Patents Assigned to Ayerst McKenna and Harrison Inc.
  • Patent number: 5206018
    Abstract: This invention provides a method of treating, inhibiting the proliferation of, reducing the size of, or eradicating malignant neoplasms in a mammal in need thereof which comprises administering an antineoplastic amount of rapamycin to said mammal. In particular, rapamycin is useful in treating, inhibiting the proliferation of, reducing the size of, or eradicating malignant mammary and skin carcinomas, and central nervous system neoplasms.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: April 27, 1993
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Surendra N. Sehgal, Claude Vezina
  • Patent number: 4946987
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating, diabetic complications.
    Type: Grant
    Filed: June 20, 1988
    Date of Patent: August 7, 1990
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4705882
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: March 28, 1986
    Date of Patent: November 10, 1987
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4604406
    Abstract: Disclosed herein are new aldose reductase inhibitors of the formula ##STR1## wherein n is an integer from 1 to 5 and X is a chalcogen, and methods of preparation. The derivatives are useful for treating or preventing diabetic complications.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: August 5, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Francesco Bellini, Kazimir Sestanj
  • Patent number: 4600724
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: July 17, 1985
    Date of Patent: July 15, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4568693
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: September 9, 1983
    Date of Patent: February 4, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4522946
    Abstract: 1,2,3,7,8,12b-Hexahydrobenzo[6,7]cyclohepta[1,2,3-de]isoquinoline derivatives, characterized by having two adjacent oxy substituents at positions 4 and 5 or at positions 5 and 6, are disclosed. Thus, the substituent at position 5 is lower alkoxy or hydroxy and the substituents at positions 4 and 6 are different and are hydrogen or hydroxy. The derivatives are neuroleptic agents, free of extrapyramidal side effects. Methods for the preparation and for the use of the derivatives also are disclosed.
    Type: Grant
    Filed: June 13, 1983
    Date of Patent: June 11, 1985
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4510157
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: April 9, 1985
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4499310
    Abstract: A process and intermediates for preparing 6-(lower alkoxy)-5-(trifluoromethyl)-1-naphthalenecarboxylic acid derivatives are disclosed. The derivatives are useful for preparing aldose reductase inhibitors. With reference to the process, 1,1,1-trifluoro-5-(2-methylphenyl)-2,3-pentadione 3-oxime is cyclized to give a key intermediate 3,4-dihydro-1-hydroxy-5-methyl-1-(trifluoromethyl)-2(1H)-naphthalenone oxime; and 3,4-dihydro-1-hydroxy-5-methyl-1-(trifluoromethyl)-2(1H)-naphthalenone is aromatized to 5-methyl-1-(trifluoromethyl)-2-naphthalenol with a dehydrating agent.
    Type: Grant
    Filed: June 22, 1983
    Date of Patent: February 12, 1985
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Steven Fung, Nedumparambil A. Abraham, Francesco Bellini
  • Patent number: 4492697
    Abstract: The invention discloses novel 4H-imidazo[2,3-c]pyrido[2,3-e][1,4]oxazine derivatives, processes 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.
    Type: Grant
    Filed: August 16, 1983
    Date of Patent: January 8, 1985
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Jean A. Gauthier, Ivo L. Jirkovsky
  • Patent number: 4470990
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 each is hydrogen or lower alkyl or R.sup.1 and R.sup.2 together form an alkylene of the formula (CH.sub.2).sub.n wherein n is an integer from 4 to 6, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: September 11, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4469694
    Abstract: 2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: September 4, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
  • Patent number: 4469695
    Abstract: 2-(4-Hydroxyalkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: September 4, 1984
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
  • Patent number: 4469693
    Abstract: 2-(4-Substituted alkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: September 4, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
  • Patent number: 4468391
    Abstract: A .beta.-adrenoceptor antagonist, which does not penetrate or penetrates poorly the brain, is combined with subtherapeutic doses of an anxiolytic agent, such as diazepam, to give a method, and pharmaceutical or veterinary composition, for treating anxiety, stress or aggressivity without deleterious side effects associated with the central nervous system.
    Type: Grant
    Filed: June 25, 1982
    Date of Patent: August 28, 1984
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventor: Katherine Voith
  • Patent number: 4454150
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: October 19, 1981
    Date of Patent: June 12, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4447452
    Abstract: Herein disclosed are N-[(2-naphthalenyl)thioxomethyl]glycine derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo or trifluoromethyl. The derivatives have aldose reductase inhibiting activity and are useful for treating diabetic complications.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: May 8, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Kazimir Sestanj
  • Patent number: 4446150
    Abstract: Disclosed herein are new aldose reductase inhibitors of the formula ##STR1## wherein R is ##STR2## wherein R.sup.1 is lower alkyl; R.sup.2 is halo and R.sup.3 is hydrogen, or R.sup.2 and R.sup.3 each is a substituent at positions 3, 4, 5 or 6 of the naphthalene ring selected from the group consisting of lower alkoxy, trihalomethyl, and halo; and R.sup.4 is lower alkyl. The derivatives are useful for treating or preventing diabetic complications.
    Type: Grant
    Filed: September 21, 1982
    Date of Patent: May 1, 1984
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Francesco Bellini
  • Patent number: 4442118
    Abstract: Disclosed are new methods of using 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-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: July 23, 1981
    Date of Patent: April 10, 1984
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4439617
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: March 27, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala