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51. 发明授权

US5561146A Modified guanidino and amidino thrombin inhibitors 失效
标题翻译：改性胍基和脒基凝血酶抑制剂
公开(公告)号：US5561146A
公开(公告)日：1996-10-01
申请号：US323336
申请日：1994-10-14
申请人： Kyoung S. Kim , Spencer D. Kimball , Jagabandhu Das , Edwin J. Iwanowicz , Wen-Ching Han
发明人： Kyoung S. Kim , Spencer D. Kimball , Jagabandhu Das , Edwin J. Iwanowicz , Wen-Ching Han
IPC分类号： C07D211/20 , A61K31/155 , A61K31/275 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K38/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D207/09 , C07D207/12 , C07D207/16 , C07D211/32 , C07D211/56 , C07D211/58 , C07D211/60 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07D211/26
CPC分类号： C07D401/12 , C07D207/09 , C07D211/60 , C07K5/0202 , C07K5/0205 , C07K5/0222 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06095 , C07K5/06104 , C07K5/06156 , C07K5/0806 , A61K38/00
摘要： Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.
摘要翻译：提供了具有下式的凝血酶抑制剂：其中Z是含有远端和近端结合位点残基的凝血酶抑制剂亚结构; 并且R 1是氰基，羟基，烷氧基，氨基，氨基烷基或硝基。

52. 发明授权

US4774239A Benzazepine derivatives 失效
公开(公告)号：US4774239A
公开(公告)日：1988-09-27
申请号：US89479
申请日：1987-08-26
申请人： Jagabandhu Das
发明人： Jagabandhu Das
IPC分类号： A61K31/55 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , C07D223/16 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14
CPC分类号： C07D223/16
摘要： A new class of benzazepine derivatives having the general formula ##STR1## including pharmaceutically acceptable salts, are disclosed. These compounds are useful as cardiovascular agents, particularly as vasodilators.

53. 发明授权

US4670453A 7-oxabicycloheptane substituted amido-carbamoyl prostaglandin analogs useful in the treatment of thrombotic disease 失效
标题翻译：可用于治疗血栓性疾病的7-氧杂双环庚烷取代的酰氨基 - 氨基甲酰基前列腺素类似物
公开(公告)号：US4670453A
公开(公告)日：1987-06-02
申请号：US860973
申请日：1986-05-08
申请人： Jagabandhu Das
发明人： Jagabandhu Das
IPC分类号： C07D493/08 , A61K31/34 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted amidocarbamoyl prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R.sup.1 is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; p is 1 to 4; X is O or S; R.sup.2 is H or lower alkyl; and R.sup.3 is lower alkyl, lower alkenyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译：提供7-氧杂双环庚烷取代的酰氨基甲酰基前列腺素类似物，其结构式为：其中m为0至4; A是-CH = CH-或-CH 2 -CH 2 - ; n为1至5; R1是CO 2 H，CO 2烷基，CO 2碱金属，CO 2多羟基胺盐，其中R 4和R 5相同或不同，是H，低级烷基，羟基，低级烷氧基或芳基，R 4和R 5中的至少一个不同于羟基，低级烷氧基 p为1〜4; X是O或S; R2是H或低级烷基; 并且R 3是低级烷基，低级烯基，芳基，芳基烷基，环烷基或环烷基烷基。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

54. 发明授权

US4654364A Hydroxamic acids of 7-oxabicycloheptane substituted ethers 失效
标题翻译： 7-氧杂二环庚烷取代醚的羟肟酸
公开(公告)号：US4654364A
公开(公告)日：1987-03-31
申请号：US797300
申请日：1985-11-12
申请人： Ravi K. Varma , Jagabandhu Das
发明人： Ravi K. Varma , Jagabandhu Das
IPC分类号： C07D493/08 , C07D493/18 , A61K31/34
CPC分类号： C07D493/08
摘要： Hydroxamic acids of 7-oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein Y is O or ##STR2## and including all stereoisomers thereof. The compounds are inhibitors of .DELTA..sup.5 -lipoxygenase and inhibitors of prostaglandin and leukotriene biosynthesis and as such are useful, for example, as anti-allergy and antiinflammatory agents and also as antipsoriatic agents.
摘要翻译：提供7-氧杂双环庚烷取代的醚前列腺素类似物的羟氨基酸，其结构式为：其中Y为O或者包含其所有立体异构体。这些化合物是DELTA5-脂肪氧合酶的抑制剂和前列腺素和白三烯生物合成的抑制剂，因此可用作例如抗过敏和抗炎剂，也可用作抗牛皮癣药。

55. 发明授权

US4536513A 7-Oxabicycloheptane substituted prostaglandin interphenylene analogs useful in the treatment of thrombolytic disease 失效
标题翻译：可用于治疗溶栓性疾病的7-氧杂双环庚烷取代的前列腺素亚氨基类似物
公开(公告)号：US4536513A
公开(公告)日：1985-08-20
申请号：US589384
申请日：1984-03-14
申请人： Jagabandhu Das , Martin F. Haslanger
发明人： Jagabandhu Das , Martin F. Haslanger
IPC分类号： A61K31/34 , A61P3/00 , A61P7/02 , A61P9/08 , A61P11/08 , A61P25/04 , A61P29/00 , C07D493/08 , C07D493/18 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted interphenylene prostaglandin ethers are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供具有结构式“IMAGE”并包括其所有立体异构体的7-氧杂双环庚烷取代的亚氨基苯基前列腺素醚。该化合物是可用于例如治疗溶栓性疾病的心血管药。

56. 发明授权

US4522949A 7-Oxabicycloheptane substituted prostaglandin interphenylene analogs useful as cardiovascular agents 失效
标题翻译：可用作心血管药物的7-氧杂双环庚烷取代的前列腺素亚磺酰类似物
公开(公告)号：US4522949A
公开(公告)日：1985-06-11
申请号：US543681
申请日：1983-10-20
申请人： Jagabandhu Das , Martin F. Haslanger
发明人： Jagabandhu Das , Martin F. Haslanger
IPC分类号： A61K31/34 , A61K31/557 , A61P7/02 , A61P11/00 , A61P43/00 , C07D493/08 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted interphenylene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供具有结构式“IMAGE”并包括其所有立体异构体的7-氧杂双环庚烷取代的亚氨基苯基前列腺素类似物。该化合物是可用于例如治疗溶栓性疾病的心血管药。

57. 发明授权

US4521539A Tetrahydrofuranyl substituted ethers 失效
标题翻译：四氢呋喃基取代的醚
公开(公告)号：US4521539A
公开(公告)日：1985-06-04
申请号：US609054
申请日：1984-05-10
申请人： Jagabandhu Das
发明人： Jagabandhu Das
IPC分类号： A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07C35/38 , C07C51/367 , C07C62/32 , C07D307/12 , C07D307/16 , C07D307/24 , C07D307/87 , C07D309/12 , C07D317/24 , C07D319/08 , C07D333/24 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/14 , C07F7/18
CPC分类号： C07D307/87 , C07C35/38 , C07C51/367 , C07C62/32 , C07D307/12 , C07D307/16 , C07D309/12 , C07D317/24 , C07D319/08 , C07D333/24 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/14 , C07F7/1856
摘要： Tetrahydrofuranyl substituted ethers are provided having the structural formula ##STR1## wherein A is (CH.sub.2).sub.2, CH.dbd.CH or a single bond, m is 1 to 5, B is a single bond or CH.dbd.CH, n is 1 to 4, X is O or ##STR2## wherein n' is 0, 1 or 2, R is H, lower alkyl or alkali metal and R.sup.1 is lower alkyl, arylalkyl, aryl, cycloalkyl, cycloalkylalkyl or lower alkenyl and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease and as antiinflammatory agents and analgesics.
摘要翻译：提供四氢呋喃基取代的醚，其结构式为：其中A为（CH 2）2，CH = CH或单键，m为1至5，B为单键或CH = CH，n为1至4， X是O或，其中n'是0,1或2，R是H，低级烷基或碱金属，R 1是低级烷基，芳基烷基，芳基，环烷基，环烷基烷基或低级烯基并且包括其所有的立体异构体。这些化合物是可用于例如治疗溶栓性疾病和作为抗炎剂和止痛剂的心血管药。

58. 发明授权

US4515972A Intermediates and method for producing intermediates useful in the preparation of 7-oxabicycloheptane prostaglandin derivatives 失效
标题翻译：用于制备可用于制备7-氧杂双环庚烷前列腺素衍生物的中间体的中间体和方法
公开(公告)号：US4515972A
公开(公告)日：1985-05-07
申请号：US543564
申请日：1983-10-19
申请人： Jagabandhu Das , Martin F. Haslanger
发明人： Jagabandhu Das , Martin F. Haslanger
IPC分类号： C07D321/00 , C07D493/08 , C07D493/18 , C07D307/77
CPC分类号： C07D493/08
摘要： A method is provided for preparing intermediates for use in preparing 7-oxabicycloheptane prostaglandin derivatives which method includes the steps of reducing (exo)hexa hydro-4,5-epoxyisobenzofuran-1,3-dione to the corresponding diol, subjecting the diol to a chloroformylation reaction to form a compound of the structure ##STR1## reacting the above with pyridine to form the cyclic carbonate reacting the cyclic carbonate with an alkanol to form the alcohol of the strucure ##STR2## tosylating the above alcohol to form the tosylate and subjecting the above tosylate to a cyanation reaction to form the cyano carbonate of the structure ##STR3## The cyano carbonate may then be reduced by, for example, reaction with diisobutyl aluminum hydride to form the hemiacetal ##STR4## which is used in preparing 7-oxabicycloheptane prostaglandin derivatives as disclosed in U.S. Pat. No. 4,143,054.New intermediates of the structures set out above, other than the hemiacetal, are also provided.
摘要翻译：提供了一种用于制备用于制备7-氧杂双环庚烷前列腺素衍生物的中间体的方法，该方法包括将六氢-4,5-环氧异苯并呋喃-1,3-二酮还原（外）至相应的二醇，使二醇进行形成结构的化合物，使上述物质与吡啶反应形成环状碳酸酯，使环状碳酸酯与链烷醇反应形成结构式的醇，以使上述醇甲酰化以形成甲苯磺酸酯，并使甲苯磺酸酯化至氰化反应以形成结构的氰基碳酸酯。然后可以通过例如与二异丁基氢化铝反应来还原氰基碳酸酯以形成用于制备7-氧杂双环庚烷前列腺素的半缩醛衍生物，如美国专利No. 第4,143,054号。还提供了除了半缩醛之外的上述结构的新中间体。

59. 发明授权

US4474972A 7-Oxabicycloheptane prostaglandin intermediates and method for preparing same 失效
标题翻译： 7-氧杂双环庚烷前列腺素中间体及其制备方法
公开(公告)号：US4474972A
公开(公告)日：1984-10-02
申请号：US474761
申请日：1983-03-14
申请人： Jagabandhu Das , Martin F. Haslanger
发明人： Jagabandhu Das , Martin F. Haslanger
IPC分类号： C07D493/08 , C07D493/18 , C07D307/00
CPC分类号： C07D493/08
摘要： Optically active 7-oxabicycloheptane prostaglandin intermediates are provided having the general structure ##STR1## wherein one of R.sup.1 and R.sup.2 is --COOH, ##STR2## or --CH.sub.2 OH and the other is ##STR3## A method for preparing the above intermediates is also provided.
摘要翻译：提供了具有通用结构“IMAGE”的光学活性的7-氧杂双环庚烷前列腺素中间体，其中R1和R2之一是-COOH，图像或-CH2OH，另一种是制备上述中间体的方法。

60. 发明授权

US09216972B2 Tricyclic heterocyclic compounds 有权
标题翻译：三环杂环化合物
公开(公告)号：US09216972B2
公开(公告)日：2015-12-22
申请号：US13504541
申请日：2010-10-29
申请人： T. G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das , Robert J. Cherney
发明人： T. G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das , Robert J. Cherney
IPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
CPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
摘要： Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其立体异构体或其盐，其中：X1，X2，X3，W，Q1，Q2和G2在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

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