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1. 发明授权

US10696648B2 Inhibitors of indoleamine 2,3-dioxygenase and methods of their use 有权
公开(公告)号：US10696648B2
公开(公告)日：2020-06-30
申请号：US16098239
申请日：2017-05-04
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： David K. Williams , Weifang Shan , James Aaron Balog
IPC分类号： C07D401/10 , C07C275/30 , C07C275/36 , C07C275/34 , C07C275/28 , C07C275/42 , C07C275/26 , A61P35/00 , A61K31/4709 , A61K31/47 , A61K31/277 , A61K31/17 , C07D401/04 , C07D215/18 , C07C275/32
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

2. 发明授权

US10519105B2 KCNQ2-5 channel activator 有权
公开(公告)号：US10519105B2
公开(公告)日：2019-12-31
申请号：US16095374
申请日：2017-04-21
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： Kentaro Yashiro , Masashi Kato , Tetsuji Saito , Takuya Okada , Daisuke Wakamatsu , Adam James Davenport , Christopher Charles Stimson
IPC分类号： C07C275/32 , C07C271/30 , A61P13/02 , A61K31/17 , A61K31/27 , A61K31/341 , A61K31/351 , A61K31/4045 , A61K31/42 , A61K31/426 , A61K31/44 , A61K31/4545 , A61K31/4965 , A61K31/505 , C07D213/74 , C07D309/04 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/28 , C07D209/14 , C07D213/40 , C07D213/64 , C07D307/52 , A61P13/10
摘要： An object of the present invention is to provide a novel compound having a strong opening action with respect to KCNQ2-5 channels. A compound represented by the general formula (I) (wherein the definition of each group is as described in the specification) is provided. The compound represented by the general formula (I) has a strong opening action with respect to KCNQ2-5 channels, and therefore is useful as a prophylactic and/or therapeutic agent for a KCNQ2-5 channel-related disease (for example, dysuria, overactive bladder, or the like).

3. 发明授权

US10059659B2 Enantiomerically pure binaphthol derivatives and method for preparing the same 有权
公开(公告)号：US10059659B2
公开(公告)日：2018-08-28
申请号：US13994328
申请日：2011-12-13
申请人： Rae Kyu Chang , Yun Soo Ahn , Heejung Jung , Hyerim Ga , Juwan Maeng , Young-Kook Koh , Young Hee Lee , Kwang Jae Lee , Joonseo Kim , Hyunil Lee , Heungsik Yoon
发明人： Rae Kyu Chang , Yun Soo Ahn , Heejung Jung , Hyerim Ga , Juwan Maeng , Young-Kook Koh , Young Hee Lee , Kwang Jae Lee , Joonseo Kim , Hyunil Lee , Heungsik Yoon
IPC分类号： C07C273/18 , C07B57/00 , C07C275/32
CPC分类号： C07C273/1854 , C07B57/00 , C07C275/32
摘要： The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2′-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost. [formula 6]

4. 发明申请

US20180215705A1 hTRPV1 CHEMICAL AGENTS 审中-公开
公开(公告)号：US20180215705A1
公开(公告)日：2018-08-02
申请号：US15546833
申请日：2016-02-05
申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
发明人： Xiang-Qun XIE , Zhiwei Feng
IPC分类号： C07C275/30 , C07C275/42 , C07C275/34 , C07C275/40 , C07C275/32 , C07D295/135
CPC分类号： C07C275/30 , C07C275/32 , C07C275/34 , C07C275/40 , C07C275/42 , C07D295/135
摘要： Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds.

5. 发明授权

US08859584B2 TRPV1 antagonists 有权
标题翻译： TRPV1拮抗剂
公开(公告)号：US08859584B2
公开(公告)日：2014-10-14
申请号：US13716837
申请日：2012-12-17
申请人： AbbVie Inc.
发明人： Kevin R. Woller , Gregory A. Gfesser , Huaqing Liu , Jerome F. Daanen , Eric A. Voight , Irene I. Drizin , Anurupa Shrestha , Kathleen H. Mortell , Philip R. Kym , Michael E. Kort , Arthur Gomtsyan
IPC分类号： A61K31/44 , A61K31/35 , A61K31/47 , A61K31/17 , C07D215/46 , C07D498/02 , C07D311/68 , A61K45/06 , C07D311/96 , C07D311/04 , C07C275/30 , A61K31/192 , C07D311/70 , A61K31/353 , C07D491/052 , A61K31/436 , C07D215/42 , C07C275/32
CPC分类号： C07D311/04 , A61K31/17 , A61K31/192 , A61K31/353 , A61K31/436 , A61K31/47 , A61K45/06 , C07C275/30 , C07C275/32 , C07D215/42 , C07D215/46 , C07D311/68 , C07D311/70 , C07D311/96 , C07D491/052
摘要： Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, Rz, A, m, n, p, q, s, and positions a and b are as 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，其中X1，L，Rx，Ry，Rz，A，m，n，p，q，s和位置a和b如本说明书中所定义。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。

6. 发明授权

US08058474B2 Urea derivative and process for preparing the same 有权
标题翻译：尿素衍生物及其制备方法
公开(公告)号：US08058474B2
公开(公告)日：2011-11-15
申请号：US12400562
申请日：2009-03-09
申请人： Toshihiko Naito
发明人： Toshihiko Naito
IPC分类号： C07C275/32 , C07C271/58
CPC分类号： C07D215/233 , C07C275/34
摘要： A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R1 has the same definition as above, with a compound (B) represented by the following formula: wherein R2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.
摘要翻译：一种制备由下式表示的化合物（C）的方法：其中R1表示氢，C1-6烷基或C3-8环烷基，R2表示氢或甲氧基，其特征在于使由下式：其中R 1具有与上述相同的定义，与下式表示的化合物（B）：其中R2具有与上述相同的定义，L表示离去基团。化合物（C）对于预防或治疗与血管生成瘤形成有关的各种疾病是有效的。

7. 发明申请

US20110071178A1 Methods and Compounds for Modulating Cannabinoid Activity 审中-公开
标题翻译：用于调节大麻素活性的方法和化合物
公开(公告)号：US20110071178A1
公开(公告)日：2011-03-24
申请号：US12761987
申请日：2010-04-16
申请人： Alexandros Makriyannis , Spyridon P. Nikas , Shakiru O. Alapafuja , Vidyanand G. Shukla
发明人： Alexandros Makriyannis , Spyridon P. Nikas , Shakiru O. Alapafuja , Vidyanand G. Shukla
IPC分类号： A61K31/438 , C07C309/68 , A61K31/255 , C07C49/175 , A61K31/12 , C07C271/12 , A61K31/222 , C07C69/96 , A61K31/265 , C07D211/60 , A61K31/445 , C07D497/10 , C07D213/56 , A61K31/4402 , C07C275/32 , A61K31/17 , C07D271/06 , A61K31/4245 , C07D275/06 , A61K31/428 , C07D263/34 , A61K31/421 , A61P3/00 , A61P35/00 , A61P15/08 , A61P25/00 , A61P29/00 , G01N33/53
CPC分类号： C07C271/28 , A61K31/00 , C07C37/055 , C07C37/62 , C07C45/41 , C07C45/44 , C07C45/45 , C07C45/673 , C07C45/68 , C07C49/255 , C07C49/84 , C07C271/38 , C07C309/82 , C07C323/43 , C07C2603/74 , C07D211/16 , C07D213/61 , C07D271/10 , C07D275/03 , C07D275/06 , C07D317/54 , C07F9/5442 , C07C47/277 , C07C47/575 , C07C49/233 , C07C49/83 , C07C39/24 , C07C39/11
摘要： Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
摘要翻译：公开了抑制单酰基甘油脂肪酶（MGL）和脂肪酸酰胺水解酶（FAAH）的作用的化合物和组合物，抑制MGL和FAAH的方法，调节大麻素受体的方法以及治疗与大麻素受体调节有关的各种疾病的方法。

8. 发明授权

US07087752B2 Alkylated urea and triaminotriazine compounds and phase change inks containing same 有权
标题翻译：烷基化脲和三氨基三嗪化合物和含有它们的相变油墨
公开(公告)号：US07087752B2
公开(公告)日：2006-08-08
申请号：US10810370
申请日：2004-03-26
申请人： Marcel P. Breton , Danielle C. Boils-Boissier , Jule W. Thomas, Jr. , Donald R. Titterington , H. Bruce Goodbrand , Jeffrey H. Banning , James D. Wuest , Dominic Laliberte , Marie-Eve Perron
发明人： Marcel P. Breton , Danielle C. Boils-Boissier , Jule W. Thomas, Jr. , Donald R. Titterington , H. Bruce Goodbrand , Jeffrey H. Banning , James D. Wuest , Dominic Laliberte , Marie-Eve Perron
IPC分类号： C07D251/46 , C07D251/52 , C07D251/70 , C09D11/00 , C07C275/32
CPC分类号： C07D251/70 , C07C275/34 , C09D11/34
摘要： Compounds of the formulae wherein Z is OR1, SR1, or NR1R2, Y is OR3, SR3, or NR3R4, at least one of R1, R2, R3, R4, R5, and R6 is hydrogen, at least one of R1, R2, R3, R4, R5, and R6 is other than hydrogen, at least one Z or Y within the compound is NR1R2 or —NR3R4, R1, R2, R3, R4, R5, R6, and R7 each, independently of the others, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R7 can also be (vi) an alkoxy, aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or wherein X is a direct bond, oxygen, sulfur, NR40— wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or CR50R60— wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R6 can also be
摘要翻译：其中Z为OR 1，SR 1或NR 1 R 2的下式化合物，其中Y为OR R 3，R 3，或NR 3 R 4，R 1，R 3， R 2，R 3，R 3，R 4，R 5和R 6， / SUB>是氢，R 1，R 2，R 3，R 4， R 5和R 6不是氢，化合物中至少一个Z或Y是NR 1 R 2，或者-NR 3 R 4，R 1，R 2，R 3， R 3，R 4，R 5，R 6和R 7各自独立地选自其中R 7也可以是（vi）烷氧基，芳氧基，芳基烷氧基，烷芳基氧基，聚亚烷基氧基，聚亚芳基氧基，聚芳基亚烷基氧基，聚烷基亚芳基氧基，甲硅烷基，硅氧烷，聚亚硅烷基，聚硅氧烷，或其中X是直接键，氧，硫，NR 40 - 其中R 40是氢，烷基，芳基，芳烷基或烷基芳基，或其中R 50是氢，各自独立地为氢，烷基，芳基，芳基烷基或烷基芳基，并且其中R 6也可以是

9. 发明授权

US06924275B2 Aminophenol derivatives and their use in cosmetics 失效
标题翻译：氨基酚衍生物及其在化妆品中的应用
公开(公告)号：US06924275B2
公开(公告)日：2005-08-02
申请号：US10125411
申请日：2002-04-19
申请人： Michel Philippe , Remy Tuloup , Christian Blaise
发明人： Michel Philippe , Remy Tuloup , Christian Blaise
IPC分类号： A61K8/30 , A61K8/00 , A61K8/41 , A61K8/42 , A61K8/46 , A61K31/045 , A61K31/135 , A61K31/17 , A61K31/175 , A61K31/21 , A61K31/27 , A61K31/325 , A61Q5/08 , A61Q19/02 , C07C271/06 , C07C271/28 , C07C275/32 , C07C275/34 , C07J9/00 , A61K31/56
CPC分类号： C07C271/28 , A61K8/415 , A61Q5/08 , A61Q19/02
摘要： Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2,wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical;R1 is a radical of formula (a), (b) or (c) below:(a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C4 hydrocarbon radical,R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, andR5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical,in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process for depigmenting and/or bleaching the skin, body hairs and/or head hairs.
摘要翻译：至少一种式（I）氨基苯酚衍生物的用途如下：其中：R表示氢原子或基团-COR 2，其中R 2表示饱和或不饱和的，直链的，环状的或支链的，任选羟基化的C 1至C 30烃或烷氧基; R 1是下式（a），（b）或（c）的基团：（a）-CO-NR 3 R 4 （b）-CO-OR 5（c）-SO 2 -R 5其中R 3表示氢原子或直链或支链，饱和或不饱和的，任选羟基化的C 1至C 4烃基，R 4代表氢原子或饱和或不饱和的，直链，环状或支链的，任选羟基化的C 1至C 30烃基，R 5表示饱和或不饱和的，直链的，环状的或支链的，任选羟基化的C 1至C 30烃基，在用于人皮肤的脱色和/或漂白化妆品组合物中，身体毛发或头发; 包含式（I）的衍生物的组合物和用于脱皮和/或漂白皮肤，身体毛发和/或头发的方法。

10. 发明申请

US20040249210A1 Alkylated urea and triaminotriazine compounds and phase change inks containing same 有权
标题翻译：烷基化脲和三氨基三嗪化合物和含有它们的相变油墨
公开(公告)号：US20040249210A1
公开(公告)日：2004-12-09
申请号：US10810370
申请日：2004-03-26
申请人： Xerox Corporation
发明人： Marcel P. Breton , Danielle C. Boils-Boissier , Jule W. Thomas JR. , Donald R. Titterington , H. Bruce Goodbrand , Jeffrey H. Banning , James D. Wuest , Dominic Laliberte , Marie-Eve Perron
IPC分类号： C07C275/32
CPC分类号： C07D251/70 , C07C275/34 , C09D11/34
摘要： Compounds of the formulae 1 2 wherein Z is nullOR1, nullSR1, or nullNR1R2, Y is nullOR3, nullSR3, or nullNR3R4, at least one of R1, R2, R3, R4, R5, and R6 is hydrogen, at least one of R1, R2, R3, R4, R5, and R6 is other than hydrogen, at least one Z or Y within the compound is nullNR1R2 or nullNR3R4, R1, R2, R3, R4, R5, R6, and R7 each, independently of the others, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R7 can also be alkoxy, aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or 3 wherein X is a direct bond, oxygen, sulfur, nullNR40null wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or nullCR50R60null wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R6 can also be 4
摘要翻译：下式化合物其中Z为-OR1，-SR1或-NR1R2，Y为-OR3，-SR3或-NR3R4，R 1，R 2，R 3，R 4，R 5和R 6中的至少一个为至少 R1，R2，R3，R4，R5和R6中的一个不是氢，化合物中至少一个Z或Y是-NR1R2或-NR3R4，R1，R2，R3，R4，R5，R6和R7各自其中R 7也可以是烷氧基，芳氧基，芳烷氧基，烷芳基氧基，聚亚烷基氧基，聚亚芳基氧基，聚芳基亚烷基氧基，聚烷基亚芳基氧基，甲硅烷基，硅氧烷，聚亚芳基，聚硅氧烷，或其中 X是直接键，氧，硫，-NR 40 - ，其中R 40是氢，烷基，芳基，芳基烷基或烷基芳基，或-CR 50 R 60 - 其中R 50和R 60各自独立地是氢，烷基，芳基，，或烷基芳基，并且其中R6也可以是

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