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31. 发明授权

US07078408B2 [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists 有权
标题翻译： [1,2,4] - 三唑双环腺苷A2a受体拮抗剂
公开(公告)号：US07078408B2
公开(公告)日：2006-07-18
申请号：US10973642
申请日：2004-10-26
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： C07D487/04 , A61K31/519 , A61P25/24 , A61P25/16
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds having the structural formula Iwherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations
摘要翻译：具有结构式I的化合物，其中：n为0,1,2或3; A是C（R 1）或N; R 1和R 2是H，（C 1 -C 6 -C 6） - 烷基，卤素，CN或 -CF 3 N 3; X是-C（O） - ， - O - ， - SO 2 - 或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二基; Y是-O-，-SO 0-2 - 或任选取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有一定条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的 - 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基; 其用于治疗帕金森病，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合的组分的试剂盒

32. 发明授权

US06875772B2 [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists 有权
标题翻译： Ä1,2,4'-三唑双环腺苷A2a受体拮抗剂
公开(公告)号：US06875772B2
公开(公告)日：2005-04-05
申请号：US10304939
申请日：2002-11-26
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： A61K31/519 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：具有结构式I的化合物，其中n为0,1,2或3; A为C（R 1）或N; R 1和R 1a为H，（C 1 -C 6） - 烷基，卤代，CN或-CF 3; X是-C（O） - ， - O - ， - SO 2 2-或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二; Y是-O-，-SOO- 取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有某些条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基;它们用于治疗帕金森病，单独或与其它用于治疗帕金森病的药物组合，其包含它们的药物组合物和包含组合。

33. 发明申请

US20130096141A1 BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：双相异构体衍生物及其使用方法
公开(公告)号：US20130096141A1
公开(公告)日：2013-04-18
申请号：US13805054
申请日：2011-06-14
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： C07D519/00
CPC分类号： C07D519/00 , C07D471/22 , C07D487/04 , C07D495/04 , A61K45/06
摘要： Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.
摘要翻译：结构式I的化合物是GPR119激动剂，可用于治疗，控制或预防对GPR119的激动作用反应的病症，例如代谢相关疾病如I型糖尿病，II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，高血糖症，高脂血症，高甘油三酯血症，高胆固醇血症，血脂异常或综合征X.该化合物也被报告用于控制体重增加，控制食物摄入和诱导哺乳动物的饱腹感。

34. 发明授权

US07384944B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US07384944B2
公开(公告)日：2008-06-10
申请号：US10668862
申请日：2003-09-23
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/497
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

35. 发明授权

US06204282B1 Benzimidazole compounds that are vitronectin receptor antagonists 失效
标题翻译：作为玻连蛋白受体拮抗剂的苯并咪唑化合物
公开(公告)号：US06204282B1
公开(公告)日：2001-03-20
申请号：US09450235
申请日：1999-11-29
申请人： Bernard R. Neustadt , Elizabeth M. Smith
发明人： Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： A61K314184
CPC分类号： C07D235/14
摘要： The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y1 each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, —CF3, and —C(O)OH; R1, R2, R3 and R4 are as defined herein; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; and wherein are positioned meta or para relative to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.
摘要翻译：本发明提供了具有式n，p，q和r各自独立地选自0或1的化合物; a，b，c和d各自独立地表示碳原子或氮原子，条件是不大于2个 a，b，c和d是氮原子; Y和Y1各自独立地表示1-4个选自烷基，烷氧基，卤素，-CF 3和-C（O）OH的任选取代基; R 1，R 2，R 3和R 4是如本文所定义; R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12独立地选自H或C 1 -C 3烷基;并且其中相对于彼此定位为间位或对位;或其不可生物酯，其可接受的盐。还提供了使用这些化合物治疗玻连蛋白介导的病症例如癌症，视网膜病变，动脉粥样硬化，血管再狭窄和骨质疏松症的方法。

36. 发明授权

US5348944A Carboxyalkyl dipeptides 失效
标题翻译：羧甲基二肽
公开(公告)号：US5348944A
公开(公告)日：1994-09-20
申请号：US261815
申请日：1988-04-04
申请人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： A61K38/00 , C07K5/02 , A61K37/02 , C07K5/06
CPC分类号： C07K5/0222 , A61K38/00
摘要： Compounds of the formula ##STR1## useful as antihypertensive agents are disclosed.
摘要翻译：公开了可用作抗高血压药的式“IMAGE”的化合物。

37. 发明授权

US4929641A Mercapto-acylamino acid antihypertensives 失效
标题翻译：巯基 - 酰氨基酸抗高血压药
公开(公告)号：US4929641A
公开(公告)日：1990-05-29
申请号：US192435
申请日：1988-05-11
申请人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： C07C323/59 , C07C327/32
CPC分类号： C07C323/59 , C07C327/32
摘要： Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
摘要翻译：公开了可用于治疗高血压的新型巯基酰基氨基酸和用于治疗高血压的巯基酰基氨基酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。

38. 发明授权

US4379166A Arylmethoxy-, arylmethylthio-, heteroarylmethoxy-, and heteroarylmethylthio-alkylaminoalcohols 失效
标题翻译：芳基甲氧基 - ，芳基甲硫基 - ，杂芳基甲氧基 - 和杂芳基甲硫基 - 烷基氨基醇
公开(公告)号：US4379166A
公开(公告)日：1983-04-05
申请号：US289339
申请日：1981-08-03
申请人： Bernard R. Neustadt , Elijah H. Gold
发明人： Bernard R. Neustadt , Elijah H. Gold
IPC分类号： A61K31/255 , A61K31/27 , C07C45/71 , C07C205/34 , C07D217/18 , A61K31/165 , A61K31/135 , C07D253/08
CPC分类号： C07C247/00 , C07C205/34 , C07C323/00 , C07C45/71
摘要： This invention relates to 5-(2-alkylamino-1-hydroxyethyl)salicylamides and 4-(2-alkylamino-1-hydroxyethyl)-2-(methylsulfinyl)phenols wherein the alkyl group is substituted by arylmethoxy, arylmethylthio, heteroarylmethoxy, or heteroarylmethylthio, pharmaceutical compositions thereof, and their use as cardiovascular agents.
摘要翻译：本发明涉及5-（2-烷基氨基-1-羟乙基）水杨酰胺和4-（2-烷基氨基-1-羟乙基）-2-（甲基亚磺酰基）苯酚，其中烷基被芳基甲氧基，芳基甲硫基，杂芳基甲氧基或杂芳基甲硫基，其药物组合物及其作为心血管药物的用途。

39. 发明授权

US4272550A Omega-[4-(polyfluoro-2-hydroxy-2-propyl)-2,3,6-substituted-phenoxy and phenylthio]alkanoic acids and compounds related thereto 失效
标题翻译： ω-[4-（多氟-2-羟基-2-丙基）-2,3,6-取代苯氧基和苯硫基]链烷酸及其相关化合物
公开(公告)号：US4272550A
公开(公告)日：1981-06-09
申请号：US089804
申请日：1979-10-31
申请人： Bernard R. Neustadt , Elijah H. Gold
发明人： Bernard R. Neustadt , Elijah H. Gold
IPC分类号： C07C59/68 , C07C59/70 , C07C317/44 , A61K31/135 , A61K31/165 , C07C93/06 , C07C103/26
CPC分类号： C07C317/44 , C07C59/68 , C07C59/70
摘要： Omega-[4-(polyfluoro-2-hydroxy-2-propyl)-2,3,6-substituted-phenoxy and phenylthio]alkanoic acids and compounds related thereto having antihypertensive activity are preparable by reaction of the appropriate 2,3,6-substituted-4-(polyfluoro-2-hydroxy-2-propyl)phenol or thiophenol with an alkyl ester of a bromoalkanoic acid, followed by hydrolysis to the free acid.
摘要翻译： ω-[4-（多氟-2-羟基-2-丙基）-2,3,6-取代苯氧基和苯硫基]链烷酸及其具有抗高血压活性的化合物可通过合适的2,3,6 - 取代的4-（多氟-2-羟基-2-丙基）苯酚或苯硫酚与溴烷酸的烷基酯反应，然后水解成游离酸。

40. 发明授权

US4267193A N-substituted-4-(polyfluoro-2-hydroxy-2-propyl)anilines and compounds related thereto 失效
标题翻译： N-取代-4-（多氟-2-羟基-2-丙基）苯胺及其相关化合物
公开(公告)号：US4267193A
公开(公告)日：1981-05-12
申请号：US35962
申请日：1979-05-04
申请人： Bernard R. Neustadt , Elijah H. Gold
发明人： Bernard R. Neustadt , Elijah H. Gold
IPC分类号： A01N37/10 , A01N37/44 , C07C101/72
CPC分类号： C07C255/00
摘要： N-substituted-4-(polyfluoro-2-hydroxy-2-propyl)anilines and compounds related thereto, useful as antihypertensive agents, are prepared by reaction of an N-substituted aniline with a polyfluoroacetone.
摘要翻译： N-取代-4-（多氟-2-羟基-2-丙基）苯胺及其相关化合物，可用作抗高血压剂，通过N-取代苯胺与多氟丙酮的反应来制备。

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