Acyclic Hydrocarbyl Alpha Substituent Patents (Class 564/364)
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Publication number: 20120244208Abstract: This invention relates to a topical cosmetic skin care method and composition. The method and composition is for treating facial skin to cause contraction and tightening of the facial skin, by effecting contraction of the collagen of the skin using an active agent/s that induces fibroblast contraction of the extra cellular matrix of the skin. A preferred active agent is a beta-2-adrenergic receptor (beta2AR) inhibitor.Type: ApplicationFiled: September 6, 2010Publication date: September 27, 2012Inventor: Hugo Barrie Nel
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Patent number: 8178679Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.Type: GrantFiled: November 10, 2008Date of Patent: May 15, 2012Assignee: Almirall, S.A.Inventors: Victor Giulio Matassa, Carlos Puig Duran, Maria Prat Quiñones, Laia Sole Feu, Oriol Llera Soldevila
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Publication number: 20100324000Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.Type: ApplicationFiled: November 10, 2008Publication date: December 23, 2010Inventors: Victor Giulio Matassa, Carlos Puig Duran, Maria Prat Quiñones, Laia Sole Fue, Oriol Llera Soldevila
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Patent number: 6900203Abstract: (R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine, and an anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analog, are disclosed. Further disclosed is a method of providing vasoconstriction in a mammal by administering the anesthetic formulation. The anesthetic composition can include an anesthetic, an (R)-chiral compound having the structure: wherein R1, R2, and R4 are independently selected from —H or —F, at least one of R1, R2, and R4 is —F, and R3 is selected from —OH, —H or —F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form. Also, a method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, employing an almond hydroxynitrile lyase enzyme, provided in the form of a reversibly soluble polymer conjugate ((R)-Finezyme™-H series biocatalysts) is disclosed.Type: GrantFiled: July 8, 2002Date of Patent: May 31, 2005Assignee: Polium Technologies, Inc.Inventors: Hamilton J. Lenox, Elena Terentieva, Mikhail Y. Gololobov
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Patent number: 6825231Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endotType: GrantFiled: December 12, 2000Date of Patent: November 30, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6586633Abstract: The present invention relates to amine derivatives represented by formula (1) or salts thereof. R3 represents C1-C3 alkyl, hydroxylated C1-C5 alkyl, C1-C5 acyl; C2-C5 alkenyl, or a halogen atom; and k, l, and m are each an integer of 1 to 4.) Exhibiting excellent antifungal effect, these compounds are highly useful as antifungal agents, antifungal compositions, drugs, etc.Type: GrantFiled: April 5, 2001Date of Patent: July 1, 2003Assignee: Pola Chemical Industries, Inc.Inventors: Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima, Takao Itoh, Takuji Nakashima, Akira Nozawa, Hiroyuki Takimoto, Kouji Yokoyama
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Patent number: 6576793Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: August 14, 2000Date of Patent: June 10, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, John H. Griffin, Seok-Ki Choi
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Patent number: 5962737Abstract: Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.Type: GrantFiled: January 8, 1997Date of Patent: October 5, 1999Inventor: Daniel David West
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Patent number: 5773617Abstract: The present invention relates to a reagent and to a process which are useful, when carrying out an organic synthesis, for cleaving an allylic group from a function which is protected with the latter.This reagent is defined in that it contains:a) a solvent system;b) a catalyst containing at least one element from column VIII of the Periodic Table of the Elements, the said element from column VIII of the Periodic Table being coordinated with at least one coordination agent which is soluble in the said solvent system;c) a compound which is at least partially soluble in the said solvent system and which contains at least one nucleophilic function.Application to organic synthesis.Type: GrantFiled: February 22, 1996Date of Patent: June 30, 1998Assignee: Rhone-Poulenc ChimieInventors: Jean-Marie Bernard, Errol Blart, Jean-Pierre Genet, Sandrine Lemaire-Audoire, Monique Savignac
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Patent number: 5527830Abstract: The invention relates to new drugs for augmenting perfusion pressure administered during cardiopulmonary resuscitation and other shock states. The compounds include phenylethanolamines and imidazolines, and fluorinated derivatives thereof, which act on adrenergic receptors in patients. The compounds of the invention enhance neurologic outcome and survival, and decrease ventricular dysrhythmias in patients suffering cardiac arrest and other shock states, relative to the outcomes, survival, and post defibrillation ventricular dysrhythmias in conventional therapy for use in resuscitation.Type: GrantFiled: September 26, 1994Date of Patent: June 18, 1996Assignee: The Ohio State UniversityInventors: Charles G. Brown, Duane D. Miller
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Patent number: 5449694Abstract: (-)-Ritodrine, that is (-)-erythro-1-(p-hydroxyphenyl)-2-[2-(p-hydroxyphenyl)ethylamino]-1-propan ol or a salt thereof substantially free from the (+)-isomer is disclosed. The compound has a strong suppressive effect on uterine contraction in comparison with (.+-.)-ritodrine and (+)-ritodrine and has the same level of toxicity as these compounds, so that it can be used as a therapeutic agent of threatened premature birth and threatened abortion as well as a therapeutic agent of dysmenorrhea having a high safety.Type: GrantFiled: March 1, 1994Date of Patent: September 12, 1995Assignee: Meiji Seika Kabushiki KaishaInventors: Naoki Yamazaki, Yoshimasa Fukuda, Yoshiaki Shibazaki, Tetsutarou Niizato, Isao Kosugi, Shin Yoshioka
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Patent number: 5338884Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.Type: GrantFiled: October 2, 1992Date of Patent: August 16, 1994Assignee: Hoechst CelaneseInventors: Ahmed M. Tafesh, Olan S. Fruchey, Charles B. Hilton
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Patent number: 5283262Abstract: The invention provides compounds of the general formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof, wherein Q represents a 1- or 2-naphthalenyl group.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 23, 1991Date of Patent: February 1, 1994Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5198587Abstract: 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.-adrenergic blocking action and are useful as an antihypertensive agent.Type: GrantFiled: July 30, 1991Date of Patent: March 30, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka, Kazuo Honda
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Patent number: 5171753Abstract: Derivatives of 2-amino-1-phenylethanol were prepared from substituted amines and benzoin, stilbene oxide or styrene oxide to give compounds of Formula: ##STR1## where R is H or (un)substituted phenyl and C is a linking group or terminal group. The compounds of this invention can inhibit ulceration in in-vivo studies in rats.Type: GrantFiled: May 15, 1991Date of Patent: December 15, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Harry R. Munson, Jr., Robert F. Boswell
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Patent number: 5145998Abstract: A method for producing an optically active amine which is an important compound as a resolving agent for medicines, agricultural chemicals, intermediates thereof, etc is disclosed.Type: GrantFiled: October 2, 1990Date of Patent: September 8, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Yoji Sakito, Gohfu Suzukamo, Yukio Yoneyoshi
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Patent number: 5109023Abstract: The invention provides a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.Type: GrantFiled: December 5, 1990Date of Patent: April 28, 1992Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5099068Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein AR represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 --, or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.Type: GrantFiled: December 5, 1990Date of Patent: March 24, 1992Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5096929Abstract: 5,6-Dimethoxy-2-[2-(4-hydroxyphenyl)-2-hydroxy-2-methylethyl]amino- 1,2,3,4-tetrahydronaphthalene has inotropic and vasodilating activities and therefore can be used in the treatment of cardiocirculatory failure. The compound can be in the form of a single stereoisomer or as a mixture of two or more stereoisomers.Type: GrantFiled: June 26, 1990Date of Patent: March 17, 1992Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Stefano Bongrani, Maurizio Delcanale, Vittorino Servadio
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Patent number: 5095017Abstract: 1,2-dihydropyrido[3,4-b]pyrazines are provided which possess antimitotic activity. The compounds have the structure: ##STR1## wherein R is a lower alkyl group and OR.sub.1 is a member selected from the group consisting of aryl-alkyl ethers having from seven to about 20 carbon atoms, alkyl carbamates having from one to about 12 carbon atoms, the alkyl portion of which may be substituted with a halogen atom, e.g., chlorine, fluorine, bromine or iodine; aryl-alkyl carbamates having from about seven to about 20 carbon atoms, aryl carbamates having from about six to about 20 carbon atoms, aryl-alkyl esters having from about 7 to about 20 carbon atoms, aryl esters having from about six to about 20 carbon atoms, alkylthiocarbamates having from about one to about 12 carbon atoms, aryl-alkylthiocarbamates having from about seven to about 20 carbon atoms, and arylthiocarbamates having from about six to about 20 carbon atoms.Type: GrantFiled: May 22, 1991Date of Patent: March 10, 1992Assignee: Southern Research InstituteInventor: Carroll G. Temple, Jr.
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Patent number: 5047433Abstract: N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.Type: GrantFiled: December 21, 1987Date of Patent: September 10, 1991Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Marzi, Maria O. Tinti, Romano Di Fabio, Domenico Misiti
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Patent number: 4997986Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein Ar represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 -- or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.Type: GrantFiled: November 14, 1988Date of Patent: March 5, 1991Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 4918231Abstract: A process for the production of 1,2-amino alcohols, in improved yields, comprising the steps of:(1) reacting a silylated cyanohydrin compound with a Grignard reagent;(2) treating the reaction product of Step 1 with either a reducing agent, or an organolithium compound;(3) hydrolyzing the reaction product of Step 2;(4) isolating the resulting 1,2-amino alcohol.The 1,2-amino alcohols thus formed are useful as pharmaceuticals or precursors therefor.Type: GrantFiled: December 15, 1988Date of Patent: April 17, 1990Assignee: Minnesota Mining and Manufacturing CompanyInventors: Larry R. Krepski, Steven M. Heilmann, Jerald K. Rasmussen
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Patent number: 4880841Abstract: 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: GrantFiled: February 3, 1989Date of Patent: November 14, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka, Kazuo Honda
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Patent number: 4835179Abstract: 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: GrantFiled: May 26, 1987Date of Patent: May 30, 1989Assignee: Sociedad Espanola de Especialidades Farmacotera peuticasInventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
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Patent number: 4820717Abstract: 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: GrantFiled: September 30, 1986Date of Patent: April 11, 1989Assignee: SanofiInventors: Madeleine Mosse, Henri Demarne, Vincenzo Proietto
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Patent number: 4806667Abstract: 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: GrantFiled: December 4, 1986Date of Patent: February 21, 1989Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Jurgen Stoltefuss, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4777294Abstract: 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: GrantFiled: April 17, 1987Date of Patent: October 11, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
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Patent number: 4701559Abstract: 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: GrantFiled: December 28, 1981Date of Patent: October 20, 1987Assignee: Takeda Chemical Industries, Inc.Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
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Patent number: 4695589Abstract: 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: GrantFiled: May 27, 1983Date of Patent: September 22, 1987Assignee: Sterling Drug Inc.Inventor: Richard E. Philion
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Patent number: 4661635Abstract: 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: GrantFiled: October 29, 1984Date of Patent: April 28, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4542159Abstract: There are prepared compounds of the formula: ##STR1## wherein X is the group >C.dbd.O or >CH(OH), Y is the group ##STR2## R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sub.3 is hydrogen or a hydroxy group and R.sub.1 is the adamantyl group or a saturated or single unsaturated C.sub.3 to C.sub.16 cycloalkyl group where the C.sub.3 to C.sub.16 cycloalkyl group can be substituted by a C.sub.1 -C.sub.4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.Type: GrantFiled: May 15, 1979Date of Patent: September 17, 1985Assignee: Degussa AkteinsellschaftInventors: Jurgen Engel, Axel Kleemann, Klaus Posselt, Fritz Stroman, Klaus Thiemer
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Patent number: 4486602Abstract: 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: GrantFiled: September 29, 1981Date of Patent: December 4, 1984Assignee: Takeda Chemical Industries, Ltd.Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
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Patent number: 4374149Abstract: 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: GrantFiled: August 30, 1978Date of Patent: February 15, 1983Assignee: Sterling Drug Inc.Inventor: Richard E. Philion
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Patent number: 4327224Abstract: 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: GrantFiled: June 25, 1976Date of Patent: April 27, 1982Assignee: Sterling Drug Inc.Inventor: Sydney Archer
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Patent number: 4282251Abstract: Cinnamylalkyl-1-naphthylmethylamines, useful as antimycotic agents, and processes for their production.Type: GrantFiled: December 3, 1979Date of Patent: August 4, 1981Assignee: Sandoz Ltd.Inventor: Daniel Berney
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Patent number: 4277420Abstract: Preparation of novel prochiral olefinic compounds which can be asymmetrically hydrogenated to enantiomers, which are converted to ephedrine and pseudoephedrine by described procedures.Type: GrantFiled: September 24, 1979Date of Patent: July 7, 1981Assignee: Monsanto CompanyInventor: Karl E. Koenig