公开(公告)号：US3852452A

公开(公告)日：1974-12-03

申请号：US24283972

申请日：1972-04-10

申请人： AYERST MCKENNA & HARRISON

发明人： BRUDERLEIN F ,  HUMBER L

IPC分类号： A61K31/47 ,  C07C233/02 ,  C07D211/76 ,  C07D455/03 ,  C07D455/04 ,  C07D471/06 ,  A61K27/00

CPC分类号： C07D455/00 ,  A61K31/47 ,  C07C233/02 ,  C07D211/76 ,  C07D455/04 ,  C07D471/06

摘要： Octahydrobenzo(6,7)- (or (5,6)-) cyclohepta-(1,2,3-de)pyrido(or pyrrolo-) (2,1-a)isoquinolines, and decahydrobenzo(6,7)- (or (5,6)-) cyclohepta(1,2,3-de)-azepino(2,1-a)isoquinolines and derivatives thereof, optionally substituted on the pyrrolidine, piperidine or azepine ring. The compounds are useful CNS depressants, anticonvulsant and antiinflammatory agents, and methods for their preparation and use are also disclosed.

摘要翻译： 八氢苯并[6,7] - （或[5,6] - ）环庚氨酸 - [1,2,3-de]吡啶并（或吡咯并）[2,1-a]异喹啉和十氢苯并[6,7] - （或[5,6] - ）环庚并[1,2,3-de] azepino [2,1-a]异喹啉及其衍生物，任选在吡咯烷，哌啶或吖庚因环上取代。 这些化合物是有用的CNS抑制剂，抗惊厥药和抗炎药，并且还公开了它们的制备和使用方法。

公开(公告)号：US3852285A

公开(公告)日：1974-12-03

申请号：US21762772

申请日：1972-01-13

申请人： AYERST MCKENNA & HARRISON

发明人： DEMERSON C ,  HUMBER L ,  DOBSON T ,  ASSELIN A ,  JIRKOVSKY I

IPC分类号： C07D209/08 ,  C07D87/46

CPC分类号： C07D209/08 ,  Y10S514/925

摘要： Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano(3,4-b)indole or thiopyrano(3,4b)indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4, 5, 6, 7, 8 and 9. The derivatives having the amino(lower)alkyl radical only at position 9 possess two substitutents at position 1 and may be optionally substituted at position 3, 4, 5, 6, 7, and 8. The derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3,4,5, 6, 7 and 8. The pyrano- and thiopyranoindole derivatives of this invention are useful antidepressant and antiulcer agents. Methods for the preparation and use of these derivatives are also disclosed.

摘要翻译： 公开了以吡喃并吲哚和噻喃并吲哚衍生物为特征的具有连接于吡喃并[3,4-b]吲哚或噻喃并[3,4-b]吲哚核的1位和9位的氨基（低级）烷基。 氨基（低级）烷基的氨基部分可进一步被一个或两个低级烷基取代或并入杂环胺基中。 仅在位置1具有氨基（低级）烷基的衍生物在1位进一步被取代，并且可以在3,4,5,6,7,8和9位任意被取代。具有氨基（低级）烷基 仅在位置9的基团在位置1具有两个取代基，并且可以任选地在3,4,5,6,7和8位被取代。具有位置1和9的氨基（低级）烷基的衍生物被进一步取代 在位置1，并且可以任选地在3,4,5,6,7和8位被取代。本发明的吡喃和噻喃并吲哚衍生物是有用的抗抑郁剂和抗溃疡剂。 还公开了这些衍生物的制备和使用方法。

公开(公告)号：US3833575A

公开(公告)日：1974-09-03

申请号：US22628772

申请日：1972-02-14

申请人： AYERST MCKENNA & HARRISON

发明人： DEMERSON C ,  DOBSON T ,  JIRKOVSKY I ,  HUMBER L ,  SANTROCH G

IPC分类号： C07D209/08 ,  C07D87/38

CPC分类号： C07D209/08 ,  Y10S514/925

摘要： OXAZINOINDOLE DERIVATIVES CHARACTERIZED BY HAVING AN AMINO(LOWER)ALKYL RADICAL ATTACHED TO THE 1 POSITION OF A 1H-1,4-OXAZINO(4,3-A)INDOLE NUCLEUS ARE DISCLOSED. THE AMINO PORTION OF THE AMINO(LOWER)ALKYL RADICAL MAY BE FURTHER SUBSTITUTED WITH ONE OR TWO LOWER ALKYL GROUPS OR INCORPORATED IN A HETEROCYCLIC AMINE RADICAL. THE DERIVATIVES ARE SUBSTITUTED FURTHER AT POSITIONS 1 AND 10 AND MAY BE OPTIONALLY SUBSTITUTED AT POSITIONS 3. 4, 6, 7, 8 AND 9. THE OXAZINOINDOLE DERIVATIVES OF THIS INVENTION ARE USEFUL ANTIDEPRESSANT AND ANTIULCER AGENTS. METHODS FOR THE PREPARATION AND USE OF THESE DEIVATIVES ARE ALSO DISCLOSED.

公开(公告)号：US3778449A

公开(公告)日：1973-12-11

申请号：US3778449D

申请日：1972-10-12

申请人： AYERST MCKENNA & HARRISON

发明人： DEMERSON C ,  DOBSON T ,  JIRKOVSKY I ,  HUMBER L

IPC分类号： C07C33/38 ,  A61K27/00 ,  C07D7/18 ,  C07D65/04

CPC分类号： C07C33/38

摘要： INDENOPYRAN- AND INDENOTHIOPYRANALKYLAMINE DERIVATIVES CHARACTERIZED BY HAVING AN AMINO (LOWER) ALKYL RADICAL ATTACHED TO HE 1 POSITION OF A INDENO(2,1-C)PYRAN OR INDENO(2,1-C)THIOPYRAN NUCLEUS ARE DISCLOSED. THE AMINO PORTION OF THE AMINO(LOWER) ALKYL RADICAL MAY BE FURTHER SUBSTITUTED WITH ONE OR TWO LOWER ALKYL GROUPS OR INCORPORATED INTO A HETEROCYCLIC AMINE RADICAL. THE DERIVATIVES ARE FURTHER SUBSTITUTED AT POSITION 1 AND MAYBE OPTIONALLY SUBSTITUTED AT POSITIONS 3, 4, 5, 6, 7, 8, AND 9. THE INDENOPYRAN- AND INDENOTHIOPYRANALKYLAMINE DERIVATIVES OF THIS INVENTION ARE USEFUL ANTIDEPRESSANT AGENTS. METHODS FOR THEIR PREPARATION AND USE ARE DISCLOSED.