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公开(公告)号:US5756530A
公开(公告)日:1998-05-26
申请号:US721787
申请日:1996-09-25
申请人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
发明人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
IPC分类号: A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/505 , A61P19/02 , A61P25/04 , A61P29/00 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D231/14
CPC分类号: C07D231/12
摘要: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyclicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.
摘要翻译: 描述了一类吡唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义:其中R 1选自氢,烷基,烯基,芳烷基,炔基,氰基烷基,羧基烷基,氨基羰基烷基,芳基氨基羰基烷基,杂环烷基和烷氧基羰基烷基; 其中R3是在可取代的位置被卤素取代的芳基; 其中R 4选自氢和卤代烷基; 并且其中R 5选自烷基和氨基; 或其药学上可接受的盐或前药。
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公开(公告)号:US5580985A
公开(公告)日:1996-12-03
申请号:US535688
申请日:1995-09-28
申请人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
发明人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
IPC分类号: A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/505 , A61P19/02 , A61P25/04 , A61P29/00 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06
CPC分类号: C07D231/12
摘要: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyciicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.
摘要翻译: 描述了一类吡唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义:其中R 1选自氢,烷基,烯基,芳烷基,炔基,氰基烷基,羧基烷基,氨基羰基烷基,芳基氨基羰基烷基,杂环烷基和烷氧基羰基烷基; 其中R3是在可取代的位置被卤素取代的芳基; 其中R 4选自氢和卤代烷基; 并且其中R 5选自烷基和氨基; 或其药学上可接受的盐或前药。
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公开(公告)号:US5486534A
公开(公告)日:1996-01-23
申请号:US278297
申请日:1994-07-21
申请人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
发明人: Len F. Lee , Thomas D. Penning , Steven W. Kramer
IPC分类号: A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/505 , A61P19/02 , A61P25/04 , A61P29/00 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04
CPC分类号: C07D231/12
摘要: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyclicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.
摘要翻译: 描述了一类吡唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义:其中R 1选自氢,烷基,烯基,芳烷基,炔基,氰基烷基,羧基烷基,氨基羰基烷基,芳基氨基羰基烷基,杂环烷基和烷氧基羰基烷基; 其中R3是在可取代的位置被卤素取代的芳基; 其中R 4选自氢和卤代烷基; 并且其中R 5选自烷基和氨基; 或其药学上可接受的盐或前药。
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4.Imino pyrrolidine derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译: 可用作一氧化氮合酶抑制剂的亚氨基吡咯烷衍生物公开(公告)号:US06448286B1
公开(公告)日:2002-09-10
申请号:US09123720
申请日:1998-07-28
申请人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
发明人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
IPC分类号: A61K3154
CPC分类号: C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
摘要翻译: 本发明公开了含有用作一氧化氮合酶抑制剂的脒基衍生物的有用的药物组合物。
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5.Imidino piperidine derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译: 可用作一氧化氮合酶抑制剂的咪嘧啶哌啶衍生物公开(公告)号:US6071906A
公开(公告)日:2000-06-06
申请号:US123822
申请日:1998-07-28
申请人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
发明人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
IPC分类号: C07D207/32 , A61K31/12 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/4458 , A61K31/4468 , A61K31/451 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07C251/44 , C07D207/22 , C07D207/263 , C07D207/273 , C07D207/28 , C07D209/44 , C07D209/46 , C07D211/72 , C07D211/74 , C07D211/76 , C07D213/16 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D223/16 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06 , C07D471/08 , C07D498/04 , C07D513/04 , C07D239/02 , C07D279/04 , C07D413/02
CPC分类号: C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
摘要翻译: 本发明公开了含有用作一氧化氮合酶抑制剂的脒基衍生物的有用的药物组合物。
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公开(公告)号:US5668161A
公开(公告)日:1997-09-16
申请号:US679462
申请日:1996-07-09
申请人: John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
发明人: John J. Talley , Jeffery S. Carter , Paul W. Collins , Steven W. Kramer , Thomas D. Penning , Donald J. Rogier, Jr. , Roland S. Rogers
IPC分类号: C07D277/24 , A61K31/425 , A61K31/426 , A61K31/44 , A61P3/00 , A61P29/00 , C07D277/20 , C07D277/26 , C07D277/28 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/40 , C07D277/42 , C07D277/50 , C07D277/52 , C07D277/56 , C07D417/04 , C07D417/12
CPC分类号: C07D417/04 , C07D277/26 , C07D277/30 , C07D277/42 , C07D277/56 , C07D417/12
摘要: A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, haloalkyl, cyanoalkyl, alkylamino, aralkyl, arylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aralkylamino, aryloxyalkyl, alkoxycarbonyl, aryl optionally substituted at a substitutable position with one or more radicals selected from halo and alkoxy, and heterocyclic optionally substituted at a substitutable position with one or more radicals selected from halo and alkyl; wherein R.sup.4 is selected from alkyl and amino; and wherein R.sup.5 is selected from aryl and heteroaryl; wherein R.sup.5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl and alkoxy; provided R.sup.5 is not phenyl at position 4 when R.sup.1 is .alpha.,.alpha.-bis(trifluoromethyl)methanol and R.sup.4 is methyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 描述了一类用于治疗炎症的取代的噻唑基化合物。 化合物由式II其中R 1选自氢,烷基,卤代烷基,氰基烷基,烷基氨基,芳烷基,芳基氨基,杂芳基磺酰基烷基,杂芳基磺酰基卤代烷基,芳烷基氨基,芳氧基烷基,烷氧基羰基,任选地在可取代的位置被取代的芳基与一个或多个 选自卤素和烷氧基的基团和任选地在可取代的位置被一个或多个选自卤素和烷基的基团取代的杂环; 其中R 4选自烷基和氨基; 并且其中R 5选自芳基和杂芳基; 其中R 5任选在可取代的位置被一个或多个选自卤素,烷基和烷氧基的基团取代; 条件是当R 1为α时,R 5不在第4位为苯基,α-双(三氟甲基)甲醇,且R 4为甲基; 或其药学上可接受的盐。
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公开(公告)号:US6046211A
公开(公告)日:2000-04-04
申请号:US73929
申请日:1998-05-06
申请人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
发明人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
IPC分类号: C07D207/32 , A61K31/12 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/4458 , A61K31/4468 , A61K31/451 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07C251/44 , C07D207/22 , C07D207/263 , C07D207/273 , C07D207/28 , C07D209/44 , C07D209/46 , C07D211/72 , C07D211/74 , C07D211/76 , C07D213/16 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D223/16 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06 , C07D471/08 , C07D498/04 , C07D513/04
CPC分类号: C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
摘要翻译: 本发明公开了含有用作一氧化氮合酶抑制剂的脒基衍生物的有用的药物组合物。
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公开(公告)号:US5854234A
公开(公告)日:1998-12-29
申请号:US448473
申请日:1995-06-06
申请人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
发明人: Donald W. Hansen, Jr. , Mark G. Currie , E. Ann Hallinan , Kam F. Fok , Timothy J. Hagen , Arija A. Bergmanis , Steven W. Kramer , Len F. Lee , Suzanne Metz , William M. Moore , Karen B. Peterson , Barnett S. Pitzele , Dale P. Spangler , R. Keith Webber , Mihaly V. Toth , Mahima Trivedi , Foe S. Tjoeng
IPC分类号: C07D207/32 , A61K31/12 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/4458 , A61K31/4468 , A61K31/451 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07C251/44 , C07D207/22 , C07D207/263 , C07D207/273 , C07D207/28 , C07D209/44 , C07D209/46 , C07D211/72 , C07D211/74 , C07D211/76 , C07D213/16 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D223/16 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06 , C07D471/08 , C07D498/04 , C07D513/04 , C07D267/06 , C07D281/02
CPC分类号: C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.
摘要翻译: PCT No.PCT / US94 / 11832 Sec。 371日期:1998年6月6日 102(e)1998年6月6日PCT 1994年10月20日PCT PCT。 出版物WO95 / 11231 日期1995年04月27日本发明公开了含有用作一氧化氮合酶抑制剂的吖庚因衍生物的有用的药物组合物。
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公开(公告)号:US06951889B2
公开(公告)日:2005-10-04
申请号:US09953049
申请日:2001-09-15
申请人: Donald W. Hansen, Jr. , Ronald Keith Webber , Barnett S. Pitzele , James Sikorski , Mark A. Massa , Timothy J. Hagen , Margaret Grapperhaus , Lijuan Jane Wang , Arija A. Bergmanis , Steven W. Kramer , E. Ann Hallinan
发明人: Donald W. Hansen, Jr. , Ronald Keith Webber , Barnett S. Pitzele , James Sikorski , Mark A. Massa , Timothy J. Hagen , Margaret Grapperhaus , Lijuan Jane Wang , Arija A. Bergmanis , Steven W. Kramer , E. Ann Hallinan
IPC分类号: C07D265/32 , A61K31/198 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/08 , A61P21/04 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C229/30 , C07C237/16 , C07C257/14 , C07C259/14 , C07C271/22 , C07D271/06 , C07D271/07 , C07D413/06 , C07F7/18 , A61K31/195 , C07C251/00
CPC分类号: C07D271/07 , C07B2200/07 , C07B2200/09 , C07C229/30 , C07C257/14 , C07C259/14 , C07C271/22 , C07D413/06 , C07F7/1804
摘要: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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10.
公开(公告)号:US6043261A
公开(公告)日:2000-03-28
申请号:US199899
申请日:1998-11-25
申请人: Donald W. Hansen, Jr. , E. Ann Hallinan , Timothy J. Hagen , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Dale P. Spangler , Mihaly V. Toth , Kam F. Fok , Arija A. Bergmanis , R. Keith Webber , Mahima Trivedi , Foe S. Tjoeng , Barnett S. Pitzele
发明人: Donald W. Hansen, Jr. , E. Ann Hallinan , Timothy J. Hagen , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Dale P. Spangler , Mihaly V. Toth , Kam F. Fok , Arija A. Bergmanis , R. Keith Webber , Mahima Trivedi , Foe S. Tjoeng , Barnett S. Pitzele
IPC分类号: C07D319/06 , A61K31/045 , A61K31/12 , A61K31/15 , A61K31/165 , A61K31/19 , A61K31/35 , A61K31/351 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/42 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/55 , A61P9/00 , A61P25/00 , A61P25/30 , A61P29/00 , A61P43/00 , C07C251/44 , C07D207/22 , C07D211/72 , C07D211/76 , C07D223/10 , C07D223/12 , C07D225/02 , C07D309/06 , C07D333/16 , C07D333/20 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , C07D521/00 , A01W57/00
CPC分类号: C07D249/08 , C07D207/22 , C07D211/72 , C07D223/12 , C07D225/02 , C07D231/12 , C07D233/56 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06
摘要: The current invention discloses useful pyrrolodino imidine derivatives useful as nitric oxide synthase inhibitors.
摘要翻译: 本发明公开了可用作一氧化氮合酶抑制剂的有用的吡咯烷亚胺衍生物。
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