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公开(公告)号：US5900426A
公开(公告)日：1999-05-04
申请号：US624746
申请日：1996-03-27
IPC分类号： C07D277/64 , A61K31/415
CPC分类号： C07D277/64
摘要： Benzothiazole derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component possess a lipid lowering activity and are useful pharmaceuticals for the treatment of hyperlipemia. The lipid lowering agents are of the formula: ##STR1## wherein R.sub.1 is halogen, trifluoromethyl, acetamido or --OX.sub.1 ; X.sub.1 is hydrogen, alkyl or acyl; R.sub.2 is hydrogen, halogen, alkyl, hydroxyalkyl, trifluoromethyl, nitro, amino which may be substituted with alkyl or acyl, carboxy which may be esterified with alkyl, or --OX.sub.2 ; X.sub.2 is hydrogen, alkyl, acyl, carboxyalkyl which may be esterified with alkyl; n is an integer from 1 to 3 denoting the number of substituents R.sub.2 ; and plural R.sub.2 may be the same or different when n is 2 or 3; with the proviso that R.sub.1 is a group other than halogen when R.sub.2 is hydrogen. The benzothiazole derivatives and their pharmaceutically acceptable salts significantly decrease cholesterol, triglyceride and low-density lipoprotein in blood.
摘要翻译： 苯并噻唑衍生物，其药学上可接受的盐和含有所述化合物作为有效成分的治疗剂具有降脂活性，并且是用于治疗高脂血症的有用药物。 降脂剂具有下式：其中R1是卤素，三氟甲基，乙酰氨基或-OX1; X1是氢，烷基或酰基; R 2是氢，卤素，烷基，羟基烷基，三氟甲基，硝基，可被烷基或酰基取代的氨基，可以被烷基或-OX 2酯化的羧基; X 2是可以被烷基酯化的氢，烷基，酰基，羧基烷基; n是1至3的整数，表示取代基R2的数目; 当n为2或3时，多个R2可以相同或不同; 条件是当R 2为氢时，R 1为卤素以外的基团。 苯并噻唑衍生物及其药学上可接受的盐显着降低血液中的胆固醇，甘油三酯和低密度脂蛋白。
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公开(公告)号：US5658918A
公开(公告)日：1997-08-19
申请号：US409054
申请日：1995-03-23
申请人： Kaoru Okamoto , Taisuke Hasegawa , Akio Namimatsu
发明人： Kaoru Okamoto , Taisuke Hasegawa , Akio Namimatsu
IPC分类号： A61K31/52 , A61K31/522 , A61P11/02 , A61P27/16 , C07D473/28
CPC分类号： C07D473/28
摘要： The present invention provides purine derivatives and pharmaceutically acceptable salts thereof which exhibit an inhibitory action towards nasal mucus secretion and are useful as pharmaceuticals for treatment of nasal secretion and rhinitis. The purine derivatives are represented by the following general formula: ##STR1## wherein R is alkyl or cycloalkyl, or optionally-substituted phenyl or phenylalkyl; R' is hydrogen or --COOX; and X is alkyl, alkenyl, alkoxyalkyl, phenyl or phenylalkyl. The compounds are useful as therapeutic and preventive agents for various types of rhinitis accompanied by acceleration of nasal mucus secretion and by the sneezing reflex such as allergic rhinitis. The compounds may be administered orally and exhibit low toxicity, little side effect and high safety. Accordingly, continuous long term administration of the pharmaceutical compositions may be performed for highly effective treatment of rhinitis.
摘要翻译： 本发明提供嘌呤衍生物及其药学上可接受的盐，其对鼻粘液分泌具有抑制作用，并且可用作治疗鼻分泌和鼻炎的药物。 嘌呤衍生物由以下通式表示：其中R是烷基或环烷基或任选取代的苯基或苯基烷基; R'是氢或-COOX; X是烷基，烯基，烷氧基烷基，苯基或苯基烷基。 这些化合物可用作各种类型的鼻炎的治疗和预防剂，伴随着加速鼻粘液分泌和喷鼻反射如过敏性鼻炎。 化合物可以口服给药，毒性低，副作用小，安全性高。 因此，可以进行药物组合物的连续长期给药以高效治疗鼻炎。
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公开(公告)号：US20120123127A1
公开(公告)日：2012-05-17
申请号：US13383441
申请日：2010-07-26
IPC分类号： C07D409/08
CPC分类号： C07D409/04
摘要： Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
摘要翻译： 公开了可用作抗组胺剂等的有效成分的噻哆烷 - 丙酸衍生物的制造方法。 根据本发明的制造方法，可以制备噻吩并薁类骨架的2位用丙酸取代的噻吩并薁 - 丙酸衍生物。 由此合成的硫代苯并薁丙酸衍生物对组胺H1受体和低脑内转移具有优异的拮抗作用，因此可用作药物组合物如抗组胺剂的活性成分。
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公开(公告)号：US08536342B2
公开(公告)日：2013-09-17
申请号：US13383441
申请日：2010-07-26
IPC分类号： C07C409/00 , A61K31/445
CPC分类号： C07D409/04
摘要： Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
摘要翻译： 公开了可用作抗组胺剂等的有效成分的噻哆烷 - 丙酸衍生物的制造方法。 根据本发明的制造方法，可以制备噻吩并薁类骨架的2位用丙酸取代的噻吩并薁 - 丙酸衍生物。 由此合成的硫代苯并薁丙酸衍生物对组胺H1受体和低脑内转移具有优异的拮抗作用，因此可用作药物组合物如抗组胺剂的活性成分。
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公开(公告)号：US20100004459A1
公开(公告)日：2010-01-07
申请号：US12448050
申请日：2007-12-12
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D401/10 , C07D413/10
摘要： The present invention is to provide the compounds useful as a treating or preventing agent for gout and hyperuricemia which are 2-phenylnicotinic acid derivatives having a uric acid lowering action due to an excellent xanthine oxidase inhibitory action. Since the 2-phenylnicotinic acid derivatives of the present invention exhibit a uric acid lowering action due to an excellent xanthine oxidase inhibitory action and also hypolipemic action, their utility is very high as a treating or preventive agent for gout and hyperuricemia which are often accompanied by hyperlipemia as a complication.
摘要翻译： 本发明提供可用作痛风和高尿酸血症的治疗或预防剂的化合物，其是由于优异的黄嘌呤氧化酶抑制作用而具有尿酸降低作用的2-苯基烟酸衍生物。 由于本发明的2-苯基烟酸衍生物由于优异的黄嘌呤氧化酶抑制作用和降血脂作用而显示出尿酸降低作用，因此其作为痛风和高尿酸血症的治疗或预防剂的效用非常高，通常伴随着 高脂血症为并发症。
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公开(公告)号：US5776942A
公开(公告)日：1998-07-07
申请号：US490297
申请日：1995-06-14
IPC分类号： C07D471/04 , C07D239/00 , A61K31/505
CPC分类号： C07D471/04
摘要： A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido�2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action. It can be used as a therapy not only for allergic asthma but also for various bronchial asthmas such as endogenous asthma, exogenous asthma and dust asthma.
摘要翻译： 具有支气管扩张作用的哮喘的快速作用补救剂包含至少一种由通式（A）表示的吡啶并[2,3-d]嘧啶衍生物或其药学上可接受的盐或金属络合物作为有效成分：
A）其中R1和R2相同或不同，R1和R2各自为氢，烷基或苄基; R3是氢，羟基，二烷基氨基亚甲基氨基或-NH-X; X是氢，烷基，烯基，羟基，氨基，羟基烷基，苄基或酰基; R4是氢，烷基，卤素，硝基，氨基，羟基，苄氧基，氰基，羧基，烷氧基羰基，烷氧基磺酰基，氨基磺酰基，二烷基氨基磺酰基或磺基; R5是氢，烷基或氨基。 由于支气管扩张作用优异，支气管哮喘的快速作用补救能够缓解哮喘发作时呼吸急促的症状。 它不仅可用作过敏性哮喘，还可用于各种支气管哮喘，如内源性哮喘，外源性哮喘和灰尘哮喘。
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