Nitrogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/402)
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Patent number: 4668681Abstract: This invention relates to 2-(4-phenylpiperazinylethyl)anilines, to methods for preparing them and to their uses in medical therapy.These compounds have the following general formula ##STR1## wherein R.sub.1 represents one or more substituents selected from the group consisting of H, CH.sub.3, CF.sub.3, F, Cl, and OCH.sub.3 ; R.sub.2 and R.sub.3, which may be the same or different, and are selected from the group consisting of H and (C.sub.1 -C.sub.4) alkoxy, or R.sub.2 and R.sub.3 taken together can form a chain selected from the group consisting of --O-- (CH.sub.2).sub.n --O--, wherein n=1 or 2 and --O--CH.sub.2 --O--CH.sub.2 with the proviso that R.sub.1 is not meta CF.sub.3 when R.sub.2 =R.sub.3 =H, and pharmaceutically non-toxic salts thereof. The compounds of this invention are useful in the treatment of allergic and anaphylatic conditions and motion sickness.Type: GrantFiled: March 21, 1986Date of Patent: May 26, 1987Assignee: Societe Cortial, S.A.Inventors: Henri Pontagnier, Marie-H/e/ l/e/ ne Creuzet, Claude Feniou, Francoise Guichard, Gis/e/ le Prat
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4650906Abstract: Ethyleneamines are recovered from an aqueous solution of carbonates of ethyleneamines by distilling an aqueous solution of carbonates of ethyleneamines including ethylenediamine, in which the molar ratio of the carbon dioxide component to the ethyleneamines including ethylenediamine is 0.01 to 0.5, whereby ethylenediamine is distilled out together with water. The aqueous solution to be distilled is advantageously prepared by heating an aqueous solution of carbonates of ethyleneamines including ethylenediamine to effect decarboxylation.Type: GrantFiled: February 29, 1984Date of Patent: March 17, 1987Assignee: Toyo Soda Manufacturing Co., Ltd.Inventors: Tsugio Murakami, Taizo Kawamoto
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Patent number: 4645862Abstract: 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: GrantFiled: April 15, 1985Date of Patent: February 24, 1987Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Yoshiyuki Tahara, Yasuhiro Komatsu, Hiroyasu Koyama, Reiko Kubota, Teruhito Yamaguchi, Toshihiro Takahashi
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Patent number: 4645837Abstract: In the transalkylation of tertiary amines, unexpected higher yields are achieved requiring substantially less catalyst and much shorter reaction times at lower reaction temperatures using a homogeneous catalyst in the presence of an alcohol solvent and carbon monoxide. The process may be exemplified by reacting triethylamine and tripropylamine in the presence of a homogeneous triosmiumdodecacarbonyl catalyst, ethanol, and carbon monoxide to prepare diethylpropylamine and ethyldipropylamine.Type: GrantFiled: November 5, 1984Date of Patent: February 24, 1987Assignee: SRI InternationalInventors: Richard M. Laine, Youval Shvo
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Patent number: 4638003Abstract: N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.Type: GrantFiled: August 1, 1984Date of Patent: January 20, 1987Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
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Patent number: 4634770Abstract: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.Type: GrantFiled: November 4, 1983Date of Patent: January 6, 1987Assignees: Asahi Kasei Kogyo Kabushiki Kaisha, Hiroyoshi HidakaInventors: Hiroyoshi Hidaka, Takanori Sone
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Patent number: 4632940Abstract: N-substituted derivatives of 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with local anesthetic activity.Type: GrantFiled: August 3, 1984Date of Patent: December 30, 1986Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
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Patent number: 4625030Abstract: The present invention concerns a potentiated nickel catalyst and its use for the catalytic amination of lower aliphatic alkane derivatives.Type: GrantFiled: May 23, 1984Date of Patent: November 25, 1986Assignee: Union Carbide CorporationInventor: Donald C. Best
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Patent number: 4620006Abstract: Novel 1-(cyanoalkyl)-4-guanylpiperazine acid salts are prepared by reacting novel 1-(cyanoalkyl)piperazines with cyanamide in the presence of an acid. The novel 1-(cyanoalkyl)-4-guanylpiperazine acid salts are advantageously employed to prepare 1-(cyanoalkyl)-4-(2-pyrimidyl)piperazines by reacting them with malonaldehyde in an acidic medium.Type: GrantFiled: August 11, 1982Date of Patent: October 28, 1986Assignee: Eastman Kodak CompanyInventors: Louise O. Sandefur, Wojciech Slusarek, Burton D. Wilson, Cataldo A. Maggiulli
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Patent number: 4620005Abstract: Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.Type: GrantFiled: October 17, 1985Date of Patent: October 28, 1986Assignee: Kowa Co., Ltd.Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Hisashi Kunieda, Koichiro Watanabe, Hiroshi Ishihama
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Patent number: 4620002Abstract: Novel 2-pyrimidyl alkanesulfonates are prepared by reacting a 2-hydroxypyrimidine acid salt with an alkanesulfonyl chloride in the presence of an acid acceptor. The novel 2-pyrimidyl alkanesulfonates are advantageously employed to prepare 1-(cyanoalkyl)-4-(2-pyrimidyl)piperazines by reacting them with a novel 1-(cyanoalkyl)piperazine in the presence of an acid acceptor.Type: GrantFiled: August 11, 1982Date of Patent: October 28, 1986Assignee: Eastman Kodak CompanyInventors: Louise O. Sandefur, Wojciech Slusarek, Burton D. Wilson, Cataldo A. Maggiulli
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Patent number: 4602091Abstract: Piperazine is substantially selectively converted to ethylenediamine and N-aminoethylpiperazine by catalytically reductively aminating piperazine in the presence of added hydrogen, ammonia and (optionally) water under reductive amination conditions selected to provide a piperazine conversion of not more than about 30%.Type: GrantFiled: January 25, 1984Date of Patent: July 22, 1986Assignee: Texaco Inc.Inventor: Michael E. Brennan
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Patent number: 4599335Abstract: Diamine derivatives of the formula ##STR1## where R.sup.1 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl or aralkyl, bicycloalkyl, alkoxy, acyl or halogen, n is 0, 1, 2 or 3, R.sup.2 is alkyl, alkenyl or alkoxy, A is unsubstituted or substituted alkylene or unsubstituted or substituted cycloalkylene, R.sup.3, R.sup.4 and R.sup.5 are each unsubstituted or substituted alkyl, alkenyl, alkynyl or unsubstituted or substituted benzyl, or R.sup.3 and R.sup.4, together with A and the two nitrogen atoms bonded to A, form an unsubstituted or substituted piperazine or perhydrodiazepine ring, or R.sup.4 and R.sup.5, together with the nitrogen atom, form an unsubstituted or substituted heterocyclic ring, R.sup.6 is alkyl, alkenyl, alkynyl or unsubstituted or substituted aralkyl or aryloxyalkyl, and Z is an anion of an acid, and fungicides containing these compounds.Type: GrantFiled: July 31, 1985Date of Patent: July 8, 1986Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Ernst Buschmann, Norbert Meyer, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4594195Abstract: Compounds of formula (I) ##STR1## and acid addition salts thereof, wherein R.sup.1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy; andone of R.sup.2, R.sup.3 and R.sup.4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl; orR.sup.2 is hydrogen and ##STR2## is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.Type: GrantFiled: December 21, 1984Date of Patent: June 10, 1986Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan, John P. Marshall
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Patent number: 4585796Abstract: The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.Type: GrantFiled: August 1, 1983Date of Patent: April 29, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4582937Abstract: Ethyleneamines are efficiently recovered from an aqueous solution thereof by extracting them from the aqueous solution into an organic phase with an extractant selected from carbonyl group-containing organic solvents, benzyl alcohol, carboxylic acids and salts thereof, alkylphosphoric acids and salts thereof, and mixed solvents containing at least one of these extractants. The ethyleneamines in the organic phase is recovered preferably from the organic phase to the aqueous phase by incorporating an acid therein, followed by phase separation.Type: GrantFiled: April 12, 1985Date of Patent: April 15, 1986Assignee: Toyo Soda Manufacturing Co., Ltd.Inventors: Yoichi Hiraga, Tsugio Murakami, Hiroyuki Saito, Osamu Fujii
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Patent number: 4582904Abstract: Synthesis of organic amines by condensation of organic hydroxy compound with ammonia or a primary or secondary amine in the presence of a rare earth metal hydrogen phosphate catalyst.Type: GrantFiled: January 6, 1984Date of Patent: April 15, 1986Assignee: Air Products and Chemicals, Inc.Inventors: James E. Wells, Victoria Eskinazi
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Patent number: 4578517Abstract: A process for preparing polyalkylene polyamine compounds is disclosed wherein ammonia or a primary or secondary amine and an alkanolamine compound are reacted in the presence of an effective amount of a Group IIIB metal acid phosphate at a temperature from about 175.degree. to 400.degree. C. under a pressure sufficient to maintain a substantial amount of the ammonia or amine in the reaction zone. The polyalkylene polyamines thus formed are recovered from the reaction mixture.Type: GrantFiled: September 16, 1983Date of Patent: March 25, 1986Assignee: Air Products and Chemicals, Inc.Inventors: Thomas A. Johnson, Michael E. Ford
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Patent number: 4567257Abstract: Disclosed is a novel class of amidinium salts having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 when taken individually are independently selected from lower-alkyl, aralkyl and cycloalkyl, and, when taken together with the respective nitrogen atoms to which they are attached, R.sub.1 together with R.sub.2, and R.sub.3 together with R.sub.4 independently represent heterocyclic groups having 5 to 7 ring atoms, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are independently selected from hydrogen, lower-alkyl, aryl, aralkyl, and cycloalkyl.The amidinium salts are very active catalysts for converting organic isocyanates to products containing isocyanurate and carbodiimide linkages.Type: GrantFiled: January 16, 1984Date of Patent: January 28, 1986Assignee: The Upjohn CompanyInventor: Dale F. Regelman
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Patent number: 4567174Abstract: A bis(1-substituted biguanide) derivative of the formula:R.sup.3 R.sup.4 N.C(:NR.sup.5)NH.C(NR.sup.9)NR.sup.1 --X--NR.sup.2.C(:NR.sup.9)NH.C(:NR.sup.6)--NR.sup.7 R.sup.8 Vor a tautomeric form thereof, wherein R.sup.1, R.sup.2 and R.sup.9, which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R.sup.1, R.sup.2 and R.sup.9 is other than hydrogen; R.sup.3, R.sup.4, R.sup.7 and R.sup.8, which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R.sup.3, R.sup.4 and the nitrogen atom to which they are attached, or R.sup.7 and R.sup.Type: GrantFiled: May 7, 1984Date of Patent: January 28, 1986Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Michael S. Large
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Patent number: 4552961Abstract: Predominantly linearly extended polyalkylene polyamines are produced, in increased conversion rates, by reacting alkylenediamines with alkylene glycols or alkanolamines using a phosphorus amide catalyst in place of phosphorus acid or acid derivative catalysts.Type: GrantFiled: May 3, 1984Date of Patent: November 12, 1985Assignee: Union Carbide CorporationInventor: William B. Herdle
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Patent number: 4544755Abstract: Phthalimides of the formula I ##STR1## where R is a substituent and the ring A can be further substituted, are cleaved by a process in which a compound of the formula I is treated with an alkanolamine.The compounds prepared according to the invention are useful intermediates for the preparation of dyes, drugs and plastics.Type: GrantFiled: May 23, 1984Date of Patent: October 1, 1985Assignee: Basf AktiengesellschaftInventors: Helmut Hagen, Rolf-Dieter Kohler
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Patent number: 4540523Abstract: Cationic styryl dyestuffs of the formula ##STR1## in which A.sup.1 is an alkyleneoxy or alkyleneamino radical,D.sup.1 is a direct bond or divalent radical,An is an anion, andthe terminal phenyl ring is unsubstituted or substituted by CN, alkyl or alkoxy. The compounds are suitable for dyeing, enscribing and printing paper for dyeing and printing synthetic fibres, especially made of polyacrylonitrile, acid-modified polyesters or polyamides.Type: GrantFiled: October 17, 1980Date of Patent: September 10, 1985Assignee: Bayer AktiengesellschaftInventor: Hermann Beecken
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Patent number: 4539319Abstract: Compounds of formula (I) ##STR1## and acid addition salts thereof, whereinR.sup.1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy;andone of R.sup.2, R.sup.3 and R.sup.4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl;orR.sup.2 is hydrogen and ##STR2## is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.Type: GrantFiled: June 14, 1983Date of Patent: September 3, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan, John P. Marshall
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Patent number: 4517366Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: April 16, 1984Date of Patent: May 14, 1985Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4515947Abstract: Novel cyanoalkylpiperazines are prepared by reacting piperazine with a haloalkylnitrile in the presence of an acid acceptor. The novel cyanoalkylpiperazines are advantageously employed to prepare 1-(cyanoalkyl)-4-(2-pyrimidyl)piperazines by reacting them with halopyrimidines in the presence of an acid acceptor.Type: GrantFiled: August 11, 1982Date of Patent: May 7, 1985Assignee: Eastman Kodak CompanyInventors: Louise O. Sandefur, Wojciech Slusarek, Burton D. Wilson, Cataldo A. Maggiulli
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Patent number: 4507318Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxylates (Z), their preparation and their use as useful drugs for the treatment of various pains.The new derivatives of the present invention have the general formula I ##STR1## in which: R represents a hydrogen or halogen atom, a C.sub.1 to C.sub.4 lower alkyl group, a C.sub.1 to C.sub.4 lower alkoxy group, or a nitro, amino, sulfamoyl or hydroxy group;n represents the values 1, 2 or 3;(R).sub.n may together with the benzene ring also form the naphthyl group;R.sub.1 represents a linear or branched C.sub.1 to C.sub.5 alkyl or alkenyl group or an aryl or benzyl group;R.sub.2 and R.sub.3 represent a hydrogen atom, a linear or branched C.sub.1 to C.sub.5 alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or dialkylaminoalkyl group or an aryl, arylalkyl or cycloalkyl group;R.sub.2 and R.sub.3 possibly also forming a heterocycle of 5 or 6 members with the adjacent nitrogen atom,provided however that when R.sub.Type: GrantFiled: June 22, 1982Date of Patent: March 26, 1985Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin, Bernard Bonnaud, Marie Charveron, Francois Fauran
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Patent number: 4487987Abstract: A method of eliminating color-causing impurities in mixtures of aminoethylpiperazine, polyoxypropylenediamines and alkylphenols by treatment with N,N-diethylhydroxylamine is described. These alkylphenols such as nonylphenol are used in epoxy resins in the automotive and electronics industry. Discoloration of the phenol and subsequent resin occurs if the phenol is not treated with N,N-diethylhydroxylamine. Quantities on the order of 20 to 500 ppm are effective. The decolorization reaction may be conducted at a temperature in the range from about 25.degree. to 50.degree. C.Type: GrantFiled: June 9, 1983Date of Patent: December 11, 1984Assignee: Texaco Inc.Inventors: James H. Paslean, Charles S. Steele
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Patent number: 4469693Abstract: 2-(4-Substituted alkyl-1-piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.Type: GrantFiled: February 25, 1980Date of Patent: September 4, 1984Assignee: Ayerst, McKenna & Harrison Inc.Inventors: Jehan F. Bagli, Tibor Bogri, Katherine Voith
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Patent number: 4448962Abstract: This invention relates to new compounds of value as antibacterial agents. More particularly, it relates to quinoline carboxylic acid derivatives, the hydrates and the acid or alkali addition salts thereof.Type: GrantFiled: October 14, 1981Date of Patent: May 15, 1984Assignee: Kyorin Seiyaku Kabushiki KaishaInventors: Tsutomu Irikura, Seigo Suzue, Akira Ito, Hiroshi Koga
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Patent number: 4446076Abstract: Method of preparing antimicrobial compounds of the formula: ##STR1## comprising the following steps: (1) halogenating allyl halide to form 1,2,3-trihalopropane; (2) dehydrohalogenating the 1,2,3-trihalopropane to form 2,3-dihalo-1-propene;(3) treating the 2,3-dihalo-1-propene with a Grignard reagent of the formula R--MgHal, where R is as defined above, followed by treatment with magnesium, to form 3-(R-substituted)-2-magnesiumhalide)-1-propene;(4) treating the 3-(R-substituted)-2-(magnesiumhalide)-1-propene with cyanogen to form 3-(R-substituted)-2-cyano-1-propene; and(5) brominating the 3-(R-substituted)-2-cyano-1-propene to form the desired product.Type: GrantFiled: December 22, 1981Date of Patent: May 1, 1984Assignee: Merck & Co., Inc.Inventor: Marshall R. Angeles
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Patent number: 4442122Abstract: Antimicrobial compounds of the formula: ##STR1## where R is C.sub.3-12 alkyl, straight or branched chain C.sub.3 -C.sub.8 cycloalkyl; C.sub.3-8 cycloalkylC.sub.1-3 alkyl; or saturated heterocyclic radical selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, and piperidinyl.Type: GrantFiled: December 22, 1981Date of Patent: April 10, 1984Assignee: Merck & Co., Inc.Inventors: John E. Engelhart, Marshall R. Angeles, Michael J. D'Errico
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Patent number: 4436908Abstract: Compounds of the formula (I):R.sub.2 N--(CH.sub.2).sub.n --NH--SO.sub.2 R.sup.1 (I)and salts thereof wherein NR.sub.2 represents a piperidyl, pyrrolidyl, or N-methylpiperazyl group any of which may be substituted by one or two methyl groups; R.sup.1 is a 1-naphthyl group substituted by one or two moieties selected from fluorine, chlorine, bromine, methoxyl, ethoxyl, hydroxyl, acetoxyl, nitro, cyano, amino optionally substituted by one or two C.sub.1-6 alkyl groups, methyl, ethyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, acetamido or carboxamido; and n is 2 or 3, pharmaceutical compositions containing them and a process for their preparation.Type: GrantFiled: March 12, 1982Date of Patent: March 13, 1984Assignee: Johann A. WuelfingInventor: Ljerka Jozic
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Patent number: 4429127Abstract: This invention relates to a new compound of value as antibacterial agent. More particularly, it relates to a quinoline carboxylic acid derivative and the acid addition salts thereof.Type: GrantFiled: February 17, 1982Date of Patent: January 31, 1984Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Tsutomu Irikura, Hiroshi Koga, Akira Ito
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Patent number: 4426521Abstract: Novel cyanoguanidine derivatives, and acid addition salts thereof useful as medicines which have pharmacological actions such as anti-secretory effect, local anesthesia action and the like; and process for the preparation thereof.Type: GrantFiled: January 28, 1982Date of Patent: January 17, 1984Assignee: Eisai Co., Ltd.Inventors: Satoru Tanaka, Katsutoshi Shimada, Kazunori Hashimoto, Kiichi Ema, Koichiro Ueda
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Patent number: 4419363Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.Type: GrantFiled: June 4, 1982Date of Patent: December 6, 1983Assignee: Imperial Chemical Industries PLCInventor: Leslie H. Smith
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Patent number: 4418209Abstract: This invention describes a new class of 1-amidino-3-phenylthiourea and N'-phenylamidinothiourea compounds wherein the phenyl group is ortho substituted, and processes for their preparation. The phenylamidinothiourea compounds may be incorporated into pharmaceutical preparations which are useful for producing anti-ulcerogenic, antisecretory, antispasmodic, antihypertensive, anti-arrhythmic, anesthetic, antidiarrheal and antiparasitic action.Type: GrantFiled: December 21, 1981Date of Patent: November 29, 1983Assignee: William H. Rorer, Inc.Inventors: George H. Douglas, Julius Diamond, William L. Studt, Stuart A. Dodson
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Patent number: 4411904Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.Type: GrantFiled: June 14, 1982Date of Patent: October 25, 1983Assignee: Warner-Lambert CompanyInventor: Ian C. Pattison
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Patent number: 4374779Abstract: The disclosed [[2-(substituted amino)-2-phenylethyl]nitrosoamino]acetonitrile derivatives and the ring closed oxadiazolium salts thereof as well as their pharmaceutically acceptable acid addition salts are antihypertensive agents useful in the treatment of hypertension.Type: GrantFiled: November 16, 1981Date of Patent: February 22, 1983Assignee: American Home Products CorporationInventor: Reinhardt P. Stein
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Patent number: 4369206Abstract: This invention relates to new ammonium salts of .alpha.-ketocarboxylic acids, to their use for the production of amines in situ by photochemical decomposition and to photochemically hardenable coating compositions containing these ammonium salts.Type: GrantFiled: July 2, 1979Date of Patent: January 18, 1983Assignee: Bayer AktiengesellschaftInventors: Wofram Mayer, Hans Rudolph, Eckhard de Cleur, Manfred Schonfelder
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Patent number: 4364954Abstract: Compounds of the formula ##STR1## where X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.Type: GrantFiled: May 29, 1981Date of Patent: December 21, 1982Assignee: Warner-Lambert CompanyInventor: Ian C. Pattison
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Patent number: 4340756Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.Type: GrantFiled: February 4, 1981Date of Patent: July 20, 1982Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4333929Abstract: A compound of formula (II) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents C.sub.1-6 alkyl; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; and R.sup.7 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.Type: GrantFiled: January 19, 1981Date of Patent: June 8, 1982Assignee: Beecham Group LimitedInventor: Barrie C. C. Cantello
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Patent number: 4334085Abstract: A transamination process for producing Mannich products comprising reacting a polyamine with a substantially formaldehyde-free mononitrogen Mannich adduct.Type: GrantFiled: September 14, 1978Date of Patent: June 8, 1982Assignee: Standard Oil Company (Indiana)Inventors: Robert J. Basalay, John H. Udelhofen
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Patent number: 4329240Abstract: Fuel compositions for internal combustion engines are provided containing deposit control additives which maintain cleanliness of intake systems without contributing to combustion chamber deposits. The additives are hydrocarbylpoly(oxyalkylene) aminocarbamates comprising a hydrocarbyl-terminated poly(oxyalkylene) moiety composed of 2-5 carbon oxyalkylene units and one or more 9-30 carbon oxyalkylene groups. Certain additives also find use as dispersants in lubricating oils.Type: GrantFiled: January 5, 1981Date of Patent: May 11, 1982Assignee: Chevron Research CompanyInventor: Jennifer E. Lilburn
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Patent number: 4324724Abstract: A process for the manufacture of polyalkylenepolyamines by reacting a primary or secondary amine with a compound of the formula ##STR1## where X is --Cl, --Br, or --OSO.sub.3 H and R.sup.1 and R.sup.2 are H or saturated alkyl of 1 to 4 carbon atoms, and with at least the stoichiometric amount, based on the compound of the formula I, of an aqueous solution, of from 15 to 45 percent strength, of an alkali metal hydroxide or alkaline earth metal hydroxide, at from 60.degree. to 200.degree. C., cooling the reaction mixture to a temperature at which 2 aqueous phases form, and separating off the upper phase, containing polyalkylenepolyamnines. The rate of reaction can be increased by adding catalytic amounts of compounds which initiate the polymerization of alkyleneimines.Type: GrantFiled: October 2, 1978Date of Patent: April 13, 1982Assignee: BASF AktiengesellschaftInventors: Hans Mueller, Klaus Wulz, Karl-Heinz Beyer, Werner Streit
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Patent number: 4322530Abstract: A process for alkylating a polyamine by contacting, in a liquid media, a polyamine, an olefinic compound, carbon monoxide, and a hydrogen source in the presence of a catalytic amount of a rhodium atom containing compound selected from metallic rhodium, rhodium salts, rhodium oxides, rhodium carbonyls and ligands thereof at a temperature of from about 50.degree. C. to 250.degree. C. and at a pressure of from about 30 to about 300 atmospheres.Type: GrantFiled: February 22, 1980Date of Patent: March 30, 1982Assignee: W. R. Grace & Co.Inventor: Felek Jachimowicz
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Patent number: 4316841Abstract: Process for production of polyalkylene polyamines, preferably non-cyclic polyalkylene polyamines, by reforming of other polyalkylene polyamines. The reforming process is effected by reacting the polyalkylene polyamine starting material in the presence of a phosphate, preferably a boron phosphate, catalyst at elevated temperature and pressure and in the presence of sufficient water and sufficient catalyst, for a reaction period and under reaction conditions otherwise adapted to bring about the desired reforming reaction.Type: GrantFiled: December 8, 1980Date of Patent: February 23, 1982Assignee: Air Products and Chemicals, Inc.Inventors: Michael E. Ford, Thomas A. Johnson
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Patent number: 4316840Abstract: Process for production of polyalkylene polyamines, preferably non-cyclic polyalkylene polyamines, by reforming of other polyalkylene polyamines. The reforming process is effected by reacting the polyalkylene polyamine starting material in the presence of a metal nitrate or sulfate, preferably a sulfate, catalyst at elevated temperature and pressure and in the presence of sufficient water and sufficient catalyst, for a reaction period and under reaction conditions otherwise adapted to bring about the desired reforming reaction.Type: GrantFiled: November 25, 1980Date of Patent: February 23, 1982Assignee: Air Products and Chemicals, Inc.Inventors: Michael E. Ford, Thomas A. Johnson