公开(公告)号：US5380854A

公开(公告)日：1995-01-10

申请号：US92402

申请日：1993-07-14

申请人： Jeffrey L. Romine ,  Nicholas A. Meanwell ,  Scott W. Martin

发明人： Jeffrey L. Romine ,  Nicholas A. Meanwell ,  Scott W. Martin

IPC分类号： C07D263/32 ,  C07D263/34 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC分类号： C07D263/34 ,  C07D263/32 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## or pharmaceutically acceptable salt thereof.

摘要翻译： 公式I r Th中公开了一系列具有增强的水溶性生物利用度和代谢稳定性的恶唑衍生物。 R2是H，CN，CO2R3或OR3; 且R 3为H或C 1 -C 4低级烷基; 或其药学上可接受的盐。

公开(公告)号：US06077861A

公开(公告)日：2000-06-20

申请号：US197887

申请日：1998-11-23

申请人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

发明人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

IPC分类号： C07D271/02 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/4245 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P43/00 ,  C07D233/32 ,  C07D233/54 ,  C07D233/64 ,  C07D233/70 ,  C07D233/74 ,  C07D233/76 ,  C07D235/12 ,  C07D249/08 ,  C07D249/12 ,  C07D249/14 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D413/10

CPC分类号： C07D263/58 ,  C07D233/64 ,  C07D233/70 ,  C07D233/76 ,  C07D235/12 ,  C07D249/12 ,  C07D249/14 ,  C07D271/113 ,  C07D413/10

摘要： Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, NO.sub.2, or ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.g, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.

摘要翻译： 式1的新型化合物可用于治疗对大电导钙激活钾通道的开放剂起反应的病症：其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; R a，R b和R c各自独立地选自氢，卤素，OH，CF 3，NO 2，或者R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶-2-基的杂环部分; Rd和Re各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自O或1的整数; Rf和Rg各自独立地为氢; C 1-4烷基; 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。

公开(公告)号：US5254576A

公开(公告)日：1993-10-19

申请号：US862680

申请日：1992-04-03

申请人： Jeffrey L. Romine ,  Nicholas A. Meanwell ,  Scott W. Martin

发明人： Jeffrey L. Romine ,  Nicholas A. Meanwell ,  Scott W. Martin

IPC分类号： C07D263/32 ,  C07D263/34 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  A61K31/54 ,  A61K31/535

CPC分类号： C07D263/34 ,  C07D263/32 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## X is ##STR2## R is CH.sub.2 R.sup.2, H; R.sup.1 is Ph or Th;R.sup.2 is ##STR3## H, CN, CO.sub.2 R.sup.3, or OR.sup.3 ; and R.sup.3 is H, or C.sub.1 -C.sub.4 lower alkyl;or pharmaceutically acceptable salt thereof.

摘要翻译： 在式I中公开了一系列具有增强的水溶性生物利用度和代谢稳定性的恶唑衍生物，其中R是CH 2 R 2，H; R1为Ph或Th; R2是H，CN，CO2R3或OR3; 且R 3为H或C 1 -C 4低级烷基; 或其药学上可接受的盐。

公开(公告)号：US06479482B2

公开(公告)日：2002-11-12

申请号：US09852983

申请日：2001-05-10

申请人： Graham S. Poindexter ,  Marc Bruce ,  Sing-Yuen Sit ,  Scott W. Martin

发明人： Graham S. Poindexter ,  Marc Bruce ,  Sing-Yuen Sit ,  Scott W. Martin

IPC分类号： C07D41714

CPC分类号： C07D401/12 ,  C07D211/90

摘要： A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

摘要翻译： 已经合成了一系列NPY的非肽能拮抗剂，其由式1的4-苯基-1,4-二氢吡啶的氨基和哌嗪衍生物组成。其中X是NPY诱导行为的CH或NAs拮抗剂，这些化合物是 预期在促进减肥和治疗进食障碍中起到有效的厌氧剂的作用。

公开(公告)号：US5869509A

公开(公告)日：1999-02-09

申请号：US902684

申请日：1997-07-30

申请人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

发明人： Jeffrey L. Romine ,  Scott W. Martin ,  Piyasena Hewawasam ,  Nicholas A. Meanwell ,  Valentin K. Gribkoff ,  John E. Starrett, Jr.

IPC分类号： C07D271/02 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/4245 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P43/00 ,  C07D233/32 ,  C07D233/54 ,  C07D233/64 ,  C07D233/70 ,  C07D233/74 ,  C07D233/76 ,  C07D235/12 ,  C07D249/08 ,  C07D249/12 ,  C07D249/14 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D413/10 ,  A61K31/42 ,  A61K31/425 ,  C07D271/06

CPC分类号： C07D263/58 ,  C07D233/64 ,  C07D233/70 ,  C07D233/76 ,  C07D235/12 ,  C07D249/12 ,  C07D249/14 ,  C07D271/113 ,  C07D413/10

摘要： Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol- 2-yl, and pyridinyl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.g, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.

摘要翻译： 式1的新型化合物可用于治疗对大电导钙激活钾通道的开放剂起反应的病症：其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; Ra，Rb和Rc各自独立地选自氢，卤素，OH，CF 3，提供的R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶基的杂环部分。 Rd和Re各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自O或1的整数; Rf和Rg各自独立地为氢; C 1-4烷基; 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。