Beta Hydroxy Phenethylamines (i.e., Hydroxy And The Benzene Ring Are Bonded Directly To The Same Carbon Of The Chain Which Consists Of Two Carbons; H Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/363)
  • Patent number: 4908386
    Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: March 13, 1990
    Assignee: Glaxo Group Limited
    Inventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
  • Patent number: 4883804
    Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.
    Type: Grant
    Filed: November 19, 1986
    Date of Patent: November 28, 1989
    Assignee: Fisons plc
    Inventors: Francis Ince, Brian Springthorpe, John Dixon
  • Patent number: 4880841
    Abstract: Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1 -3; and n is an integer of 0-2 and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adreneregic blocking action and are useful as an antihypertensive agent.
    Type: Grant
    Filed: February 3, 1989
    Date of Patent: November 14, 1989
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka, Kazuo Honda
  • Patent number: 4863959
    Abstract: There are provided novel anthranilonitrile derivatives and related compounds which are useful for promoting growth, improving feed efficiency and for increasing the lean meat to fat ratio of warm-blooded animals.
    Type: Grant
    Filed: September 24, 1986
    Date of Patent: September 5, 1989
    Assignee: American Cyanamid Company
    Inventors: Terence J. Bentley, Goro Asato
  • Patent number: 4845127
    Abstract: Optically active N-3-(4-substituted phenyl)propyl-.beta.-phenethanolamines are provided as well as pharmaceutical compositions containing such compounds. A method for effecting weight control in obese animals utilizing optically active phenethanolamine is disclosed. Novel intermediates useful in the preparation of optically active .beta.-phenethanolamines are provided.
    Type: Grant
    Filed: December 14, 1984
    Date of Patent: July 4, 1989
    Assignee: Eli Lilly and Company
    Inventors: Jack Mills, Klaus K. Schmiegel, Walter N. Shaw
  • Patent number: 4835315
    Abstract: The present invention relates to new compounds belonging to the family of fluorophenacyl-amine derivates of formula: ##STR1## [wherein A is CO or CHOH and R is CH(CH.sub.3).sub.2 or C(CH.sub.3).sub.3 ] and selected from the group consisting of N-(4-fluorophenacyl)-isopropylamine, N-(2-fluorophenacyl)-tertiarybutylamine, 1-(2-fluorophenyl)-2-tertiarybutylamino-1-ethanol, 1-(4-fluorophenyl)-2-tertiarybutylamino-1-ethanol, and their addition salts, These new derivatives are useful in therapeutics, particularly as anti-aggressive agents, anti-anorexia nervosa agents, sedative agents, and CNS- antidepressants.
    Type: Grant
    Filed: July 1, 1987
    Date of Patent: May 30, 1989
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4835179
    Abstract: Dihydrodibenzocycloheptyliden-ethylene derivatives of the general formula: ##STR1## in which, R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; andR.sub.3 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or --CO--(C.sub.1 -C.sub.4 alkyl),are disclosed. These compounds are useful in the treatment of ulcer conditions.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: May 30, 1989
    Assignee: Sociedad Espanola de Especialidades Farmacotera peuticas
    Inventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
  • Patent number: 4820717
    Abstract: The present invention relates to new aromatic derivatives of formula: ##STR1## wherein: Alk is an alkylene group with 1 to 10 carbon atoms,R.sub.1 is hydrogen or an alkyl with 1 to 6 carbon atoms,R.sub.2 and R.sub.3 are similar or different and represent a cycloalkyl with 3 to 6 carbon atoms or a striaght or branched alkyl with 1 to 6 carbon atoms, either substituted or non-substituted by a phenyl or methyl phenyl group, or R.sub.2 and R.sub.3 form, together with the atom of nitrogen to which they are bonded, a mono-nitrogenous heterocycle containing no other heteroatom, such as pyrrolidino, piperidino, azepino, hexamethylene-imino, 4-methyl-piperidino, 4-phenyl-piperidino, 1,2,3,4-tetrahydro-2-isoquinolyl, 4-benzyl-piperidino;R.sub.4 is hydrogen, halogen, methyl or phenyl,R.sub.5 is hydrogen, halogen or methyl,or R.sub.4 and R.sub.5 together with the benzene ring to which they are bonded, constitute a 1-naphthyl or 2-naphthyl group,and the pharmaceutically acceptable salts with mineral or organic acids.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: April 11, 1989
    Assignee: Sanofi
    Inventors: Madeleine Mosse, Henri Demarne, Vincenzo Proietto
  • Patent number: 4806667
    Abstract: A method for promoting production of useful livestock comprising administering to such livestock an amount effective therefor of a monosilylated aminopheylethylamine derivative of the formula ##STR1## in which X and Y are identical or different and represent hydrogen or CN,R.sup.2 represents hydrogen or methyl,R.sup.3 represents t-butyl, isopropyl, monofluoro-t-butyl or 1-cyclohexyl-ethyl, andR.sup.4, R.sup.5 and R.sup.6 denote a straight-chain or branched alkyl rdical,or a physiologically tolerated salt thereof.Those compounds wherein R.sup.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: February 21, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Boshagen, Jurgen Stoltefuss, Friedrich Berschauer, Anno de Jong, Martin Scheer
  • Patent number: 4777294
    Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group, or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, B is hydrogen or hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against .alpha.-glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.
    Type: Grant
    Filed: April 17, 1987
    Date of Patent: October 11, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
  • Patent number: 4754047
    Abstract: There is provided a method for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby, which involves, orally or parenterally, administering to said animals a growth-enhancing amount of a phenylethanolamine compound or the acid addition salt thereof.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: June 28, 1988
    Assignee: American Cyanamid Company
    Inventors: Jane A. Kiernan, Pamela K. Baker
  • Patent number: 4721717
    Abstract: The present invention provides aminoalcohols of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be same or different, are hydrogen atoms, hydroxyl groups, C.sub.1 -C.sub.4 -alkoxy, benzyloxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkanesulphonylamino, C.sub.1 -C.sub.4 -alkanesulphinyl or C.sub.1 -C.sub.4 -alkanesulphonyl radicals, m is 2, 3 or 4, X and Y, which can be the same or different, are hydrogen atoms or benzyl radicals and R.sub.3 is a phenyl radical substituted twice by C.sub.1 -C.sub.6 -alkyl radicals, a nitrophenyl radical, an aminophenyl radical, a 1,3,5-tri-C.sub.1 -C.sub.6 -alkyl-2,4-dioxo-1H,3H-pyrimidin-6-yl radical, an indolyl radical, an indazolyl radical, a benzimidazolyl radical, a 1,4-di-C.sub.1 -C.sub.6 -alkylpyrazol-5-yl radical or a radical of the general formula: ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different, are C.sub.1 -C.sub.4 -alkyl radicals and R.sub.6 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: July 29, 1985
    Date of Patent: January 26, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventors: Walter-Gunar Friebe, Wolfgang Kampe, Erwin Bohm, Klaus Strein
  • Patent number: 4701559
    Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group, or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, B is hydrogen or hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against .alpha.-glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.
    Type: Grant
    Filed: December 28, 1981
    Date of Patent: October 20, 1987
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
  • 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: 4645862
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.3 each is benzyl or substituted with up to 3 methoxy groups, R.sub.2 is a hydrogen atom and (alkylene) is lower alkyl and the compounds are useful for controlling viral infections.
    Type: Grant
    Filed: April 15, 1985
    Date of Patent: February 24, 1987
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Yoshiyuki Tahara, Yasuhiro Komatsu, Hiroyasu Koyama, Reiko Kubota, Teruhito Yamaguchi, Toshihiro Takahashi
  • Patent number: 4622342
    Abstract: Compounds of formula (II): ##STR1## or salt thereof; wherein R.sup.1 is hydrogen or methyl,R.sup.2 is hydrogen or methyl,R.sup.3 is hydrogen, C.sub.1-12 straight or branched alkyl, C.sub.3-10 cycloalkyl, phenyl(C.sub.1-4)-alkyl or benzyl optionally substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen;R.sup.4 is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl or C.sub.1-4 alkoxy,R.sup.5 is hydrogen or fluorine,R.sup.6 is hydrogen or fluorine,R.sup.7 is halogen; andn is 1 or 2,have anti-obesity and/or anti-hyperglycaemic activity.
    Type: Grant
    Filed: November 2, 1984
    Date of Patent: November 11, 1986
    Assignee: Beecham Group P.L.C.
    Inventors: Barrie C. C. Cantello, Richard M. Hindley
  • Patent number: 4602044
    Abstract: .beta.-Phenethanolamines are useful as antiobesity agents.
    Type: Grant
    Filed: December 19, 1983
    Date of Patent: July 22, 1986
    Assignee: Eli Lilly and Company
    Inventors: Klaus K. Schmiegel, Walter N. Shaw
  • Patent number: 4588749
    Abstract: Compounds of formula (II): ##STR1## or a pharmaceutically acceptable salt thereof, in which X is an oxygen atom or a bond, R.sup.1 is a hydrogen, fluorine, chlorine or bromine atom or a trifluoromethyl or C.sub.1-4 alkyl group, each of R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-4 alkyl group, R.sup.4 is a C.sub.1-4 alkyl group, R.sup.5 is a hydrogen atom or a C.sub.1-4 alkyl group, and n is an integer of from 1 to 3; are useful as anti-obesity and/or anti-hyperglycaemic agents.
    Type: Grant
    Filed: May 3, 1984
    Date of Patent: May 13, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Michael J. Ferris
  • Patent number: 4587248
    Abstract: 4-alkyl-thiophenyl-ethanolamines are disclosed, which are compounds having a therapeutical activity against blood-platelet aggregation, and against lipemia and improving the cerebral circulation, said ethanolamines having the general formula: ##STR1## wherein R and R.sub.1 are alkyl substituents and R.sub.2 is a substituent having an amine character. Due to the presence of two asymmetry centers in their molecule, the compounds concerned can be prepared in the "threo" and the "erythro" configuration: mixtures of the "threo" and the "erythro" forms have also proven effective.
    Type: Grant
    Filed: May 27, 1982
    Date of Patent: May 6, 1986
    Inventors: Giorgio Cantarelli, Giampaolo Picciola, Franco Ravenna, Mario Riva
  • Patent number: 4552897
    Abstract: Novel acid addition salts of 1-(aminodihalophenyl)-2-aminoethanols and method of preparation thereof. The invention describes certain non-dusting, antilipogenic compositions used as animal feed supplements and/or concentrates and a method for increasing weight gain and improving the lean meat to fat ratio of warm-blooded animals.
    Type: Grant
    Filed: February 1, 1983
    Date of Patent: November 12, 1985
    Assignee: American Cyanamid Company
    Inventors: Goro Asato, Lawrence J. Ross
  • Patent number: 4514573
    Abstract: This invention relates to new isoprenylamine derivatives and acid addition salts thereof, which are useful for controlling virus infection of vertebrate animals.
    Type: Grant
    Filed: May 12, 1982
    Date of Patent: April 30, 1985
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Yoshiyuki Tahara, Yasuhiro Komatsu, Hiroyasu Koyama, Reiko Kubota, Teruhito Yamaguchi, Toshihiro Takahashi
  • Patent number: 4490392
    Abstract: A benzylalcohol derivative of the formula: ##STR1## wherein R is hydroxy, benzyloxy, halogen or alkoxy having one to four carbon atoms, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl, or a pharmaceutically acceptable acid addition salt thereof is prepared by reducing a compound of the formula: ##STR2## wherein R' is benzyloxy, halogen or alkoxy having one to four carbon atoms, and Ring A is the same as defined above, to give a compound of the formula: ##STR3## wherein R' and Ring A are the same as defined above, and when R' is benzyloxy, if required, further subjecting the compound [I'] to catalytic hydrogenation to give a compound of the formula: ##STR4## wherein Ring A is the same as defined above. The benzylalcohol derivative [I] is useful as an anti-diabetic agent.
    Type: Grant
    Filed: July 27, 1978
    Date of Patent: December 25, 1984
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Muneyoshi Ikezaki, Takeshi Kanno, Hajime Iwai, Masanori Inamasu
  • Patent number: 4486602
    Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group; or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.
    Type: Grant
    Filed: September 29, 1981
    Date of Patent: December 4, 1984
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
  • Patent number: 4414210
    Abstract: This invention relates to 2-hydroxyarylethyl-1,2,4-triazoles, their acid addition salts and metal salt complexes. This invention also relates to the method of preparation and use of these compounds. These compounds and salts thereof are highly active broad-spectrum systemic fungicides effective in controlling phytopathogenic fungi such as barley net blotch (Helminthosporium teres), grey mold (Botrytis fabae), bean powdery mildew (Erysiphe polygoni), grape downy mildew (Plasmopora viticola), rice blast (Piricularia oryzae), tomato late blight (Phytophthora infestans) and wheat stem rust (Puccinia graminis f. sp. tritici race 158-2).
    Type: Grant
    Filed: May 19, 1981
    Date of Patent: November 8, 1983
    Assignee: Rohm and Haas Company
    Inventors: George A. Miller, Hak-Foon Chan
  • Patent number: 4396627
    Abstract: Compounds having the formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Y and X are as defined hereinbelow, are useful for the reduction of abnormally high blood glucose and lipid levels in the treatment of obesity or hyperglycaemia.
    Type: Grant
    Filed: March 15, 1982
    Date of Patent: August 2, 1983
    Assignee: Beecham Group Limited
    Inventors: Anthony T. Ainsworth, David G. Smith
  • Patent number: 4391826
    Abstract: Optically active N-3-(4-substituted phenyl)propyl-.beta.-phenethanolamines are provided as well as pharmaceutical compositions containing such compounds. A method for effecting weight control in obese animals utilizing optically active phenethanolamines is disclosed. Novel intermediates useful in the preparation of optically active .beta.-phenethanolamines are provided.
    Type: Grant
    Filed: November 21, 1979
    Date of Patent: July 5, 1983
    Assignee: Eli Lilly and Company
    Inventors: Jack Mills, Klaus K. Schmiegel, Walter N. Shaw
  • Patent number: 4382958
    Abstract: A compound of formula (I): ##STR1## or a salt thereof; wherein R.sup.1 is hydrogen, methyl or ethyl; R.sup.2 is hydrogen, methyl or ethyl; R.sup.3 is hydrogen, fluorine, chlorine, bromine or trifluoromethyl; each of R.sup.4 and R.sup.5 is hydrogen, fluorine, chlorine, bromine, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; n is 1 or 2; and X is C.sub.1-12 straight or branched alkylene, and salts thereof, are anti-obesity, hypoglycaemic, anti-inflammatory and platelet aggregation inhibiting agents.
    Type: Grant
    Filed: November 9, 1981
    Date of Patent: May 10, 1983
    Assignee: Beecham Group Limited
    Inventor: David M. Duckworth
  • Patent number: 4379166
    Abstract: This invention relates to 5-(2-alkylamino-1-hydroxyethyl)salicylamides and 4-(2-alkylamino-1-hydroxyethyl)-2-(methylsulfinyl)phenols wherein the alkyl group is substituted by arylmethoxy, arylmethylthio, heteroarylmethoxy, or heteroarylmethylthio, pharmaceutical compositions thereof, and their use as cardiovascular agents.
    Type: Grant
    Filed: August 3, 1981
    Date of Patent: April 5, 1983
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Elijah H. Gold
  • 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: 4372969
    Abstract: The present invention relates to addition salts of substituted aralkylamines of formula:A--CH.sub.2 --NH--R (I)[wherein A is a 3,4-methylenedioxyphenyl group or an .alpha.-hydroxybenzyl, and R is CH(CH.sub.3).sub.2 or C(CH.sub.3).sub.3 ]It relates also to the method for preparing these salts and to their application as pharmaceuticals and in particular as central nervous system antidepressants.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: February 8, 1983
    Assignee: Societe Anonyme Dite: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4337272
    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, carboamido 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: October 2, 1980
    Date of Patent: June 29, 1982
    Assignee: Valeas S. R. L. Industria Chimica E Farmaceutica
    Inventors: Virgilio Bernareggi, Giuseppe Crespi, Giuseppe Bugada
  • Patent number: 4327224
    Abstract: Alpha-[(lower alkylamino)alkyl]-4-hydroxy-3-(alkylthio, akylsulfinyl or alkylsulfonyl)benzenemethanols which have .beta.-adrenergic blocking activity and which are therefore useful in controlling tachycardia are prepared by reduction of the corresponding (lower alkylamino)alkyl 4-hydroxy-3-(akylthio, akylsulfinyl or alkylsulfonyl)phenyl ketones.
    Type: Grant
    Filed: June 25, 1976
    Date of Patent: April 27, 1982
    Assignee: Sterling Drug Inc.
    Inventor: Sydney Archer
  • Patent number: 4317930
    Abstract: Novel phenethylamine derivatives represented by the general formula: ##STR1## wherein R is a lower alkyl group, C.sub.n H.sub.2n is a branched or straight alkylene group, A is a phenyl group unsubstituted or substituted with hydroxy, a lower alkoxy or a lower alkylene dioxy group, and n is an integer from 1 to 4, and pharmacologically acceptable acid addition salts thereof, and bronchdilator containing the same. These bronchdilator has an intense and durable bronchdilating effect and a weak heart stimulating action.
    Type: Grant
    Filed: March 16, 1977
    Date of Patent: March 2, 1982
    Assignee: Eisai Co., Ltd.
    Inventors: Noriyasu Hirose, Shigeru Souda
  • Patent number: 4314079
    Abstract: Processes for reacting arylvinyl oxides and alkoxyethylamines to provide novel N-substituted alkoxyethylamines; processes for reacting the novel N-substituted amines with nitriles to provide novel amidoamines; processes for preparing novel diamines from the amidoamines, together with the novel nitrogen-containing products so produced, such products being useful for the preparation of various imidazothiazoles including tetramisole.
    Type: Grant
    Filed: May 21, 1980
    Date of Patent: February 2, 1982
    Assignee: American Cyanamid Company
    Inventor: Sivaraman Raghu
  • 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
  • Patent number: T103206
    Abstract: A two-stage continuous crystallization process for production of urea phosphate by reaction of impure wet-process orthophosphoric acid (about 54 percent P.sub.2 O.sub.5) and urea with simultaneous addition of a selected acidifying agent (sulfuric acid, hydrochloric acid, or phosphoric acid) to clarified mother liquor used as recycle in the process. Addition of the acidifying agent decreases pH in the crystallization process whereby the solubility of a contaminating water-insoluble iron phosphate-urea salt [FeH.sub.3 (PO.sub.4).sub.2.2CO(NH.sub.2).sub.2 ] is increased, purity of the crystalline urea phosphate product is improved significantly, and the useful storage life of the recycle mother liquor is prolonged.
    Type: Grant
    Filed: November 24, 1981
    Date of Patent: July 5, 1983
    Inventors: Harry T. Lewis, Ewell F. Dillard