The Substituent Nitrogen Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Nonionic Bonding Patents (Class 564/164)
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Patent number: 4933369Abstract: The present invention relates to new compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R.sup.1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R.sup.2 wherein R.sup.2 is lower alkyl, alkenyl, alkoxy, or aralkyl; n is an integer of from 2-4; m is an integer of from 0-4; A is S(O).sub.x wherein x is an integer of from 0-2; and Ar is phenyl or thienyl. These compounds are useful as analgesics.Type: GrantFiled: September 30, 1988Date of Patent: June 12, 1990Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Donald W. Hansen, Jr., Gilbert W. Adelstein
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Patent number: 4921945Abstract: Disazo dyes which are useful for dyeing and printing, of the formula ##STR1## in which: D is the radical of a substituted or unsubstituted, homocyclic or heterocyclic diazo component, V.sup.1 and V.sup.2 independently of one another are hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, halogen or cyano, X is hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, halogen, cyano or a group of the formula --NH--CHO, --NH--CO--NH.sub.2, --NH--CO--NH--Q or --NH--CO--(0).sub.m --Q in which m is zero or 1 and Q is substituted or unsubstituted C.sub.1 -C.sub.4 alkyl or phenyl, Z is C.sub.1 -C.sub.4 alkyl--CO--, --CN, --COO--C.sub.1 -C.sub.4 alkyl, --CONH.sub.2 or --CO--C.sub.6 H.sub.5, R.sup.1, R.sup.2 and R.sup.3 independently of one another are in each case a substituted or unsubstituted alkyl radical or R.sup.1 and R.sup.2, together with the nitrogen atom linking them, or R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: May 25, 1988Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventor: Willy Stingelin
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Patent number: 4918196Abstract: A process for optically isomerizing an optically active alpha-amino acid amide comprising heating a D-alpha-amino acid amide or an L-alpha-amino acid amide in the presence of a strongly basic compound; and a process for producing an L-alpha-amino acid, which comprises(1) subjecting a D,L-alpha-amino acid amide or a mixture of a major amount of a D-alpha-amino acid amide and a minor amount of an L-alpha-amino acid amide to the action of a microorganism having the ability to hydrolyze the L-alpha-amino acid to obtain a hydrolyzate containing the L-alpha-amino acid and D-alpha-amino acid,(2) separating the L-alpha-amino acid from the hydrolyzate and recovering the remaining D-alpha-amino acid amide.Type: GrantFiled: February 21, 1986Date of Patent: April 17, 1990Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Masaharu Doya, Toshio Kondo, Hideo Igarashi, Takako Uchiyama
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Patent number: 4891058Abstract: 1-alkyl-3-arylimidazolidine-2,4-diones are prepared by reacting the herbicidally active intermediate N-phenyl-2-substituted-2-alkylamino acetamides with 1,1'-carbonyldiimidazole in a suitable solvent. These herbicidally active intermediates are prepared by reacting alpha-haloacetanilides with the primary amine of choice in an alcohol solvent, in the presence or absence of water, at ambient temperature.Type: GrantFiled: July 18, 1988Date of Patent: January 2, 1990Assignee: ICI Americas Inc.Inventor: Siok H. H. Wee
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Patent number: 4880839Abstract: An acylanilide of the formula: ##STR1## wherein R.sup.1 or R.sup.2 which may be the same or different, each is an electron-withdrawing substituent, alkylthio or phenylthio or R.sup.1 is hydrogen, alkyl or alkoxy; wherein R.sup.3 is hydrogen or halogen; wherein R.sup.4 is hydrogen or acyl wherein A is branched-chain alkylene; and wherein R.sup.5 is phenyl, substituted phenyl or naphthyl. The compounds possess progestational activity.Type: GrantFiled: June 16, 1987Date of Patent: November 14, 1989Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
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Patent number: 4870096Abstract: Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.Type: GrantFiled: December 11, 1986Date of Patent: September 26, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Ian H. Coates, David E. Bays, Colin F. Webb
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Patent number: 4849530Abstract: The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1988Date of Patent: July 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Gerhard Zol, Gerhard Pfarrhofer
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Patent number: 4847412Abstract: The invention relates to a process for racemizing an optically active N-benzylidene amino-acid amide, characterized in that a solution of the N-benzylidene amino-acid amide is mixed in a water-miscible organic solvent with at least 0.05 mole strong base per liter solution.The invention further relates to a process for preparing an L-amino acid by enzymatic separation of the corresponding DL-amino-acid amide with an enzyme preparation from Pseudomonas putida, in which process also unconverted D-amino-acid amide is left behind in solution, characterized in that benzaldehyde is added to the solution, during which addition a precipitate of D-N-benzylidene amino-acid amide is being formed, this precipitate is subsequently, after being separated off, dissolved in an acetone-water mixture, 0.08-0.15 mole KOH/liter solution is subsequently added, the resulting solution is stirred for 1-20 hours at 20.degree.-60.degree. C.Type: GrantFiled: April 10, 1986Date of Patent: July 11, 1989Assignee: Stamicarbon B.V.Inventors: Wilhelmus H. J. Boesten, Hans E. Schoemaker, Bernardus H. N. Dassen
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Patent number: 4808624Abstract: Novel substituted benzamides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.Type: GrantFiled: May 6, 1985Date of Patent: February 28, 1989Assignee: Bristol-Myers CompanyInventors: Ivo Monkovic, David Willner
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Patent number: 4797152Abstract: Novel cyclohexenonecarboxylic acid derivatives exhibit herbicidal and plant growth regulating activity.The cyclohexanedionecarboxylic derivatives are of the formula I ##STR1## wherein A is an aliphatic or aromatic alcohol, or is an amino group which may be substituted by halogen, lower alkoxy, lower alkylthio, nitro or cyano, or is a heterocyclic amino group which is unsubstituted or substituted,R is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 alkylnyl,B is an aliphatic or aromatic radical or is an aliphatic or aromatic carbonyl or sulfonyl group which may be substitued by halogen, lower alkoxy, lower alkylthio, nitro or cyano.The compounds are suitable for selectively controlling grasses in crops of useful plants.Type: GrantFiled: November 14, 1986Date of Patent: January 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4767781Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.Type: GrantFiled: December 8, 1986Date of Patent: August 30, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada
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Patent number: 4767784Abstract: The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.Type: GrantFiled: November 28, 1986Date of Patent: August 30, 1988Inventors: Gerhard Zolss, Gerhard Pfarrhofer
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Patent number: 4760146Abstract: Novel compounds and processes for making and using them. The compounds include ethyl 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxylate, 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxyamide, and N,N-dimethyl-1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxam ide.Type: GrantFiled: February 18, 1986Date of Patent: July 26, 1988Assignee: Pennwalt CorporationInventor: Bruce H. Toder
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Patent number: 4760179Abstract: Substituted aminoxy propionamide derivatives corrsponding to the formula ##STR1## said derivatives being useful as color improvers and stabilizers in various polymeric substrates.Type: GrantFiled: April 4, 1986Date of Patent: July 26, 1988Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 4754047Abstract: 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: GrantFiled: December 10, 1984Date of Patent: June 28, 1988Assignee: American Cyanamid CompanyInventors: Jane A. Kiernan, Pamela K. Baker
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Patent number: 4751255Abstract: The invention relates to a polymeric polyamine having a molecular weight of from 1000 to 16000 and containing from 2 to 4 primary amino groups per molecule, the polymeric polyamine being the condensation product of a polycarboxylic acid or ester with a stoichiometric excess of a polyamine having terminal aminopropoxy groups and a molecular weight below 500.Type: GrantFiled: March 19, 1987Date of Patent: June 14, 1988Assignee: Imperial Chemical Industries PLCInventors: James M. Bentley, James P. Brown, Guy Frijns, David J. Sparrow
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Patent number: 4746737Abstract: Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.Type: GrantFiled: July 16, 1986Date of Patent: May 24, 1988Assignee: Kowa Co., Ltd.Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Koichiro Watanabe, Tomio Ohta, Nobuo Yokoo, Masahiko Nagakura
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Patent number: 4743595Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.Type: GrantFiled: June 12, 1985Date of Patent: May 10, 1988Assignee: Fuji Photo Film Co., Ltd.Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
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Patent number: 4732916Abstract: A guanidinomethylbenzoic acid derivative represented by the formula ##STR1## or a salt thereof. An antiulcer agent comprising the compounds of the afore-said formula as an effective ingredient is also disclosed.Type: GrantFiled: July 16, 1986Date of Patent: March 22, 1988Assignees: Kabushiki Kaisha Med-Creat, Toshio SatohInventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa
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Patent number: 4730075Abstract: A process for the production of (1) an ether or (2) a second amine comprises reacting an activated olefin with respectively an alcohol or first amine in the presence of a catalyst which is either (a) an amidine or (b) a Lewis base and epoxide. The same catalyst may also be used to carry out the reverse reaction in which an activated olefin and an alcohol or first amine are produced from the appropriate ether or second amine.Type: GrantFiled: June 20, 1986Date of Patent: March 8, 1988Assignee: BP Chemicals LimitedInventor: Michael J. Green
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4681898Abstract: Compounds of the formula ##STR1## where n is 0 or 1,R is alkyl, phenyl or R.sub.4 -substituted phenyl,R.sub.2 and R.sub.3 are, independently, alkyl orR.sub.2 and R.sub.3 together with N is ##STR2## m is 1, 2 or 3, R.sub.1 and R.sub.4 are, independently hydrogen, halo, alkyl or alkoxy, andR.sub.5 is hydrogen or alkyl of 1 to 6 carbon atomsor their pharmaceutically acceptable salts are useful as anti-diabetic agents, in particular, as hypoglycemic agents or inhibitors of post-prandial hypoglycemia.Type: GrantFiled: May 8, 1984Date of Patent: July 21, 1987Assignee: Sandoz Pharmaceuticals Corp.Inventor: Jeffrey Nadelson
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Patent number: 4673700Abstract: Amide substituted benzylhydroxylamine derivatives are effective in stabilizing polyolefin compositions containing a stabilizer or mixture of stabilizers selected from the group consisting of the phenolic antioxidants, the hindered amine light stabilizers, the alkylated hydroxybenzoate light stabilizers, the ultraviolet light absorbers, the organic phosphorus compounds, the alkaline metal salts of fatty acids and the thiosynergists, against degradation upon high temperature extrusion, exposure to the combustion products of natural gas, gamma irradation or upon storage for extended periods. These amide substituted benzylhydroxylamine derivatives exhibit resistance to loss or extraction during processing and in end-use applications.Type: GrantFiled: November 21, 1985Date of Patent: June 16, 1987Assignee: Ciba-Geigy CorporationInventors: Ramanathan Ravichandran, Thomas E. Snead
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Patent number: 4668703Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
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Patent number: 4661510Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.Type: GrantFiled: October 21, 1985Date of Patent: April 28, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano
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Patent number: 4659733Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.Type: GrantFiled: December 6, 1984Date of Patent: April 21, 1987Assignee: Alcon Laboratories, Inc.Inventors: Mark T. DuPriest, Billie M. York, Jr.
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Patent number: 4658061Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.Type: GrantFiled: December 24, 1984Date of Patent: April 14, 1987Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Richard L. Simon
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Patent number: 4642378Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.Type: GrantFiled: April 11, 1985Date of Patent: February 10, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, L. David Waterbury
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Patent number: 4639468Abstract: A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.Type: GrantFiled: August 23, 1985Date of Patent: January 27, 1987Assignee: Continental Pharma Inc.Inventors: Romeo Roncucci, Claude L. Gillet, Alexis H. Cordi, Mark A. Martens, Joseph L. Roba, Paul J. Niebes, Georges E. Lambelin, William R. Van Dorsser
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Patent number: 4629727Abstract: Compounds of formula I ##STR1## in which n=0 or 1; in which, when n=0, R.sub.1 is H, an alkyl, a cycloalkyl, a cycloalkylmethyl, an alkenyl or, an alkynyl group a heterocyclic ring or an optionally substituted phenyl ring or when n=1, R.sub.1 is H or an alkyl group;in which R.sub.2 and R.sub.3 are H or an alkyl group;in which A is a group of formula III--(CH.sub.2).sub.x --W--(CH.sub.2).sub.y -- IIIin which W is an oxygen atom or a group of formula --S(O).sub.m --, a group of formula --CR.sub.12 R.sub.13 --, a cycloalkylidene group or a cycloalkylene group; x is 0 or an integer from 1 to 5; y is 0 or an integer from 1 to 5.in which R.sub.4 is a carbocyclic ring, a heterocyclic ring, a cyano group, a carbamoyl group, an alkoxycarbonyl group, an amido group, an acyloxy group, a hydroxy group, a thiol group, or a group of formula --OR.sub.20, --SR.sub.20, --SOR.sub.20 or SO.sub.2 R.sub.20.in which R.sub.5, R.sub.6 and R.sub.Type: GrantFiled: September 28, 1983Date of Patent: December 16, 1986Assignee: The Boots Company PLCInventors: Antonin Kozlik, Wilfred H. Wells
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Patent number: 4604128Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(.dbd.B)NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.Type: GrantFiled: September 10, 1985Date of Patent: August 5, 1986Assignee: ICI Australia LimitedInventors: Keith G. Watson, John D. Wishart, Graeme J. Farquharson, Graham J. Bird, Lindsay E. Cross
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Patent number: 4601839Abstract: Novel .alpha.-aminoacetamides are powerful stabilizers for organic materials subject to oxygen and heat degradation, and particularly for synthetic natural rubber, synthetic ester lubricants and synthetic resinous materials. A wide range of substituents on the amine and amide N atoms, at least one of which substituents is an alkylene imine (cyclic), and an even wider range of substituents on the saturated carbon atom, yields an array of stabilizers having a wide range of compatibility in compositions comprising various synthetic resinous compounds to be stabilized.Novel syntheses are provided utilizing at least one amine nucleophilic agent, a trichloromethide ion generating agent, and an alkoxide ion generating agent, which together in the presence of aqueous alkali and an onium salt, yield novel .alpha.-aminoacetamides in which a wide choice of substituents may be introduced. The nucleophilic agent may be a primary or secondary amine, or one of each. The trichloromethide ion generating agent is a haloform.Type: GrantFiled: November 13, 1981Date of Patent: July 22, 1986Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4595759Abstract: The 2-aryl-1-aminoalkylcyclohexane nitrile, carboxylic acid or amide and derivatives thereof and methods of preparing same.Type: GrantFiled: February 15, 1985Date of Patent: June 17, 1986Assignee: Pennwalt CorporationInventors: Thomas A. Davidson, Telfer L. Thomas
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Patent number: 4585894Abstract: Processes are described for preparing pharmaceutical 9-carbamoyl-9-aminoalkylfluorenes and intermediates in their preparation.Type: GrantFiled: October 19, 1983Date of Patent: April 29, 1986Assignee: Eli Lilly and CompanyInventors: Derek Johnson, Alan C. Spreadbury
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Patent number: 4564695Abstract: An N.sup..alpha. -protected-N.sup.G -protected-arginyl-p-nitro-anilide with high purity can be produced in high yield by reacting an N.sup..alpha. -protected-N.sup.G -protected-arginine with p-nitroaniline in pyridine in the presence of a condensing agent.Type: GrantFiled: September 13, 1984Date of Patent: January 14, 1986Assignee: Nitto Boseki Co., Ltd.Inventors: Katsumasa Kuroiwa, Shuichi Nakatsuyama, Takeshi Nagasawa
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Patent number: 4560795Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.Type: GrantFiled: February 6, 1984Date of Patent: December 24, 1985Assignee: Merrell Dow France et Cie.Inventors: Philippe Bey, Michel Jung
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Patent number: 4559361Abstract: Novel compounds of the formula: ##STR1## wherein R is phenyl-C.sub.1-6 alkyl, and salts thereof, have intraocular pressure depressant action.Type: GrantFiled: October 5, 1983Date of Patent: December 17, 1985Assignee: Senju Pharmaceutical Co., Ltd.Inventor: Yoshikazu Oka
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Patent number: 4552982Abstract: 9-Carbamoyl-9-(2-cyanoethyl)fluorenes are converted to 9-carbamoyl-9-(3-aminopropyl)fluorenes by catalytic hydrogenation in the presence of a strong acid.Type: GrantFiled: August 1, 1983Date of Patent: November 12, 1985Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, William Pfeifer
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Patent number: 4548756Abstract: Novel oxime ethers and oxime esters of the formula I given herein have various advantageous effects with regard to stimulation of plant growth, particularly in the early stage of development of the plant. Furthermore, such compounds have the property of rendering, in the sense of an antidote action, agricultural chemicals which would otherwise damage the plants (phytotoxic chemicals) more compatible with the cultivated plants. Herbicides that are insufficiently selective can be used for example in the presence of such oxime derivatives in specific cultivated crops for combating weeds, without disadvantageous consequences for the cultivated plants.Type: GrantFiled: December 7, 1984Date of Patent: October 22, 1985Assignee: Ciba Geigy CorporationInventor: Henry Martin
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Patent number: 4545995Abstract: The novel unsaturated arylalkyl ammonium salts described herein are useful as antiarrhythmic agents. A method of treating arrhythmia by increasing the refractoriness of cardiac tissue is provided, as well as pharmaceutical formulations containing such ammonium salts.Type: GrantFiled: July 12, 1983Date of Patent: October 8, 1985Assignee: Schering A.G.Inventors: William C. Lumma, Jr., Ronald A. Wohl
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Patent number: 4530798Abstract: Novel oxime ethers and oxime esters of the formula I given herein have various advantageous effects with regard to stimulation of plant growth, particularly in the early stage of development of the plant. Furthermore, such compounds have the property of rendering, in the sense of an antidote action, agricultural chemicals which would otherwise damage the plants (phytotoxic chemicals) more compatible with the cultivated plants. Herbicides that are insufficiently selective can be used for example in the presence of such oxime derivatives in specific cultivated crops for combating weeds, without disadvantageous consequences for the cultivated plants.Type: GrantFiled: September 30, 1982Date of Patent: July 23, 1985Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4529556Abstract: The invention bis((aryl)vinyl)benzenes wherein the aryl and benzene moieties may be substituted, and the vinyl carbon alpha to the central benzene ring may be further substituted with an aliphatic group.Type: GrantFiled: August 19, 1983Date of Patent: July 16, 1985Assignee: The Dow Chemical CompanyInventor: Kenneth J. Bruza
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Patent number: 4526999Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: April 25, 1983Date of Patent: July 2, 1985Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Timothy F. Gallagher
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Patent number: 4508735Abstract: 9-(N-alkanoylaminoalkyl)-fluorenes are anti-arrhythmic agents.Type: GrantFiled: September 21, 1983Date of Patent: April 2, 1985Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Terry D. Lindstrom
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Patent number: 4503232Abstract: The invention provides a novel method for the preparation of an .alpha.-ketoamide imine having a characteristic structure expressed by the formula ##STR1## in which R is a group such as an alkyl, aryl or the like group, in a one-step reaction in which a halogen-containing organic compound reacts with a primary amine and carbon monoxide in the presence of a carbonylation catalyst. The product compound is useful as an intermediate for the synthesis of various kinds of organic compounds including medicines and agricultural chemicals.Type: GrantFiled: September 24, 1982Date of Patent: March 5, 1985Assignee: Agency of Industrial Science & TechnologyInventors: Toshiaki Kobayashi, Masato Tanaka
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Patent number: 4497745Abstract: Novel oxime ethers and oxime esters of the formula I given herein have various advantageous effects with regard to stimulation of plant growth, particularly in the early stage of development of the plant. Furthermore, such compounds have the property of rendering, in the sense of an antidote action, agricultural chemicals which would otherwise damage the plants (phytotoxic chemicals) more compatible with the cultivated plants. Herbicides that are insufficiently selective can be used for example in the presence of such oxime derivatives in specific cultivated crops for combating weeds, without disadvantageous consequences for the cultivated plants.Type: GrantFiled: September 30, 1982Date of Patent: February 5, 1985Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4486592Abstract: 9-Carbamoylfluorene derivatives are useful intermediates in a synthesis of 9-carbamoyl-9-(3-aminopropyl)fluorene antiarrhythmic agents.Type: GrantFiled: October 19, 1983Date of Patent: December 4, 1984Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Terry D. Lindstrom
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Patent number: 4478836Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group;n represents the value 1 or 2;R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom;R.sub.1 and R.sub.2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom;R.sub.3 and R.sub.4 represent a hydrogen atom or a lower alkyl group;R.sub.3 and R.sub.Type: GrantFiled: June 22, 1982Date of Patent: October 23, 1984Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Bernard Bonnaud, Michel Morre, Antoine Stenger
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Patent number: 4466822Abstract: Novel oxime ethers and oxime esters of the formula I given herein have various advantageous effects with regard to stimulation of plant growth, particularly in the early stage of development of the plant. Furthermore, such compounds have the property of rendering, in the sense of an antidote action, agricultural chemicals which would otherwise damage the plants (phytotoxic chemicals) more compatible with the cultivated plants. Herbicides that are insufficiently selective can be used for example in the presence of such oxime derivatives in specific cultivated crops for combating weeds, without disadvantageous consequences for the cultivated plants.Type: GrantFiled: March 11, 1980Date of Patent: August 21, 1984Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4466977Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.Type: GrantFiled: November 4, 1982Date of Patent: August 21, 1984Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz