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1. 发明授权

US6025361A Trisubstituted thioxanthines 失效
标题翻译：三取代噻吨烷
公开(公告)号：US6025361A
公开(公告)日：2000-02-15
申请号：US860674
申请日：1997-09-29
申请人： David Cavalla , Peter Hofer , Mark Chasin
发明人： David Cavalla , Peter Hofer , Mark Chasin
IPC分类号： A61K31/522 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07D473/18 , C07D473/20 , C07D473/22 , C07D473/38 , A61K31/52 , C07D239/56
CPC分类号： C07D473/18 , C07D473/20 , C07D473/22 , C07D473/38
摘要： Disclosed are compounds of formula (I), wherein R.sup.1, R.sup.3 and R.sup.8 are independently alkyl, aryl or aralkyl, and R.sup.2 is selected from the group consisting of S and O, R.sup.6 is selected from the group consisting of S and O, provided that R.sup.2 and R.sup.6 are not both O. The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition. Methods of treatment using the compounds are also disclosed.
摘要翻译： PCT No.PCT / US95 / 16724 Sec。 371日期：1997年9月29日 102（e）日期1997年9月29日PCT提交1995年12月12日PCT公布。公开号WO96 / 18400 日期1996年6月20日公开是式（I）化合物，其中R 1，R 3和R 8独立地为烷基，芳基或芳烷基，R 2选自S和O，R 6选自S 和O，条件是R2和R6不都是O.化合物是有效的PDE IV抑制剂，并且具有改善的PDE IV抑制和改善PDE III抑制的选择性。还公开了使用该化合物的治疗方法。

2. 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。

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

US6066641A Aryl thioxanthines 失效
标题翻译：芳基硫代黄嘌呤
公开(公告)号：US6066641A
公开(公告)日：2000-05-23
申请号：US860680
申请日：1997-06-11
申请人： David Cavalla , Peter Hofer , Mark Chasin
发明人： David Cavalla , Peter Hofer , Mark Chasin
IPC分类号： A61K31/52 , A61K31/522 , A61P11/06 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07D473/18 , C07D473/22 , C07D401/04 , C07D473/04
CPC分类号： C07D473/18 , C07D473/22
摘要： The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.
摘要翻译： PCT No.PCT / US95 / 16723 Sec。 371日期：1997年8月18日 102（e）日期1997年8月18日PCT提交1995年12月12日PCT公布。第WO96 / 18399号公报日期：1996年6月20日本发明涉及新的式（I）化合物：其中Q3R3和Q8R8在本文中描述。该化合物对PDE-III抑制具有PDE-IV抑制活性和改善的选择性。还公开了利用所公开的化合物的药物组合物和治疗方法。

5. 发明授权

US5665737A Substituted benzoxazoles 失效
标题翻译：取代苯并恶唑
公开(公告)号：US5665737A
公开(公告)日：1997-09-09
申请号：US321730
申请日：1994-10-12
申请人： John David Cavalla , Lloyd J. Dolby , Peter Hofer , Mark Chasin
发明人： John David Cavalla , Lloyd J. Dolby , Peter Hofer , Mark Chasin
IPC分类号： C07D277/64 , A61K31/42 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61P11/00 , A61P11/06 , A61P17/00 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P31/12 , A61P37/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D263/56 , C07D263/57 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D263/56 , C07D263/57 , C07D413/06 , C07D413/12 , 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 III inhibition.
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，与PDE III抑制有关，具有改善的选择性。

6. 发明授权

US06440979B1 Aryl isoguanines 失效
标题翻译：芳基异鸟嘌呤
公开(公告)号：US06440979B1
公开(公告)日：2002-08-27
申请号：US09547898
申请日：2000-04-12
申请人： David Cavalla , Peter Hofer , Mark Chasin
发明人： David Cavalla , Peter Hofer , Mark Chasin
IPC分类号： C07D47322
CPC分类号： C07D473/18 , C07D473/22
摘要： Disclosed are compounds having formula (II): wherein: Q3, Q6a, Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-8 alkynylene, and R3, R6a, R6b and R8 are independently hydrogen, aryl or heteroraryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided that: Q3R3 is not hydrogen or methyl. The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition.
摘要翻译：公开了具有式（II）的化合物：其中：Q3，Q6a，Q6b和Q8独立地为键，C1-8亚烷基，C2-8亚烯基和C2-8亚炔基，R3，R6a，R6b和R8独立地为氢，芳基或杂芳基，任选被卤素，羟基，烷氧基，硝基，氰基和羧基取代，条件是：Q3R 3不是氢或甲基。这些化合物是有效的PDE IV抑制剂，并具有改善的PDE IV抑制和改善PDE III抑制的选择性。

7. 发明授权

US06372770B1 Benzoxazoles 失效
标题翻译：苯并恶唑
公开(公告)号：US06372770B1
公开(公告)日：2002-04-16
申请号：US09151949
申请日：1998-09-11
申请人： Mark Chasin , David Cavalla , Peter Hofer , Lloyd Dolby
发明人： Mark Chasin , David Cavalla , Peter Hofer , Lloyd Dolby
IPC分类号： A61K3142
CPC分类号： C07D263/56 , C07D263/57 , C07D413/06 , C07D413/12 , 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 III inhibition.
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，与PDE III抑制有关，具有改善的选择性。

8. 发明授权

US06268373B1 Trisubstituted thioxanthines 失效
标题翻译：三取代噻吨烷
公开(公告)号：US06268373B1
公开(公告)日：2001-07-31
申请号：US09361196
申请日：1999-07-26
申请人： David Cavalla , Peter Hofer , Mark Chasin
发明人： David Cavalla , Peter Hofer , Mark Chasin
IPC分类号： C07D47320
CPC分类号： C07D473/38 , C07D473/20
摘要： Disclosed is a compound selected from the group consisting of 1,3,8-triethyl-2,6-dithioxanthine; 1,3,8-triethyl-2-thioxanthine; 8-cyclopropyl-1-ethyl-3-(2-methyl-butyl)-6-thioxanthine; 1,3-diethyl-8-isopropyl-6-thioxanthine; 8-cyclopropyl-1,3-dipropyl-6-thioxanthine; 8-isopropyl-1,3-dipropyl-6-thioxanthine; 1,3-diethyl-8-cyclopropyl-2,6-dithioxanthine; 1-(4-chlorobenzyl)-3-ethyl-8-isopropyl-6-thioxanthine; and 8-cyclopropyl-1,3-diethyl-6-thioxanthine. Also disclosed is a pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and a compound selected from the group above. Also disclosed is a method of effecting PDE IV inhibition which comprises administering to a patient suffering from a disease or disorder selected from the group consisting of asthma, allergies, PDE IV modulated inflammation, and depression, a therapeutically effective amount of a compound selected from the group above.
摘要翻译：公开了选自1,3,8-三乙基-2,6-二硫代黄嘌呤的化合物; 1,3,8-三乙基-2-硫代黄嘌呤; 8-环丙基-1-乙基-3-（2-甲基 - 丁基）-6-硫代黄嘌呤; 1,3-二乙基-8-异丙基-6-硫代黄嘌呤; 8-环丙基-1,3-二丙基-6-硫代黄嘌呤; 8-异丙基-1,3-二丙基-6-硫代黄嘌呤; 1,3-二乙基-8-环丙基-2,6-二硫黄嘌呤; 1-（4-氯苄基）-3-乙基-8-异丙基-6-硫代黄嘌呤; 和8-环丙基-1,3-二乙基-6-硫代黄嘌呤。还公开了包含至少一种药学上可接受的载体和选自上述的化合物的药物组合物。还公开了实施PDE IV抑制的方法，其包括对患有选自哮喘，过敏，PDE IV调节的炎症和抑郁症的疾病或病症的患者施用治疗有效量的选自上面的组。

9. 发明授权

US5864037A Methods for the synthesis of chemical compounds having PDE-IV inhibitory activity 失效
标题翻译：合成具有PDE-IV抑制活性的化合物的方法
公开(公告)号：US5864037A
公开(公告)日：1999-01-26
申请号：US659767
申请日：1996-06-06
申请人： Mark Chasin , David Cavalla , Peter Hofer
发明人： Mark Chasin , David Cavalla , Peter Hofer
IPC分类号： A61K31/52 , A61P11/08 , A61P29/00 , A61P43/00 , C07D473/34 , C07D473/22 , C07D473/40
CPC分类号： C07D473/34
摘要： Disclosed is a process for the preparation of a compound of Formula IV having the structure: ##STR1## wherein R.sub.6 is N(R.sub.6a)(R.sub.6b);R.sub.3 represents a C.sub.2-8, alkyl which is unbranched or branched and unsubstituted or substituted; C.sub.3-8 cycloalkyl which is unsubstituted or substituted; C.sub.4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted; aryl or benzyl which is optionally unsubstituted or substituted; ar(C.sub.1-4)alkyl; a heterocyclyl group, ring optionally substituted; heterocyclyl (C.sub.1 -C.sub.4) alkyl ring optionally substituted;which comprises:(a) treating a compound of Formula I: ##STR2## with an effective amount of a dethionating agent to produce a compound of Formula II: ##STR3## (b) treating a compound of Formula II with an effective halogenating agent under conditions effective to produce a compound of Formula III: ##STR4## and (c) treating a compound of Formula III with an effective aminating agent under conditions effective to produce a compound of Formula IV.
摘要翻译：公开了制备式IV化合物的方法，其具有以下结构：其中R 6为N（R 6a）（R 6b）; R3表示C2-8烷基，其为无支链或未支链且未被取代或取代的; 未取代或取代的C 3-8环烷基; C4-8环烷基烷基，其中环烷基部分是未取代或取代的; 任选未取代或取代的芳基或苄基; 芳（C 1-4）烷基; 杂环基，任选取代的环; 任选取代的杂环基（C 1 -C 4）烷基; 其包括：（a）用有效量的去离子体处理式I的化合物：I，以产生式II的化合物：（b）用有效的卤化剂处理式II的化合物在有效产生式III化合物的条件下：（III）和（c）在有效制备式IV化合物的条件下用有效的胺化剂处理式III化合物。

10. 发明授权

US5744473A PDE IV inhibitors: "bis-compounds" 失效
标题翻译： PDE IV抑制剂：“双 - 化合物”
公开(公告)号：US5744473A
公开(公告)日：1998-04-28
申请号：US714581
申请日：1996-09-16
申请人： Mark Chasin , Peter Hofer , David Cavalla
发明人： Mark Chasin , Peter Hofer , David Cavalla
IPC分类号： C07D473/24 , C07D519/00 , A61K31/44 , A61K31/505 , A61K31/52
CPC分类号： C07D473/24
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. Also provided is a process of making compounds of Formula I. Compounds of the present invention are represented by Formula I: ##STR1## its pharmaceutically acceptable salts, hydrochloride salts, or prodrug forms thereof, wherein: X.sub.1a, X.sub.1b are independently selected from --NH and --N-lower alkyl; X.sub.2a, X.sub.2b are optionally present and are independently selected from S(O)n, O, CH.sub.2, and NH; P.sub.1a, P.sub.1b, P.sub.2a, P.sub.2b, P.sub.4a, and P.sub.4b are independently selected from N, or CH; R.sub.1a, R.sub.1b, R.sub.2a, R.sub.2b, R.sub.3a and R.sub.3b are independently selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 branched alkyl, C.sub.3 -C.sub.6 cycloalkyl, said alkyl groups being optionally substituted with halogen, aryl or heteroaryl group(s), said aryl and heteroaryl group(s) being optionally substituted with hydroxy, alkoxy, cycloalkoxy, halogen, alkyl, or cycloalkyl; and n is an integer from 0 to 2.
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。还提供了制备式I化合物的方法。本发明化合物由式I表示：其盐，盐酸盐或其前药形式，其中：X1a，X1b独立地选自-NH和-N-低级烷基; X2a，X2b任选存在并且独立地选自S（O）n，O，CH 2和NH; P1a，P1b，P2a，P2b，P4a和P4b独立地选自N或CH; R1a，R1b，R2a，R2b，R3a和R3b独立地选自H，C1-C6烷基，C3-C6支链烷基，C3-C6环烷基，所述烷基任选被卤素，芳基或杂芳基取代，所述芳基和杂芳基任选被羟基，烷氧基，环烷氧基，卤素，烷基或环烷基取代; n为0〜2的整数。

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