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1. 发明授权

US07169925B2 Indole derivatives as interleukin-4 gene expression inhibitors 失效
标题翻译：吲哚衍生物作为白细胞介素-4基因表达抑制剂
公开(公告)号：US07169925B2
公开(公告)日：2007-01-30
申请号：US10421511
申请日：2003-04-23
申请人： Gregory H. Merriman , Philip M. Weintraub , Jeffrey S. Sabol , Ramalinga M. Dharanipragada , Nicholas J. Hrib , John G. Jurcak , Alexandre Gross , Brian Whiteley , Kwon Yon Musick , Joseph T. Klein
发明人： Gregory H. Merriman , Philip M. Weintraub , Jeffrey S. Sabol , Ramalinga M. Dharanipragada , Nicholas J. Hrib , John G. Jurcak , Alexandre Gross , Brian Whiteley , Kwon Yon Musick , Joseph T. Klein
IPC分类号： C07D403/12 , C07D401/00
CPC分类号： A61K31/381 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
摘要翻译：本发明公开了一种用于治疗过敏，哮喘，鼻炎，皮炎，B细胞淋巴瘤，肿瘤和与细菌，鼻病毒或呼吸道合胞病毒（RSV）感染相关的疾病的新一类吲哚衍生物。现在已经发现，本发明的化合物能够调节T辅助细胞Th1 / Th2，从而能够抑制白细胞介素-4（IL-4）信号，IL-4释放或IL的转录 -4生产。

2. 发明授权

US5240927A Benzo[.beta.]thiophen-3-yl piperazines as antipsychotic agents 失效
标题翻译：苯硫酚噻吩-3-基哌嗪作为抗精神病药
公开(公告)号：US5240927A
公开(公告)日：1993-08-31
申请号：US885331
申请日：1992-05-19
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/495 , A61P25/18 , C07D333/66 , C07D333/72 , C07D409/04
CPC分类号： C07D333/66
摘要： There are disclosed various compounds of the formula depicted below, ##STR1## where the parameters m, n, p, q, X and R are as defined in the specification, as being useful as antipsychotic agents.
摘要翻译：公开了下文描述的各种化合物，其中参数m，n，p，q，X和R如说明书中所定义，作为抗精神病药有用。

3. 发明授权

US5229388A 3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds 失效
标题翻译： 3- [4-（1-取代-4-哌嗪基）丁基] -4-噻唑烷酮及相关化合物
公开(公告)号：US5229388A
公开(公告)日：1993-07-20
申请号：US795608
申请日：1991-11-21
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D277/14 , C07D277/60 , C07D277/82 , C07D417/12 , C07D417/14 , C07D513/10
CPC分类号： C07D277/60 , C07D277/14 , C07D277/82 , C07D417/12 , C07D417/14
摘要： There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.
摘要翻译：公开了下式的化合物，其中n为0,1或2; A是每一次出现的X独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; Y在每次出现时独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢，低级烷基，低级或芳基，除了当R 1是芳基或芳基时，R 2是氢，或者R 1 + R 2与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，茚满或哌啶环; R3和R4独立地是氢或低级烷基，或者R3 + R4与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，吡咯烷或哌啶环，术语表示未取代的苯基的芳基或被1,2或3个取代基取代的苯基，各自独立地为低级烷基，低级烷氧基，羟基，卤素，低级烷硫基，氰基，氨基或三氟甲基，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。

4. 发明授权

US5143923A Benzoisothiazole- and benziosoxazole-3-carboxamides 失效
标题翻译：苯并噻唑和苯并异恶唑-3-甲酰胺
公开(公告)号：US5143923A
公开(公告)日：1992-09-01
申请号：US693168
申请日：1991-04-29
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61P25/18 , C07D261/20 , C07D275/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D275/04 , C07D261/20 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Novel benzisothiazole- and benzisoxazole-3-carboxamides, processes and intermediates for the preparation thereof, and methods of treating psychoses utilizing compounds and compositions thereof are disclosed.
摘要翻译：公开了新的苯并异噻唑和苯并异恶唑-3-甲酰胺，其制备方法和中间体，以及利用化合物及其组合物治疗精神病的方法。

5. 发明授权

US5130315A 1-piperazinyl-2-butenes and -2-butynes 失效
标题翻译： 1-哌嗪-2-基和2-丁基
公开(公告)号：US5130315A
公开(公告)日：1992-07-14
申请号：US639639
申请日：1991-01-10
申请人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
发明人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
IPC分类号： A61K31/495 , A61P25/18 , C07D209/48 , C07D221/20 , C07D239/42 , C07D277/14 , C07D277/20 , C07D277/34 , C07D295/12 , C07D295/125 , C07D401/12 , C07D403/12 , C07D409/00 , C07D409/12 , C07D417/12 , C07D471/04
CPC分类号： C07D209/48 , C07D221/20 , C07D239/42 , C07D277/34 , C07D295/125 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.

6. 发明授权

US4933453A 3-[4-(1-Substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds 失效
标题翻译： 3- [4-（1-取代-4-哌嗪基）丁基] -4-噻唑烷酮化合物
公开(公告)号：US4933453A
公开(公告)日：1990-06-12
申请号：US430688
申请日：1989-10-31
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D277/14 , C07D277/60 , C07D277/82 , C07D417/12 , C07D417/14 , C07D513/10
CPC分类号： C07D277/60 , C07D277/14 , C07D277/82 , C07D417/12 , C07D417/14
摘要： 3-[4-1-substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.
摘要翻译： 3- [4-1-取代-4-哌嗪基）丁基] -4-噻唑烷酮化合物，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。

7. 发明授权

US5440048A 1-piperazinyl-2-butenes and -2-butynes 失效
标题翻译： 1-哌嗪基-2-丁烯和-2-丁炔
公开(公告)号：US5440048A
公开(公告)日：1995-08-08
申请号：US238283
申请日：1994-05-05
申请人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
发明人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
IPC分类号： A61K31/495 , A61P25/18 , C07D209/48 , C07D221/20 , C07D239/42 , C07D277/14 , C07D277/20 , C07D277/34 , C07D295/12 , C07D295/125 , C07D401/12 , C07D403/12 , C07D409/00 , C07D409/12 , C07D417/12 , C07D471/04
CPC分类号： C07D209/48 , C07D221/20 , C07D239/42 , C07D277/34 , C07D295/125 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新颖的1-哌嗪基-2-丁烯和-2-丁炔，其制备方法及其制备方法，以及利用化合物或其组合物治疗精神病的方法。

8. 发明授权

US5272148A Heteroarenylpiperazines 失效
标题翻译：杂芳基哌嗪
公开(公告)号：US5272148A
公开(公告)日：1993-12-21
申请号：US942232
申请日：1992-09-09
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/435 , A61K31/38 , A61K31/495 , A61P25/18 , C07D241/04 , C07D333/10 , C07D495/04 , C07D401/04
CPC分类号： C07D495/04
摘要： Novel heteroarenylpiperazines, intermediates and processes for the preparation thereof, and methods for treating psychoses utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新型杂芳基哌嗪，其中间体及其制备方法，以及利用化合物或其组合物治疗精神病的方法。

9. 发明授权

US5194436A 1-piperazinyl-2-butenes and -2-butynes 失效
标题翻译： 1-哌嗪基-2-丁烯和-2-丁炔
公开(公告)号：US5194436A
公开(公告)日：1993-03-16
申请号：US875477
申请日：1992-04-29
申请人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
发明人： Helen H. Ong , Nicholas J. Hrib , Joseph Perez , John G. Jurcak
IPC分类号： C07D209/48 , C07D221/20 , C07D239/42 , C07D277/34 , C07D295/125 , C07D401/12 , C07D403/12 , C07D409/00 , C07D417/12 , C07D471/04
CPC分类号： C07D209/48 , C07D221/20 , C07D239/42 , C07D277/34 , C07D295/125 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新颖的1-哌嗪基-2-丁烯和-2-丁炔，其制备方法及其制备方法，以及利用化合物或其组合物治疗精神病的方法。

10. 发明授权

US5136037A 3-(4-substituted-4-piperazinyl)butyl-4-thiazolidinone and related compounds 失效
标题翻译： 3-（4-取代-4-哌嗪基）丁基-4-噻唑烷酮和相关化合物
公开(公告)号：US5136037A
公开(公告)日：1992-08-04
申请号：US713247
申请日：1991-06-07
申请人： Nicholas J. Hrib , John G. Jurcak
发明人： Nicholas J. Hrib , John G. Jurcak
IPC分类号： A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D277/14 , C07D277/60 , C07D277/82 , C07D417/12 , C07D417/14 , C07D513/10
CPC分类号： C07D277/60 , C07D277/14 , C07D277/82 , C07D417/12 , C07D417/14
摘要： There are disclosed compounds of the formula, ##STR1## where n is 0 or 1; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, ##STR3## or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.
摘要翻译：公开了下式的化合物，其中n为0或1; 其中每次出现的X独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，低级烷氧基，低级烷氧基，氰基，三氟甲基或甲硫基; Y在每次出现时独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢，低级烷基，或者R1 + R2与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，茚满或哌啶环; R3和R4独立地是氢或低级烷基，或者R3 + R4与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，吡咯烷或哌啶环，术语表示未取代的苯基的芳基或被1,2或3个取代基取代的苯基，各自独立地为低级烷基，低级烷氧基，羟基，卤素，低级烷硫基，氰基，氨基或三氟甲基，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。

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