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公开(公告)号：US5807864A
公开(公告)日：1998-09-15
申请号：US807164
申请日：1997-02-27
IPC分类号： A61K31/00 , A61K31/505 , A61P9/00 , A61P9/10 , C07D239/22 , C07D239/56
CPC分类号： C07D239/22
摘要： This invention relates to the use of 2-thioxotetrahydropyrimidin-4-one derivatives to increase HDL cholesterol concentration and as therapeutic compositions for treating atherosclerotic conditions such as dyslipoproteinemias and coronary heart disease. The compounds of this invention are represented by the formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkynyl; and R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, halogen or lower alkyl.
摘要翻译： 本发明涉及2-硫代四氢嘧啶-4-酮衍生物用于增加HDL胆固醇浓度和用作治疗动脉粥样硬化病症如脂蛋白血症和冠心病的治疗组合物。 本发明的化合物由下式表示：其中：R为C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; 并且R 1，R 2和R 3独立地为氢，卤素或低级烷基。
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公开(公告)号：US5684030A
公开(公告)日：1997-11-04
申请号：US482600
申请日：1995-06-07
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P43/00 , C07D235/28 , C07D235/04 , C07D235/24
CPC分类号： C07D235/28
摘要： Disclosed herein are compounds of the formula: ##STR1## where R.sub.1 is substituted phenyl in which the substituents are one or two halogens, alkyl groups, carboxyl groups or alkoxycarbonyl groups; R.sub.2 is H or alkyl; R.sub.3 and R.sub.4 are, independently, H, alkyl, halogen or nitro; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.
摘要翻译： 本文公开的是下式的化合物：其中R 1是取代的苯基，其中取代基是一个或两个卤素，烷基，羧基或烷氧基羰基; R2是H或烷基; R 3和R 4独立地为H，烷基，卤素或硝基; n为1,2或3; 或其药学上可接受的盐，其可用作平滑肌细胞增殖的抑制剂。
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13.发明授权Use of 2-thioxo-imidazolin-4-one derivatives in the treatment of atherosclerosis 失效2-硫代 - 咪唑啉-4-酮衍生物在动脉粥样硬化治疗中的应用
公开(公告)号：US5554607A
公开(公告)日：1996-09-10
申请号：US563325
申请日：1995-11-28
IPC分类号： A61K31/4166 , A61K31/4174 , A61K31/4439 , A61K31/395 , A61K31/44 , A61K31/445 , A61K31/55
CPC分类号： A61K31/4439 , A61K31/4166 , A61K31/4174 , Y10S514/824
摘要： A method for increasing the HDL cholesterol concentration in the blood of a mammal in need of increased HDL cholesterol blood concentration, which comprises administering to said mammal, orally or parenterally, a compound of formula I: ##STR1## wherein R is alkyl; a substituted or unsubstituted aromatic N, O or S heterocycle; substituted or unsubstituted aryl, arylalkyl, benzhydryl or indanyl, in which the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkyl or hydroxy; and R.sup.1 is aryl, alkyl, alkenyl, alkynyl or substituted aryl where the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkoxy or hydroxy.
摘要翻译： 一种用于增加需要增加HDL胆固醇血液浓度的哺乳动物血液中的HDL胆固醇浓度的方法，其包括向所述哺乳动物口服或肠胃外给药式I化合物：其中R为烷基; 取代或未取代的芳族N，O或S杂环; 取代或未取代的芳基，芳基烷基，二苯甲基或茚满基，其中取代基是一个至三个独立地选自烷基，烷氧基，烷硫基，烯基，炔基，卤素，全氟烷基，全氟烷基或羟基的成员; 并且R 1是芳基，烷基，烯基，炔基或取代的芳基，其中取代基是一个至三个独立地选自烷基，烷氧基，烷硫基，烯基，炔基，卤素，全氟烷基，全氟烷氧基或羟基的成员。
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公开(公告)号：US4812574A
公开(公告)日：1989-03-14
申请号：US133823
申请日：1987-12-23
IPC分类号： C07B61/00 , C07D513/04 , C07D513/14
CPC分类号： C07D513/04 , C07D513/14
摘要： The invention concerns a process for preparing a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are as defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
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15.发明授权
公开(公告)号：US4889936A
公开(公告)日：1989-12-26
申请号：US295410
申请日：1989-01-10
IPC分类号： C07B61/00 , C07D513/04 , C07D513/14
CPC分类号： C07D513/04 , C07D513/14
摘要： The invention concerns a process for preparng a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are a defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
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公开(公告)号：US4055553A
公开(公告)日：1977-10-25
申请号：US609254
申请日：1975-09-02
申请人： Sie-Yearl Chai , John P. Yardley
发明人： Sie-Yearl Chai , John P. Yardley
IPC分类号： A61K38/00 , C07K14/655 , C07C103/52 , A61K37/00
CPC分类号： C07K14/655 , A61K38/00 , Y10S514/806 , Y10S930/16
摘要： The growth hormone release inhibiting compound: ##STR1## in which R is hydroxyl, dimethylamino, alkylamino of 1-5 carbon atoms or phenethylamine, the protamine zinc, protamine aluminum and non-toxic acid addition salts thereof as well as the corresponding linear heptadecapeptide and intermediates therefore are herein described.
摘要翻译： 生长激素释放抑制化合物：其中R是羟基，二甲基氨基，1-5个碳原子的烷基氨基或苯乙胺，鱼精蛋白锌，鱼精蛋白铝及其无毒酸加成盐以及相应的线性十七肽和 因此在此描述中间体。
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