Abstract: Herein is disclosed 2H-benzothieno[3,2-c]pyrazol-3-amine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for producing analgesia in a mammal. In addition, some of the derivatives are useful for inhibiting gastric acid secretion, convulsions, anxiety and aggression, and producing muscle relaxation, hypnosis and sedation in a mammal.
Type:
Grant
Filed:
May 24, 1982
Date of Patent:
February 14, 1984
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Adolf Philipp, Ivo Jirkovsky, Rene Martel
Abstract: Disclosed are new methods of using 1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
Type:
Grant
Filed:
August 17, 1981
Date of Patent:
December 27, 1983
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Dushan M. Dvornik, Nicole Simard-Duquesne
Abstract: Disclosed are new methods of using 5-fluoro-2-methyl-1-[[4-(methylthio)phenyl]methylene]-1H-indene-3-acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
Type:
Grant
Filed:
December 21, 1981
Date of Patent:
December 27, 1983
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Dushan M. Dvornik, Nicole Simard-Duquesne
Abstract: Disclosed are new methods of using 5-fluoro-2-methyl-1-[[4-(methylsulfonyl)phenyl]methylene]-1H-indene-3-acet ic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
Type:
Grant
Filed:
December 21, 1981
Date of Patent:
December 27, 1983
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Dushan M. Dvornik, Nicole Simard-Duquesne
Abstract: Aldose reductase inhibitors of the formula ##STR1## wherein R.sup.1 and R.sup.2 each is lower alkyl, or a therapeutically acceptable salt thereof with an organic or inorganic base, are useful for treating diabetic complications.
Type:
Grant
Filed:
November 13, 1981
Date of Patent:
July 5, 1983
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Francesco Bellini, Kazimir Sestanj, Leslie G. Humber
Abstract: Herein disclosed are N-(naphthalenylthioxomethyl)aminoacid derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
Type:
Grant
Filed:
November 13, 1981
Date of Patent:
July 5, 1983
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
Abstract: Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is CH.sub.2 COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl; R.sup.2 is COOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl; and R.sup.3 is lower alkoxy, benzyloxy or CH.sub.2 COOR.sup.6 wherein R.sup.6 is hydrogen or lower alkyl; with the provisos that when R.sup.4 is hydrogen then R.sup.5 and R.sup.6 is hydrogen; and that when R.sup.4 is lower alkyl then R.sup.5 and R.sup.6 are lower alkyl with R.sup.4 and R.sup.6 being the same lower alkyl; are useful for treating diabetic complications.
Type:
Grant
Filed:
August 21, 1981
Date of Patent:
May 3, 1983
Assignee:
Ayerst, McKenna & Harrison, Inc.
Inventors:
Bozidar Palameta, Tibor Bogri, Jehan Bagli
Abstract: Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is COOH and R.sup.2 is hydrogen, 8-halo or 6-hydroxy, or R.sup.1 is CON(R.sup.3)-CH.sub.2 COOH wherein R.sup.3 is lower alkyl and R.sup.2 is hydrogen or 8-halo are useful for treating diabetic complications.
Type:
Grant
Filed:
August 21, 1981
Date of Patent:
April 26, 1983
Assignee:
Ayerst, McKenna & Harrison, Inc.
Inventors:
Bozidar Palameta, Tibor Bogri, Jehan Bagli
Abstract: Antibiotic AY24,668 is producible by culturing Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium. AY24,668 has antifungal properties. Methods for its preparation and use are disclosed.
Abstract: Ravidomycin is produced by culturing Streptomyces ravidus NRRL 11,300 in an aqueous nutrient medium. Ravidomycin is useful as an antibacterial and antitumor agent. Methods for its preparation and use are disclosed.
Abstract: Herein are disclosed compounds of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl or --(CH.sub.2).sub.m --NR.sup.4 R.sup.5 wherein m is an integer from 2 to 6 and R.sup.4 and R.sup.5 each is hydrogen or lower alkyl; R.sup.2 is hydrogen, bromo or chloro; and R.sup.3 is hydrogen or halo; with the requirement that when R.sup.2 is bromo or chloro, then R.sup.3 is bromo or chloro or a therapeutically acceptable salt thereof. The compounds inhibit lens aldose reductase in a diabetic mammal.
Abstract: Disclosed are new methods of using .gamma.-oxo-8-fluoranthenebutanoic acid, or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
Type:
Grant
Filed:
August 17, 1981
Date of Patent:
November 30, 1982
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Dushan M. Dvornik, Nicole Simard-Duquesne
Abstract: Disclosed herein are 1,2-dihydro-2-oxo(or 2-thioxo)cyclohepta[b]-pyrrole-1-acetic acid derivatives having optional substitution at positions 3, on the cycloheptatriene ring and on the acetic acid side chain. The compounds are aldose reductase inhibitors and thus are useful for treating diabetic complications.
Type:
Grant
Filed:
August 21, 1981
Date of Patent:
June 29, 1982
Assignee:
Ayerst, McKenna & Harrison Inc.
Inventors:
Adi Treasurywala, Bozidar Palameta, Tibor Bogri, Jehan Bagli
Abstract: Herein is described a method of treating benign prostatic hyperlasia without affecting testicular weight in a male mammal by administering an effective amount of gonadorelin.
Abstract: Disclosed are monoacyl and diacyl derivatives of rapamycin, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful, inter alia, as antifungal antibiotics.
Abstract: This invention discloses novel 1-oxo-5H-pyrimidol[2,1-c][1,4]benzoxa(or thia)zinc-2-carboxylic acid lower alkyl esters, derivatives thereof, process for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful in the treatment of anaphylactic reactions and allergic conditions in a mammal.
Abstract: Disclosed are new methods of using (Z)-5-fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-1H-indene-3- acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
Type:
Grant
Filed:
June 19, 1980
Date of Patent:
December 22, 1981
Assignee:
Ayerst, McKenna & Harrison, Inc.
Inventors:
Dushan M. Dvornik, Nicole Simard-Duquesne
Abstract: Herein is disclosed ethanocarbazole derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful for treating depression in a mammal and are represented by the following formula ##STR1## in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 and R.sup.3 each is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom form a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-morpholinyl or 4-thiomorpholinyl ring, and m is an integer from 0 to 3.
Abstract: 3-Oxo-5H-pyrimido[2,1-c][1,4]benzoxazine derivatives, optionally substituted with a hydroxymethyl, carboxy or loweer alkoxycarbonyl at position 1 and optionally substituted at positions 8 or 9, with a lowr alkyl or halo are disclosed. The derivatives are antiallergy agents and methods for their preparation and use are given.