Patents Assigned to Ayerst McKenna and Harrison Inc.
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Patent number: 5206018Abstract: 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: GrantFiled: October 29, 1991Date of Patent: April 27, 1993Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Surendra N. Sehgal, Claude Vezina
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Patent number: 4946987Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating, diabetic complications.Type: GrantFiled: June 20, 1988Date of Patent: August 7, 1990Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
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Patent number: 4705882Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.Type: GrantFiled: March 28, 1986Date of Patent: November 10, 1987Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
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Patent number: 4604406Abstract: 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: GrantFiled: November 16, 1984Date of Patent: August 5, 1986Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Francesco Bellini, Kazimir Sestanj
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Patent number: 4600724Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.Type: GrantFiled: July 17, 1985Date of Patent: July 15, 1986Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
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Patent number: 4568693Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.Type: GrantFiled: September 9, 1983Date of Patent: February 4, 1986Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
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Patent number: 4522946Abstract: 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: GrantFiled: June 13, 1983Date of Patent: June 11, 1985Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Andre A. Asselin, Leslie G. Humber
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Patent number: 4510157Abstract: 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: GrantFiled: December 27, 1982Date of Patent: April 9, 1985Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Andre A. Asselin, Leslie G. Humber
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Patent number: 4499310Abstract: 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: GrantFiled: June 22, 1983Date of Patent: February 12, 1985Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Steven Fung, Nedumparambil A. Abraham, Francesco Bellini
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Patent number: 4492697Abstract: 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: GrantFiled: August 16, 1983Date of Patent: January 8, 1985Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Jean A. Gauthier, Ivo L. Jirkovsky
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Patent number: 4470990Abstract: 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: GrantFiled: March 14, 1983Date of Patent: September 11, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Andre A. Asselin, Leslie G. Humber
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Patent number: 4469694Abstract: 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: GrantFiled: February 25, 1980Date of Patent: September 4, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
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Patent number: 4469695Abstract: 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: GrantFiled: February 25, 1980Date of Patent: September 4, 1984Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
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Patent number: 4469693Abstract: 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: GrantFiled: February 25, 1980Date of Patent: September 4, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
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Patent number: 4468391Abstract: 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: GrantFiled: June 25, 1982Date of Patent: August 28, 1984Assignee: Ayerst, McKenna & Harrison, Inc.Inventor: Katherine Voith
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Patent number: 4454150Abstract: 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: GrantFiled: October 19, 1981Date of Patent: June 12, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Andre A. Asselin, Leslie G. Humber
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Patent number: 4447452Abstract: 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: GrantFiled: November 13, 1981Date of Patent: May 8, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventor: Kazimir Sestanj
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Patent number: 4446150Abstract: 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: GrantFiled: September 21, 1982Date of Patent: May 1, 1984Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Francesco Bellini
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Patent number: 4442118Abstract: 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: GrantFiled: July 23, 1981Date of Patent: April 10, 1984Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
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Patent number: 4439617Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.Type: GrantFiled: November 13, 1981Date of Patent: March 27, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala