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1. 发明授权

US5086176A Tricyclic fused adenine derivatives 失效
标题翻译：三环稠合腺嘌呤衍生物
公开(公告)号：US5086176A
公开(公告)日：1992-02-04
申请号：US709957
申请日：1991-06-04
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07D487/14 , C07H19/04
CPC分类号： C07D487/14 , C07H19/04
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷拮抗剂起作用的腺苷类似物。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，并且体内腺苷受体活性与体内腺苷受体活性相关。可以基于本文公开的化合物的选择性结合活性来制备本发明化合物的药物制剂，其可以预期在增加某些生理效应的同时最小化其它物质，例如降低血压而不降低心率。

2. 发明授权

US5256650A Selective adenosine receptor agents 失效
标题翻译：选择性腺苷受体剂
公开(公告)号：US5256650A
公开(公告)日：1993-10-26
申请号：US954178
申请日：1992-09-30
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16 , C07H19/06 , A61K31/70 , C07D473/30
CPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷拮抗剂起作用的腺苷类似物。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，并且体内腺苷受体活性与体内腺苷受体活性相关。本发明化合物的药物制剂可以基于本文公开的化合物的选择性结合活性来制备，这将增强某些生理效应，同时使其他方式最小化，例如降低血压而不降低心率。

3. 发明授权

US5391739A Selective adenosine receptor agents 失效
标题翻译：选择性腺苷受体剂
公开(公告)号：US5391739A
公开(公告)日：1995-02-21
申请号：US27338
申请日：1994-03-08
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16 , A61K31/52
CPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷拮抗剂起作用的腺苷类似物。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，体内腺苷受体活性与体内腺苷受体活性相关。本发明化合物的药物制剂可以基于本文公开的化合物的选择性结合活性来制备，这将增强某些生理效应，同时使其他方式最小化，例如降低血压而不降低心率。

4. 发明授权

US5208240A 8-substituted purines as selective adenosine receptor agents 失效
标题翻译：作为选择性腺苷受体药剂的8替代品
公开(公告)号：US5208240A
公开(公告)日：1993-05-04
申请号：US667943
申请日：1991-03-12
申请人： Norton P. Peet , Nelsen L. Lentz , Mark W. Dudley
发明人： Norton P. Peet , Nelsen L. Lentz , Mark W. Dudley
IPC分类号： A61K31/52 , A61K31/522 , A61P9/00 , A61P11/00 , A61P25/28 , A61P43/00 , C07D473/06
CPC分类号： C07D473/06
摘要： The present invention relates to certain novel 8-substituted purines as selective A.sub.1 -adenosine receptor antagonists which are useful in the treatment of patients suffering from Alzheimer's disease, congestive heart failure or pulmonary bronchoconstriction.

5. 发明授权

US5426101A 2-substituted adenosines with A-2 receptor affinity 失效
标题翻译：具有A-2受体亲和力的2-取代腺苷
公开(公告)号：US5426101A
公开(公告)日：1995-06-20
申请号：US306847
申请日：1994-09-15
申请人： Norton P. Peet , David R. Borcherding , Nelsen L. Lentz , Philip M. Weintraub , Philip R. Kastner
发明人： Norton P. Peet , David R. Borcherding , Nelsen L. Lentz , Philip M. Weintraub , Philip R. Kastner
IPC分类号： C07H19/16 , C07H19/167 , A61K31/70
CPC分类号： C07H19/16
摘要： The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.
摘要翻译：其结构如下所示的化合物（R）-2 - [（苯基异丙基）氨基]腺苷：其中A选择性为约2个数量级 -1和A-2腺苷受体比其非对映异构体。该化合物可用于降低血压。

6. 发明授权

US5329007A Selective adenosine receptor agents 失效
标题翻译：选择性腺苷受体剂
公开(公告)号：US5329007A
公开(公告)日：1994-07-12
申请号：US099023
申请日：1993-07-29
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16 , C07D487/06 , C07D473/30 , C07H19/06
CPC分类号： C07D473/00 , C07D473/34 , C07D487/04 , C07H19/16
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷拮抗剂起作用的腺苷类似物。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，并且体内腺苷受体活性与体内腺苷受体活性相关。本发明化合物的药物制剂可以基于本文公开的化合物的选择性结合活性来制备，这将增强某些生理效应，同时使其他方式最小化，例如降低血压而不降低心率。

7. 发明授权

US5734052A 8-substituted xanthines as selective adenosine receptor agents 失效
标题翻译： 8-取代黄嘌呤作为选择性腺苷受体剂
公开(公告)号：US5734052A
公开(公告)日：1998-03-31
申请号：US553253
申请日：1995-11-01
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： A61K31/52 , A61K31/522 , C07D473/06 , C07D473/08
CPC分类号： C07D473/06
摘要： Xanthine derivatives having general structure (I) including the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently (C.sub.1 -C.sub.4)lower alkyl or (C.sub.2 -C.sub.4)lower alkenyl, Z is (II) or (III) or (IV) wherein R.sub.3 is hydrogen, (C.sub.1 -C.sub.3)lower alkyl, nitro, amino, hydroxy, fluoro, bromo or chloro, R.sub.4 is (C.sub.1 -C.sub.4)lower alkyl and n is 1 or 2 which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as descreasing blood pressure without descreasing heart rate.
摘要翻译： PCT No.PCT / US94 / 04038 Sec。 371 1995年10月26日第 102（e）日期1995年10月26日PCT 1994年4月13日PCT PCT。第WO94 / 26744号公报（IV）具有通式（I）的（R）和（S）对映异构体和外消旋的（Ⅳ）的黄嘌呤衍生物，其混合物及其药学上可接受的盐，其中R 1和R 2各自独立地为（C 1 -C 4）低级烷基或（C 2 -C 4）低级烯基，Z为（II）或（III）或（Ⅳ），其中R 3为氢，（C1-C3）低级烷基，硝基，氨基，羟基，氟，溴或氯，R4是（C1-C4）低级烷基，n是1或2，其在腺苷受体上有选择性作用，并且通常作为腺苷拮抗剂起作用被披露。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，并且体内腺苷受体活性与体内腺苷受体活性相关。本发明化合物的药物制剂可以基于本文公开的化合物的选择性结合活性来制备，这将增强某些生理效应，同时使其他物质最小化，例如降低血压而不降低心率。

8. 发明授权

US5359131A Sulfonic acid derivatives in the treatment of viral diseases 失效
标题翻译：磺酸衍生物治疗病毒性疾病
公开(公告)号：US5359131A
公开(公告)日：1994-10-25
申请号：US106311
申请日：1993-08-13
申请人： Alan D. Cardin , Norton P. Peet , Nelsen L. Lentz
发明人： Alan D. Cardin , Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07C309/42 , C07C309/45 , C07C309/51 , C07C327/40 , C07C327/42 , C07C329/04 , C07C329/10 , C07C329/20 , C07C333/08 , C07C333/24 , C07C335/16 , C07C335/20 , C07C229/00
CPC分类号： C07C309/42 , C07C309/51 , C07C327/42 , C07C329/04 , C07C329/20 , C07C333/08 , C07C333/24 , C07C335/20
摘要： Sulfonic acid stilbenes are disclosed which block the infection of cells by HSV, HIV and CMV.
摘要翻译：披露了磺酸二苯乙烯，其阻断HSV，HIV和CMV对细胞的感染。

9. 发明授权

US5064947A Selective adenosine reseptor compounds 失效
标题翻译：选择性腺苷受体化合物
公开(公告)号：US5064947A
公开(公告)日：1991-11-12
申请号：US544811
申请日：1990-06-27
申请人： Norton P. Peet , Nelsen L. Lentz
发明人： Norton P. Peet , Nelsen L. Lentz
IPC分类号： C07D487/14 , C07H19/04
CPC分类号： C07D487/14 , C07H19/04
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷拮抗剂起作用的腺苷类似物。从体外研究可以看出，具体的生理作用可以作为这种选择性的结果来区分，并且体内腺苷受体活性与体内腺苷受体活性相关。可以基于本文公开的化合物的选择性结合活性来制备本发明化合物的药物制剂，其可以预期在增加某些生理效应的同时最小化其它物质，例如降低血压而不降低心率。

10. 发明授权

US4748274A 4-hydroxy-4-(substituted alkenyl)cyclohexanecarboxylic acids 失效
标题翻译： 4-羟基-4-（取代的链烯基）环己烷羧酸
公开(公告)号：US4748274A
公开(公告)日：1988-05-31
申请号：US928759
申请日：1986-11-07
申请人： Robert J. Cregge , Nelsen L. Lentz
发明人： Robert J. Cregge , Nelsen L. Lentz
IPC分类号： C07D303/38 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/215 , A61P11/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C69/732 , C07C313/00 , C07C323/55 , C07C323/58 , C07C323/60 , C07C149/26 , C07C149/273
CPC分类号： C07C323/55 , A61K31/16 , A61K31/19 , A61K31/215 , C07C2101/14 , Y02P20/582 , Y10S514/826
摘要： The present invention relates to compounds which are 4-hydroxy-4-alkenylcyclohexanecarboxylic acid derivatives possessing leukotriene antagonist activity. The compounds are useful in the treatment of allergic diseases, particularly in the treatment of human asthma. They are prepared by the reaction of an appropriate oxaspiro compound with a mercaptoalkanoic acid derivative.

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