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91. 发明申请

US20100204272A1 Compounds which have activity at M1 receptor and their uses in medicine 失效
标题翻译：具有M1受体活性的化合物及其在药物中的用途
公开(公告)号：US20100204272A1
公开(公告)日：2010-08-12
申请号：US12678347
申请日：2008-09-18
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
IPC分类号： A61K31/47 , C07D401/04 , A61K31/454 , A61P25/18 , A61P25/28
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

92. 发明申请

US20100197727A1 Quinoline Derivatives as Antibacterial Agents 审中-公开
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US20100197727A1
公开(公告)日：2010-08-05
申请号：US11917091
申请日：2006-06-26
申请人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , David Francis Alain Lancois , Magali Madeleine Simone Motte , Jérôme Emile Georges Guillemont
发明人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , David Francis Alain Lancois , Magali Madeleine Simone Motte , Jérôme Emile Georges Guillemont
IPC分类号： A61K31/47 , C07D215/227 , C07D409/06 , A61K31/4709 , C07D401/06 , C07D215/36 , A61P31/04
CPC分类号： C07D409/06 , A61K31/47 , A61K31/4709 , C07D215/227 , C07D215/36 , C07D401/06
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein A− is a counter ion; R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or wherein Y is CH2, O, S, NH or N-alkyl; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form —CH═CH—CH═CH—; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 taken together form —CH═CH—N═; R10 is alkyl, alkylcarbonyl, Ar, Ar-alkyl, Ar-carbonyl, Het1-alkyl or Het1-carbonyl.
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，N-氧化物，互变异构体形式或其立体化学异构体形式，其中A-是抗衡离子; R 1是氢，卤素，卤代烷基，氰基，羟基，Ar，Het，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar） p为1〜4; R2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或其中Y是CH2，O，S，NH或N-烷基; R3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为0〜4; R4和R5各自独立地为氢，烷基或苄基; 或R4和R5可以一起包括它们所连接的N; R 6是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）或两个连位的R6基团可以一起形成-CH = CH-CH = CH-; r为1〜5; R7是氢，烷基，Ar或Het; R8是氢或烷基; R9是氧代; 或R8和R9一起形成-CH = CH-N =; R10是烷基，烷基羰基，Ar，Ar-烷基，Ar-羰基，Het1-烷基或Het1-羰基。

93. 发明授权

US07745462B2 Quinoline-2-one derivatives for the treatment of airways diseases 有权
标题翻译：喹啉-2-酮衍生物用于治疗气道疾病
公开(公告)号：US07745462B2
公开(公告)日：2010-06-29
申请号：US10552023
申请日：2004-04-02
申请人： Robin Alec Fairhurst , David Andrew Sandham , David Beattie , Ian Bruce , Bernard Cuenoud , Reamonn Madden , Neil John Press , Roger John Taylor , Katharine Louise Turner , Simon James Watson
发明人： Robin Alec Fairhurst , David Andrew Sandham , David Beattie , Ian Bruce , Bernard Cuenoud , Reamonn Madden , Neil John Press , Roger John Taylor , Katharine Louise Turner , Simon James Watson
IPC分类号： A61K31/02 , C07D215/38
CPC分类号： C07D215/227 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Compounds of formula I in free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的式I化合物，其中-C-Y-，R 1和R 2为G具有本说明书中指出的含义，可用于治疗通过活化2-肾上腺素受体而预防或缓解的病症。还描述了含有化合物的药物组合物和制备该化合物的方法。

94. 发明申请

US20100144742A1 MULTIPLY-SUBSTITUTED TETRAHYDRONAPHTHALENE DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS 失效
标题翻译：多取代四氢萘基衍生物及其生产工艺及其作为抗炎剂的用途
公开(公告)号：US20100144742A1
公开(公告)日：2010-06-10
申请号：US12642121
申请日：2009-12-18
申请人： Hartmut REHWINKEL , Stefan Baeurle , Markus Berger , Norbert Schmees , Heike Schaecke , Konrad Krolikiewicz , Anne Mengel , Duy Nguyen , Stefan Jaroch , Werner Skuballa
发明人： Hartmut REHWINKEL , Stefan Baeurle , Markus Berger , Norbert Schmees , Heike Schaecke , Konrad Krolikiewicz , Anne Mengel , Duy Nguyen , Stefan Jaroch , Werner Skuballa
IPC分类号： A61K31/517 , A61K31/472 , A61K31/47 , C07D237/30 , C07D239/72 , C07D215/00 , A61P29/00
CPC分类号： C07D217/24 , A61K31/47 , A61K31/472 , A61K31/517 , C07C215/44 , C07C255/58 , C07C2602/10 , C07D209/34 , C07D209/46 , C07D213/74 , C07D215/04 , C07D215/22 , C07D215/227 , C07D215/38 , C07D215/48 , C07D215/58 , C07D231/56 , C07D237/32 , C07D239/74 , C07D239/76 , C07D277/64 , C07D307/88 , C07D317/70 , C07D405/12 , C07D471/04
摘要： The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
摘要翻译：本发明涉及式（I）的多取代四氢萘衍生物的制备方法及其作为抗炎剂的用途。

95. 发明授权

US07728013B2 Method of modulating stress-activated protein kinase system 有权
标题翻译：调节应激激活蛋白激酶系统的方法
公开(公告)号：US07728013B2
公开(公告)日：2010-06-01
申请号：US11431132
申请日：2006-05-09
申请人： Lawrence M. Blatt , Scott D. Seiwert , Leonid Beigelman , Ramachandran Radhakrishnan , Karl Kossen , Vladimir Serebryany
发明人： Lawrence M. Blatt , Scott D. Seiwert , Leonid Beigelman , Ramachandran Radhakrishnan , Karl Kossen , Vladimir Serebryany
IPC分类号： A61K31/44 , A01N43/40 , C07D213/62 , C07D213/44
CPC分类号： A61K31/4412 , A61K31/44 , A61K31/444 , A61K31/45 , A61K31/4704 , A61K31/7052 , A61K47/56 , A61K47/58 , C07D213/16 , C07D213/26 , C07D213/63 , C07D213/64 , C07D213/69 , C07D215/227 , C07H15/26 , C07K1/1077 , C08F289/00 , Y02A50/401 , Y02A50/409 , Y02A50/411 , Y02A50/475
摘要： Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
摘要翻译：公开了用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制至少一种p38MAPK的能力; 并且其中所述接触以对所述化合物抑制至少一种p38MAPK的低百分比抑制浓度的SAPK-调节浓度进行。还公开了吡非尼酮的衍生物。这些衍生物可以调节应激活化蛋白激酶（SAPK）系统。

96. 发明授权

US07728007B2 Therapeutic amides 失效
标题翻译：治疗酰胺
公开(公告)号：US07728007B2
公开(公告)日：2010-06-01
申请号：US12260296
申请日：2008-10-29
申请人： Jerome P. Horwitz , Thomas H. Corbett , Eduardo Palomino , Lisa Polin , Stuart T. Hazeldine
发明人： Jerome P. Horwitz , Thomas H. Corbett , Eduardo Palomino , Lisa Polin , Stuart T. Hazeldine
IPC分类号： A61K31/47 , C07D215/227
CPC分类号： C07D215/227 , C07D241/44
摘要： The invention provides compounds of the formula: wherein X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.
摘要翻译：本发明提供了下式的化合物：其中X，Y和Z如说明书中所定义。这些化合物是有效的抗肿瘤剂。本发明还提供了包含上式化合物或其盐的药物组合物，可用于制备上式化合物的中间体，以及包括将上式化合物或其盐施用于有需要的哺乳动物的治疗方法。

97. 发明申请

US20100130744A1 PROCESS FOR THE PREPARATION OF ARIPIPRAZOLE 审中-公开
标题翻译：制备阿维哌唑的方法
公开(公告)号：US20100130744A1
公开(公告)日：2010-05-27
申请号：US12451775
申请日：2008-05-29
申请人： Mahesh Nagarimadugu , Vipin Kumar Kaushik , Ramesh Dandala , Sivakumaran Meenakshisunderam
发明人： Mahesh Nagarimadugu , Vipin Kumar Kaushik , Ramesh Dandala , Sivakumaran Meenakshisunderam
IPC分类号： C07D401/12
CPC分类号： C07D215/227
摘要： The present invention relates to an improved process for the preparation of 7-[4-[4-(2,3-dichlorophenyl)-1-piper-azinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone of Formula (I).
摘要翻译：本发明涉及制备7- [4- [4-（2,3-二氯苯基）-1-哌嗪基]丁氧基] -3,4-二氢-2（1H） - 喹啉酮的改进方法式（I）。

98. 发明授权

US07714129B2 Methods of preparing anhydrous aripiprazole form II 失效
标题翻译：制备无水阿立哌唑II的方法
公开(公告)号：US07714129B2
公开(公告)日：2010-05-11
申请号：US11529969
申请日：2006-09-29
申请人： Hagit Eisen-Nevo , Zhanna Pavlov
发明人： Hagit Eisen-Nevo , Zhanna Pavlov
IPC分类号： C07D401/12
CPC分类号： C07D215/20 , C07D215/227
摘要： Provided is a method of preparing aripiprazole anhydrous Form II from aripiprazole.
摘要翻译：提供从阿立哌唑制备无水形式II的阿立哌唑的方法。

99. 发明授权

US07696246B2 Bicyclic androgen and progesterone receptor modulator compounds and methods 有权
标题翻译：双环雄激素和孕激素受体调节剂的化合物和方法
公开(公告)号：US07696246B2
公开(公告)日：2010-04-13
申请号：US11165769
申请日：2005-06-23
申请人： Lin Zhi , Cornelis Arjan Van Oeveren , Esther Martinborough
发明人： Lin Zhi , Cornelis Arjan Van Oeveren , Esther Martinborough
IPC分类号： A61K31/352 , C07D311/18
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要翻译：本发明涉及用于调节由AR和PR介导的过程的化合物，药物组合物和方法。更具体地，本发明涉及非甾类化合物和组合物，其是高亲和力，高特异性激动剂，部分激动剂（即部分激活剂和/或组织特异性激活剂）和AR和PR的拮抗剂。还提供制备这些化合物和药物组合物的方法，以及用于其合成的关键中间体。

100. 发明申请

US20100069366A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：US20100069366A1
公开(公告)日：2010-03-18
申请号：US12515593
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Ismet Dorange , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Ismet Dorange , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
IPC分类号： A61K31/4704 , C07D215/227 , C07D243/14 , A61K31/551 , A61P31/04
CPC分类号： C07D215/227 , C07D215/04 , C07D215/14 , C07D215/36 , C07D403/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, wherein Q represents a radical of formula a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof.The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其中Q表示式的基团N-氧化物，其药学上可接受的盐或其溶剂合物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗细菌感染的药物中的用途和制备所要求保护的化合物。

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