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91. 发明授权

US08802711B2 TRPV1 antagonists 有权
标题翻译： TRPV1拮抗剂
公开(公告)号：US08802711B2
公开(公告)日：2014-08-12
申请号：US13426732
申请日：2012-03-22
申请人： Arthur Gomtsyan , Jerome F. Daanen , Gregory A. Gfesser , Michael E. Kort , Chih-Hung Lee , Heath A. McDonald , Pamela S. Puttfarcken , Eric A. Voight , Philip R. Kym
发明人： Arthur Gomtsyan , Jerome F. Daanen , Gregory A. Gfesser , Michael E. Kort , Chih-Hung Lee , Heath A. McDonald , Pamela S. Puttfarcken , Eric A. Voight , Philip R. Kym
IPC分类号： C07D265/36 , C07D215/38 , C07D217/02 , C07D231/56 , A61K31/17 , A61K31/538 , A61K31/192 , A61K31/472
CPC分类号： C07C275/32 , C07C2601/08 , C07C2602/08 , C07D209/08 , C07D215/38 , C07D217/02 , C07D231/56 , C07D239/80 , C07D263/48 , C07D265/36 , C07D401/04 , C07D413/12 , C07D417/12
摘要： Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：本文公开了式（I）化合物或其药学上可接受的盐，溶剂化物或其组合，其中X1，X2，X3，X4，J，K，L，X5，X6，Rb，G2和m在本说明书中定义。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

92. 发明授权

US08716285B2 N-hydroxy-benzamids for the treatment of cancer 有权
标题翻译： N-羟基苯甲酰胺用于治疗癌症
公开(公告)号：US08716285B2
公开(公告)日：2014-05-06
申请号：US13226567
申请日：2011-09-07
申请人： Lei Guo , Guozhi Tang , Zhanguo Wang , Jason Christopher Wong , Weixing Zhang
发明人： Lei Guo , Guozhi Tang , Zhanguo Wang , Jason Christopher Wong , Weixing Zhang
IPC分类号： A61K31/535 , A61K31/517 , A61K31/505 , A61K31/47 , A61K31/44 , C07D413/12 , C07D239/72 , C07D401/12 , C07D215/38 , C07D213/02 , C07D211/70 , C07C255/24
CPC分类号： C07C259/10 , C07C311/07 , C07C311/20 , C07C311/29 , C07C2602/10 , C07D213/56 , C07D213/71 , C07D213/74 , C07D215/48 , C07D239/42 , C07D239/47 , C07D401/04 , C07D401/14 , C07D405/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，酯或立体异构体，其中R1至R3和X具有本文给出的含义。本发明还涉及制备所述化合物的方法和所述化合物的用途，特别是其用作药物，更具体地说，其用作治疗癌症中的药物。

93. 发明授权

US08710229B2 Hepatitis C virus inhibitors 有权
公开(公告)号：US08710229B2
公开(公告)日：2014-04-29
申请号：US13901637
申请日：2013-05-24
申请人： Bristol-Myers Squibb Company
发明人： Alan Xiangdong Wang , Li-Qiang Sun , Sing-Yuen Sit , Ny Sin , Paul Michael Scola , Yan Chen
IPC分类号： C07D215/38
CPC分类号： A61K38/06 , A61K31/40 , A61K38/00 , A61K38/005 , A61K45/06 , C07D207/16 , C07D217/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/14 , C07D491/04 , C07K5/06034 , C07K5/06052 , C07K5/0808 , C07K5/0827 , A61K2300/00
摘要： Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

94. 发明授权

US08710079B2 Quinoline compounds and their use for treating viral infection 有权
标题翻译：喹啉化合物及其用于治疗病毒感染的用途
公开(公告)号：US08710079B2
公开(公告)日：2014-04-29
申请号：US13091895
申请日：2011-04-21
申请人： Hsing-Pang Hsieh , Tsu-An Hsu , Jiann-Yih Yeh , Yu-Sheng Chao
发明人： Hsing-Pang Hsieh , Tsu-An Hsu , Jiann-Yih Yeh , Yu-Sheng Chao
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Quinoline compounds of formula (I): in which A, B, D, E, F, G, R1, R2, R3, X, Y, n, p, and q are defined herein. Also disclosed is a method for treating a viral infection with a compound of formula (I).
摘要翻译：式（I）的喹啉化合物：其中A，B，D，E，F，G，R 1，R 2，R 3，X，Y，n，p和q如本文所定义。还公开了用式（I）化合物治疗病毒感染的方法。

95. 发明授权

US08703798B2 Antifungal and antiparasitic indoloquinoline derivatives 有权
标题翻译：抗真菌和抗寄生吲哚喹啉衍生物
公开(公告)号：US08703798B2
公开(公告)日：2014-04-22
申请号：US13404307
申请日：2012-02-24
申请人： Seth Y. Ablordeppey
发明人： Seth Y. Ablordeppey
IPC分类号： A61K31/47 , C07D215/38
CPC分类号： C07D471/04 , C07D215/44 , C07D495/04
摘要： An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R10, O, S, S═O, CH2, or C═O, where R10 is a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is —CH3 and the 10 position is N—(CH2)5-Ph.
摘要翻译：吲哚喹啉，其中N-5原子是直链C（1-5）链，支链C（1-5）链，杂原子链，由环烷基或芳环末端取代的直链，支链取代末端由环烷基或芳环，末端被环烷基或芳环取代的杂原子链; 10位是N-R10，O，S，S = O，CH2或C = O，其中R10是支链C（1-5）链，杂原子链，由环烷基或芳族末端取代的直链环，被环烷基或芳环末端取代的支链，被环烷基或芳环末端取代的杂原子链。在一个实施方案中，季末N-5原子是-CH 3，10位是N-（CH 2）5-Ph。

96. 发明申请

US20140107155A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
标题翻译：取代的杂环化合物作为离子通道调节剂
公开(公告)号：US20140107155A1
公开(公告)日：2014-04-17
申请号：US14101813
申请日：2013-12-10
申请人： Gilead Sciences, Inc.
发明人： Matthew Abelman , Robert H. Jiang , Jeff Zablocki
IPC分类号： C07D215/54 , C07D401/06 , C07D215/38
CPC分类号： C07D215/54 , C07D215/14 , C07D215/18 , C07D215/38 , C07D401/06 , C07D413/04
摘要： The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
摘要翻译：本发明涉及式（I）的钠通道抑制剂：其中R1，R2，R3，R4，R5，X，Y和Z如本文所定义，以及它们在治疗各种疾病状态中的用途，包括心血管疾病和糖尿病。本发明还涉及制备化合物的方法以及含有这些化合物的药物组合物。

97. 发明申请

US20140080831A1 COMPOUNDS USEFUL FOR TREATING CANCER 有权
标题翻译：化合物可用于治疗癌症
公开(公告)号：US20140080831A1
公开(公告)日：2014-03-20
申请号：US14087762
申请日：2013-11-22
申请人： CENTRE NATIONALE DE RECHERCHE SCIENTIFIQUE , UNIVERSITE MONTPELLIER 2 , SOCIETE SPLICOS , INSTITUT CURIE
发明人： Pierre ROUX , Florence MAHUTEAU , Romain NAJMAN , Jamal TAZI , Gilles GADEA , Didier SCHERRER , Carsten BROCK , Nathalie CAHUZAC
IPC分类号： C07D401/12 , C07D215/46 , C07D403/12 , C07D215/42 , C07D215/38 , C07D241/44
CPC分类号： C07D403/12 , A61K31/4709 , A61K31/4985 , C07D213/74 , C07D215/38 , C07D215/42 , C07D215/46 , C07D241/44 , C07D401/12
摘要： A method of preventing, inhibiting, or treating cancer that includes contacting a cell with at least one compound of formula (Ia) or a pharmaceutically acceptable salt thereof: where: R independently represents a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a —NR1R2 group, or a (C1-C3)alkoxy group; R′ is a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —NO2 group, a (C1-C3)alkoxy group, or a —NR1R2 group; and R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group.
摘要翻译：一种预防，抑制或治疗癌症的方法，包括使细胞与至少一种式（Ia）化合物或其药学上可接受的盐接触：其中：R独立地表示氢原子，卤素原子，（C1-C3 ）烷基，-CN基，羟基，-COOR1基，（C1-C3）氟代烷基，-NO2基，-NR1R2基或（C1-C3）烷氧基; R'是氢原子，卤素原子，（C1-C3）烷基，-NO2基，（C1-C3）烷氧基或-NR1R2基团; 并且R 1和R 2是氢原子或（C 1 -C 3）烷基。

98. 发明授权

US08642767B2 Process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof 有权
标题翻译：制备6-（7 - （（1-氨基环丙基）甲氧基）-6-甲氧基喹啉-4-基氧基）-N-甲基-1-萘甲酰胺的方法及其合成中间体
公开(公告)号：US08642767B2
公开(公告)日：2014-02-04
申请号：US13256722
申请日：2010-03-11
申请人： Silvano Spinelli , Valeria Livi
发明人： Silvano Spinelli , Valeria Livi
IPC分类号： C07D215/38
CPC分类号： C07D215/22 , C07C217/44 , C07C269/04 , C07C271/24 , C07C2601/02 , Y02P20/55
摘要： A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
摘要翻译：式（I）化合物6-（7-4（1-氨基环丙基）甲氧基）-6-甲氧基喹啉-4-基氧基）-N-甲基-1-萘甲酰胺及其制备方法描述了其药学上可接受的盐。该方法与先前描述的方法相比具有多种优点，特别是它避免使用酰基叠氮化物中间体及其柯曲斯重排。还描述了可用于制备化合物（I）的新型中间体。

99. 发明申请

US20140005178A1 AZABIPHENYLAMINOBENZOIC ACID DERIVATIVES AS DHODH INHIBITORS 审中-公开
标题翻译：作为DHODH抑制剂的亚氨基苯甲酸苯甲酸衍生物
公开(公告)号：US20140005178A1
公开(公告)日：2014-01-02
申请号：US13964181
申请日：2013-08-12
申请人： Almirall, S.A.
发明人： Julio Cesar CASTRO PALOMINO LARIA , Emma Terricabras Belart , Montserrat Erra Sola , Eloisa Navarro Romero , Siliva Fonquerna Pou , Aranzazu Cardus Figueras , Maria Estrella Lozoya Toribio
IPC分类号： C07D213/74 , A61K31/5377 , A61K31/505 , A61K31/47 , C07D413/10 , A61K31/444 , A61K31/44 , C07D239/42 , C07D215/38 , A61K45/06 , A61K31/55 , A61K31/4545
CPC分类号： C07D213/74 , A61K31/44 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D215/38 , C07D239/42 , C07D401/04 , C07D401/10 , C07D413/10
摘要： The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
摘要翻译：本公开涉及式（I）的新的氮杂二苯胺基苯甲酸衍生物; 以及它们的制备方法，包含它们的药物组合物及其在治疗中作为脱氢山梨醇二氢化酶（DHODH）抑制剂的用途。

100. 发明授权

US08609847B2 Dihydroquinolinone derivatives 有权
标题翻译：二氢喹啉酮衍生物
公开(公告)号：US08609847B2
公开(公告)日：2013-12-17
申请号：US13144591
申请日：2010-02-05
申请人： Toshio Nakamura , Seiji Masuda , Aya Futamura
发明人： Toshio Nakamura , Seiji Masuda , Aya Futamura
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04
摘要： The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A dihydroquinolinone derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein Q represents the following formula (A) or (B)}
摘要翻译：本发明提供了用于痴呆，阿尔茨海默病，注意缺陷多动障碍，精神分裂症，进食障碍，肥胖，糖尿病，高脂血症，睡眠障碍，发作性睡眠障碍，睡眠呼吸暂停综合征，昼夜节律紊乱，抑郁，过敏性鼻炎或其他疾病由式（1）表示的二氢喹啉酮衍生物或其药学上可接受的盐：其中Q表示下式（A）或（B）}

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