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公开(公告)号:US06599914B2
公开(公告)日:2003-07-29
申请号:US09841506
申请日:2001-04-24
IPC分类号: A61K3148
CPC分类号: A61K31/473 , Y10S514/853 , Y10S514/854 , Y10S514/887
摘要: Methods of inhibiting the generation of pro-inflammatory cytokines such as IL-4 and IL-13 in a human patient in need of such inhibiting are disclosed.
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公开(公告)号:US06358967B1
公开(公告)日:2002-03-19
申请号:US09743869
申请日:2001-04-19
申请人: Ralf Wyrwa , Albert Haertl , Erika Glusa , Susanne Grabley , Ralf Thiericke
发明人: Ralf Wyrwa , Albert Haertl , Erika Glusa , Susanne Grabley , Ralf Thiericke
IPC分类号: A61K3148
CPC分类号: C07F15/025 , C07D457/02 , C07F17/02
摘要: The invention relates to novel derivatives of ergoline of the general formula 1 in which R1 together with the two adjacent N atoms is the residue of a diamine and R4 together with the two adjacent carbonyl groups is the residue of a dicarboxylic acid. R2, R3, R6, R7, R8 can be H or an organic radical. R7 and R8 are H or together are a bond. The compounds show a strong antihypertensive effect. These effects moreover occur after intravenous and enteral administration even at dosages in the region of a few &mgr;g/kg (body weight). The compounds can accordingly be used as pharmaceuticals for hypertensive diseases in human medicine.
摘要翻译: 本发明涉及通用1的麦角灵素的新衍生物,其中R1与两个相邻的N原子一起是二胺的残基,R4与两个相邻的羰基一起是二羧酸的残基。 R2,R3,R6,R7,R8可以是H或有机基团。 R7和R8是H或一起是一个键。化合物显示出强烈的抗高血压作用。 即使在几公斤/公斤(体重)的剂量下,静脉内和肠内给药也会发生这些影响。 因此,这些化合物可以用作人类医学中的高血压疾病的药物。
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公开(公告)号:US06800635B2
公开(公告)日:2004-10-05
申请号:US10698664
申请日:2003-10-31
IPC分类号: A61K3148
CPC分类号: C07D457/06
摘要: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from s solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline forms I and II in a solvent at a temperature below 30° C.
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4.
公开(公告)号:US06355666B1
公开(公告)日:2002-03-12
申请号:US09602688
申请日:2000-06-23
申请人: Ching-San Lai , Tingmin Wang
发明人: Ching-San Lai , Tingmin Wang
IPC分类号: A61K3148
CPC分类号: A61K47/555 , A61K47/54
摘要: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
摘要翻译: 根据本发明,提供了非甾体抗炎药的正常修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂,其提供NSAIDs的治疗益处,同时引起副作用的发生率低得多,然后通常用这些药剂观察到。
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公开(公告)号:US06680327B2
公开(公告)日:2004-01-20
申请号:US10221165
申请日:2002-09-18
IPC分类号: A61K3148
CPC分类号: C07D457/06 , A61K31/4745
摘要: Crystalline form VII of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise a slurry procedure using form I or mixture of forms I and VII of cabergoline in a solvent at a temperature above 30° C.
摘要翻译: 公开了卡麦角林的结晶形式VII,含有它的药物组合物及其制备方法。 该方法可以包括在高于30℃的温度下在溶剂中使用形式I或卡麦角林的形式I和VII的混合物的浆料方法。
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公开(公告)号:US06673806B2
公开(公告)日:2004-01-06
申请号:US10239562
申请日:2003-01-16
IPC分类号: A61K3148
CPC分类号: C07D457/06
摘要: Crystalline form II of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise crystallization from a solution of raw cabergoline in an organic solvent at low temperatures or submitting to a slurry procedure a mixture of cabergoline Forms I and II in a solvent at a temperature below about 30° C.
摘要翻译: 公开了卡麦角林的结晶形式II,含有它的药物组合物及其制备方法。 该方法可以包括在低温下从原料卡麦角林在有机溶剂中的溶液结晶,或者在低于约30℃的温度下在溶剂中将卡麦角林I型和II型混合物悬浮在浆液程序中。
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公开(公告)号:US06429223B1
公开(公告)日:2002-08-06
申请号:US09715767
申请日:2000-11-17
申请人: Ching-San Lai , Tingmin Wang
发明人: Ching-San Lai , Tingmin Wang
IPC分类号: A61K3148
CPC分类号: A61K47/555 , A61K47/54 , A61K47/545
摘要: In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
摘要翻译: 根据本发明,提供非甾体抗炎药(NSAID)的修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂,其提供NSAIDs的治疗益处,同时引起副作用的发生率低得多,然后通常用这些药剂观察到。
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8.
公开(公告)号:US06362166B1
公开(公告)日:2002-03-26
申请号:US09689717
申请日:2000-10-13
申请人: Stephen E. Webber , Peter S. Dragovich , Thomas J. Prins , Siegfried H. Reich , Thomas L. Little, Jr. , Ethel S. Littlefield , Joseph T. Marakovits , Robert E. Babine , Ted M. Bleckman
发明人: Stephen E. Webber , Peter S. Dragovich , Thomas J. Prins , Siegfried H. Reich , Thomas L. Little, Jr. , Ethel S. Littlefield , Joseph T. Marakovits , Robert E. Babine , Ted M. Bleckman
IPC分类号: A61K3148
CPC分类号: C07K5/06139 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06052
摘要: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
摘要翻译: 通过化学合成获得的微小RNA病毒3C蛋白酶抑制剂抑制或阻断小核糖核酸病毒3C蛋白酶的生物学活性。 这些化合物以及含有这些化合物的药物组合物适用于治疗感染了一种或多种微小核糖核酸病毒的患者或宿主。 可以使用几种新的方法和中间体来制备本发明的新型微核糖核酸病毒3C蛋白酶抑制剂。
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