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    • 22. 发明申请
      WO1993016055A1 HYPOLIPIDAEMIC BENZOTHIAZEPINE COMPOUNDS 审中-公开
    • HYPOLIPIDAEMIC BENZOTHIAZEPINE COMPOUNDS
    • HYPOLIPIDAEMIC BENZOTHIAZEPINE化合物
    • WO1993016055A1
    • 1993-08-19
    • PCT/GB1993000328
    • 1993-02-16
    • THE WELLCOME FOUNDATION LIMITED , BRIEADDY, Lawrence, Edward
    • THE WELLCOME FOUNDATION LIMITED
    • C07D281/10
    • C07D281/10
    • The present invention is concerned with compounds of formula (I) wherein 1 is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected from halogen, nitro, phenylalkoxy, C1-4 alkoxy, C1-6 alkyl and -O(CH2)pSO3R" wherein p is an integer of from 1 to 4 and R" is hydrogen or C1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R is a C1-6 straight alkyl group; and R is a C2-6 straight alkyl group; and their salts, solvates and physiologically functional derivatives, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidaemic conditions, such as atherosclerosis.
    • 本发明涉及式（I）化合物，其中1为0-4的整数; m为0〜5的整数; n为0〜2的整数。 R和R'是独立地选自卤素，硝基，苯基烷氧基，C 1-4烷氧基，C 1-6烷基和-O（CH 2）p SO 3 R“的原子或基团，其中p是1至4的整数，R”是氢或 C 1-6烷基，其中所述苯基烷氧基，烷氧基和烷基任选被一个或多个卤素原子取代; R 4是C 1-6直链烷基; R 5为C 2-6直链烷基; 以及它们的盐，溶剂合物和生理功能衍生物，其制备方法和新的中间体，含有它们的药物组合物及其在药物中的用途，特别是用于预防和治疗高脂血症病症如动脉粥样硬化。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 23. 发明申请
      WO1993013055A1 AMIDINO DERIVATIVES AND THEIR USE AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
    • AMIDINO DERIVATIVES AND THEIR USE AS NITRIC OXIDE SYNTHASE INHIBITORS
    • 氨基衍生物及其作为氮氧化物合成酶抑制剂的用途
    • WO1993013055A1
    • 1993-07-08
    • PCT/GB1992002387
    • 1992-12-23
    • THE WELLCOME FOUNDATION LIMITED , BEAMS, Richard, Mansfield , HODSON, Harold, Francis , PALMER, Richard, Michael, John
    • THE WELLCOME FOUNDATION LIMITED
    • C07C257/14
    • C07C323/58 , A61K31/195 , C07C257/14 , C07C2601/02
    • Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C1-3alkyl groups; a group of formula -(CH2)pX(CH2)q- where p is 2 or 3, q is 1 or 2 and X is S(O)x where x is 0, 1 or 2, O or NR where R is H or C1-6alkyl; or a group of formula -(CH2)rA(CH2)s- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C1-6alkyl, C1-6alkoxy, hydroxy, halo, nitro, cyano, trifluoroC1-6alkyl, amino, C1-6alkylamino or diC1-6alkylamino; and pharmaceutical formulations containing them are described for use in medicine, novel compounds of formula (I) and the preparation of such novel compounds are also disclosed.
    • 式（I）的脒基衍生物及其盐及其药学上可接受的酯和酰胺，其中：R 1是C 1-6直链或支链烷基，C 2-6烯基，C 2-6炔基， C 3-6环烷基或C 3-6环烷基C 1-6烷基; Q是具有3至6个碳原子的亚烷基，亚烯基或亚炔基，其可以任选地被一个或多个C 1-3烷基取代; 式（ - ） - （CH2）pX（CH2）q-，其中p为2或3，q为1或2，X为S（O）x，其中x为0,1或2，O或NR 2， R 2是H或C 1-6烷基; 或式 - （CH 2）r A（CH 2）s - 的基团，其中r为0,1或2，s为0,1或2，A为可任选被一个取代基的3至6元碳环或杂环 或更合适的取代基如C 1-6烷基，C 1-6烷氧基，羟基，卤素，硝基，氰基，三氟C 1-6烷基，氨基，C 1-6烷基氨基或二C 1-6烷基氨基; 和含有它们的药物制剂被描述用于药物，还公开了新的式（I）化合物和这些新化合物的制备。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 29. 发明申请
      WO1992006075A1 ANTI-ATHEROSCLEROTIC ARYL COMPOUNDS 审中-公开
    • ANTI-ATHEROSCLEROTIC ARYL COMPOUNDS
    • 抗甲状腺素ARYL化合物
    • WO1992006075A1
    • 1992-04-16
    • PCT/GB1991001646
    • 1991-09-25
    • THE WELLCOME FOUNDATION LIMITED , FRANZMANN, Karl, Witold
    • THE WELLCOME FOUNDATION LIMITED
    • C07C275/34
    • C07D333/28 , C07C45/71 , C07C47/575 , C07C217/58 , C07C275/30 , C07C275/34 , C07D317/22 , Y10S514/824
    • The present invention is concerned with compounds of formula (I) wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, -NRR where R and R are independently selected from hydrogen, C1-8 alkyl and C1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C1-8 thioalkyl, said alkyl, alkoxy and/or thioalkyl group(s) being optionally substituted by one or more halogen atoms, aryl, aryloxy, aralkyl and aralkyloxy, said aryl, aryloxy, aralkyl and/or aralkyloxy group(s) being optionally substituted by one or more atoms or groups independently selected from halogen, alkyl, alkoxy, alkanoyl, hydroxyalkyl, perfluoroalkyl, perfluoroalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, and C3-8 polyether groups containing from one to three oxygen atoms; D is -CH2-, -NH-, or -O-; E is ( alpha ) or ( beta ); F is -O- or ( psi ); G is C3-12 straight, branched, or cyclic alkyl, or aralkyl, said aralkyl group being optionally substituted by one or more atoms or groups independently selected from halogen, amino, N-(C1-6 alkyl)amino, N,N-di(C1-6 alkyl)amino, C1-6 alkyl and C1-6 alkoxy, or a C3-8 polyether group containing one to three oxygen atoms; J is a bond or C1-6 straight or branched alkylene; X is a C2-8 straight, branched, or cyclic alkylene group optionally substituted by one or more halogen atoms or C1-4 alkoxy groups, wherein one or two of the linear carbon atom(s) is/are replaced by oxygen; and Z is hydrogen, hydroxy, C1-4 alkyl, C2-5 alkanoyl, or carboxyl, said alkyl group being optionally substituted by one or more halogen atoms; and their physiologically functional derivatives, with processes for their preparation, with medicaments containing them and with their use as therapeutic agents, particularly in the prophylaxis and treatment of atherosclerosis.
    • 本发明涉及式（I）化合物，其中Ar是任选含有一个或两个独立地选自氮，氧和硫的杂原子的单环或双环芳基，所述基团任选被一个或多个独立地被一个或多个原子或基团取代 选自卤素，硝基，氨基，-NRR 1，其中R和R 1独立地选自氢，C 1-8烷基和C 1-8烷酰基，氰基，羧基烷氧基，烷氧基羰基烷氧基，C 1-8烷基（包括环烷基和 环烷基烷基），C 1-8烷氧基（包括环烷氧基和环烷基烷氧基），C1-8硫代烷基，所述烷基，烷氧基和/或硫代烷基任选被一个或多个卤素原子，芳基，芳氧基，芳烷基和芳烷氧基取代，所述 芳基，芳氧基，芳烷基和/或芳烷氧基任选被一个或多个独立地选自卤素，烷基，烷氧基，烷酰基，羟烷基，全氟烷基，全氟烷氧基，羧烷氧基，烷氧基 芳基烷氧基和含1-3个氧原子的C3-8聚醚基团; D是-CH 2 - ， - NH-或-O-; E为（α）或（β）; F为-O-或（psi）; G为C3-12直链，支链或环状烷基或芳烷基，所述芳烷基任选被一个或多个独立选自卤素，氨基，N-（C 1-6烷基）氨基，N， 二（C 1-6烷基）氨基，C 1-6烷基和C 1-6烷氧基，或含有1-3个氧原子的C 3-8聚醚基团; J是键或C1-6直链或支链亚烷基; X是任选被一个或多个卤素原子或C 1-4烷氧基取代的C 2-8直链，支链或环状亚烷基，其中一个或两个直链碳原子被氧代替; Z为氢，羟基，C 1-4烷基，C 2-5烷酰基或羧基，所述烷基任选被一个或多个卤素原子取代; 及其生理功能衍生物，其制备方法，含有它们的药物和用作治疗剂，特别是用于预防和治疗动脉粥样硬化。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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