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1. 发明授权

US06319928B1 Purine derivatives having phosphodiesterase IV inhibition activity 失效
标题翻译：具有磷酸二酯酶IV抑制活性的嘌呤衍生物
公开(公告)号：US06319928B1
公开(公告)日：2001-11-20
申请号：US09418331
申请日：1999-10-14
申请人： Mark Chasin , David J. Cavalla , Peter Hofer , Peter Wintergerst , Andre Gehrig
发明人： Mark Chasin , David J. Cavalla , Peter Hofer , Peter Wintergerst , Andre Gehrig
IPC分类号： C07D47318
CPC分类号： C07D473/20 , C07D473/18 , C07D473/24 , C07D473/34
摘要： A compound of the formula: wherein R2 is O or S; R3, R6a and R8 are the same or different and each represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl; R6b represents a H or R6a, or together R6b, N, and R6a make a 3 to 8 member ring containing at least one carbon, from one to three nitrogen atoms, from zero to two oxygen atoms, from zero to two sulfur atoms, said ring optionally substituted with alkoxy, CO2H, CONH2, ═NOH, ═NOCONH2, ═O; and where aryl is phenyl or naphthyl, the heterocyclyl is a 5, 6 or 7 membered ring including from one to three nitrogen atoms, and from zero to two oxygen atoms, from zero to two sulfur atoms, and can be substituted as in aryl on the carbons or nitrogens of that ring; or a pharmaceutically acceptable salt thereof, provided that when R3 is propyl, R8 is not cyclopentyl, noradamantyl, or dicyclopropylmethyl.
摘要翻译：下式的化合物：其中R 2是O或S; R 3，R 6a和R 8相同或不同，并且各自表示未支链或未支化或被OH，烷氧基，CO 2 H，= NOH = NOCONH2或= O; 未取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基，其中环烷基部分未被取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代; 未取代或被Cl，NH 2，烷基氨基，二烷基氨基，酰氨基，C 1 -C 8烷基酰氨基，C 1 -C 3二烷基氨基，OH，烷氧基，HC = NOH，HC = NOCONH 2，C 1 -C 3烷基，苯基或苄基取代的芳基; 芳烷基（C1-4）; 杂环基杂环基烷基（C1-C4）; 和杂芳基; R6b表示H或R6a，或R6b，N和R6a一起形成含有至少一个碳，1-3个氮原子，0至2个氧原子，0至2个硫原子的3至8元环所述环任选被烷氧基取代，CO 2 H，CONH 2，= NOH，= NOCONH 2，= O; 并且其中芳基为苯基或萘基，杂环基为5,6或7元环，包括1至3个氮原子，0至2个氧原子，0至2个硫原子，并且可以如该环的碳或氮; 或其药学上可接受的盐，条件是当R 3为丙基时，R 8不是环戊基，去甲金刚烷基或二环丙基甲基。

2. 发明授权

US06228859B1 Purine derivatives having phosphodiesterase IV inhibition activity 失效
标题翻译：具有磷酸二酯酶IV抑制活性的嘌呤衍生物
公开(公告)号：US06228859B1
公开(公告)日：2001-05-08
申请号：US09210556
申请日：1998-12-11
申请人： David J. Cavalla , Mark Chasin , Peter Hofer , Andre Gehrig , Peter Wintergerst
发明人： David J. Cavalla , Mark Chasin , Peter Hofer , Andre Gehrig , Peter Wintergerst
IPC分类号： C07D47334
CPC分类号： C07D473/30 , C07D473/34
摘要： Disclosed are compounds of the formula (I): wherein R3 is selected from the group consisting of C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy substituent is optionally substituted in one position with hydroxy; R8 is selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy is optionally substituted in one position with hydroxy; R6a and R6b are independently selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl, or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; and pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）的化合物：其中R 3选自C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基，其中所述烷基，烯基，环烷基环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基，其中所述苄基在一个或两个位置任选被卤素，烷氧基，环烷氧基或多环烷基取代，并且其中所述烷氧基或环烷氧基取代基的所述烷基部分任选在一个位置被羟基取代; R 8选自的氢，C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基，其中所述烷基，烯基，环烷基，环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基，其中所述苄基在一个或两个位置任选被卤素，烷氧基，环烷氧基或多环烷基取代，并且其中所述烷氧基或环烷氧基的所述烷基部分任选在一个位置被羟基取代; R 6a和R 6b独立地选自由氢，C 1-10烷基，C 1-10烯基，C 3-10环烷基，C 4-10环烷基烷基或C 3-10环烯基组成的基团，其中所述烷基，链烯基，环烷基，环烷基烷基或环烯基任选在一个位置被羟基取代 ;及其药学上可接受的盐。

3. 发明授权

US6075016A 6,5-fused aromatic ring systems having enhanced phosphodiesterase IV inhibitory activity 失效
标题翻译：具有增强的磷酸二酯酶IV抑制活性的6,5-稠合芳环体系
公开(公告)号：US6075016A
公开(公告)日：2000-06-13
申请号：US833893
申请日：1997-04-10
申请人： Mark Chasin , David Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst
发明人： Mark Chasin , David Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst
IPC分类号： C07D263/56 , C07D413/06 , C07D417/06 , A61K31/40 , A61K31/435 , C07D471/04 , C07D498/04
CPC分类号： C07D263/56 , C07D413/06 , C07D417/06
摘要： Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. The present invention includes compounds of Formula I: ##STR1##
摘要翻译：公开了作为有效的PDE IV抑制剂的新型化合物。与茶碱或咯利普兰相比，该化合物具有改善的PDE IV抑制，关于例如PDE V抑制具有改善的选择性。本发明包括式I的化合物：

4. 发明授权

US06413975B1 Purine derivatives having phosphodiesterase iv inhibition activity 失效
标题翻译：具有磷酸二酯酶iv抑制活性的嘌呤衍生物
公开(公告)号：US06413975B1
公开(公告)日：2002-07-02
申请号：US09539571
申请日：2000-03-31
申请人： Mark Chasin , David J. Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst
发明人： Mark Chasin , David J. Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst
IPC分类号： C07D47334
CPC分类号： C07D473/18 , C07D473/20 , C07D473/24 , C07D473/34
摘要： Disclosed are compounds of the formula: wherein R3, R6a, R6b and R8 are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need thereof.
摘要翻译：公开了下式的化合物：其中R 3，R 6a，R 6b和R 8如本文所公开的被取代。该化合物在有需要的患者中有效地实现PDE IV抑制。

5. 发明授权

US06294541B1 Purine derivatives having phosphodiesterase IV inhibition activity 失效
标题翻译：具有磷酸二酯酶IV抑制活性的嘌呤衍生物
公开(公告)号：US06294541B1
公开(公告)日：2001-09-25
申请号：US09418330
申请日：1999-10-14
申请人： David J. Cavalla , Mark Chasin , Peter Hofer , Andre Gehrig , Peter Wintergerst
发明人： David J. Cavalla , Mark Chasin , Peter Hofer , Andre Gehrig , Peter Wintergerst
IPC分类号： C07D27320
CPC分类号： C07D473/24 , C07D473/18 , C07D473/20 , C07D473/30 , C07D473/34
摘要： A compound of the formula: wherein R3 represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl; R8 represents H or a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl.
摘要翻译：下式的化合物：其中R 3表示未支链或未支化或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基，其中环烷基部分未被取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代; 未取代或被Cl，NH 2，烷基氨基，二烷基氨基，酰氨基，C 1 -C 8烷基酰氨基，C 1 -C 3二烷基氨基，OH，烷氧基，HC = NOH，HC = NOCONH 2，C 1 -C 3烷基，苯基或苄基取代的芳基; 芳烷基（C1-4）; 杂环基杂环基烷基（C1-C4）; R 8表示H或未分支或未被取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基，其中环烷基部分未被取代或被OH，烷氧基，CO 2 H，= NOH，= NOCONH 2或= O取代; 未取代或被Cl，NH 2，烷基氨基，二烷基氨基，酰氨基，C 1 -C 8烷基酰氨基，C 1 -C 3二烷基氨基，OH，烷氧基，HC = NOH，HC = NOCONH 2，C 1 -C 3烷基，苯基或苄基取代的芳基; 芳烷基（C1-4）; 杂环基杂环基烷基（C1-C4）; 和杂芳基。

6. 发明授权

US5911586A System, device and method for locking and unlocking power flow to an electrical cord 失效
标题翻译：用于锁定和解锁电源到电源线的系统，设备和方法
公开(公告)号：US5911586A
公开(公告)日：1999-06-15
申请号：US866420
申请日：1997-05-30
申请人： H. Peter Wintergerst
发明人： H. Peter Wintergerst
IPC分类号： H01R13/639 , H01R13/70 , H01R31/06 , H01R13/44
CPC分类号： H01R13/70 , H01R13/6397 , H01R31/065 , H01R13/6392 , Y10T70/65
摘要： This disclosure describes an electrical power cord or adapter which, by using a lock and key mechanism, will enable or disable power from flowing through said power cord or adapter. It also describes various methods for locking and unlocking a plug to and from the female receptacle of said power cord or adapter. The purpose of such a power cord or adapter is to prevent unauthorized use of any electrical device that may be plugged in to said power cord or adapter, by disabling a flow of current to that device and by locking the plug of that device to the female receptacle of said power cord or adapter. When the appropriate key is used, power flow may be resumed, or the plug may be removed.
摘要翻译：本公开描述了一种电源线或适配器，其通过使用锁定和钥匙机构将使能或禁止通过所述电源线或适配器的电力。它还描述了用于将插头锁定到所述电源线或适配器的母插座的方式和从插座的插座解锁的各种方法。这种电源线或适配器的目的是防止未经授权使用可能插入到所述电源线或适配器的任何电气设备，通过禁止对该设备的电流流动并且将该设备的插头锁定到母线所述电源线或适配器的插座。当使用适当的钥匙时，可以恢复动力流量，或者可以去除塞子。

7. 发明授权

US06365606B1 6,5-fused aromatic ring systems having enhanced phosphodiesterase IV inhibitory activity 失效
标题翻译：具有增强的磷酸二酯酶IV抑制活性的6,5-稠合芳环体系
公开(公告)号：US06365606B1
公开(公告)日：2002-04-02
申请号：US09506624
申请日：2000-02-18
申请人： David Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst , Mark Chasin
发明人： David Cavalla , Peter Hofer , Andre Gehrig , Peter Wintergerst , Mark Chasin
IPC分类号： A61K314402
CPC分类号： C07D263/56 , C07D413/06 , C07D417/06
摘要： Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. The present invention includes compounds of Formula I: wherein the substituents are as disclosed herein.
摘要翻译：公开了作为有效的PDE IV抑制剂的新型化合物。与茶碱或咯利普兰相比，该化合物具有改善的PDE IV抑制作用，具有关于例如PDE V抑制的改善的选择性。本发明包括式I的化合物：其中取代基如本文所公开。

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