Benzene Ring Containing Patents (Class 564/47)
- The benzene ring is part of a substituent which contains sulfur (Class 564/49)
- The benzene ring is part of a substituent which contains nitrogen (Class 564/50)
- The benzene ring is part of a substituent which contains oxygen (Class 564/52)
- The benzene ring is part of a substituent which contains halogen bonded directly to carbon (Class 564/53)
- Plural benzene rings bonded directly to urea nitrogen (Class 564/55)
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Patent number: 5236953Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.ident.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: October 30, 1991Date of Patent: August 17, 1993Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, Howard Tucker
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Patent number: 5227401Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: October 29, 1991Date of Patent: July 13, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5223535Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: October 29, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5198582Abstract: A process for preparing N,N'-disubstituted urea derivatives of the following formula (I) ##STR1## wherein Ar represents an unsubstituted aromatic radical or an aromatic radical substituted with a halogen atom, an alkyl group, or an alkoxy group, which comprises reacting an aromatic mono-nitro compound, an aromatic primary amine, and synthesis gas in the presence of a catalyst consisting essentially of a divalent palladium compound as a main catalyst component and an ammonium or a phosphonium salt containing halogen atom as a co-catalyst component, and a non-polar solvent.Type: GrantFiled: October 22, 1991Date of Patent: March 30, 1993Assignee: Lucky Ltd.Inventors: Jae S. Oh, Sang M. Lee
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Patent number: 5179231Abstract: Hexene-1,6-dioic acids, e.g., hex-3-ene-1,6-dioic acid, are prepared by reacting carbon monoxide with at least one butenediol, in a polar, aprotic, basic solvent, in the presence of a catalytically effective amount of palladium values and at least one inorganic halide, the cation of which halide being an alkali or alkaline earth metal and the anion thereof being a chloride or bromide.Type: GrantFiled: December 13, 1990Date of Patent: January 12, 1993Assignee: Rhone-Poulenc ChimieInventor: Philippe Denis
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Patent number: 5118709Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.Type: GrantFiled: August 29, 1990Date of Patent: June 2, 1992Assignee: Ciba-Geigy CorporationInventors: Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
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Patent number: 5091571Abstract: A process for preparing N, N-disubstituted urea and more particularly, to an improved process for preparing N,N'-disubstituted urea derivatives of the following formula (I) comprising ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents unsubstituted aromatic radical or aromatic radical substituted with halogen, atom, alkyl group, or alkoxy group, and Ar.sup.1 and Ar.sup.2 are the same or different, reacting aromatic mono-nitro compound, aromatic primary amines, and carbon monoxide in the presence of the catalyst composition consisting of a palladium compound as a main catalyst and an ammonium or a phosphonium salt containing halogen atom aS a co-catalyst, and a non-polar solvent.Type: GrantFiled: October 31, 1990Date of Patent: February 25, 1992Assignee: Lucky, Ltd.Inventors: Chul Woo Lee, Jae Sung Lee, Sang Moo Lee
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Patent number: 5055544Abstract: This invention relates to novel polymeric polyamines containing internal urea, biuret, thiourea, dithiobiuret, amide, and/or thioamide moieties, and to polymers prepared therefrom. This invention also relates to novel isocyanate-functional prepolymers containing urea, biuret, thiourea, dithiobiuret, amide, and/or thioamide moieties and to polymers prepared therefrom.Type: GrantFiled: February 27, 1990Date of Patent: October 8, 1991Assignee: The Dow Chemical CompanyInventors: Robert F. Harris, Michael D. Joseph
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 5030738Abstract: To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R.sub.1 is hydrogen or together with R.sub.2 represents the rest of a cycloaliphatic or heterocyclic optionally substituted ring with 5 or 6 carbon atoms, R.sub.2 represents H, alkyl, alkyl substituted with a simple or substituted aromatic ring or with a single or substituted heterocyclic ring, Ar represents a simple or substituted phenyl group, a simple or substituted heterocyclic aromatic group, N=1, 2, 3, 4, 5 or 6 and X represents CH--NO.sub.2, S, N--C.tbd.N, the compound (II) is prepared through the following process sequence: ##STR2## wherein Z=H, NO.sub.2, halogen and R.sub.3 =--(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n, --(CH.sub.2).sub.n --S--CH.sub.2 Ar Y being halogen.Type: GrantFiled: May 22, 1990Date of Patent: July 9, 1991Assignee: Janus Farmaceutici S.r.l.Inventor: Alberto Reiner
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Patent number: 5021429Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.Type: GrantFiled: December 22, 1986Date of Patent: June 4, 1991Assignee: Allen & Hansburys LimitedInventor: Michael Martin-Smith
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Patent number: 4977170Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.Type: GrantFiled: May 3, 1989Date of Patent: December 11, 1990Assignee: Shionogi & Co., Ltd.Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
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Patent number: 4977153Abstract: Compounds of formula (I), ##STR1## characterized in that R signifies optionally substituted heteroaryl-, heteroarylakyl or heteroarylalkenyl, R.sub.1 signifies hydrogen or a substituent, R.sub.2 is hydroxy or a group --z--(CH.sub.2).sub.n --Y--R.sub.3 wherein R.sub.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxygen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or imino, and X signifies a bond or imino, and their physiologically hydrolyzable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Processes for the preparation of the compounds are also disclosed.Type: GrantFiled: January 14, 1987Date of Patent: December 11, 1990Assignee: William J. LouisInventors: William J. Louis, Richard Berthold, Max-Peter Seiler, Andre Stoll
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Patent number: 4968829Abstract: Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests.Type: GrantFiled: June 19, 1989Date of Patent: November 6, 1990Assignee: Sandoz Ltd.Inventor: Clive A. Henrick
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4950301Abstract: A method of treating natural or synthetic polyamide or cellulosic textiles comprises applying an effective amount of an arylating agent, preferably to the dyebath. The arylating agent may be of a formula Ar--(X--Y).sub.n wherein Ar is an aromatic residue such as substituted or unsubstituted benzene or naphthalene ring; X is a bridging group such as --SO.sub.2, --CO-- or --NH--; Y is a reactive group; and n is 1 to 3. The arylating agent reduces fibre damage of natural polyamide fibres during dyeing and proves the degree of dye fibre reaction in dyeing of polyamide and cellulosic textiles to improve wet fastness. Furthermore, on cellulosic textiles, wet and dry wrinkle recovery properties are improved as is the yield of reactive dye fixation. On keratinous fibres shrink resistant and moth resistant properties are improved also. Certain novel arylating compounds are disclosed also.Type: GrantFiled: December 22, 1988Date of Patent: August 21, 1990Assignee: Wool Development International LimitedInventor: David M. Lewis
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Patent number: 4929737Abstract: Disclosed is an improved process for the preparation of haloaromatic amines by the catalytic hydrogenation of halonitroaromatic compounds in the presence of a chromium-containing Raney cobalt catalyst. The catalyst gives good hydrogenation rates while minimizing formation of dehalogenated by-products.Type: GrantFiled: February 3, 1988Date of Patent: May 29, 1990Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, Edward T. Mullins, Charles L. Gibson
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Patent number: 4906767Abstract: There is disclosed a family of new vinyl monomers capable of forming polymers by free radical polymerization. The vinyl monomer is of the formula ##STR1## wherein R.sub.1 and R.sub.2 are substituted or unsubstituted hydrocarbons, X is O, NH or NR.sub.3, and R.sub.3 is substituted or unsubstituted hydrocarbon.The intermediates in the synthesis of these monomers are new beta-chloroalanine ureas. The polymers are useful in film and fiber formation and display good toughness. These new vinyl monomers also form a cyclic monomer.Type: GrantFiled: June 30, 1987Date of Patent: March 6, 1990Assignee: The University of Southern MississippiInventors: Lon J. Mathias, David W. Kurz
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Patent number: 4872902Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.Type: GrantFiled: February 8, 1988Date of Patent: October 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4840967Abstract: A compound which is a carbamate or urea derivative of general formula (I) ##STR1## wherein X is hydrogen, halogen or methylthio,Y is oxygen or ##STR2## R is C.sub.1 -C.sub.4 alkyl, R.sub.1 is hydrogen, one or two halogen atoms or trifluoromethyl groups, a methyl group, a methyl group, a cyano group, a nitro group, a methoxycarbonyl group, a methylenedioxy group linked to two adjacent carbon atoms of the benzene ring to which it is attached, or a fused benzo group forming an .alpha.-naphthyl or .beta.-naphthyl group with the benzene ring to which it is attached,R.sub.2 is a linear or branched C.sub.1 -C.sub.8 alkyl or alkenyl group optionally substituted with halogen atoms or a methoxy group, a cyclopropylmethyl group, or a phenyl group optionally substituted with one or two halogen atoms or methyl groups,n is 1 or 2, andm is 2 or 3, or an addition salt thereof with a pharmacologically acceptable acid is pharmacologically active as a calcium antagonist.Type: GrantFiled: July 7, 1987Date of Patent: June 20, 1989Assignee: SynthelaboInventors: Nigel Beeley, Gerard Cremer
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Patent number: 4810725Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: October 14, 1986Date of Patent: March 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
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Patent number: 4749806Abstract: The present invention relates to a process for the synthesis of isocyanates and of isocyanate derivatives. Isocyanates are obtained by reacting an organic halide with a metal cyanate in an organic medium in the presence of a catalyst consisting of a complex of nickel with at least one organic ligand, in which complex the nickel is in the zero oxidation state.A carbamate or a urea, respectively, are obtained by a subsequent reaction with a hydroxy compound or a primary or secondary amine.Isocyanates and their derivatives are used especially either as refined synthesis agents for the production of pesticides and medications, or as monomers or comonomers for the preparation of many macromolecular compounds.Type: GrantFiled: August 25, 1987Date of Patent: June 7, 1988Assignee: Societe Nationale des Poudres et ExplosifsInventors: Igor Tkatchenko, Rabih Jaouhari, Michel Bonnet, Gordon Dawkins, Serge Lecolier
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Patent number: 4661515Abstract: Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.Type: GrantFiled: January 17, 1986Date of Patent: April 28, 1987Assignee: USV Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John J. Piwinski
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Patent number: 4636501Abstract: Compounds of the formula ##STR1## having beta receptor blocking properties, are disclosed.Type: GrantFiled: July 22, 1985Date of Patent: January 13, 1987Assignee: Aktiebolaget HassleInventors: Bill B. R. Gustafsson, Sven A. Hedberg, Bo T. Lundgren
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Patent number: 4634713Abstract: Certain 3-(ureidocyclohexyleneamino)propane-1,2-diol derivatives, such as the compounds of formula III below, represent novel and useful pharmaceutical agents, e.g. potent antihypertensive and cardioactive agents demonstrating both .alpha.- and .beta.-adrenergic blocking activity. ##STR1## R.sub.3 is hydrogen or lower alkyl; R.sub.7 is cyano, lower alkoxycarbonyl, pyrrolyl, morpholino, alkenyloxy of 3 to 6 carbon atoms, alkynyloxy of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms substituted by cyclopropyl.Type: GrantFiled: August 19, 1985Date of Patent: January 6, 1987Assignee: Ciba-Geigy CorporationInventors: Lincoln H. Werner, Neville Ford
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Patent number: 4629467Abstract: Use of 1-ureidoalkyl amino-4-nitrobenzene compounds of formula I ##STR1## whereby R denotes hydrogen or an hydroxyalkyl residue with 2 to 4 carbon atoms and n a whole number of 2 to 4, as a direct dyeing hair dye in hair dyeing compositions. The dye agents of the formula I have very favorable toxicological characteristics. They deliver pure lemon yellow dyes with a high dye depth and are resistant against bases and reduction agents. A further object of the invention are new compounds of formula II ##STR2## whereby R' denotes an hydroxyalkyl residue with 2 to 4 carbon atoms and n is a whole number from 2 to 4.Type: GrantFiled: August 14, 1985Date of Patent: December 16, 1986Assignee: Wella AktiengesellschaftInventors: Thomas Clausen, Eugen Konrad
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Patent number: 4628061Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.Type: GrantFiled: August 23, 1983Date of Patent: December 9, 1986Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4597902Abstract: N-(arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue.Type: GrantFiled: June 20, 1985Date of Patent: July 1, 1986Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., Christopher P. Johnson, III
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Patent number: 4536598Abstract: A new color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor in a photographic material and process enables formation of a dye image by means of cross-oxidation without the need for a coupling reaction. The color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor is useful in a photographic silver halide material for producing (i) a dye image, or (ii) a dye image and silver image. The exposed photographic material is processed to produce (a) a positive dye image, (b) a negative dye and negative silver image, (c) a negative dye image or (d) a positive dye image and a positive silver image. New naphthoquinoneimide dyes are also described.Type: GrantFiled: March 10, 1983Date of Patent: August 20, 1985Assignee: Eastman Kodak CompanyInventors: James E. Klijanowicz, Csaba A. Kovacs
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Patent number: 4525590Abstract: The invention relates to an improved process for the production of polyamines containing urethane and/or urea and/or biuret and/or isocyanurate groups and, preferably, also alkylene ether, carbonate and/or acetal groups by the alkaline hydrolysis of corresponding compounds containing terminal aliphatic and/or aromatic isocyanate groups.To this end, the compounds containing terminal NCO-groups, preferably NCO-preadducts, are converted by means of selected bases into the carbamates and neutralized by introduction into equivalent quantities of acid or by the simultaneous introduction of the components in equivalent quantities into a reaction vessel, after which the polyamines are directly isolated by methods known per se.The invention also relates to the use of the polyamines obtained by the process for the production of polyurethanes.Type: GrantFiled: July 15, 1982Date of Patent: June 25, 1985Assignee: Bayer AktiengesellschaftInventors: Werner Rasshofer, Klaus Konig, Holger Meyborg, Walter Meckel, Armin Zenner
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Patent number: 4488993Abstract: Novel phenylamidinourea compounds and processes for their preparation are described. These compounds have an effective degree of anti-hypertensive properties and exert activities on the cardiovascular system. A method for the treatment of hypertensive disorders is also described.Type: GrantFiled: October 25, 1982Date of Patent: December 18, 1984Assignee: William H. Rorer, Inc.Inventors: George H. Douglas, Julius Diamond
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Patent number: 4472568Abstract: This invention relates to an improved process for the preparation of aromatic polyamines containing urethane and/or biuret and/or urea and/or isocyanurate groups and preferably also ether groups by the hydrolysis of poly-N-monoaryl-N',N'-dialkyl urea compounds (1-aryl-3,3-dialkyl ureas). The ureas are obtained by the reaction of secondary aliphatic, cycloaliphatic or saturated heterocyclic amines with divalent to tetravalent isocyanate compounds containing isocyanate end groups attached to aromatic residues. The ureas correspond to the general formula: ##STR1## wherein R.sup.1, R.sup.2 denote alkyl or cycloalkyl groups, or together form a ring andA denotes a divalent to tetravalent residue attached to the ureas by aromatic groups.Hydrolysis is carried out in the presence of water and up to two equivalents of a base containing hydroxide ions and/or up to two equivalents of a compound containing tertiary amino groups, optionally in the presence of solvents.Type: GrantFiled: October 28, 1982Date of Patent: September 18, 1984Assignee: Bayer AktiengesellschaftInventors: Werner Rasshofer, Gerhard Grogler
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Patent number: 4460602Abstract: A compound, or pharmaceutically acceptable salt thereof, having the formula: ##STR1## wherein X is O or S; wherein n=1 or 0; wherein R is C.sub.3 -C.sub.12 alkyl or aralkyl, branched or unbranched, aryl or haloaryl, or C.sub.3 -C.sub.22 alkenyl, branched or unbranched; wherein R.sub.1 is OCH.sub.3, and wherein R.sub.2 is OH. These urea derivatives have analgesic and anti-irritant activity when administered to humans and lower animals.Type: GrantFiled: May 25, 1982Date of Patent: July 17, 1984Assignee: The Procter & Gamble CompanyInventors: Brian L. Buckwalter, Thomas R. LaHann
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Patent number: 4456768Abstract: Prostaglandin and prostacyclin compounds which are fluorine substituted in any one or more of the following positions 4,4; 7,7; 10,10; and 5.Type: GrantFiled: May 1, 1981Date of Patent: June 26, 1984Assignee: The University of ChicagoInventor: Josef Fried
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Patent number: 4435567Abstract: A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.Type: GrantFiled: December 28, 1981Date of Patent: March 6, 1984Assignee: Chinoin Gyogyszer es Vesgyeszeti Termekek Gyara R. T.Inventors: Gyorgy Lugosi, Antal Simay, Janos Bodnar, Laszlo Simandi, Eva Somfai
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Patent number: 4427685Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: a is 1 to 3;b is 0 to 2;c is 2 to 4;d is 1 to 5;X is sulphur, oxygen or --CH.sub.2 --;Y is oxygen, sulphur, NR.sub.4 or CHR.sub.5 wherein R.sub.4 is hydrogen, C.sub.1-4 alkyl, NO.sub.2 or CN, C.sub.1-4 alkylsulphonyl or phenylsulphonyl optionally substituted in the phenyl moiety by one or two substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, fluorine, chlorine or bromine, and R.sub.5 is NO.sub.2, C.sub.1-4 alkylsulphonyl or optionally substituted phenylsulphonyl as defined for R.sub.4 ;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 cycloalkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached represent a pyrrolidino or piperidino ring;R.sub.6 and R.sub.7 are independently hydrogen or C.sub.Type: GrantFiled: February 3, 1982Date of Patent: January 24, 1984Assignee: Beecham Group P.L.C.Inventor: Geoffrey Stemp
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Patent number: 4425362Abstract: The compounds of formula I, ##STR1## wherein the substituents have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form, are useful as cardioselective .beta.-adrenoceptor blocking agents.Type: GrantFiled: November 4, 1981Date of Patent: January 10, 1984Assignee: Sandoz Ltd.Inventors: Richard Berthold, William J. Louis
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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: 4417896Abstract: Novel compounds of the general formula ##STR1## wherein Z represents a substituted lower alkyl radical; each of R.sub.1 and R.sub.2 is hydrogen atom, a lower alkyl or a substituted lower alkyl identical with or different from Z and the functional groups NO.sub.2 and NR.sub.1 R.sub.2 can occupy all ring positions in relation to OZ, with the exception that if Z is .beta.-hydroxyethyl, --NO.sub.2 is in the 4 position and --N(R.sub.1)(R.sub.2) is in the 2 position then either R.sub.1 or R.sub.2 is other than hydrogen.The novel compounds are for dyeing human hair in a variety of yellow shades. The compounds of formula (I) may be used as aqueous or water-alcohol solutions to form dye compositions for dyeing human hair.Type: GrantFiled: April 6, 1982Date of Patent: November 29, 1983Assignee: Societe Anonyme dite: L'OrealInventors: Andree Bugaut, Patrick Andrillon
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Patent number: 4407816Abstract: New derivatives of 3-furyl-, 3-thienyl- and 3-phenyl-2-propenimidamides are disclosed, which are useful as anti-ulcer agents. These new compounds are synthesized by reacting an imino ether derived from a corresponding 3-substituted-2-propenenitrile with a suitable amine.Type: GrantFiled: August 4, 1981Date of Patent: October 4, 1983Assignee: Kotobuki Seiyaku Company LimitedInventors: Tsuyoshi Tomiyama, Akira Tomiyama
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Patent number: 4384140Abstract: The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.Type: GrantFiled: February 16, 1982Date of Patent: May 17, 1983Assignee: Kefalas A/SInventors: Peter Bregnedal, Jorn L. M. Buus
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Patent number: 4376783Abstract: The novel acylated guanidines, ureas and substituted ureas correspond to the general formula: ##STR1## in which R.sub.1 repesents a substituted or unsubstituted aromatic ring, R.sub.2 represents an alkyl, aryl, or arylalkyl group, R.sub.4 repesents hydrogen or a variously substituted aryl group, X is oxygen or an imine group: NH and Y represent an alkyl aryl alkyloxy or aryloxy group or a hydrogen atom when X represents oxygen or the group COR.sub.3 with R.sub.3 representing an aromatic group, an aryloxy, aralkyloxy or alkyloxy group when X represents the NH group. They are prepared by heating an appropriate compound under reflux with an oxyaminoalcohol, in a suitable solvent. The products are useful as medicaments for the treatment of arterial hypertension, ischemica diseases of the heart and rhythmic disorders of the latter.Type: GrantFiled: March 4, 1981Date of Patent: March 15, 1983Assignee: Compagnie Francaise de SucerieInventors: Jesus Anatol, deceased, by Marie-Francoise Anatol, legal representative, by Andre-Manuel Anatol, legal representative, Jean Berecoechea, Pierre Duchene-Marullaz, Alain Eschalier
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Patent number: 4369189Abstract: Novel unsymmetrical formamidine-sulfenylated carbamate compounds exhibit broad-spectrum insecticidal, miticidal and nematocidal activity.Type: GrantFiled: December 10, 1980Date of Patent: January 18, 1983Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4355045Abstract: The invention relates to topically anti-inflammatory 1-phenylethanolamine derivatives of the general formula I: ##STR1## or acid-addition salts thereof, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. A representative compound is 1-(4-amino-3,5-dichlorophenyl)-2-[1,1-dimethyl-2-(2-phenylacetamido)ethyla mino]ethanol. The derivatives are useful in particular for the treatment of inflammatory diseases or conditions of the skin.Type: GrantFiled: August 3, 1978Date of Patent: October 19, 1982Assignee: Imperial Chemical Industries LimitedInventors: John Preston, Austin J. Reeve
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Patent number: 4350706Abstract: The invention relates to new urea and thiourea compounds as insecticides.The compounds, after having been processed to compositions, can successfully be used to control insects in a dosage from 10 to 5000 g of active substance per hectare.Type: GrantFiled: June 27, 1979Date of Patent: September 21, 1982Assignee: Duphar International Research B.V.Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt
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Patent number: 4337061Abstract: Novel compounds of the general formula ##STR1## wherein Z represents a substituted lower alkyl radical; each of R.sub.1 and R.sub.2 is hydrogen atom, a lower alkyl or a substituted lower alkyl identical with or different from Z and the functional groups NO.sub.2 and NR.sub.1 R.sub.2 can occupy all ring positions in relation to OZ, with the exception that if Z is .beta.-hydroxyethyl, --NO.sub.2 is in the 4 position and --N(R.sub.1)(R.sub.2) is in the 2 position then either R.sub.1 or R.sub.2 is other than hydrogen.The novel compounds are for dyeing human hair in a variety of yellow shades. The compounds of formula (I) may be used as aqueous or water-alcohol solutions to form dye compositions for dyeing human hair.Type: GrantFiled: May 3, 1976Date of Patent: June 29, 1982Assignee: Societe Anonyme dite: L'OREALInventors: Andree Bugaut, Patrick Andrillon
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Patent number: 4335219Abstract: The reaction of an isocyanate such as toluene diisocyanate with itself to form an isocyanurate or with an active hydrogen compound such as diethylene glycol to form a urethane is catalyzed by the presence of an ar-ammonium areneoxide such as 4-dodecyl-2-trimethylammonium phenoxide.Type: GrantFiled: April 6, 1981Date of Patent: June 15, 1982Assignee: The Dow Chemical CompanyInventors: Donald H. Clarke, George J. Pomranky, Donald L. Schmidt
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Patent number: 4327113Abstract: Novel 1-heterocyclyloxy- or 1-aryloxy-3-amidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. The compounds possess .beta.-adrenergic blocking activity. Representative of the compounds disclosed is 1-(4-indolyloxy)-3-.beta.-isobutyramidoethylamino-2-propanol.Type: GrantFiled: December 12, 1980Date of Patent: April 27, 1982Assignee: Imperial Chemical Industries LimitedInventor: Leslie H. Smith