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71. 发明公开

EP1380562A4 CARBOXYLIC ACID DERIVATIVE AND SALT THEREOF 审中-公开
标题翻译：羧酸衍生物及其盐
公开(公告)号：EP1380562A4
公开(公告)日：2006-03-08
申请号：EP02720489
申请日：2002-04-18
申请人： EISAI CO LTD
发明人： MATSUURA FUMIYOSHI , EMORI EITA , SHINODA MASANOBU , CLARK RICHARD , KASAI SHUNJI , YOSHITOMI HIDEKI , YAMAZAKI KAZUTO , INOUE TAKASHI , MIYASHITA SADAKAZU , HIHARA TARO , HARADA HITOSHI , OHASHI KAYA
IPC分类号： C07C59/64 , A61P1/00 , A61P1/04 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P19/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/02 , C07C59/58 , C07C59/68 , C07C59/72 , C07C233/25 , C07C235/24 , C07C251/48 , C07C251/52 , C07C251/54 , C07C255/37 , C07C255/54 , C07C259/10 , C07C271/14 , C07C271/16 , C07C271/22 , C07C271/28 , C07C271/58 , C07C309/73 , C07C309/75 , C07C311/19 , C07C317/18 , C07C317/22 , C07C323/20 , C07D209/08 , C07D209/18 , C07D209/24 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D215/14 , C07D215/18 , C07D215/26 , C07D235/06 , C07D235/12 , C07D277/56 , C07D295/096 , C07D295/192 , C07D307/79 , C07D317/54 , C07D413/12 , C07D417/12
CPC分类号： C07D413/12 , C07C59/58 , C07C59/68 , C07C59/72 , C07C233/25 , C07C235/24 , C07C251/48 , C07C251/52 , C07C251/54 , C07C255/37 , C07C255/54 , C07C259/10 , C07C271/14 , C07C271/16 , C07C271/22 , C07C271/28 , C07C271/58 , C07C309/73 , C07C309/75 , C07C311/19 , C07C317/18 , C07C317/22 , C07C323/20 , C07D209/08 , C07D209/18 , C07D209/24 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D215/14 , C07D215/18 , C07D215/26 , C07D235/06 , C07D235/12 , C07D277/56 , C07D295/096 , C07D295/192 , C07D307/79 , C07D317/54 , C07D417/12
摘要： A medicine containing as the active ingredient a novel carboxylic acid derivative useful as an insulin resistance ameliorant. The carboxylic acid derivative is represented by the following general formula (I). Also provided are a salt or ester of the derivative and a hydrate of either. (I) In the formula, R1 represents carboxyl, alkyl, alkoxy, etc.; L and T each represents a single bond, alkylene, alkynylene, etc.; M represents alkylene, etc.; W represents carboxyl; X represents oxygen, -NRX1CQ1O-, -OCQ1NRX1-, -CQ1NRX1O- (wherein Q1 represents oxygen, etc. and RX1 represents hydrogen, alkyl, etc.), etc.; and Y and Z each represents an optionally substituted 5- to 14-membered aromatic group, etc.

72. 发明授权

EP1169298B1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药剂师VERBINDUNGEN
公开(公告)号：EP1169298B1
公开(公告)日：2006-01-04
申请号：EP00926870.7
申请日：2000-04-11
申请人： NICOX S.A.
发明人： DEL SOLDATO, Piero
IPC分类号： C07C219/06 , C07C219/22 , C07C219/24 , C07D219/10 , C07D233/64 , C07D277/06 , C07D277/14 , C07D309/30 , C07D401/12 , C07D405/14 , C07D417/06 , C07D473/18 , C07D495/04 , C07D499/68 , C07F9/38 , C07H15/252 , C07K5/02 , A61K31/21
CPC分类号： C07H15/252 , C07C219/06 , C07C219/22 , C07C219/24 , C07C271/28 , C07C2601/14 , C07F9/3873 , C07K5/0222
摘要： Compounds or their salts having general formulas (I) and (II) wherein: s = is an integer equal to 1 or 2, preferably s = 2; b0 = 0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
摘要翻译：具有通式（I）和（II）的化合物或其盐，其中：s =等于1或2，优选s = 2的整数; b0 = 0或1; A是药物的基团，并且是为了满足说明书中报道的药理学试验，C和C 1是两个二价基团。基团B和B 1的前体是满足说明书中报道的药理学试验。

73. 发明授权

EP1379516B1 ALKOXYCARBONYLAMINO BENZOIC ACID OR ALKOXYCARBONYLAMINO TETRAZOLYL PHENYL DERIVATIVES AS IP ANTAGONISTS 有权
标题翻译：作为IP拮抗剂的烷氧基羰基氨基苯甲酸或烷氧基羰基氨基酰氨基四唑基苯基衍生物
公开(公告)号：EP1379516B1
公开(公告)日：2005-11-16
申请号：EP02722127.4
申请日：2002-02-25
申请人： F. HOFFMANN-LA ROCHE AG
发明人： LOPEZ-TAPIA, Francisco, Javier , NITZAN, Dov , O'YANG, Counde
IPC分类号： C07D307/80 , C07D409/12 , C07D405/12 , C07D409/04 , C07D405/04 , C07C271/28 , C07D239/26 , A61K31/34 , A61K31/38 , A61K31/395 , A61K31/41 , A61P9/00 , A61P11/06 , A61P13/02 , A61P29/00
CPC分类号： C07D405/04 , C07C271/28 , C07D307/80 , C07D405/12 , C07D409/04 , C07D409/12

74. 发明公开

EP1575495A2 COMPOUNDS AND METHODS 审中-公开
标题翻译： VERBINDUNGEN UND VERFAHREN
公开(公告)号：EP1575495A2
公开(公告)日：2005-09-21
申请号：EP03745638.1
申请日：2003-03-26
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： THOMPSON, Scott, K. , FRAZEE, James, S. , KALLANDER, Lara, S. , MA, Chun , MARINO, Joseph, P. , NEEB, Michael, J. , BHAT, Ajita , MCATEE, John, Jeffrey , STAVENGER, Robert, A.
IPC分类号： A61K6/00
CPC分类号： C07C311/29 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/36 , C07C219/22 , C07C229/34 , C07C233/25 , C07C271/28 , C07C275/34 , C07C291/02 , C07C309/73 , C07C311/08 , C07C311/09 , C07C311/21 , C07C323/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D211/34 , C07D211/60 , C07D213/38 , C07D213/64 , C07D213/74 , C07D231/14 , C07D233/64 , C07D239/42 , C07D249/08 , C07D257/04 , C07D295/096 , C07D295/125 , C07D295/185 , C07D307/66 , C07D307/68 , C07D317/58 , C07D317/68 , C07D319/18 , C07D333/20
摘要： Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
摘要翻译：公开了具有下式的化合物：其药学上可接受的盐或溶剂合物和含有该化合物的药物组合物，其中结构变量如本文所定义。本发明的化合物，盐和溶剂化物可用作LXR激动剂。

75. 发明公开

EP1503981A2 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：取代的四环素
公开(公告)号：EP1503981A2
公开(公告)日：2005-02-09
申请号：EP03714236.1
申请日：2003-03-18
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi , FRECHETTE, Roger , ABATO, Paul , ASSEFA, Haregewein , BANDARAGE, Upul , BERNIAC, Joel , BHATIA, Beena , CHEN, Jackson , ISMAIL, Mohamed, Y. , KIM, Oak, A. , MATHEWS, Jude , HONEYMAN, Laura , NIHLAWI, Mohammed , PEARSON, Andre , REDDY, Laxma , SHEAHAN, Paul , SIZENSKY, Emmanuelle , TOURIGNY, Justin , VISKI, Peter , WARCHOL, Tadeusz , AMOO, Victor , MECHICHE, Rachid , VERMA, Atul K.
IPC分类号： C07C237/26 , C07C43/00 , C07C49/00
CPC分类号： C07D307/52 , C07C237/26 , C07C239/18 , C07C251/08 , C07C251/48 , C07C255/25 , C07C255/43 , C07C255/58 , C07C255/59 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07C2603/46 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/68 , C07D317/54 , C07D401/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

76. 发明授权

EP1138678B1 Process for making N-((4-phenyl) methylphenyl) piperazines 有权
标题翻译：哌嗪（（4-苯基）甲基苯基） - 制备N-过程
公开(公告)号：EP1138678B1
公开(公告)日：2004-12-22
申请号：EP01115281.6
申请日：1998-10-30
申请人： Daiichi Suntory Pharma Co., Ltd.
发明人： Annoura, Hirokazu , Nakanishi, Kyoko , Tamura, Shigeki
IPC分类号： C07D295/073
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55

77. 发明公开

EP1051397A4 METHOD FOR PREPARING AN N- (ALIPHATIC OR AROMATIC)CARBONYL]-2-AMINOACETAMIDE COMPOUND AND A CYCLYZED COMPOUND 有权
标题翻译：制造方法N - [（ALIPHATHISCH或芳族）羰基] -2-氨基乙酰胺连接和环状化合物
公开(公告)号：EP1051397A4
公开(公告)日：2004-09-29
申请号：EP99904421
申请日：1999-01-29
申请人： AVENTIS PHARM PROD INC
发明人： HULME CHRISTOPHER , MORTON GEORGE C , SALVINO JOSEPH M , LABAUDINIERE RICHARD F , MASON HELEN J , MORRISSETTE MATTHEW M , MA LIANG , CHERRIER MARIE-PIERRE
IPC分类号： C07D243/14 , C07B61/00 , C07C231/14 , C07C237/22 , C07C269/04 , C07C269/06 , C07C271/22 , C07C271/28 , C07D207/14 , C07D207/26 , C07D207/273 , C07D233/28 , C07D233/54 , C07D233/64 , C07D233/90 , C07D241/08 , C07D241/18 , C07D241/36 , C07D241/44 , C07D243/24 , C07D295/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D521/00 , C07F9/645 , C07D205/00 , C07D205/08 , C07D207/00 , C07D207/12 , C07D231/00 , C07D233/22 , C07D241/04 , C07D243/12 , C07D401/00
CPC分类号： C07D207/273 , C07C231/14 , C07C269/06 , C07C2601/02 , C07C2601/16 , C07D231/12 , C07D233/28 , C07D233/56 , C07D233/64 , C07D241/18 , C07D241/44 , C07D243/24 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07F9/645 , C40B40/00 , Y02P20/55 , C07C237/22 , C07C271/28
摘要： The present invention relates to a method for preparing an N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound of formula (I) wherein Ra is (II); Raa is hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rb is hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rca and Rcb are independently hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rd is (III); and Rda is optionally substituted aliphatic or optionally substituted aromatic; and Raa is substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Rb, Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rb is substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Raa, Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rca and Rcb are independently substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Raa, Rb, Rca, Rcb or Rda where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rda is substituted with a primary or secondary protected amine that upon deprotection can react with at least one of Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring, provided that when Raa is substituted with a primary or secondary protected amine that upon deprotection can react with Rb at least substituted with an activated carboxylic acid, then Raa is other than substituted aliphatic, comprising reacting the following four compounds: a carbonyl compound of formula (IV), an amine compound of formula NH2Rb, an isonitrile compound of formula NCRda, and an acid compound of formula RaCO2H, to produce the N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound, and the N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound. The invention is also directed to a method for cyclizing N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound to a cyclic compound selected from the group consisting of a 1,4-benzodiazepine-2,5-dione derivative, diketopiperazine derivative, ketopiperazine derivative, lactam derivative, 1,4-benzodiazapine derivative and dihydroquinoxalinones derivative, and the cyclized compound.
摘要翻译：本发明涉及一种用于N个制备 - [（脂肪族或芳香族）羰基]式（I）-2-氨基乙酰胺化合物worin R a是（II）; RAA是氢，任选取代的脂或任选取代的芳族的; R b是氢，任选取代的脂或任选取代的芳族的; RCA和RCB是unabhängig氢，任选substituiertem脂肪族或芳香族OPTIONALLY substituiertem; R d是（III）; 和RDA任选substituiertem脂肪族或芳香族OPTIONALLY substituiertem; 和拉加与伯或仲保护的胺取代的并在去保护后能够与* AB或*分贝碳反应，或R b，RCA或RCB，其中每个是至少substituiertem与活化的羧酸，以形成一个5中的至少一个 -7元环; 或R b与伯或仲保护的胺取代的在去保护并可以通过* AB或*分贝碳反应，或拉加，RCA或RCB，其中每个是至少substituiertem与活化的羧酸，以形成一个5中的至少一个 -7元环; 或RCA和RCB是unabhängigsubstituiertem与伯或仲保护的胺并在去保护后能够与* AB或*分贝碳反应，或拉加，RB，RCA，RCB或RDA中的至少一个，其中每个是至少substituiertem与活化的羧酸形成5-7元环; 或RDA是用伯或仲胺保护基取代并在去保护后能够与RCA或RCB中的至少一个，其中每个是至少substituiertem与活化的羧酸，以形成5-7元环状环反应，提供并当拉加是与伯或仲胺保护时substituiertem脱保护确实可以与RB反应至少substituiertem与活化的羧酸，然后拉加比substituiertem脂肪族其他方法，包括将下列四种化合物：式的羰基化合物（IV）为胺式NH2Rb的化合物，以异腈式NCRda的化合物，并在式RaCO2H的酸化合物，以产生N - [（脂肪族或芳香族）羰基] -2-氨基乙酰胺化合物，以及N - [（脂肪族或芳香族）羰基 ] -2-氨基乙酰胺化合物。因此，本发明涉及用于环化N A方法 - [（脂肪族或芳香族）羰基] -2-氨基乙酰胺化合物由1,4-苯并二氮杂-2,5-二酮衍生物，二酮哌嗪从组中选择的环式化合物衍生物，ketopiperazine衍生物，内酰胺衍生物，1,4-苯二氮衍生物和dihydroquinoxalinones衍生物，环化化合物。

78. 发明授权

EP1320521B1 2-THIOCARBAMOYLOXY AND 2-CARBAMOYLOXY DERIVATIVES OF CYCLOPENTYL-HEPTAN(EN)OIC ACID AS THERAPEUTIC AGENTS 有权
标题翻译： 2-巯基乙酰氧基 - 二羧酸衍生物环戊二烯酸（EN）SLEAL ALS THERAPEUTISCHE MITTEL
公开(公告)号：EP1320521B1
公开(公告)日：2004-07-21
申请号：EP01964329.5
申请日：2001-08-22
申请人： Allergan, Inc.
发明人： BURK, Robert, M.
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C271/28 , A61K31/5575 , C07B2200/07 , C07C271/12 , C07C271/14 , C07C333/04 , C07C2601/08
摘要： The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-thiocarbamoyloxy and carbamoyloxy as therapeutic agents e.g. as ocular hypotensives. The compounds used in accordance with the invention are represented by formula (I) wherein a wavy segments indicate either the alpha (α) or beta (β) configuration; the dashed bond represents a double bond or a single bond; Z is O or S; Ar is selected from the group consisting of aryl or heteroaryl radicals having from 4 to 10 carbon atoms and substituted derivatives of said aryl and heteroaryl radicals; n is 0 or an integer of from 1 to 4; x and y are 1 or 0, provided that when x is 1, y is 0 and when x is 0, y is 1; R1 is hydrogen or a lower alkyl radical or a substituted lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of -OR1 and -N(R1)2; Y is =O or represents 2 hydrogen radicals, and the 9 and/or 11 esters thereof and/or the pharmaceutically acceptable salts of said compounds and/or esters.
摘要翻译：本发明涉及环戊烷庚烷（烯）酸，2-硫代氨基甲酰氧基和氨基甲酰氧基作为治疗剂的用途。作为眼睛的视力。根据本发明使用的化合物由下式I表示：其中波状区段表示α（α）或β（β）构型; 虚键表示双键或单键; Ar选自具有4至10个碳原子的芳基或杂芳基和所述芳基和杂芳基的取代衍生物; n为0或1〜4的整数; x和y为1或0，条件是当x为1时，y为0，当x为0时，y为1; R1是氢或低级烷基或具有至多6个碳原子的取代的低级烷基; X选自-OR1和-N（R1）2; Y为= O或表示2个氢原子，以及其9和/或11个酯和/或所述化合物和/或酯的药学上可接受的盐。

79. 发明公开

EP1191019A4 INTERMEDIATES FOR THE SYNTHESIS OF BENZIMIDAZOLE COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译：合成苯并咪唑和方法中间体用于生产
公开(公告)号：EP1191019A4
公开(公告)日：2004-06-02
申请号：EP00940856
申请日：2000-06-27
申请人： SANKYO CO
发明人： KISHI NAOYUKI , NAKAMURA YOSHITAKA , ABE NARUMI , TAKEBAYASHI TOYONORI
IPC分类号： C07C211/50 , A61K31/427 , A61P3/10 , C07C209/62 , C07C211/52 , C07C217/82 , C07C217/84 , C07C269/06 , C07C271/28 , C07D235/02 , C07D277/00 , C07D277/34 , C07D417/12
CPC分类号： C07C271/28 , C07D277/34 , C07D417/12 , Y02P20/55
摘要： Problem: To provide intermediates for the synthesis of benzimidazole compounds having an excellent antihyperglycemic activity or salts thereof and a process for the preparation thereof. Means for solutions: A process for the preparation of benzimidazole compounds (I), characterized by condensing an amine derivative (III) with a carboxylic acid derivative (II) to form a compound (IV) and subjecting the compound (IV) to ring closure in the presence of an acid (wherein R1 is C1-C6alkyl, C1-C6alkoxy, or the like; R2 is C1-C6alkyl; and R3 is hydrogen or a protective group).

80. 发明授权

EP0919545B1 Benzyloxy substituted aromatics and their use as fungicides 有权
标题翻译：苄氧基取代物芳香化合物及其配制物Anwendung als Fungizide
公开(公告)号：EP0919545B1
公开(公告)日：2004-05-26
申请号：EP98309234.7
申请日：1998-11-11
申请人： Dow AgroSciences LLC
发明人： Ross, Ronald , Fujimoto, Ted Tsutomo , Szapacs, Edward Michael , Shaber, Steven Howard
IPC分类号： C07C271/28 , C07D213/50 , C07D239/26 , C07D333/22 , A01N47/24
CPC分类号： C07D239/26 , A01N47/24 , C07C271/28 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/50 , C07D333/22

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