自闭症，自闭症谱系障碍，和炎症，也被公开。

99. 发明申请

US20140066445A1 Composition and Methods for Modulating a Kinase Cascade 有权
标题翻译：调节激酶级联的组成和方法
公开(公告)号：US20140066445A1
公开(公告)日：2014-03-06
申请号：US14015030
申请日：2013-08-30
申请人： Kinex Pharmaceuticals, LLC
发明人： David G. Hangauer, Jr.
IPC分类号： C07D213/56 , C07C303/32 , C07C309/29
CPC分类号： C07D213/56 , C07C303/32 , C07C309/29
摘要： The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relates to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.
摘要翻译：本发明涉及用于调节激酶级联的一种或多种组分的化合物和方法。本发明还涉及基本上纯的化合物1和基本上纯的化合物1盐（例如化合物1盐酸盐和化合物1苯磺酸盐）。本发明还涉及制备基本上纯的化合物1和化合物1盐的方法。

100. 发明授权

US08648101B2 Nematicidal agent composition and method of using the same 有权
标题翻译：杀线虫剂组合物及其使用方法
公开(公告)号：US08648101B2
公开(公告)日：2014-02-11
申请号：US12593436
申请日：2008-04-11
申请人： Akiyuki Suwa
发明人： Akiyuki Suwa
IPC分类号： A01N43/40 , A61K31/44 , C07D213/56
CPC分类号： A01N43/40 , A01N43/56 , A01N43/60 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D401/12
摘要： The present invention provides a nematocide containing, as an active ingredient, an N-2-(pyridyl)ethylcarboxamide derivative represented by the formula (I): wherein Ar is a substituted phenyl group having one or more, the same or different substituents selected from a halogen atom, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkylthio group, a halo(C1-C6)alkylthio group, a (C1-C6)alkoxy group and a halo(C1-C6)alkoxy group, and the like, X may be the same or different, and is a hydrogen atom, a halogen atom, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, and the like, and n is the integer 0 to 4, or a salt thereof, and a method of controlling nematodes, including applying the above compound. The present invention can provide a nematocide or a method of controlling nematodes that exerts a reduced impact on the global environment, exhibits a broad nematode control spectrum at low application rates, and has an excellent nematode control effect.
摘要翻译：本发明提供含有作为活性成分的式（I）所示的N-2-（吡啶基）乙基羧酰胺衍生物的杀线虫剂：其中Ar是具有一个或多个相同或不同的取代基的取代苯基，所述取代基选自卤素原子，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷硫基，卤代（C1-C6）烷硫基，（C1-C6）烷氧基和卤素（C 1 -C 6）烷氧基等，X可以相同或不同，为氢原子，卤素原子，（C1-C6）烷基，卤代（C1-C6）烷基基等，n为整数0〜4，或其盐，以及控制线虫的方法，包括施用上述化合物。本发明可以提供一种防治线虫的方法，其对全球环境的影响降低，在低施用率下呈现广泛的线虫控制谱，并且具有优良的线虫控制效果。

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