公开(公告)号：US4739072A

公开(公告)日：1988-04-19

申请号：US888254

申请日：1986-07-23

申请人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

发明人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

IPC分类号： C07D403/06 ,  A61K31/415 ,  C07C221/00 ,  C07C225/14 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00 ,  C07D403/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.

摘要翻译： 本发明涉及一种制备通式（I）化合物的方法，其中R1表示氢原子或C1-10烷基，C3-7环烷基，C3-7环烷基 - （C1- 4）烷基，C 3-6烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基，并且由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3 -7环烷基，C 2-6烯基或苯基 - （C 1-3）烷基，其它可以相同或不同的两个基团表示氢原子或C 1-6烷基; 或其盐或被保护的衍生物，通过使通式（II）化合物（II）其中R 1，R 2，R 3和R 4如上所定义的化合物或其盐或其保护的衍生物环化。 式（I）化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂。

公开(公告)号：US4855314A

公开(公告)日：1989-08-08

申请号：US1469

申请日：1987-01-08

申请人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb ,  Michael D. Dowle ,  Keith Mills ,  Colin D. Eldred

发明人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb ,  Michael D. Dowle ,  Keith Mills ,  Colin D. Eldred

IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16

CPC分类号： C07D209/16

摘要： Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 is halogen, a C.sub.1-3 alkoxy, R.sub.6 R.sub.7 NCO(CH.sub.2).sub.p --, R.sub.6 CONH(CH.sub.2).sub.p --, R.sub.6 R.sub.7 NSO.sub.2 (CH.sub.2).sub.p --, or R.sub.8 SO.sub.2 NH(CH.sub.2).sub.p -- (where R.sub.6 and R.sub.7 each represents hydrogen or C.sub.1-3 alkyl, R.sub.8 represents C.sub.1-3 alkyl and p is zero or 1);R.sub.2 represents hydrogen or C.sub.1-3 alkyl; R.sub.3 represents hydrogen or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 each represents hydrogen, C.sub.1-3 alkyl or 2-propenyl;A represents --CO-- or --SO.sub.2 --;n represents an integer from 2 to 5; and m represents zero or an integer from 1 to 4; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with physiologically acceptable carriers or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.

公开(公告)号：US5389659A

公开(公告)日：1995-02-14

申请号：US666746

申请日：1991-03-08

申请人： Barry C. Ross ,  David Middlemiss ,  Colin D. Eldred ,  John G. Montana ,  Pritom Shah

发明人： Barry C. Ross ,  David Middlemiss ,  Colin D. Eldred ,  John G. Montana ,  Pritom Shah

IPC分类号： A61K31/415 ,  A61P5/38 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P27/02 ,  A61P43/00 ,  C07C45/45 ,  C07C49/175 ,  C07C49/213 ,  C07C49/255 ,  C07C59/29 ,  C07C63/331 ,  C07C65/30 ,  C07C205/45 ,  C07C271/06 ,  C07C311/08 ,  C07D231/12 ,  C07D231/14 ,  C07D257/04 ,  C07D403/10 ,  A61K31/41

CPC分类号： C07D231/12 ,  C07C205/45 ,  C07C45/455 ,  C07C49/175 ,  C07C49/255 ,  C07D231/14 ,  C07D403/10

摘要： The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

摘要翻译： 本发明提供了通式（I）的化合物：其中（I）或其生理学上可接受的盐，溶剂合物（例如水合物）或其代谢不稳定的酯。 该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

公开(公告)号：US5252593A

公开(公告)日：1993-10-12

申请号：US883380

申请日：1992-05-15

申请人： Barry C. Ross ,  David Middlemiss ,  David I. C. Scopes ,  Torquil I. M. Jack ,  Kevin S. Cardwell ,  Michael D. Dowle ,  Colin D. Eldred ,  John G. Montana ,  Pritom Shah ,  Stephen P. Watson

发明人： Barry C. Ross ,  David Middlemiss ,  David I. C. Scopes ,  Torquil I. M. Jack ,  Kevin S. Cardwell ,  Michael D. Dowle ,  Colin D. Eldred ,  John G. Montana ,  Pritom Shah ,  Stephen P. Watson

IPC分类号： A61K31/415 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/18 ,  A61P25/28 ,  C07D405/06 ,  C07D405/14 ,  A61K31/41 ,  C07D405/02

CPC分类号： C07D405/06 ,  C07D405/14

摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.