The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 544/389)
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Patent number: 5026853Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: September 20, 1990Date of Patent: June 25, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 5025005Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: July 23, 1990Date of Patent: June 18, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
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Patent number: 5017619Abstract: The invention is directed to phenethanolamine derivatives and their pharmaceutically compatible salts, having the formula ##STR1## wherein n is the number 1 or 2; L.sup.1 and L.sup.2 are hydrogen, C.sub.1-3 -(alkyl)carbonyl or C.sub.1-3 (alkoxy) carbonyl; T is hydrogen or methyl; X.sup.1 and X.sup.2 are phenyl or phenyl which is monosubstituted in the m-position by Br, Cl, F, CF.sub.3 and NO.sub.2 ; Y is --(CH.sub.2).sub.1-6 --O--G, --(CH.sub.2).sub.1-6 --CH.dbd.CH--C(O)--Z, --C(O)--Z or --CH(COOR").sub.2 ; G is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or --(CH.sub.2).sub.1-4 --Q; Q is phenoxy, phenyl, p-fluorophenyl or p-phenoxyphenyl; Z is a --OR or --N(R,R'); R and R' are hydrogen or C.sub.1-4 -alkyl or R and R' together with the N-atom to which they are attached form a 5- or 6-membered saturated ring which optionally contains an O-atom or an additional N-atom; and R" is C.sub.1-4 -alkyl.Type: GrantFiled: December 16, 1988Date of Patent: May 21, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5011928Abstract: The reaction of N-substituted piperazines with carboxylic acids or their active derivatives such as lower-alkyl esters or the acid chlorides, leads to the formation of new piperazine carboxamides of general structural formula I: ##STR1## These compounds and the physiologically acceptable salts thereof are useful as analgesics and antiinflammatory agents.Type: GrantFiled: February 28, 1990Date of Patent: April 30, 1991Assignee: Fabrica Espanola de Productos Quimicos y Farmeceuti Cos S.A. (FAES)Inventors: Aurelio O. Venero, Antonio T. Avello
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Patent number: 5006577Abstract: N-hydroxy-substituted hindered amine light stabilizers impart outstanding stabilization properties to ambient cured coatings based on a variety of resins, the stabilized coatings exhibiting improved durability, weatherability, and the like.Type: GrantFiled: October 19, 1988Date of Patent: April 9, 1991Assignee: Ciba-Geigy CorporationInventors: Rudolf A. Behrens, Andrew Mar
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Patent number: 4997836Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: November 9, 1989Date of Patent: March 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa
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Patent number: 4977141Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: December 11, 1990Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4977156Abstract: Amino piperazine esters, preferably of the formula: ##STR1## wherein x is 0 or 1 and each R is independently hydrogen or inert substitution, are produced by reacting an (optionally substituted) N-(2-aminoethyl) piperazine with an (optionally substituted) alkylene carbonate. The novel compounds are biocides that retard the growth of fungi and are also useful in preparing polymers.Type: GrantFiled: July 26, 1988Date of Patent: December 11, 1990Assignee: The Dow Chemical CompanyInventors: Jimmy Myers, Wilfred W. Wilson
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Patent number: 4963680Abstract: A piperazine derivative of formula (I) ##STR1## in which: R is hydrogen or a straight or branched (C.sub.1 -.sub.4) alkoxycarbonyl group; andA is a 7-methoxy-1-naphthalenyl, 6-methoxy-2,3-dihydro-1-(1H)-indenyl or 7-methoxy-1,2,3,4-tetrahydro-1-naphthalenyl group, or an optically active isomer thereof, or a salt thereof.Type: GrantFiled: August 2, 1989Date of Patent: October 16, 1990Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Daniel Obitz, Gerard Defosse, Elisabeth Dewitte, Corinne Veronique
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Patent number: 4918073Abstract: A compound I ##STR1## in which R.sup.1 is cycloalkyl, alkenyl, cycloalkenyl, phenyl, ##STR2## whereJ, L, M, and E are methine or nitrogen and J', L', M', and E' are methylene, carbonyl or imino;R.sup.2 is phenyl or phenylalkyl;a is various amine radicals;m is 2, 3 or 4; andn is 1, 2, 3, or 4 is described; salts of these compounds I are also described. Compounds I and the salts are calcium antagonists.Type: GrantFiled: January 7, 1987Date of Patent: April 17, 1990Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Ruger, Hansjorg Urbach, Wilhelm Bartmann, Joachim Kaiser
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Patent number: 4895847Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: September 21, 1988Date of Patent: January 23, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4894466Abstract: This invention discloses intermediates and a process for the preparation of 6-desmethyl-6-.beta.-hydroxymethyl derivatives of lovastatin and analogs thereof at the 8-acyl side chain.Type: GrantFiled: February 29, 1988Date of Patent: January 16, 1990Assignee: Merck & Co., Inc.Inventors: Ta Jyh Lee, William F. Hoffman
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Patent number: 4894465Abstract: This invention discloses intermediates and processes for the preparation of 6-desmethyl-6-.alpha. hydroxymethyl derivatives of lovastatin and analogs thereof at the 8-acyl side chain.Type: GrantFiled: February 29, 1988Date of Patent: January 16, 1990Assignee: Merck & Co., Inc.Inventors: Ta J. Lee, William F. Hoffman
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Patent number: 4885365Abstract: Compounds having the formula: ##STR1## wherein: a. R is an organic radical selected from an alkyl group, an alkenyl group, an aryl group or an aralkyl group in which the alkyl or alkenyl groups contain up to 32 carbon atoms and the aryl or aralkyl groups contain up to 15 carbon atoms;b. R.sup.1 is hydrogen or an organic radical selected from an alkyl group or alkenyl group, an aryl or aralkyl group in which the alkyl or alkenyl groups contain up to 32 carbon atoms and the aryl or aralkyl groups contain up to 15 carbon atoms;c. R.sup.2 and R.sup.3 are the same or different alkyl groups containing from 1 to 32, more preferably 4 to 8, carbon atoms eachare effective antiwear and antioxidant additives in lubricating oil.Type: GrantFiled: May 20, 1988Date of Patent: December 5, 1989Assignee: Ethyl Petroleum Additives, Inc.Inventor: William Y. Lam
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Patent number: 4880808Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: March 9, 1988Date of Patent: November 14, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4876279Abstract: Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 26, 1988Date of Patent: October 24, 1989Assignee: Merck & Co., Inc.Inventors: Ta J. Lee, William F. Hoffman, Clarence S. Rooney
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Patent number: 4864038Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: June 10, 1988Date of Patent: September 5, 1989Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
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Patent number: 4857547Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##Type: GrantFiled: January 7, 1988Date of Patent: August 15, 1989Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee
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Patent number: 4857546Abstract: Novel 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##Type: GrantFiled: January 7, 1988Date of Patent: August 15, 1989Assignee: Merck & Co., Inc.Inventors: Mark Duggan, George D. Hartman
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Patent number: 4855292Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.2 is 1-pyrrolidinyl which may have 1 to 2 substituents selected from the group consisting of (i) C.sub.1 -C.sub.6 alkyl, (ii) amino-(C.sub.1 -C.sub.6)alkyl, said amino being optionally substituted by 1 or 2 substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl, and C.sub.1 -C.sub.6 alkoxycarbonyl, (iii) amino which may be substituted by 1 or 2 substituents selected from C.sub.1 -C.sub.6 alkyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, and C.sub.1 -C.sub.6 alkanoyl, and (iv) 2-oxo-1,3-dioxolenemethylamino which is substituted by C.sub.1 -C.sub.6 alkyl; or 1-piperidinyl which may have 1 to 3 substituents selected from oxo, hydroxy, halogen and C.sub.1 -C.sub.6 alkyl, and R.sup.3 is C.sub.1 -C.sub.Type: GrantFiled: July 23, 1987Date of Patent: August 8, 1989Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hiraki Ueda, Hisashi Miyamoto, Shinji Aki, Tatsuya Otsuka
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4780495Abstract: N-(substituted)-1-(piperazinealkyl)-.alpha.-(3,5-dialkyl-4-hydroxyphenyl)-. alpha.,.alpha.-disubstited acetamides, are novel compounds prepared by a novel modification of the ketoform process. The compounds are useful as stabilizers for organic materials subject to degradation in an environment in which the materials are exposed to heat, oxidation and light, particularly ultraviolet light. The compounds are especially useful in combination with known secondary stabilizers.Type: GrantFiled: January 25, 1988Date of Patent: October 25, 1988Assignee: The B. F. Goodrich CompanyInventors: John T. Lai, Pyong N. Son
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Patent number: 4772695Abstract: A process for the preparation of vinyl carbamates of formula I ##STR1## is described which comprises heating an .alpha.-halogeno-carbamate of formula II ##STR2## in which X is a halogen atom at a temperature between 70.degree. and 250.degree. C. for a period of time between several minutes up to several hours. R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different. The process is applicable to a great variety of products in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 have different meanings. The process permits to prepare in a simple and economical fashion, vinyl carbamates, which have industrial value and novel vinyl carbamates.Type: GrantFiled: September 19, 1983Date of Patent: September 20, 1988Assignee: Societe Nationale des Poudres et ExplosifsInventors: Roy A. Olofson, Gary P. Wooden, Jonathan T. Martz
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Patent number: 4737518Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: September 12, 1986Date of Patent: April 12, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
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Patent number: 4624953Abstract: Compounds having the general formula ##STR1## as herein defined and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions containing said compounds. Methods of treatment of humans and animals by such compounds and compositions.Type: GrantFiled: July 28, 1983Date of Patent: November 25, 1986Inventors: Anders K. Bjork, Erik G. Christensson
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Patent number: 4550164Abstract: Isobutylene carbonate and certain 1-substituted piperazine compounds are reacted in a process that forms 2-methyl-2-hydroxypropyl 4-substituted piperazine-1-carboxylate compounds which are medicinal agents or synthetic intermediates for such agents. The features of the process allow the preparation of an essentially pure 2-methyl-2-hydroxypropyl carboxylate compound.Type: GrantFiled: April 24, 1981Date of Patent: October 29, 1985Assignee: Pfizer Inc.Inventors: Irving M. Goldman, Donald E. Kuhla, Constantine Sklavounos
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Patent number: 4423049Abstract: 1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-pyrimidyl substituents in the 4- position have been synthesized and demonstrate useful anxiolytic properties. The compound 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedi one, which has selective anxiolytic activity, constitutes the preferred embodiment of the invention.Type: GrantFiled: December 28, 1981Date of Patent: December 27, 1983Assignee: Mead Johnson & CompanyInventor: Davis L. Temple, Jr.
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Patent number: 4374990Abstract: A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting of(A) an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,(B) substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.Type: GrantFiled: October 26, 1979Date of Patent: February 22, 1983Assignee: Hoechst AktiengesellschaftInventors: Rolf-Ortwin Weber, Alfons Soder, Istvan Boksay
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Patent number: 4274837Abstract: 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: July 2, 1979Date of Patent: June 23, 1981Assignee: Chevron Research CompanyInventor: Jennifer E. Lilburn
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Patent number: 4252804Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.Type: GrantFiled: January 13, 1978Date of Patent: February 24, 1981Assignee: Metabio-JoullieInventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
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Patent number: 4247549Abstract: Piperazine-1-carboxylic acid esters which are useful as antidepressants and as analgesics.Type: GrantFiled: December 27, 1978Date of Patent: January 27, 1981Assignee: ICI Americas Inc.Inventors: Cyrus J. Ohnmacht, Jeffrey B. Malick
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Patent number: 4204064Abstract: A method, composition and compounds useful in said compositions for treating the skin and scalp characterized by an excessive secretion of sebum to improve the condition thereof by reducing said excessive secretion of sebum includes topically applying to a human having skin and/or a scalp so characterized a cosmetic composition containing as an active ingredient a derivative of cysteine or cysteamine. The composition contains about 0.1-5 weight percent of said derivative and also contains as a carrier for the active ingredient, water, a mixture of water and a lower alkanol, a lower alkanol, a mixture of a lower alkanol and a cosmetic resin, a reducing agent, a neutralizing agent or a vegetable oil.Type: GrantFiled: January 24, 1978Date of Patent: May 20, 1980Assignee: L'OrealInventor: Gregoire Kalopissis
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Patent number: 4183933Abstract: 2,3,4,7,8,9-Substituted octahydropyrazinopyrimidinones and acid addition salts thereof. A process for the preparation of said compounds. A pharmaceutical composition comprising such a compound and a conventional carrier. A process for the preparation of said composition. Method of medical treatment of human beings and animals using such compounds.Type: GrantFiled: August 30, 1978Date of Patent: January 15, 1980Assignee: AB FerrosanInventors: Anders K. K. Bjork, Aina L. Abramo, Sven E. H. Hernestam, Bengt E. S. Kjellberg
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Patent number: 4182872Abstract: Compounds of the formula ##STR1## wherein R is hydrogen (lower)alkyl, phen(lower)alkyl, benzoyl(lower)alkyl, or p-halobenzoyl(lower)alkyl; R.sup.1 is hydrogen or (lower)alkyl; R.sup.2 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, trifluoromethyl, or amino in the 7-, 8-, or 9-position; R.sup.3 is hydrogen, or (lower)alkyl; and R.sup.4 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, or trifluoromethyl in the 7-, 8-, or 9-position; or the non-toxic acid addition salts thereof; exert a hypotensive effect in hypertensive animals. Also disclosed are chemical intermediates, including 4-(lower)alkyl-1-(o-nitrophenyl)piperazine-2-carboxylic acids.Type: GrantFiled: September 25, 1978Date of Patent: January 8, 1980Assignee: American Home Products CorporationInventors: Meier E. Freed, John R. Potoski
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Patent number: 4160648Abstract: Fuel compositions for internal combustion engines are provided which contain deposit control additives which maintain cleanliness of intake systems without contributing to combustion chamber deposits. The additives are polyloxyalkylene carbamates comprising a hydroxy- or hydrocarbyloxy-terminated polyloxyalkylene chain of 2-5 carbon oxyalkylene units bonded through an oxycarbonyl group to a nitrogen atom of a polyamine having from 2 to 10 amine nitrogens and from 2 to 40 carbons with a carbon:nitrogen ratio between about 1:1 and 10:1.Type: GrantFiled: May 27, 1977Date of Patent: July 10, 1979Assignee: Chevron Research CompanyInventors: Robert A. Lewis, Lewis R. Honnen
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Patent number: 4139621Abstract: 1-(3,5-Dichlorophenyl)piperazines bearing a fluoro, chloro, methyl, nitro, hydroxy, methoxy, cyano, amino, methylamino or dimethylamino substituent in the 4-position of the phenyl ring and being further optionally substituted in the 4-position of the piperazine ring by tetrahydropyranyl, alkyl, formyl, carboxy, alkanoyl or carboalkoxy, and the acid addition salts thereof, are tranquilizers. A typical embodiment is 1-(3,4,5-trichlorophenyl)piperazine hydrochloride.Type: GrantFiled: December 5, 1977Date of Patent: February 13, 1979Assignee: Beecham Group LimitedInventors: Derek V. Gardner, Alexander C. Goudie
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Patent number: 4138567Abstract: Compounds of the formula ##STR1## wherein R is hydrogen (lower)alkyl, phen(lower)alkyl, benzoyl(lower)alkyl, or p-halobenzoyl(lower)alkyl; R.sup.1 is hydrogen or (lower)alkyl; R.sup.2 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, trifluoromethyl, or amino in the 7-, 8-, or 9-position; R.sup.3 is hydrogen, or (lower)alkyl; and R.sup.4 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, or trifluoromethyl in the 7-, 8-, or 9-position; or the non-toxic acid addition salts thereof; exert a hypotensive effect in hypertensive animals.Type: GrantFiled: September 22, 1977Date of Patent: February 6, 1979Assignee: American Home Products CorporationInventors: Meier E. Freed, John R. Potoski
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Patent number: 4125612Abstract: This invention relates to N-1(p-biphenylalkyl) piperazines, to the processes for making such compounds and to the use of such compounds as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis.Type: GrantFiled: June 20, 1977Date of Patent: November 14, 1978Assignee: Schering CorporationInventor: Margaret H. Sherlock
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Patent number: 4112091Abstract: Inhibiting methanogenesis by adding polyhaloalkyl or alkenyl alcohol esters of piperazino acids of the formula ##STR1## wherein X and Z are oxygen or sulphur.Type: GrantFiled: April 4, 1977Date of Patent: September 5, 1978Assignee: Sandoz Ltd.Inventors: Hans Nesvadba, Hellmuth Reinshagen
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Patent number: 4110450Abstract: 1,2-Dithiole derivatives of the formula: ##STR1## WHEREIN Het represents an aromatic heterocyclic radical with six atoms in the ring two of which are nitrogen atoms, the heterocyclic radical optionally carrying a single substituent selected from halogen, alkyl, alkoxy, mercapto, alkylthio, dialkylamino, pyrrolidin-1-yl, piperidino, morpholino and 4-alkylpiperazin-1-yl and R represents halogen, alkyl (optionally substituted by alkoxycarbonyl), carboxy, alkoxycarbonyl, carbamoyl, N-alkylcarbamoyl or a group R.sub.1 --C(OH)-- in which R.sub.1 represents hydrogen or alkyl, the said alkyl, alkoxy and alkylthio radicals or alkyl or alkoxy moieties containing 1 to 4 carbon atoms except in the case of R.sub.1 which contains 1 to 3 carbon atoms when an alkyl radical, are new compounds useful in the treatment of bilharziasis.Type: GrantFiled: February 9, 1977Date of Patent: August 29, 1978Assignee: Rhone-Poulenc IndustriesInventors: Michel Barreau, Claude Cotrel, Claude Jeanmart
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Patent number: 4105664Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.Type: GrantFiled: March 18, 1977Date of Patent: August 8, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
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Patent number: 4092318Abstract: Compounds are provided having the structure ##STR1## WHEREIN N IS 1, 2 OR 3, M AND M' ARE 0, 1 OR 2, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## or lower alkoxyalkylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR3## These compounds are useful in the treatment of hypertension.Type: GrantFiled: March 15, 1976Date of Patent: May 30, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic Peter Hauck, Joyce Reid, Venkatachala L. Narayanan, Christopher M. Cimarusti, Rudiger D. Haugwitz, Joseph E. Sundeen
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Patent number: 4089958Abstract: Compounds of the formula ##STR1## WHEREIN R is hydrogen (lower)alkyl, phen(lower)-alkyl, benzoyl(lower)alkyl, or p-halobenzoyl-(lower)alkyl; R.sup.1 is hydrogen or (lower)alkyl; R.sup.2 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, trifluoromethyl, or amino in the 7-, 8-, or 9-position; R.sup.3 is hydrogen, or (lower)alkyl; and R.sup.4 is hydrogen, (lower)-alkyl, (lower)alkoxy, chlorine, fluorine, or trifluoromethyl in the 7-, 8-, or 9-position; or the non-toxic acid addition salts thereof; exert a hyptotensive effect in hypertensive animals.Type: GrantFiled: December 20, 1976Date of Patent: May 16, 1978Assignee: American Home Products CorporationInventors: Meier E. Freed, John R. Potoski