Abstract: 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[3,4-b]indole nucleus or having said radical attached to the 1 position of a pyrano[4,3-b]indole or thiopyrano[4,3-b]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.
Type:
Grant
Filed:
March 5, 1975
Date of Patent:
January 18, 1977
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Christopher A. Demerson, Lesie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
Abstract: Indenopyran- and indenothiopyranalkylamine derivatives characterized by having an amino(lower)alkyl radical attached to the 1 position of an indeno[2,1-c]pyran or indeno[2,1-c]thiopyran nucleus are disclosed. Also included are the corresponding derivatives having an indeno[1,2-c]pyran and an indeno[1,2-c]-thiopyran nucleus. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incoporated into a heterocyclic amine radical. The derivatives are further substituted at position 1 and may be 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.
Type:
Grant
Filed:
May 19, 1975
Date of Patent:
November 30, 1976
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Ivo Jirkovsky, Leslie G. Humber, Christopher A. Demerson, Thomas A. Dobson
Abstract: Antibiotic rapamycin is producible by culturing Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium. Rapamycin has antifungal properties. Methods for its preparation and use are disclosed.
Type:
Grant
Filed:
September 25, 1975
Date of Patent:
November 23, 1976
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Surendra N. Sehgal, Teodora M. Blazekovic, Claude Vezina
Abstract: Octahydrobenzo[6,7]- (or [5,6]-) cyclohepta-[1,2,3-de]pyride- (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.
Type:
Grant
Filed:
October 29, 1974
Date of Patent:
October 12, 1976
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Francois T. Bruderlein, Leslie G. Humber
Abstract: A new antibiotic complex, complex 484, components 484-A and 484-B thereof and a process for their preparation are disclosed. These antibiotic substances are producible by culturing a microorganism of the species Streptomyces in an aqueous nutrient medium under submerged aerobic fermentation conditions. The substances are useful against a broad spectrum of pathogenic bacteria. Methods for their use are disclosed also.
Type:
Grant
Filed:
June 26, 1975
Date of Patent:
September 28, 1976
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Surendra N. Sehgal, Kartar Singh, Claude Vezina
Abstract: 1,3-Dihydropyrrolo[4,3,2-de]isoquinoline derivatives characterized by an amino or hydrazino substituent at position 5 are disclosed. Also included are the related 4,6-dihydropyrrolo[4,3,2-de]-s-triazolo[3,4-a]isoquinoline and its 8-methyl derivative. The compounds are antidepressant and antihypertensive agents. Methods for their preparation and use are disclosed.
Type:
Grant
Filed:
May 19, 1975
Date of Patent:
August 31, 1976
Assignee:
Ayerst, McKenna and Harrison Ltd.
Inventors:
Adolf H. Philipp, Christopher A. Demerson, Leslie G. Humber
Abstract: 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 derivatives are also disclosed.
Type:
Grant
Filed:
May 28, 1974
Date of Patent:
June 8, 1976
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Christopher A. Demerson, Leslie G. Humber, George Santroch, Thomas A. Dobson, Ivo Jirkovsky
Abstract: 1,3,4,5-Tetrahydropyrrolo[4,3,2-de]isoquinoline and its N-alkyl derivatives are disclosed. The compounds are antidepressant and antihypertensive agents. Methods for their preparation and use are disclosed.
Type:
Grant
Filed:
November 6, 1973
Date of Patent:
April 13, 1976
Assignee:
Ayerst, McKenna and Harrison Ltd.
Inventors:
Adolf H. Philipp, Christopher A. Demerson, Leslie G. Humber