公开(公告)号：US20160347725A1

公开(公告)日：2016-12-01

申请号：US15116764

申请日：2015-02-04

Applicant: Bialal Abou ALEIWI ,  UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

Inventor： Charles Ryan Yates ,  Duane D. Miller ,  Frank Park ,  Jordan J. Toutounchian ,  Vanessa Moraies-Tirado ,  Shivaputra Patil ,  Jayaprakash Pagadala ,  Bial Abou Aleiwi

IPC: C07D265/18 ,  C07D211/84 ,  C07D265/12

CPC classification number: C07D265/18 ,  A61K9/0048 ,  A61K9/1075 ,  A61K47/14 ,  C07D211/84 ,  C07D215/36 ,  C07D221/10 ,  C07D239/82 ,  C07D265/12 ,  C07D498/04

Abstract: This disclosure relates to small molecule inhibitors of paxillin and paxillin binding, and related compositions and methods of treatment.

Abstract translation: 本公开涉及桩蛋白和桩蛋白结合的小分子抑制剂，以及相关组合物和治疗方法。

公开(公告)号：US09376387B2

公开(公告)日：2016-06-28

申请号：US14763222

申请日：2014-01-24

Applicant: INSA (INSTITUT NATIONAL DES SCIENCES APPLIQUEES) DE ROUEN ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITE DE ROUEN ,  VFP THERAPIES

Inventor： Francis Marsais ,  Vincent Levacher ,  Cyril Papamicael ,  Pierre Bohn ,  Ludovic Peauger ,  Vincent Gembus ,  Nicolas Le Fur ,  Marie-Laurence Dumartin-Lepine

IPC: C07D211/84 ,  C07D213/61 ,  C07D401/06 ,  C07D405/06 ,  C07D213/50 ,  C07D213/56 ,  C07D213/80 ,  C07D213/803 ,  C07D213/71 ,  C07D213/70 ,  C07D213/57 ,  C07D213/82 ,  C07D213/85 ,  C07D211/82 ,  C07D211/90

CPC classification number: C07D213/50 ,  C07D211/82 ,  C07D211/84 ,  C07D211/90 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/70 ,  C07D213/71 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82 ,  C07D213/85 ,  C07D401/06 ,  C07D405/06

Abstract: A compound of formula (I) in which the dotted lines indicate the presence of at least one double bond; n=0 to 4; R3 and R4 are H, or when n=1, R3 and R4 can also form together a double bond between the carbon atoms, and m=0, 1 or 2, Z is CH or N or Z is C and —CHR3— is ═CH— linked by the double bond to cyclopentanone; or −(−)m- is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N heteroaryl; R8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR′, CN, COR, CF3, SOR, SO2R, SONRR′, SO2NRR′, NO2, halogen, heteroaryl; and the pharmaceutical salts and stereisomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.

Abstract translation: 式（I）的化合物，其中虚线表示存在至少一个双键; n = 0〜4; R3和R4是H，或当n = 1时，R3和R4也可以一起形成碳原子之间的双键，m = 0,1或2，Z是CH或N或Z是C，-CHR 3 - 是 ═CH-通过双键连接到环戊酮; 或 - （ - ）m-，Z为NH，N-烷基，N-苯基，N-苄基或> N杂芳基; R8是可任意取代的烷基，芳基或杂芳基; EWG表示选自COOR，COSR，CONRR'，CN，COR，CF 3，SOR，SO 2 R，SONRR'，SO 2 NRR'，NO 2，卤素，杂芳基的吸电子基团; 及其药物盐和立体异构体。 式（I）化合物在治疗神经变性疾病如阿尔茨海默氏病中是有效的。

公开(公告)号：US20140213791A1

公开(公告)日：2014-07-31

申请号：US14238299

申请日：2012-08-24

Applicant: Nozomu Nakanishi ,  Yoshimasa Fukuda ,  Shigeki Kitsuda ,  Ikuya Ohno

Inventor： Nozomu Nakanishi ,  Yoshimasa Fukuda ,  Shigeki Kitsuda ,  Ikuya Ohno

IPC: A01N43/40 ,  C07D211/84

CPC classification number: A01N43/40 ,  A01N43/54 ,  A01N43/78 ,  C07D211/84 ,  C07D213/75 ,  C07D401/06 ,  C07D417/06

Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].

Abstract translation: 为了以稳定且低成本的方式提供具有2-酰基亚氨基吡啶结构并且由下式（I）表示的衍生物作为害虫防治剂所需的量，提供的方法包括以下步骤：酰化氨基 通过使用酰化剂由式（A）表示的化合物的第2位，从而制备由式（B）表示的化合物; 并进一步烷化式（B）表示的化合物的第1位的氮原子：[其中Ar表示苯基或5-至6-元杂环，R 1表示C 1-6烷基，Y表示氢 原子; 卤素原子; 羟基; 可被卤素原子取代的C1-6烷基; 可被卤素原子取代的C 1-6烷氧基; 氰基; 甲酰基; 或硝基]。

公开(公告)号：US08791147B2

公开(公告)日：2014-07-29

申请号：US13123468

申请日：2009-10-07

Applicant: Christopher Fotsch ,  Paul Harrington

Inventor： Christopher Fotsch ,  Paul Harrington

IPC: A61K31/44 ,  C07D211/72 ,  C07D211/84 ,  C07D213/62 ,  C07D213/78 ,  C07D211/70 ,  C07D211/82 ,  C07D213/24

CPC classification number: A61K31/44 ,  A61K31/437 ,  A61K31/4412

Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.

Abstract translation: 本发明一般涉及新型的拟钙化合物和包含它们的药物组合物。 本发明还涉及使用式（I）表示的化合物治疗与钙感受受体的功能有关的疾病或病症的方法。 其中Cy1是吡啶基，吡啶基，喹啉基或9-乙基-9H-咔啉基，其各自任选被取代，Cy2是苯基萘基。

公开(公告)号：US08748462B2

公开(公告)日：2014-06-10

申请号：US13119951

申请日：2009-10-13

Applicant: Sean P. Brown ,  Paul Dransfield ,  Xiaohui Du ,  Zice Fu ,  Jonathan Houze ,  XianYun Jiao ,  Sujen Lai ,  An-Rong Li ,  Jiwen Liu ,  Zhihua Ma ,  Julio C. Medina ,  Vatee Pattaropong ,  Wang Shen ,  Marc Vimolratana ,  Yingcai Wang ,  Zhongyu Wang ,  Ming Yu ,  Liusheng Zhu

Inventor： Sean P. Brown ,  Paul Dransfield ,  Xiaohui Du ,  Zice Fu ,  Jonathan Houze ,  XianYun Jiao ,  Sujen Lai ,  An-Rong Li ,  Jiwen Liu ,  Zhihua Ma ,  Julio C. Medina ,  Vatee Pattaropong ,  Wang Shen ,  Marc Vimolratana ,  Yingcai Wang ,  Zhongyu Wang ,  Ming Yu ,  Liusheng Zhu

IPC: A61K31/19 ,  C07C69/76 ,  C07D211/72 ,  C07D211/84 ,  C07D213/62 ,  A61K31/44

CPC classification number: C07C62/34 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D213/643 ,  C07D217/24 ,  C07D253/065 ,  C07D277/22 ,  C07D311/04 ,  C07D401/12

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract translation: 本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。 这些化合物具有通式IA，IB，I'A或I'B：其中本文提供变量的定义。 本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

公开(公告)号：US07785678B2

公开(公告)日：2010-08-31

申请号：US12297062

申请日：2007-03-21

Applicant: Michael Junge ,  Ursula Patwal ,  Volker Reiffenrath

Inventor： Michael Junge ,  Ursula Patwal ,  Volker Reiffenrath

IPC: C09K19/34 ,  C09K19/32 ,  C09K19/30 ,  C09K19/12 ,  C07D211/84 ,  C07D213/60 ,  C07D405/04

CPC classification number: C09K19/3444 ,  C09K19/42 ,  Y10T428/10

Abstract: The present invention relates to liquid-crystalline mixtures and to novel compounds therefor, and to the use thereof in nematic liquid-crystal displays having positive dielectric anisotropy, such as, for example, STN or IPS displays, which are characterised in that they comprise one or more compounds of the formula (I) in which R1, A1, A2, Z1, Z2, n are as defined in claim (1).

Abstract translation: 本发明涉及液晶混合物及其新型化合物及其在具有正介电各向异性的向列型液晶显示器中的用途，例如STN或IPS显示器，其特征在于它们包括一种 或更多的式（I）化合物，其中R1，A1，A2，Z1，Z2，n如权利要求（1）中所定义。

公开(公告)号：US20090318464A1

公开(公告)日：2009-12-24

申请号：US12307279

申请日：2007-07-02

Applicant: Kay Brickmann ,  Fabrizio Giordanetto ,  Johan Johansson ,  Fredrik Zetterberg

Inventor： Kay Brickmann ,  Fabrizio Giordanetto ,  Johan Johansson ,  Fredrik Zetterberg

IPC: A61K31/497 ,  C07D409/14 ,  C07D211/84 ,  A61K31/4545 ,  A61P7/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

Abstract translation: 本发明涉及式（I）的某些新的吡啶类似物，用于制备这些化合物的方法，其用作P2Y12抑制剂和抗血栓形成剂等，它们作为心血管疾病中的药物的用途以及含有它们的药物组合物。

公开(公告)号：US20080119451A1

公开(公告)日：2008-05-22

申请号：US11814340

申请日：2006-01-17

Applicant: Keith Hopkinson Gibson ,  Elaine Sophie Elizabeth Stokes ,  Michael James Waring ,  David Michael Andrews ,  Zbigniew Stanley Matusiak

Inventor： Keith Hopkinson Gibson ,  Elaine Sophie Elizabeth Stokes ,  Michael James Waring ,  David Michael Andrews ,  Zbigniew Stanley Matusiak

IPC: A61K31/496 ,  A61K31/4439 ,  C07D403/02 ,  C07D211/84 ,  C07D213/56

CPC classification number: C07D213/73 ,  C07D213/38 ,  C07D213/56 ,  C07D213/75 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12

Abstract: The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, integer m, integer n and W have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).

Abstract translation: 本发明涉及式（I）的苯甲酰胺衍生物，其中R 1a，R 1b，R 1c，R 2， R 3，R 4，整数m，整数n和W具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

公开(公告)号：US07332498B2

公开(公告)日：2008-02-19

申请号：US11284806

申请日：2005-11-23

Applicant: Pu-Ping Lu ,  David J. Morgans, Jr. ,  Bing Yao ,  Dashyant Dhanak ,  Steven David Knight

Inventor： Pu-Ping Lu ,  David J. Morgans, Jr. ,  Bing Yao ,  Dashyant Dhanak ,  Steven David Knight

IPC: A61K31/519 ,  A61K31/5025 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D211/78 ,  C07D211/82 ,  C07D211/70 ,  C07D211/90 ,  C07D211/72 ,  C07D211/84 ,  C07D213/84 ,  C07D213/72 ,  C07D213/78 ,  C07D213/46 ,  C07D213/56

CPC classification number: C07D471/04 ,  C07D475/02 ,  C07D487/04

Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.

Abstract translation: 一种在体外调节KSP驱动蛋白活性的方法，包括使KSP驱动蛋白与至少一种选自式I表示的化合物的化学实体及其药学上可接受的盐接触，其中变量如本文进一步定义。

公开(公告)号：US07196198B2

公开(公告)日：2007-03-27

申请号：US10737901

申请日：2003-12-18

Applicant: Kousuke Tani ,  Kaoru Kobayashi ,  Takayuki Maruyama

Inventor： Kousuke Tani ,  Kaoru Kobayashi ,  Takayuki Maruyama

IPC: C07D211/72 ,  C07D211/84

CPC classification number: C07D213/30 ,  C07B2200/07 ,  C07C233/55 ,  C07C235/38 ,  C07C235/84 ,  C07C255/60 ,  C07C323/62 ,  C07C2601/02 ,  C07C2603/18 ,  C07D213/75 ,  C07D213/80 ,  C07D215/06 ,  C07D215/12 ,  C07D215/14 ,  C07D263/34 ,  C07D307/68 ,  C07D333/38

Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.

Abstract translation: 包含式（I）的苯甲酸的试剂