Single Bond Between 3,4-positions Patents (Class 546/150)
  • Patent number: 4349678
    Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth, are described.
    Type: Grant
    Filed: December 12, 1980
    Date of Patent: September 14, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Patent number: 4288591
    Abstract: This invention provides a novel class of 2-iminoimidazolidines which include 4-substituted derivatives such as 4-(2-chloroethyl)-1-methyl-2-methylimino-3-phenyl imidazolidine fumarate: ##STR1## This illustrated 4-substituted 2-iminoimidazolidine compound exhibits cardiovascular hypotensive, hypoglycemic (glucose tolerance, and sugar cataract) and anti-inflammatory (pleural effusion) pharmacological activities in test animals.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: September 8, 1981
    Assignee: A. H. Robins Company, Inc.
    Inventor: Albert D. Cale, Jr.
  • Patent number: 4287197
    Abstract: Isoquinoline derivatives of the formula: ##STR1## wherein R.sub.1 represents alkyl of 1 through 8 carbon atoms, and n represents 1 or 2, are new compounds possessing useful pharmacological properties. They are particularly valuable as analgesic, anti-inflammatory, antipyretic or antiviral agents.
    Type: Grant
    Filed: May 6, 1980
    Date of Patent: September 1, 1981
    Assignee: Rhone-Poulenc Industries
    Inventors: Daniel Farge, Alain Jossin, Gerard Ponsinet, Daniel Reisdorf
  • Patent number: 4251660
    Abstract: A method for preparing 1,2,3,4-tetrahydroisoquinolines comprising heating N-halo or hydroxyethyl-N-benzylamines in an aluminum chloride melt at 160.degree.-210.degree..
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: February 17, 1981
    Assignee: SmithKline Corporation
    Inventors: Bing L. Lam, Wilford L. Mendelson, Charles B. Spainhour, Jr.
  • Patent number: 4228170
    Abstract: 1,2,3,4-Tetrahydroisoquinoline compounds having 7- and/or 8-sulfur substituents are inhibitors of phenylethanolamine N-methyltransferase.
    Type: Grant
    Filed: August 30, 1979
    Date of Patent: October 14, 1980
    Assignee: SmithKline Corporation
    Inventors: William E. Bondinell, Robert G. Pendleton
  • Patent number: 4220778
    Abstract: 8-Aryl-1,2,3,4-tetrahydroisoquinoline and derivatives thereof having the formula ##STR1## and the non-toxic pharmacologically acceptable acid addition salts thereof; wherein R is hydrogen, benzyl, or an alkyl radical of 1 to 7 carbon atoms; R.sup.1 is hydrogen or an alkyl radical of 1 to 7 carbon atoms; R.sup.2 in each occurrence is hydrogen, an alkyl radical of 1 to 7 carbon atoms or alkoxy radical of 1 to 7 carbon atoms, alike or different; Ar is phenyl optionally substituted with one or more halogen, an alkyl radical of 1 to 7 carbon atoms, or alkoxy radical of 1 to 7 carbon atoms; and n is positive integer less than 4, are disclosed. These compounds are useful because of their anti-arrhythmic, antimicrobial and central nervous system activity.
    Type: Grant
    Filed: October 30, 1978
    Date of Patent: September 2, 1980
    Assignee: G. D. Searle & Co.
    Inventors: Charles R. Ellefson, Kathleen Prodan
  • Patent number: 4220647
    Abstract: 1,2,3,4-tetrahydroisoquinolines have the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkenyl, acyl, aryl or ar(lower)alkyl, in which aryl and the aryl moiety of the ar(lower)alkyl may contain at least one substituent selected from the group consisting of halogen, lower alkoxy, amino, nitro, hydroxy, acyloxy, ar(lower)alkoxy, lower alkylenedioxy, halo(lower)alkyl, acylamino, ar(lower)alkylamino and aryl, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 5, 1975
    Date of Patent: September 2, 1980
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teiji Kishimoto, Hiromu Kochi, Masayuki Kato
  • Patent number: 4202894
    Abstract: Heterocyclic compounds characterized by the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and z are as hereinafter set forth,prepared, inter alia, by reacting a compound characterized by the formula ##STR2## with an amine characterized by the formula ##STR3## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and Y are as hereinafter set forth,are described. The end products are useful as fungicidal agents.
    Type: Grant
    Filed: November 18, 1977
    Date of Patent: May 13, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Albert Pfiffner
  • Patent number: 4200754
    Abstract: A novel process for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline by cyclizing N-acetyl-2,3-dichlorobenzylaminoacetaldehyde dimethyl acetal with a Lewis acid, reducing, and hydrolyzing the resulting acylated isoquinoline is disclosed.
    Type: Grant
    Filed: February 2, 1979
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl D. Perchonock