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1. 发明授权

US4908385A .alpha.-halogenated dicarboxylic acids, pharmaceutical compositions and method of use 失效
标题翻译： α-卤代二羧酸，药物组合物和使用方法
公开(公告)号：US4908385A
公开(公告)日：1990-03-13
申请号：US106557
申请日：1987-10-06
申请人： Jacob Bar-Tana , Yoelit Migron , Jochanan Blum , Bruno Dreckmann , Johannes Pill
发明人： Jacob Bar-Tana , Yoelit Migron , Jochanan Blum , Bruno Dreckmann , Johannes Pill
IPC分类号： C07C69/63 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/22 , A61K31/225 , A61K31/23 , A61P3/06 , A61P3/08 , A61P9/10 , C07C51/00 , C07C51/363 , C07C55/02 , C07C55/21 , C07C55/32 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/05
CPC分类号： C07C55/02 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/225 , A61K31/23 , C07C55/21 , C07C55/32
摘要： The present invention provides pharmaceutical compositions containing at least one .alpha.-halogenated dicarboxylic acid of the general formula: ##STR1## wherein Hal is a chlorine, bromine or fluorine atom, R is a hydrogen atom or Hal and m is a number of from 4 to 16, and/or at least one pharmacologically acceptable salt, ester or amide thereof.The present invention also provides new compounds of general formula (I) but in which m is a number of from 8 to 16 and processes for the preparation thereof.

2. 发明授权

US4711896A .alpha., .omega.-dicarboxylic acids and medicaments which contain these compounds 失效
标题翻译： α，ω-二羧酸和含有这些化合物的药物
公开(公告)号：US4711896A
公开(公告)日：1987-12-08
申请号：US840563
申请日：1986-02-21
申请人： Jacob Bar-Tana , Ernst-Christian Witte , Bernd Hagenbruch , Johannes Pill , Karlheinz Stegmeier
发明人： Jacob Bar-Tana , Ernst-Christian Witte , Bernd Hagenbruch , Johannes Pill , Karlheinz Stegmeier
IPC分类号： C07C55/02 , A61K31/19 , A61P3/06 , A61P3/08 , C07C51/00 , C07C55/28 , C07C55/32 , C07C57/13 , C07C57/30 , C07C57/34 , C07C57/38 , C07C57/42 , C07C57/52 , C07C59/245 , C07C59/305 , C07C59/84 , C07C67/00 , C07C121/48 , C07C121/50
CPC分类号： C07C57/42 , C07C55/28 , C07C55/32 , C07C57/13 , C07C57/34 , C07C57/38 , C07C59/245 , C07C59/305 , C07C59/84
摘要： ##STR1## α, ω-dicarboxylic acids having the general formula (I') in which: R
1 and R
2 , which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C
3 -C
7 -cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R
1 and R
2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R
1 and R
2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.
摘要翻译： PCT No.PCT / EP85 / 00288 Sec。 371日期1986年2月21日 102（e）日期1986年2月21日PCT归档1985年6月15日PCT公布。公开号WO86 / 00298 日本1月16日，1986年1月16日，具有通式（I'）的α，ω-二羧酸，其中：R1和R2可以不同或相同，表示可被羟基，低级烷氧基，卤素或苯基取代的低级烷基，苯基能够被羟基，低级烷氧基，低级烷基或卤素取代一次或几次; 低级烯基或炔基; 可以被羟基，卤素，低级烷基或低级烷氧基取代的C 3 -C 7 - 环烷基或苯基，X和Y可以不同或相同，表示氢，低级烷基，低级烷氧基，羟基，氰基，卤素，羧基，低级烷氧基羰基或氨基甲酰基，Q表示具有8-14个C原子的非分支，饱和或不饱和的烷基链，其可被取代，被杂原子间隔并形成环系的一部分，如以及它们的体内羧酸衍生物，条件是当Q表示具有8-14个C原子的未饱和的饱和烷基链时，R 1和R 2表示甲基且Y表示氢，X可以不表示氢，乙氧羰基，溴，氰基或甲基，并且如果R 1和R 2表示甲基且X和Y氢，则Q可以不表示任何式（II）基团。其制备方法和含有这些化合物的药物，其具有抗糖尿病作用并降低脂质水平。

3. 发明授权

US4689344A Long-chain .alpha.,.omega.-dicarboxylic acids and derivatives thereof and pharmaceutical compositions containing them 失效
标题翻译：长链α，ω-二羧酸及其衍生物和含有它们的药物组合物
公开(公告)号：US4689344A
公开(公告)日：1987-08-25
申请号：US623673
申请日：1984-06-22
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： A61K31/20 , A61K31/16 , A61K31/225 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , C07C51/00 , C07C55/02 , C07C55/32 , C07C67/00 , C07C69/34 , C07C231/00 , C07C233/04 , C07C233/05 , C07C253/00 , C07C255/22 , A61K31/275
CPC分类号： C07C255/00 , C07C55/02 , C07C55/32
摘要： A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof,whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or hetercyclyl radical;X and Y each independently represents hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteratom chain members optionally forming part of a ring structure.

4. 发明授权

US4634795A Long-chain .alpha.,.omega.-di-carboxylic acids and derivatives thereof and pharmaceutical compositions containing them 失效
标题翻译：长链α，ω-二羧酸及其衍生物和含有它们的药物组合物
公开(公告)号：US4634795A
公开(公告)日：1987-01-06
申请号：US769765
申请日：1985-08-27
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： A61K31/20 , A61K31/16 , A61K31/225 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , C07C51/00 , C07C55/02 , C07C55/32 , C07C67/00 , C07C69/34 , C07C231/00 , C07C233/04 , C07C233/05 , C07C253/00 , C07C255/22 , C07C121/20
CPC分类号： C07C255/00 , C07C55/02 , C07C55/32
摘要： A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism. The active compounds have the general formula ##STR1## or in-vivo hydrolysable functional derivatives of the carboxylic groups thereof, whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or heterocyclyl radical;X and Y each independently represent hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteroatom chain members optionally forming part of a ring structure.The invention also provides pharmaceutical compositions comprising the aforementioned compounds of formula (I) for the treatment of obesity, hyperlipidemia and maturity-onset diabetes.
摘要翻译：已经发现一类新的化合物在体内阻断胆固醇和中性脂质合成而不会不利地影响能量代谢。活性化合物具有通式（I）或其羧基的体内可水解的官能衍生物，其中R1和R2各自独立地表示未取代或取代的烃基或杂环基; X和Y各自独立地表示氢，任选取代的低级烷基，卤素，氰基，羧基，低级烷氧基羰基或氨基甲酰基; 并且Q表示由8至14个碳原子的直链形成的双基，其中一个或多个可被杂原子替代，所述链任选被惰性取代基取代，并且一个或多个所述碳或杂原子链构件任选地形成部分的环结构。本发明还提供了包含上述式（I）化合物用于治疗肥胖症，高脂血症和成熟发作型糖尿病的药物组合物。

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