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Assignee: Ayerst McKenna and Harrison Ltd.


Location: Montreal, CA
No. of patents: 25

NumberTitleIssue Date
4252795N-substituted dimeric cyclopeptide derivatives and preparation thereof
The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R1 is lower alkyl, phenyl or pheny(lower) alkylene; R2 is lower alkyl, cyclo(lower)al...
02/24/1981
4244947Carba decapeptide derivatives of [TYR6 ]-somatostatin
Peptides of formula I ##STR1## in which X is (CH2)2, S--CH2 or CH2 --S or a therapeutically acceptable acid addition salt thereof are disclosed. The peptides of formula I are useful as agents for the treatm...
01/13/1981
4170653Antidepressant naphthyloxy piperidino and pyrrolidino propanol ethers
Disclosed herein are compounds of the formula ##STR1## in which Ar is phenyl or 1-naphthyl; R1 is hydrogen or lower alkyl; and R2 and R3 together with the nitrogen atom to which they are joined form a heterocyclic ami...
10/09/1979
4071552Aryloxy aminobutanols, their preparation and use thereof
Disclosed herein are compounds of the formula ##STR1## in which Ar is phenyl or 1-naphthyl; R1 is hydrogen or lower alkyl; and R2 and R3 are either the same or different selected from the group consisting of hydrogen ...
01/31/1978
4066763Thiazinoindoles useful as antidepressants
Thiazinoindole derivatives characterized by having an amino(lower)alkyl radical attached to the 1 position of a 1H-1,4-thiazino[4,3-a]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or t...
01/03/1978
4066780Pyranoindole derivatives as antiulcer agents
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 positio...
01/03/1978
4062851Process for the resolution of certain octahydrobenzocycloheptapyridoisoquinolinols
An efficient, commercially feasible process for the resolution of the organic bases, (&#b1;)-(4a,13b-trans)-(3-hydroxy,13b-trans)-3-isopropyl-2,3,4,4a,8,9,13b,1 4-octahydro-1H-benzo[6,7]cyclohepta[1,2,-3-de)pyrido[2,1-a]isoquinolin-3-ol and (&#b1...
12/13/1977
40606133-Aryloxy-2(4-loweralkyl-1-piperazinyl)propanols, their alkylethers, and use thereof
Disclosed herein are compounds of the formula ##STR1## in which Ar is phenyl or 1-naphthyl; R1 is hydrogen or lower alkyl; and R2 and R3 together with the nitrogen atom to which they are joined form a hyterocyclic ami...
11/29/1977
40606191,4-Dihydro-4-oxo-benzothiopyrano (4,3-b)pyridine-2-carboxylates and derivatives
Compounds of formula 1 ##STR1## in which R1, R2, R3 and R4 are the same or different selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy, or R1...
11/29/1977
4059585Process for preparing an intermediate for CNS depressants
Disclosed is a process for preparing (4a,13b-trans)-1,2,4,4a,8,9,13b,14-octahydro-3H-benzo[6,7]cyclohepta[1,2,3 -de]-pyrido[2,1-a]isoquinolin-3-one involving a 1,3-cycloaddition of a 4-halo-1-butene to 1,7,8,12b-tetrahydrobenzo[1,2]cyclohepta-[3,4,5-d...
11/22/1977
4056537Process for making pyrano- and thiopyranoindole derivatives
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 are disclosed. The amino portion of the amino(lo...
11/01/1977
4041169Pharmaceutical method for using pyrano-and thiopyranoindole derivatives
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 positio...
08/09/1977
4036856Cyclopentanone derivatives
A process for preparing 11-deoxyprostaglandin E1, E2 and E3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared ...
07/19/1977
4035495Pyrrolobenzoxazines, pyrrolobenzothiazines and process therefor
4H-Pyrrolo[2,1-c][1,4]benzoxazines and 4H-pyrrolo[2,1-c]-[1,4]benzothiazines characterized by having an alkylamine substituent at position 4 are disclosed. The compounds are characterized further by having an alkyl substituent on the same carbon atom...
07/12/1977
4020157Shortened analogs of somatostatin
Compounds of the formula 1 or 1a ##STR1## In which R is hydrogen or NHR1 in which R1 is lower aliphatic acyl containing from 1 - 6 carbon atoms or benzoyl, and pharmaceutically acceptable salts thereof are disclosed. The compounds of...
04/26/1977
4018912Tripeptide derivatives with central nervous system activity and preparation thereof
The tripeptide derivatives of formula 1 in which R1 is hydrogen, lower alkyl or NR4 R5 wherein R4 and R5 each are lower alkyl, R2 is hydrogen or lower alkyl, R3 is amino, lower alkyla...
04/19/1977
4006136Prostaglandin intermediates
A process for preparing 11-deoxyprostaglandin E1, E2 and E3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared ...
02/01/1977
4003902Naphthyridinomycin antibiotics
Naphthyridinomycin complex, a major component thereof called naphthyridinomycin A and a minor component thereof called naphthyridinomycin B are disclosed. These antibiotic substances exhibit antibacterial activity. The substances are producible by culturi...
01/18/1977
4004027Prostaglandin antagonists
2-(1-Hydroxy-2-octynyl)- and 2-(3-hydroxy-1-octynyl)-5-oxocyclopentaneheptanoic acids, their salts and their corresponding lower alkyl esters are disclosed. The compounds inhibit the actions of prostaglandins. Methods for their preparation and use ar...
01/18/1977
4003913Pyrano- and thiopyranoindole derivatives, compositions and methods of use
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 positio...
01/18/1977
3995052Indenopyran- and indenothiopyranalkylamines III in the treatment of depression
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 derivative...
11/30/1976
3993749Rapamycin and process of preparation
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....
11/23/1976
3985751Benzocycloheptaisoquinoline derivatives
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, pip...
10/12/1976
3983231Antibiotic substances and preparation
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 ...
09/28/1976
3962236Oxazinoindole- and thiazinoindole derivatives
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...
06/08/1976
 
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