专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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.

3. 发明授权

US06800772B2 Carboxylic acids and derivatives thereof and pharmaceutical compositions containing them 有权
标题翻译：羧酸及其衍生物和含有它们的药物组合物
公开(公告)号：US06800772B2
公开(公告)日：2004-10-05
申请号：US09881812
申请日：2001-06-18
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： C07C59235
CPC分类号： C07C69/602 , C07C55/02
摘要： The invention relates to carboxylic acids and derivatives thereof and pharmaceutical compound containing them. The active compounds are represented by the formula compound represented by formula I, wherin R1-R4 each independently represents an unsubstituted or substituted hydrocarbyl or heterocyclyl radical, Q represents a diradical consisting of a linear chain of 11 to 18 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, and where one or both of de carboxyl groups can be substituted by an in vitro hydrolyzable physiologically acceptable substituent; with the proviso that: compounds wherein R1-R4 each represents CH3 and Q represents a linear chain of 14 carbons, are excluded; and compounds wherein Q represents a linear chain of carbon atoms one of which is replaced by oxygen or sulfur, are excluded.
摘要翻译：本发明涉及羧酸及其衍生物和含有它们的药物化合物。活性化合物由式I表示的式化合物表示，R 1 -R 4各自独立地表示未取代或取代的烃基或杂环基，Q表示由11至18个碳原子的直链键组成的双基，其中一个或多个其可以被杂原子替代，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环结构的一部分，并且其中一个或两个脱羧基可被体外取代可水解的生理学上可接受的取代基; 条件是：其中R 1 -R 4各自表示CH 3且Q表示14个碳的直链的化合物; 和其中Q表示碳原子的直链链，其中一个被氧或硫取代的化合物被排除。

4. 发明申请

US20090018199A1 Methods of Administering 3, 3, 14, 14 Tetramethyl Hexadecane 1, 16 Dioic Acid 审中-公开
标题翻译：施用3,3,14,14四甲基十六烷1,16二酸的方法
公开(公告)号：US20090018199A1
公开(公告)日：2009-01-15
申请号：US10585017
申请日：2004-12-30
申请人： Jacob Bar-Tana , Ihor Bekersky
发明人： Jacob Bar-Tana , Ihor Bekersky
IPC分类号： A61K31/194 , A61P3/00
CPC分类号： A61K31/20
摘要： The present invention provides methods for lowering LDL, VLDL, total cholesterol, triglycerides, Insulin resistance and hypertension, and methods for elevating HDL in subjects in need thereof. Additionally, the present invention provides methods of administering 3,3,14,14 tetramethyl hexadecane 1,16 dioic acid for the above indications.
摘要翻译：本发明提供了降低LDL，VLDL，总胆固醇，甘油三酯，胰岛素抵抗和高血压的方法，以及用于在有需要的受试者中升高HDL的方法。此外，本发明提供了针对上述适应症施用3,3,14,14四甲基十六烷1,16二酸的方法。

5. 发明授权

US06303653B1 Carboxylic acids and derivatives thereof and pharmaceutical compositions containing them 失效
标题翻译：羧酸及其衍生物和含有它们的药物组合物
公开(公告)号：US06303653B1
公开(公告)日：2001-10-16
申请号：US09104880
申请日：1998-06-25
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： A61K31255
CPC分类号： A61K31/7076 , A61K31/00 , A61K31/192 , A61K31/20 , A61K31/201 , A61K31/202 , A61K31/69 , Y10S514/824 , Y10S514/825 , Y10S514/903
摘要： In accordance with the present invention, there are provided therapeutically effective compounds comprising an amphipathic carboxylate of the formula R—COOH, or a salt or an ester or amide of such compound, where R designates a saturated or unsaturated alkyl chain of 10-24 carbon atoms, one or more of which may be replaced by heteroatoms, where one or more of said carbon or heteroatom chain members optionally forms part of a ring, and where said chain is optionally substituted by a hydrocarbyl radical, heterocyclyl radical, lower alkoxy, hydroxyl-substituted lower alkyl, hydroxyl, carboxyl, halogen, phenyl or (hydroxy-, lower alkyl-, lower alkoxy-, lower alkenyl- or lower alkinyl)-substituted phenyl, C3-C7 cycloalkyl or (hydroxy-, lower alkyl-, lower alkoxy-, lower alkenyl- or lower alkinyl)-substituted C3-C7 cycloalkyl wherein said amphipathic carboxylate is capable of being endogenously converted to its respective coenzyme A thioester.
摘要翻译：根据本发明，提供治疗有效的化合物，其包含式R-COOH的两亲性羧酸盐或该化合物的盐或酯或酰胺，其中R表示饱和或不饱和的10-24碳的烷基链原子，其中一个或多个可以被杂原子替代，其中一个或多个所述碳或杂原子链构件任选地形成环的一部分，并且其中所述链任选被烃基取代，杂环基，低级烷氧基，羟基取代的低级烷基，羟基，羧基，卤素，苯基或（羟基 - ，低级烷基 - ，低级烷氧基 - ，低级烯基或低级炔基）取代的苯基，C3-C7环烷基或（羟基 - ，低级烷基 - ，低级烷氧基 - ，低级烯基或低级炔基） - 取代的C 3 -C 7环烷基，其中所述两亲羧酸酯能够内源转化成其各自的辅酶A硫酯。

6. 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.

7. 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。

8. 发明授权

US06284903B1 Carboxylic acids and derivatives thereof and pharmaceutical compositions containing them 有权
标题翻译：羧酸及其衍生物和含有它们的药物组合物
公开(公告)号：US06284903B1
公开(公告)日：2001-09-04
申请号：US09331895
申请日：1999-10-05
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： C07C59235
CPC分类号： C07C69/602 , C07C55/02
摘要： The present invention relates to a novel class of compounds for treating hyperlipidemia, obesity and impaired glucose tolerance/noninsulin dependent diabetes mellitus without adversely affecting energy metabolism, and pharmaceutical compositions comprising the aforementioned compounds for the treatment of obesity, hyperlipidemia and maturity-onset diabetes.
摘要翻译：本发明涉及新一类用于治疗高脂血症，肥胖症和葡萄糖耐量降低/非胰岛素依赖性糖尿病而不会不利地影响能量代谢的化合物，以及包含上述用于治疗肥胖症，高脂血症和成熟发作型糖尿病的化合物的药物组合物。

9. 发明申请

US20100240683A1 COMBINATION THERAPY, COMPOSITION AND METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
标题翻译：联合治疗，治疗心血管疾病的组合物和方法
公开(公告)号：US20100240683A1
公开(公告)日：2010-09-23
申请号：US12528678
申请日：2008-02-26
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： A61K31/505 , A61K31/20 , A61K31/366 , A61K31/265 , A61K31/47 , A61K31/405 , A61K31/40 , A61K31/4418 , A61K31/195 , A61P3/00 , A61P7/02 , A61P9/00
CPC分类号： A61K31/20 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/47 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a combination therapy for the treatment of cardiovascular disorders. More particularly, the invention relates to compositions combining long-chain optionally substituted amphipatic carboxylates (known as MEDICA drugs) and particularly, M16αα, M16ββ and M18γγ, with HMG-CoA reductase inhibitors (known as statins). The compositions of the invention may particularly be used for the treatment of cardiovascular disorders, for elevating HDL-cholesterol levels, decreasing non-HDL-cholesterol and particularly triglycerides, and decreasing insulin resistance in a subject suffering from Metabolic Syndrome or cardiovascular disorders. The invention further provides methods of treatment of such disorders using these combined compositions.
摘要翻译：本发明涉及用于治疗心血管疾病的组合疗法。更具体地，本发明涉及组合长链任选取代的两性羧酸盐（称为MEDICA药物），特别是M16αα，M16和bgr; 和M18γγ，与HMG-CoA还原酶抑制剂（称为他汀类）。本发明的组合物可特别用于治疗心血管疾病，用于升高HDL-胆固醇水平，降低非HDL-胆固醇，特别是甘油三酯，以及降低患有代谢综合征或心血管疾病的受试者的胰岛素抵抗。本发明还提供了使用这些组合组合物治疗这种病症的方法。

10. 发明申请

US20100113599A1 AMPHIPATHIC CARBOXYLATES FOR THE TREATMENT OF IMMUNE-RELATED DISORDERS 审中-公开
标题翻译：用于治疗与免疫相关的疾病的AMPHIPATHIC CARBOXYLATES
公开(公告)号：US20100113599A1
公开(公告)日：2010-05-06
申请号：US12528706
申请日：2008-02-26
申请人： Jacob Bar-Tana
发明人： Jacob Bar-Tana
IPC分类号： A61K31/194 , A61P37/02 , A61P37/00 , A61P29/00 , A61P35/00 , A61P25/28 , A61P9/00 , C07C55/20
CPC分类号： A61K31/20 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/47 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of at least one long-chain optionally-substituted amphipatic carboxylates (known as MEDICA drugs) or any salt, ester or amid thereof or any combination or mixture thereof, for the treatment and prevention of immune-related disorders, particularly, inflammatory conditions. More specifically, the invention relates to particular analogs of these MEDICA drugs, the 3,3,14,14 tetramethyl-hexadecanedioic acid (M16ββ), 4,4,15,15 tetramethyl-octadecanedioic acid (M18γγ) and 2,2,15,15-tetramethyl-hexadecanedioic acid (M16αα). The invention further provides methods, oral compositions and kits for the treatment and prevention of immune-related disorders using these MEDICA drugs. The disease is any one of multiple sclerosis, neurodegenerative disease, an atherosclerotic disease, inflammatory bowel diseases, arthritis. Wherein said atheroslerotic disease is any one of cardiovascular disease, cerebrovascular disease and peripheral vessel disease, and a malignant proliferative disorder line carcinoma, myeloma, leukemia, lymphoma, sarcoma and melanoma.
摘要翻译：本发明涉及至少一种长链任选取代的两性羧酸盐（称为MEDICA药物）或其任何盐，酯或其盐或其任何组合或混合物用于治疗和预防免疫相关疾病的用途，特别是炎性病症。更具体地，本发明涉及这些MEDICA药物的特定类似物，3,3,14,14四甲基十六烷二酸（M16＆amp; bgr），4,4,15,15-四甲基十八烷二酸（M18γγ）和2， 2,15,15-四甲基 - 十六烷二酸（M16αα）。本发明还提供了使用这些MEDICA药物治疗和预防免疫相关疾病的方法，口腔组合物和试剂盒。该疾病是多发性硬化症，神经变性疾病，动脉粥样硬化疾病，炎性肠病，关节炎中的任何一种。其中所述动脉粥样硬化性疾病是心血管疾病，脑血管疾病和外周血管疾病中的任何一种，以及恶性增殖性疾病线癌，骨髓瘤，白血病，淋巴瘤，肉瘤和黑素瘤。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式