Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxomethyl]-N-methylgl ycine S-oxide (tolrestat S-oxide) and the amide thereof and methods of their preparation. The S-oxides are new aldose reductase inhibitors useful for the treatment of prevention of diabetic complications.
Type:
Grant
Filed:
November 25, 1986
Date of Patent:
March 29, 1988
Assignee:
American Home Products Corp.
Inventors:
Eckhardt S. Ferdinandi, Michael S. Malamas, Kazimir Sestanj, Surendra N. Sehgal
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation. The compounds are useful analgesic and anti-inflammatory agents.
Type:
Grant
Filed:
March 31, 1987
Date of Patent:
November 24, 1987
Assignee:
American Home Products Corp.
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.
Type:
Grant
Filed:
February 18, 1987
Date of Patent:
October 20, 1987
Assignee:
American Home Products Corporation
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.
Type:
Grant
Filed:
August 26, 1986
Date of Patent:
August 18, 1987
Assignee:
American Home Products Corporation
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at position 8. The derivatives are useful anti-inflammatory and analgesic agents and methods and chemical intermediates for their preparation are also disclosed. Included are compounds of the formula ##STR1## wherein R.sup.1 is --H or lower alkyl containing 1 to 3 carbon atoms; R.sup.2 is --NH.sub.2, --NHCHO, --NHCONH.sub.2, --OCH.sub.3, oxo; R.sup.3 is --H or lower alkyl containing 1 to 3 carbon atoms and the pharmaceutically acceptable salts thereof when R.sup.1 is --H.
Type:
Grant
Filed:
August 15, 1986
Date of Patent:
August 11, 1987
Assignee:
American Home Products Corporation
Inventors:
Eckhardt S. Ferdinandi, Dominick Mobilio, Joseph P. Sabatucci, Leslie G. Humber
Abstract: A gelatin capsule dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the pharmaceutical binder methylcellulose in combination with low doses of a surfactant or a carbonate salt as disintegrants.
Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at positions 5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.
Type:
Grant
Filed:
March 11, 1986
Date of Patent:
June 2, 1987
Assignee:
American Home Products Corporation
Inventors:
Alan H. Katz, Christopher A. Demerson, Leslie G. Humber
Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.
Type:
Grant
Filed:
July 18, 1986
Date of Patent:
May 12, 1987
Assignee:
American Home Products Corp.
Inventors:
Ivo Jirkovsky, Gary King, Reinhardt Baudy, Victor DeNoble
Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.
Type:
Grant
Filed:
December 20, 1985
Date of Patent:
November 25, 1986
Assignee:
American Home Products Corporation
Inventors:
Ivo Jirkovsky, Gary King, Reinhardt Baudy, Victor DeNoble
Abstract: Herein is disclosed amino-pyrimidine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for increasing cardiac contractility in a mammal.
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.
Type:
Grant
Filed:
November 13, 1985
Date of Patent:
October 7, 1986
Assignee:
American Home Products Corporation
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Therapeutic liquid oral dosage formulations of propranolol hydrochloride are provided which contain lecithin and/or a basic amino acid to impart taste masking characteristics and/or contain a basic amino acid to impart anesthesia masking characteristics.
Abstract: A process for preparing 1,8-diethyl-1,3,4,9-tetrahydro[3,4-b]-indole-1-acetic acid (etodolac) is disclosed. Etodolac is a useful antiinflammatory and analgesic agent.
Type:
Grant
Filed:
May 6, 1985
Date of Patent:
April 29, 1986
Assignee:
American Home Products Corporation
Inventors:
Christopher A. Demerson, Leslie G. Humber
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.
Type:
Grant
Filed:
May 31, 1985
Date of Patent:
April 22, 1986
Assignee:
American Home Products Corporation
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.
Type:
Grant
Filed:
May 31, 1985
Date of Patent:
March 25, 1986
Assignee:
American Home Products Corporation
Inventors:
Dominick Mobilio, Christopher A. Demerson, Leslie G. Humber
Abstract: Pharmaceutical composition of skin respiratory factor (SRF), sodium chloride, bicarbonate, fluoride and zinc chloride in a suitable toothpaste vehicle provides effective therapy for gingivitis when brushed on the teeth and gingivae.Pharmaceutical composition of SRF in a viscous composition suitable for application to the gingivae and effective over an extended period of time for healing tissue damaged by gingevitis. A toothpaste tube for packaging a pharmaceutical composition of SRF, sodium chloride, bicarbonate, fluoride and zinc chloride.
Abstract: The effect of prolonged treatment with etodolac on the articular pathology associated with adjuvant arthritis in the rat has been compared to the effects produced by similar treatment with naproxen and ibuprofen. Drug effects were assessed by radiologic and histopathologic examinations. The effects on hindpaw edema, hindleg function, and body weight gain were also evaluated. Treatment was initiated on day 16 after adjuvant injection and continued for 28, 56 or 84 days. The degree of relapse which occurred during 28 days of non-treatment after dosage was stopped after 28 or 56 days of treatment was also assessed. Etodolac prevented the progression of the disease. Further, it appeared to diminish the severity of the articular lesions already present on day 16 before drug treatment began. All the parameters measured were improved and there was good agreement between the radiologic and histopathologic assessments of articular damage.
Abstract: The present invention provides 5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen or halogen atoms or lower alkyl or alkoxy radicals, R.sup.3 is a hydrogen atom or a lower alkyl radical, R.sup.4 is a hydrogen atom or a lower alkyl or alkanoyl radical and n is 1 or 2; and the pharmaceutically acceptable salts thereof formed with inorganic and organic acids; but excluding 6-benzyl-2,12-dimethoxy-1-hydroxy-7-methyl-5,6;8,9-tetrahydro-7H-dibenz(d, f)azonine in which case R.sup.1, R.sup.2 and R.sup.4 are hydrogen, n is 1 and R.sup.3 is methyl. The lower alkyl, alkanoyl and alkoxy radicals are straight chained or branched radicals containing 1 to 5 carbon atoms.The present invention also provides a process for the preparation of these compounds, as well as pharmaceutical compositions containing them.
Type:
Grant
Filed:
February 24, 1981
Date of Patent:
November 15, 1983
Assignee:
Godecke Aktiengesellschaft
Inventors:
Gerhard Satzinger, Manfred Herrmann, Edgar Fritschi, Heinrich Bahrmann, Volker Ganser, Bernd Wagner, Wolfgang Steinbrecher
Abstract: Substituted 6-phenyl-3(2H)-pyridazinone compounds are useful as cardiotonic agents.Said compounds cause a significant increase in myocardial contractility in the anesthetized dog. Said compounds are produced by reacting substituted benzoylpropionic acids with suitably substituted hydrazines to provide 6-phenyl-4,5-dihydro-3(2H)-pyridazinones which are dehydrogenated to the desired product.The intermediate 6-phenyl-4,5-dihydro-3(2H)-pyridazinones are themselves useful as cardiotonic agents.
Abstract: Pharmaceutical salts of 4'-(9-acridinylamino)-methanesulfon-m-anisidide, methods for their preparation and use of said salts in the form of pharmaceutical compositions as antineoplastic agents.