Hydroxy Or Ether Oxygen Bonded Directly To The Aryl Ring Or Ring System (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/365)
  • Patent number: 4695589
    Abstract: Alpha-(aminoalkyl)-4-hydroxy-3-(alkylthio)benzenemethanols useful as intermediates and as antihypertensive agents are prepared by reduction of the corresponding aminoalkyl 4-hydroxy-3-(alkylthio)phenyl ketones.
    Type: Grant
    Filed: May 27, 1983
    Date of Patent: September 22, 1987
    Assignee: Sterling Drug Inc.
    Inventor: Richard E. Philion
  • Patent number: 4661635
    Abstract: Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2 q, Alk, R.sup.3, n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.
    Type: Grant
    Filed: October 29, 1984
    Date of Patent: April 28, 1987
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4652679
    Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.
    Type: Grant
    Filed: May 9, 1983
    Date of Patent: March 24, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4603019
    Abstract: This invention relates to new N-(methoxyphenacyl)-amine derivatives selected from the group consisting of(i) the N-(methoxyphenacyl)-alkylamines of the general formula ##STR1## wherein A is OCH.sub.3, and R is C.sub.3 -C.sub.8 -alkyl or C.sub.3 -C.sub.8 -hydroxyalkyl; and,(ii) addition salts thereof.These new derivatives are useful as pharmaceuticals, in particular as peripheral vasodilating agents.
    Type: Grant
    Filed: November 23, 1984
    Date of Patent: July 29, 1986
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4579972
    Abstract: New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed by a borohydride reduction.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: April 1, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: Kathleen L. Wert, Alan W. Tremper
  • Patent number: 4540819
    Abstract: New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed by a borohydride reduction.
    Type: Grant
    Filed: April 28, 1983
    Date of Patent: September 10, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: Kathleen L. Wert, Alan W. Tremper
  • Patent number: 4374149
    Abstract: The instant invention is directed to .alpha.-(aminoalkyl)-4-hydroxy-3-(alkylsulfinylbenzenemethanols and to a method of utilizing the compounds for reducing blood pressure in mammals.
    Type: Grant
    Filed: August 30, 1978
    Date of Patent: February 15, 1983
    Assignee: Sterling Drug Inc.
    Inventor: Richard E. Philion
  • Patent number: 4304790
    Abstract: 2-(Alkylthio, alkylsulfinyl or alkylsulfonyl)-4-[2-(anilinoalkylamino)-1-hydroxyalkyl]phenols and derivatives thereof, particularly useful as agents for the treatment of hypertension, are disclosed herein.
    Type: Grant
    Filed: June 12, 1979
    Date of Patent: December 8, 1981
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Elijah H. Gold
  • Patent number: 4284587
    Abstract: A new radioenzymatic assay for catecholamines utilizing the catechol-O-methyl transferase transfer of a methyl group from a labeled methyl donor to the catecholamines followed by isolation of the O-methylated(.sup.3 H)catecholamine and the subsequent measurement of radioactivity.
    Type: Grant
    Filed: October 12, 1978
    Date of Patent: August 18, 1981
    Assignee: The Upjohn Company
    Inventors: Garland A. Johnson, Jacob D. Peuler
  • Patent number: 4282251
    Abstract: Cinnamylalkyl-1-naphthylmethylamines, useful as antimycotic agents, and processes for their production.
    Type: Grant
    Filed: December 3, 1979
    Date of Patent: August 4, 1981
    Assignee: Sandoz Ltd.
    Inventor: Daniel Berney
  • Patent number: 4276304
    Abstract: A benzylalcohol derivative of the formula: ##STR1## wherein R is hydroxy, benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl is prepared by reducing a compound of the formula: ##STR2## wherein R' is benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is the same as defined above, and when R' is benzyloxy, if required, further subjecting the product to catalytic hydrogenation.The compounds (I) and pharmaceutically acceptable acid addition salts thereof are used as anti-diabetic agents.
    Type: Grant
    Filed: January 18, 1980
    Date of Patent: June 30, 1981
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Muneyoshi Ikezaki, Katsuyuki Noguchi, Hajime Iwai, Masanori Inamasu
  • Patent number: 4252824
    Abstract: New compounds of the formula ##STR1## are disclosed wherein R.sub.1 =H, linear or branched alkyl-radical with from 1 to 6 carbon atoms, cycloalkyl radical with from 3 to 6 carbon atoms, alkylphenyl radical where the phenyl group may be in turn substituted with a hydroxy or methoxy group;R.sub.2 =hydroxy, hydromethylR.sub.3 =H, alkyl with 1-4 carbon atoms, formyl, carboalkyl where the alkyl groups have 1-3 carbon atoms, carbomido group simple or mono- or di-substituted on the nitrogen atom with alkyl radicals containing 1-3 carbon atoms.The new compounds are useful in the treatment of bronchial affections. They are endowed with unique properties in that they provide the desired bronchial dilation effect without any concomitant cardiac stimulation.
    Type: Grant
    Filed: November 10, 1976
    Date of Patent: February 24, 1981
    Assignee: Valeas S.R.L., Industria Chimica e Farmaceutica
    Inventors: Virgilio Bernareggi, Giuseppe Crespi, Giuseppe Bugada