公开(公告)号：US4880801A

公开(公告)日：1989-11-14

申请号：US198971

申请日：1988-05-26

申请人： John Kitchin ,  Peter C. Cherry ,  Adrian J. Pipe ,  Andrew J. Crame ,  Alan D. Borthwick

发明人： John Kitchin ,  Peter C. Cherry ,  Adrian J. Pipe ,  Andrew J. Crame ,  Alan D. Borthwick

IPC分类号： A61K31/40 ,  A61P1/12 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  A61P7/02 ,  A61P9/12 ,  A61P25/04 ,  A61P25/06 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D319/20 ,  C07D491/04 ,  C07D491/056

CPC分类号： C07D491/04 ,  C07D319/20

摘要： Compounds of the general formula (I) ##STR1## (R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO, R.sup.1 and R.sup.2 are independently halogen, alkyl, alkoxy, hydroxyl, cyano, nitro or --NR.sup.3 R.sup.4 where R.sup.3 and R.sup.4 are independently H or alkyl and R.sup.2 may be H) and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action.The compounds may be prepared by amination of compounds of the general formula (II) ##STR2## (where R.sup.1 and R.sup.2 are as defined above and X is a leaving group.

公开(公告)号：US4496579A

公开(公告)日：1985-01-29

申请号：US545191

申请日：1983-10-25

申请人： Andrew J. Crame ,  Alan D. Borthwick

发明人： Andrew J. Crame ,  Alan D. Borthwick

IPC分类号： A61K31/40 ,  A61P1/00 ,  A61P1/10 ,  A61P1/14 ,  A61P3/04 ,  A61P3/08 ,  A61P7/02 ,  A61P9/12 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D317/22 ,  C07D319/20 ,  C07D491/04 ,  C07D491/056 ,  C07D209/48

CPC分类号： C07D491/04 ,  C07C309/00 ,  C07D317/22 ,  C07D319/20

摘要： Compounds are disclosed of general formula ##STR1## where R is H, C.sub.1-6 alkyl optionally substituted by C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl or alkynyl, C.sub.3-7 cycloalkyl, aralkyl or --CHOand the physiologically acceptable salts thereof. The compounds have selective .alpha..sub.2 -adrenoreceptor antagonist action and are indicated as potentially useful for the treatment or prevention of migraine, thrombosis, diabetes, obesity, hypertension, constipation, paralytic ileus, senile dementia and analepsis, and for use in appetite suppression and for the treatment of depression; they may be formulated as pharmaceutical compositions in conventional manner. The compounds may be prepared, for example, by amination of a compound of formula ##STR2## where X is a leaving group such as halogen or a hydrocarbylsulphonyloxy group.

摘要翻译： 公开了通式为“IMAGE”的化合物，其中R为H，任选被C 3-7环烷基，C 3-6烯基或炔基取代的C 1-6烷基，C 3-7环烷基，芳烷基或-CHO及其生理上可接受的盐。 这些化合物具有选择性的α2-肾上腺素受体拮抗剂作用，并且被认为可能用于治疗或预防偏头痛，血栓形成，糖尿病，肥胖，高血压，便秘，麻痹性肠梗阻，老年痴呆和分析，并且用于食欲抑制和 治疗抑郁症; 它们可以以常规方式配制成药物组合物。 化合物可以例如通过胺化式（VI）的化合物来制备，其中X是离去基团如卤素或烃基磺酰氧基。