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11. 发明授权

US5532245A Substituted N-heteroaryl-1,2-diaminocyclobutene-3,4-dione compounds 失效
标题翻译：取代的N-杂芳基-1,2-二氨基环丁烯-3,4-二酮化合物
公开(公告)号：US5532245A
公开(公告)日：1996-07-02
申请号：US477840
申请日：1995-06-07
申请人： John A. Butera , Schuyler A. Antane , Bradford H. Hirth
发明人： John A. Butera , Schuyler A. Antane , Bradford H. Hirth
IPC分类号： C07D239/42 , A61K31/135 , A61K31/275 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/472 , A61P13/02 , A61P15/00 , A61P43/00 , C07C225/20 , C07C255/58 , C07C255/60 , C07D213/38 , C07D213/75 , C07D215/38 , C07D217/02 , C07D231/56 , C07D235/04 , C07D213/02 , A61K31/505 , C07D239/24
CPC分类号： C07D213/75 , C07C225/20 , C07C255/58 , C07C255/60 , C07C2101/04
摘要： The compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.2 is hydrogen, straight or branched chain alkyl or cyclic or bicyclic alkyl; A is selected from the following: ##STR2## wherein R.sub.9 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, mono- or dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro or iodo; n is an integer from 0 to 6; R.sub.3 and R.sub.4, independent from each other, are hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, perfluoroalkyl, hydroxyalkyl, alkoxyalkyl, fluoro, or, when taken together, form a spirocyclic ring; R.sub.5 and R.sub.6, independent from each other, are selected from the following: cyano, nitro, amino, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, mono- or dialkylamino, sulfonamide, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, carboalkoxy, hydroxyl, or hydrogen; and the pharmaceutically acceptable salts thereof relax smooth muscles.
摘要翻译：下式的化合物：其中R 1为氢，直链或支链烷基，环状或双环烷基，烷酰基，烷基磺酰基，芳酰基，芳基烯酰基，芳基磺酰基，芳基烷酰基或芳基烷基磺酰基; R2是氢，直链或支链烷基或环状或双环烷基; A选自以下：其中R9是氢，烷基，全氟烷基，烷氧基，全氟烷氧基，氨基，一烷基氨基或二烷基氨基，烷基亚磺酰氨基，烷基羧酰氨基，硝基，氰基，羧基，氯，溴，氟或碘 ; n为0〜6的整数; R 3和R 4彼此独立地是氢，直链或支链烷基，环状或双环烷基，全氟烷基，羟基烷基，烷氧基烷基，氟，或当它们一起形成螺环时; R 5和R 6彼此独立地选自：氰基，硝基，氨基，烷基，全氟烷基，烷氧基，全氟烷氧基，一烷基氨基或二烷基氨基，磺酰胺，烷基磺酰氨基，芳基亚磺酰氨基，烷基羧酰氨基，芳基羧酰氨基，烷基磺酰基，全氟烷基磺酰基，芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基，烷氧羰基，羟基或氢; 其药学上可接受的盐使平滑肌松弛。

12. 发明授权

US06451827B2 2,3,5-substituted biphenyls useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：用于治疗胰岛素抵抗和高血糖症的2,3,5-取代联苯
公开(公告)号：US06451827B2
公开(公告)日：2002-09-17
申请号：US09771469
申请日：2001-01-26
申请人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
发明人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
IPC分类号： A61K3144
CPC分类号： C07D213/40 , C07C17/16 , C07C45/68 , C07C45/71 , C07C47/575 , C07C205/35 , C07C205/37 , C07C309/77 , C07D209/08 , C07D233/54 , C07D263/58 , C07D307/58 , C07D307/80 , C07D307/81 , C07D317/54 , C07D333/74 , C07D413/12 , C07F9/4006 , C07C22/04
摘要： This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有结构的式I化合物，其中B，C，D和R 1如本说明书中所定义，或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

13. 发明授权

US5466712A Substituted n-aryl-1,2-diaminocyclobutene-3,4-diones 失效
标题翻译：取代的n-芳基-1,2-二氨基环丁烯-3,4-二酮
公开(公告)号：US5466712A
公开(公告)日：1995-11-14
申请号：US334475
申请日：1994-11-04
申请人： John A. Butera , Schuyler A. Antane , Bradford H. Hirth
发明人： John A. Butera , Schuyler A. Antane , Bradford H. Hirth
IPC分类号： C07D239/42 , A61K31/135 , A61K31/275 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/472 , A61P13/02 , A61P15/00 , A61P43/00 , C07C225/20 , C07C255/58 , C07C255/60 , C07D213/38 , C07D213/75 , C07D215/38 , C07D217/02 , C07D231/56 , C07D235/04 , C07C225/08
CPC分类号： C07D213/75 , C07C225/20 , C07C255/58 , C07C255/60 , C07C2101/04
摘要： The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##
摘要翻译：式（I）的化合物或其药学上可接受的盐是平滑肌松弛剂（I）

14. 发明授权

US5872139A Heterocyclymethylamino derivatives of cyclobutene-3,4-diones 失效
标题翻译：环丁烯-3,4-二酮的杂环甲基氨基衍生物
公开(公告)号：US5872139A
公开(公告)日：1999-02-16
申请号：US873132
申请日：1997-06-10
申请人： David R. Herbst , John A. Butera , Russell F. Graceffa
发明人： David R. Herbst , John A. Butera , Russell F. Graceffa
IPC分类号： C07D213/38 , C07D307/81 , C07D307/82 , A61K31/34 , A61K31/44 , C07D213/50
CPC分类号： C07D307/82 , C07D213/38 , C07D307/81
摘要： The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight chain alkyl, branched chain alkyl, cycloalkyl, bicycloalkyl or aralkyl, wherein the aromatic moiety of the aralkyl group may be optionally substituted with one to three straight chain alkyl, halogen, nitro, cyano, alkoxy, alkoxycarbonyl, trifluoromethyl or trifluoromethoxy groups; R.sub.3 is hydrogen, formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein n is 0 or 1; R.sub.4, R.sub.5 and R.sub.6 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkanoyl, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen; or a pharmaceutically acceptable salt thereof, relax smooth muscles.
摘要翻译：下式的化合物：其中R 1和R 2独立地是氢，直链烷基，支链烷基，环烷基，双环烷基或芳烷基，其中芳烷基的芳族部分可以任选地被一个三个直链烷基，卤素，硝基，氰基，烷氧基，烷氧基羰基，三氟甲基或三氟甲氧基; R 3是氢，甲酰基，烷酰基，烯酰基，烷基磺酰基，芳酰基，芳基烯酰基，芳基磺酰基，芳基烷酰基或芳基烷基磺酰基; A选自由以下组成的组：其中n为0或1; R 4，R 5和R 6独立地是氰基，硝基，氨基，烷基，全氟烷基，烷氧基，全氟烷氧基，烷基氨基，二烷基氨基，氨基磺酰基，烷基磺酰氨基，芳基磺酰氨基，烷基羧酰氨基，芳基羧酰氨基，烷酰基，烷基磺酰基，全氟烷基磺酰基，芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基或氢; 或其药学上可接受的盐，使平滑肌松弛。

15. 发明授权

US06765021B2 2,3,5-substituted biphenyls useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：用于治疗胰岛素抵抗和高血糖症的2,3,5-取代联苯
公开(公告)号：US06765021B2
公开(公告)日：2004-07-20
申请号：US10215438
申请日：2002-08-09
申请人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
发明人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
IPC分类号： A61K3117
CPC分类号： C07F9/4006 , C07B2200/07 , C07C17/16 , C07C45/68 , C07C45/71 , C07C47/575 , C07C205/35 , C07C205/37 , C07C225/20 , C07C233/43 , C07C235/46 , C07C235/48 , C07C235/52 , C07C237/30 , C07C255/54 , C07C271/12 , C07C271/16 , C07C271/28 , C07C271/30 , C07C309/77 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/40 , C07D233/54 , C07D263/58 , C07D295/088 , C07D295/13 , C07D307/58 , C07D307/80 , C07D307/81 , C07D317/54 , C07D333/74 , C07D413/12 , C07C22/04
摘要： This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.
摘要翻译：本发明提供具有本文定义的B，D，C和R 1结构的式I化合物。

16. 发明授权

US06214877B1 2,3,5-substituted biphenyls useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：用于治疗胰岛素抵抗和高血糖症的2,3,5-取代联苯
公开(公告)号：US06214877B1
公开(公告)日：2001-04-10
申请号：US09307850
申请日：1999-05-10
申请人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
发明人： John A. Butera , Craig E. Caufield , Russell F. Graceffa , Alexander Greenfield , Eric G. Gundersen , Lisa Marie Havran , Alan H. Katz , Joseph R. Lennox , Scott C. Mayer , Robert E. McDevitt
IPC分类号： A61K31166
CPC分类号： C07F9/4006 , C07B2200/07 , C07C17/16 , C07C45/68 , C07C45/71 , C07C47/575 , C07C205/35 , C07C205/37 , C07C225/20 , C07C233/43 , C07C235/46 , C07C235/48 , C07C235/52 , C07C237/30 , C07C255/54 , C07C271/12 , C07C271/16 , C07C271/28 , C07C271/30 , C07C309/77 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D213/40 , C07D233/54 , C07D263/58 , C07D295/088 , C07D295/13 , C07D307/58 , C07D307/80 , C07D307/81 , C07D317/54 , C07D333/74 , C07D413/12 , C07C22/04
摘要： This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有结构的式I化合物，其中B，C，D和R 1如本说明书中所定义，或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

17. 发明授权

US07879825B2 Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and methods of use thereof 失效
标题翻译： [2-（8,9-二氧代-2,6-二氮杂双环[5.2.0]壬-1（7） - 烯-2-基）烷基]膦酸的衍生物及其使用方法
公开(公告)号：US07879825B2
公开(公告)日：2011-02-01
申请号：US11757006
申请日：2007-06-01
申请人： Reinhardt B. Baudy , John A. Butera
发明人： Reinhardt B. Baudy , John A. Butera
IPC分类号： A61P25/00 , A61K31/675 , C07D223/00
CPC分类号： C07F9/645
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.
摘要翻译：提供式（I）化合物或其药学上可接受的盐，其中R 2或R 3中的至少一个不是氢。本发明的化合物是N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，可用于治疗受益于抑制NMDA受体的哺乳动物中存在的各种病症。

18. 发明授权

US5506252A Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones 失效
标题翻译：取代的N-杂芳基和N-芳基-1,2-二氨基环丁烯-3,4-二酮
公开(公告)号：US5506252A
公开(公告)日：1996-04-09
申请号：US333165
申请日：1994-10-02
申请人： John A. Butera , Schuyler A. Antane
发明人： John A. Butera , Schuyler A. Antane
IPC分类号： C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D217/02 , C07D231/56 , A61K31/135 , C07C87/50
CPC分类号： C07D217/02 , C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D231/56 , C07C2101/04 , C07C2102/42
摘要： The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is a substituted phenyl group containing one cyano substituent and one substituent selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
摘要翻译：下式的化合物：其中：R 1和R 2独立地是氢，直链或支链烷基或单或双环烷基; A是含有一个氰基取代基和一个选自氰基，硝基，烷基，全氟烷基，烷氧基，全氟烷氧基，氨基，烷基氨基，二烷基氨基，氨基磺酰基，烷基亚磺酰氨基，芳基亚磺酰氨基，烷基羧酰氨基，芳基羧酰氨基，烷基磺酰基，全氟烷基磺酰基，溴，氟，碘，1-咪唑基或羧基; 或其药学上可接受的盐是平滑肌松弛剂。

19. 发明授权

US5397790A Substituted isoquinolinyl-1-2-diaminocyclobutene-3,4,-diones 失效
标题翻译：取代的异喹啉基-1,2-二氨基环丁烯-3,4，二酮
公开(公告)号：US5397790A
公开(公告)日：1995-03-14
申请号：US259220
申请日：1994-06-13
申请人： John A. Butera , Schuyler A. Antane
发明人： John A. Butera , Schuyler A. Antane
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/472 , A61P9/08 , A61P11/08 , C07C255/50 , C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D215/42 , C07D217/02 , C07D231/56 , C07D217/12
CPC分类号： C07D217/02 , C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D231/56 , C07C2101/04 , C07C2102/42
摘要： The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; andA is an isoquinoline group which may be substituted by alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
摘要翻译：下式的化合物：其中：R 1和R 2独立地是氢，直链或支链烷基或单或双环烷基; A是可被烷基，全氟烷基，烷氧基，全氟烷氧基，氨基，烷基氨基，二烷基氨基，烷基亚磺酰氨基，烷基酰胺基，硝基，氰基或羧基取代的异喹啉基; 或其药学上可接受的盐是平滑肌松弛剂。

20. 发明授权

US5354763A Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones 失效
标题翻译：取代的N-杂芳基和N-芳基-1,2-二氨基环丁烯-3,4-二酮
公开(公告)号：US5354763A
公开(公告)日：1994-10-11
申请号：US153706
申请日：1993-11-17
申请人： John A. Butera , Schuyler A. Antane
发明人： John A. Butera , Schuyler A. Antane
IPC分类号： A61K31/395 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/472 , A61P9/08 , A61P11/08 , C07C255/50 , C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D215/42 , C07D217/02 , C07D231/56 , C07D213/02
CPC分类号： C07D217/02 , C07C255/58 , C07C311/43 , C07D213/74 , C07D215/38 , C07D215/40 , C07D231/56 , C07C2101/04 , C07C2102/42
摘要： The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is an N-heterocycle which may be substituted by alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl;or, A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl;or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
摘要翻译：下式的化合物：其中：R 1和R 2独立地是氢，直链或支链烷基或单或双环烷基; A是可被烷基，全氟烷基，烷氧基，全氟烷氧基，氨基，烷基氨基，二烷基氨基，烷基亚磺酰氨基，烷基羧酰氨基，硝基，氰基或羧基取代的N-杂环; 或者A是含有一个或两个选自氰基，硝基，烷基，全氟烷基，烷氧基，全氟烷氧基，氨基，烷基氨基，二烷基氨基，氨基磺酰基，烷基亚磺酰氨基，芳基亚磺酰氨基，烷基羧酰氨基，芳基羧酰胺基，烷基砜，全氟烷基砜，芳基砜，溴，氟，碘，1-咪唑基或羧基; 或其药学上可接受的盐是平滑肌松弛剂。

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