Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/247)
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Patent number: 5258138Abstract: A process for stabilizing an ethylenically unsaturated monomer or oligomer from premature polymerization is disclosed whereby a stabilizing amount of an amine, preferably a substituted hindered amine, in combination with phenothiazine or other related heterocyclic moiety is added to said polymerizable monomer or oligomer. The ethylenically unsaturated monomer or oligomer encompass vinyl monomers or oligomers bearing at least one polymerizable moiety. The combination of substituted hindered amine plus phenothiazine inhibits premature polymerization in the liquid and/or vapor phase.Type: GrantFiled: October 2, 1992Date of Patent: November 2, 1993Assignee: Ciba-Geigy CorporationInventors: Leslie R. Gatechair, Raymond Seltzer, James L. Hyun
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Patent number: 5256657Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.Type: GrantFiled: August 19, 1991Date of Patent: October 26, 1993Assignee: Sterling Winthrop, Inc.Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
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Patent number: 5217979Abstract: The present invention relates to a group of compounds which are novel substituted alkyl piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.Type: GrantFiled: March 17, 1992Date of Patent: June 8, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Charlotte L. Barney, Marion W. Wannamaker
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Patent number: 5214056Abstract: A 1,3,2-dioxathiolane oxide derivative is represented by the following formula: ##STR1## wherein X represents --S(O)-- or --S(O).sub.2 --;R.sup.1 represents a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group;R.sup.2 represents a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, andR.sup.3 and R.sup.4 may be the same or different and independently represent a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together form an alkylene group.Type: GrantFiled: August 20, 1991Date of Patent: May 25, 1993Assignee: Japan Tobacco Inc.Inventors: Jun-ichi Haruta, Masahiro Tanaka, Itsuo Uchida, Akira Ohta, Shin Hara
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Patent number: 5189046Abstract: PKC modulating compounds of the formula ##STR1## Also disclosed are pharmaceutical compositions including these compounds which inhibit PKC activity, methods of using these compounds to inhibit PKC activity in mammals, and intermediates useful in preparing the PKC modulating compounds.Type: GrantFiled: June 4, 1991Date of Patent: February 23, 1993Assignee: Nova Pharmaceutical CorporationInventors: Ronald M. Burch, Raymond J. Patch, Barry G. Shearer, John J. Perumattam
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Patent number: 5145893Abstract: 1-Hydrocarbyloxy substituted hindered amine compounds which also contain a reactive functional group such as hydroxy, amino, oxirane or carboxyl can be chemically attached to selected polymer substrates by condensation reactions to give polymers containing a chemically-bonded, non-migrating stabilizer having excellent stabilization efficacy for protecting said polymer substrate from the adverse effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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Patent number: 5137923Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 --OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which: 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.Type: GrantFiled: June 21, 1990Date of Patent: August 11, 1992Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 5122523Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined or a salt thereof, which is useful as hypotensive drugs.Type: GrantFiled: September 6, 1988Date of Patent: June 16, 1992Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5120738Abstract: Compounds represented by general formula (I) below ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represent a hydrogen atom or a protective group for a hydroxyl group;R.sup.3 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, or a group of formula ##STR2## where R.sup.4 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, andR.sup.5 represents a hydrogen atom, or a saturated or unsaturated, linear, branched or cyclic, monovalent hydrovarbon group which may be substituted with an aromatic group;Q represents(a) a group of formula --X.sup.1 --A--Y.sup.1 --, where A represents a saturated or unsaturated, linear, branched or cyclic divalent C.sub.2 .about.C.sub.Type: GrantFiled: October 5, 1990Date of Patent: June 9, 1992Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Nobuo Kobayashi, Jun Kusunoki
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Patent number: 5081294Abstract: There are disclosed quaternary ammonium salts which are obtainable by reacting basic carbamides containing a quaternisable nitrogen atom with epihalohydrins.These quaternary ammonium salts are particularly suitable for enhancing the color yield and the wet fastness properties of dyeings or printings produced on cellulosic fibre materials with anionic dye, e.g. reactive or direct dyes.Type: GrantFiled: March 21, 1989Date of Patent: January 14, 1992Assignee: Ciba-Geigy CorporationInventors: Rosemarie Topfl, Jorg Binz
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Patent number: 5051511Abstract: Compounds which contain peroxide linkages as well as a hindered amine light stabilizer moiety of low basicity function as free radical polymerization initiators and provide a polymer containing a hindered amine stabilizer chemically bonded to said polymer. The low basicity of the instant compounds prevents interaction with acid catalysts used in some polymerization systems.Type: GrantFiled: February 14, 1990Date of Patent: September 24, 1991Assignee: Ciba-Geigy CorporationInventors: Raymond Seltzer, Roland A. E. Winter, Peter J. Schirmann
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Patent number: 5047417Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydrogen or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: May 19, 1989Date of Patent: September 10, 1991Assignee: Eisai Co. Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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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: 5021480Abstract: Compounds which contain azo linkages as well as a hindered amine light stabilizer moiety of low basicity function as free radical polymerization initiators and provide a polymer containing a hindered amine stabilizer chemically bonded to said polymer. The low basicity of the instant compounds prevents interaction with acid catalysts used in some polymerization systems.Type: GrantFiled: February 14, 1990Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 5010097Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; R.sub.3 is C.sub.3-6 alkyl;R.sub.4 is hydrogen, alkyl, --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl, or a group ##STR3## where R.sub.11 is hydrogen, alkyl, or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.12 is hydrogen or alkyl; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.Type: GrantFiled: December 20, 1988Date of Patent: April 23, 1991Assignee: Beecham PharmaceuticalsInventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes, Laramie M. Gaster
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Patent number: 5001156Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.Type: GrantFiled: December 1, 1987Date of Patent: March 19, 1991Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 4990614Abstract: A compound of the formula: ##STR1## wherein ##STR2## represents a cyclic amino group, A represents a methylene group or a carbonyl group, m represents an integer of 1 to 3, n represents an integer of 0 to 4 and p represents an integer of 1 to 2, or a salt thereof, which has glutamate receptor inhibiting activity is provided.Type: GrantFiled: October 5, 1988Date of Patent: February 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Terumi Nakajima, Koichi Shudo, Giichi Goto
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Patent number: 4988688Abstract: 4-(N-Substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: August 2, 1989Date of Patent: January 29, 1991Assignee: Warner-Lambert CompanyInventors: Jeffrey A. Kester, Walter H. Moos, Anthony J. Thomas
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Patent number: 4987130Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.Type: GrantFiled: December 22, 1989Date of Patent: January 22, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
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Patent number: 4981963Abstract: A new process is described for the preparation of oxalic acid esters and amides of general formula (I) ##STR1## wherein Z designates an --OR or --NR.sup.1 R.sup.2 group, wherein R represents substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or aryl-alkyl, R.sup.1 is hydrogen or substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or aryl-alkyl, R.sup.2 represents substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or aryl-alkyl, or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a saturated 5-, 6-, 7-, or 8-membered heterocyclic ring, which may contain an additional heteroatom selected from --O--, --S--, and --N(H, Alkyl)--, and optionally bear one or more alkyl or alkenyl substituents, andZ.sup.1 designates an --OR or --NR.sup.1 R.sup.2 group, wherein R, R.sup.1, and R.sup.2 are as defined before, or a group --NHCOCH.sub.3, which comprises the base-catalysed reaction of diacetyloxamide with an alcohol ROH or/and an amine HNR.sup.1 R.sup.2.Type: GrantFiled: April 21, 1989Date of Patent: January 1, 1991Assignee: Enichem Anic S.p.A.Inventors: Giuseppe Messina, Giovanni M. Sechi, Loreno Lorenzoni, Giovanni Chessa
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Patent number: 4978699Abstract: This invention provides novel hindered amine light stabilizers with flame retardant properties. The compounds of this invention protect polymeric compositions against the degradative effects of heat and light and simultaneously improve the flammability rating of the polymeric composition, while also contributing antioxidant and metal deactivation properties to the polymeric compositions.The compositions of this invention are prepared by reacting halogenated flame retardant containing a cyclic anhydride group with hindered amine light stabilizers containing primary amino or reactive hydrazido functional groups. The preparation of the novel compositions may be carried out in inert solvents or in inert polymeric compositions in a melt blending step.Type: GrantFiled: October 24, 1988Date of Patent: December 18, 1990Assignee: Atochem North America, Inc.Inventors: Robert T. Kazmierczak, Ronald E. MacLeay
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Patent number: 4914227Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 3, 1990Assignee: Banyu Pharmaceutical Company, Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Ryosuke Ushijima, Susumu Nakagawa
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Patent number: 4895840Abstract: Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.Type: GrantFiled: June 10, 1987Date of Patent: January 23, 1990Assignee: A. H. Robins Company, IncorporatedInventor: James R. Shanklin, Jr.
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Patent number: 4845090Abstract: Diagnostic media suitable for NMR diagnoses contain compounds of Formula I ##STR1## wherein is a single bond or a double bond, X is the grouping --(CH.sub.2).sub.n -- or, if is a single bond, also the grouping --NHCO(CH.sub.2).sub.n -- wherein n means 0 to 4,m means the numbers 0, 1, or 2,R.sub.1 is an alkyl residue substituted by hydroxy groups, acyloxy groups and/or alkylidenedioxy groups,R.sub.2 has the same meanings as R.sub.1 or is a hydrogen atom or an alkyl residue,R.sub.3 and R.sub.4 are alkyl residues, andR.sub.5 and R.sub.6 are alkyl residues optionally substituted by hydroxy groups.Type: GrantFiled: September 24, 1985Date of Patent: July 4, 1989Assignee: Schering AktiengesellschaftInventors: Heinz Gries, Ulrich Niedballa, Hanns-Joachim Weinmann
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Patent number: 4836958Abstract: The instant invention relates to fluorinated cationic compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxy-perfluoroalkyl group;R.sub.1 is alkylene optionally interrupted by --O--, --S--, --SO.sub.2 --, --SO.sub.2 NR'--, --CO.sub.2 --, --NR'--, or --CONR'-- where R' is hydrogen or lower alkyl;m is 0, 1 or 2;R.sub.2 is linear or branched alkylene;R.sub.3, R.sub.4, and R.sub.5 independently of one another represent alkyl or arylalkyl groups which are unsubstituted or substituted by hydroxyl, lower alkoxy, halogen, cyano or by polyalkyleneoxy, or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical or R.sub.3, R.sub.4 and R.sub.5 together with nitrogen atom that links them represent a substituted or unsubstituted pyridine ring; andA.sup..crclbar. represents the anion of an organic or inorganic acid; and their particular use as surfactants.Type: GrantFiled: July 31, 1986Date of Patent: June 6, 1989Assignee: Ciba-Geigy CorporationInventor: Athanasios Karydas
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Patent number: 4824884Abstract: Amic acids, cyclic imides and mixtures thereof which contain both diacyl hydrazide functionalities and hindered amine functionalities are prepared by reacting non-halogenated cyclic anhydrides with hindered amine light stabilizers containing reactive hydrazido funtionalities in inert solvents or in inert polymeric compositions in a melt blending step. The compositions protect polymeric compositions against the degradative effects of heat and light.Type: GrantFiled: August 12, 1987Date of Patent: April 25, 1989Assignee: Pennwalt CorporationInventors: Ronald E. MacLeay, Robert T. Kazmierczak
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Patent number: 4812442Abstract: Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.Type: GrantFiled: May 4, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Ben E. Evans, Mark G. Bock
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Method for controlling emesis caused by chemotherapeutic agents and antiemetic agents useful therein
Patent number: 4772459Abstract: A method for alleviating emesis caused by chemotherapy which comprises administering an antiemetic agent or a pharmaceutically acceptable salt thereof to a patient in conjunction with the administration of a chemotherapeutic agent, said antiemetic agent being represented by the formula (I) ##STR1## wherein Z represents a substituent such as a lower alkyl group, a methoxyethoxymethyl group, or a benzoylmethyl group; or Z in conjunction with the adjacent position represents the atoms necessary to complete a 5 to 7 membered saturated or unsaturated oxygen-containing ring; R represents a hydrogen atom, a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, an amino group, an alkylsulfonyl group, a lower alkyl-substituted amino group, an acylamido group, a sulfamoyl group, a sulfonamido group or a nitro group; n is an integer of 1 to 3; W is a straight chain or branched chain alkylene group of 1 to 4 carbon atoms; and X represents the atoms necessary to complete a 5 or 6 membered ring; saidType: GrantFiled: September 9, 1986Date of Patent: September 20, 1988Assignee: Erbamont, Inc.Inventors: Jung-Hui Sun, Chih-Yun J. Tu -
Patent number: 4762829Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.Type: GrantFiled: October 23, 1986Date of Patent: August 9, 1988Assignee: Eisai Co., Ltd.Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
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Patent number: 4749701Abstract: Disclosed are an aminostyryl compound represented by Formula I: ##STR1## wherein A represents a linking group having 3 to 4 chain members; B represents an unsubstituted or substituted 5 to 6-membered monocyclic type heterocyclic residue containing 1 to 2 hetero atoms, an unsubstituted or substituted condensed heterocyclic residue which contains 5 to 6-membered monocyclic type heterocycle containing 1 to 2 hetero atoms, a naphthyl group or an alkyl group having 5 to 7 carbon atoms,a composition having leukotriene antagonism which contains an aminostyryl compound represented by Formula I as the effective ingredient, and a method of antagonizing SRS based on leukotriene antagonistic activity by employing the same.Type: GrantFiled: December 15, 1986Date of Patent: June 7, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Yoshio Hayashi, Tomei Oguri, Masaki Shinoda, Kazuo Takahashi
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Patent number: 4742058Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.Type: GrantFiled: July 14, 1986Date of Patent: May 3, 1988Assignee: Eisai Co., Ltd.Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
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Patent number: 4739106Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 19, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Nobuo Harada
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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: 4730017Abstract: A compound useful as a light-stabilizer for polymeric material of formula I ##STR1## in which R is hydrogen, oxygen, C.sub.1-8 alkyl or --CO--R.sub.5, where R.sub.5 is --C(R.sub.10).dbd.CH.sub.2, C.sub.1-6 alkyl, phenyl, --CO--O--C.sub.1-4 alkyl or --NR.sub.7 R.sub.8 and where R.sub.7 is hydrogen, C.sub.1-12 alkyl, C.sub.5-6 -cycloalkyl, phenyl, phenylC.sub.1-4 alkyl or C.sub.1-12 alkylphenyl and R.sub.8 is C.sub.1-12 alkyl or hydrogen;each R.sub.1, independently, is --CH.sub.3 or --CH.sub.2 (C.sub.1-4 alkyl) or both groups R.sub.1 form a group --(CH.sub.2).sub.5 --;each R.sub.2, independently, is --CH.sub.3 or --CH.sub.2 (C.sub.1-4 alkyl) or both groups R.sub.2 form a group --(CH.sub.2).sub.5);R.sub.10 is hydrogen or C.sub.1-4 alkyl; andR.sub.4 is an amide- or ester-forming group.Type: GrantFiled: September 12, 1986Date of Patent: March 8, 1988Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4680403Abstract: The invention relates to a process for producing N-protected-.alpha.L-aspartyl-L-phenylalanine methyl ester, which comprises esterifying L-phenylalanine with methanol in the presence of a strong acid catalyst, adding, to the resulting solution, an aqueous alkaline solution to neutralize the acid catalyst and a water-immiscible organic solvent to extract the free L-phenylalanine methyl ester thus formed, collecting the organic layer, and reacting the L-phenylalanine methyl ester dissolved in said collected organic layer with N-protected-L-aspartic anhydride.Type: GrantFiled: December 10, 1985Date of Patent: July 14, 1987Assignee: Ajinomoto Co., Inc.Inventors: Kunio Hisamitsu, Tadashi Takemoto, Toyoto Hijiya, Satoji Takahashi
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Patent number: 4675441Abstract: This invention is directed to novel catalysts characterized as compounds of tin or zinc containing a direct metal-nitrogen bond. The novel catalysts are derived from a primary or secondary amine such as an alkyl amine, a heterocyclic amine, an aromatic amine, etc. The amine is reacted with a tin compound such as a tin chloride, a tin bromide, a tin oxide, or a tin alkoxide. Alternatively, the amine may be reacted with a zinc halide, a zinc alkoxide or an organozinc compound.In another aspect of the present invention, the novel catalysts are used to catalyze the reaction of an acrylate or methacrylate ester with an amine in order to prepare N-substituted acrylamides or methacrylamides in good yield and with high selectivity.Type: GrantFiled: March 6, 1986Date of Patent: June 23, 1987Assignee: Texaco Inc.Inventors: Edward E. McEntire, Kathy B. Sellstrom
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Patent number: 4657904Abstract: Sulfur-containing bis-amino carbamate compounds exhibit outstanding acaricidal, nematocidal and insecticidal activity.Type: GrantFiled: May 19, 1986Date of Patent: April 14, 1987Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4632986Abstract: Thiocarbamylsulfenamides are readily recovered from solutions of the thiocarbamylsulfenamides by the addition of a dilute aqueous caustic solution, to flash off the solvent separating the thiocarbamylsulfenamide from the resulting water slurry and drying the thiocarbamylsulfenamide.Type: GrantFiled: July 29, 1985Date of Patent: December 30, 1986Assignee: The BFGoodrich CompanyInventors: Enrique G. Reynes, John O. Leising
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Patent number: 4613695Abstract: The invention concerns N-nitroso compounds having the general formula: ##STR1## wherein A is lower alkyl or halolower alkyl;B is hydrogen; lower alkenyl; lower alkynyl; 3-6 C cycloalkyl; --RSO.sub.2 NR.sup.3 R.sup.4, or lower alkyl optionally monosubstituted with lower alkoxy, or 3-6 C cycloalkyl;R is straight or branched 2-5 C alkylene, optionally monosubstituted with SO.sub.2 NR.sup.3 R.sup.4 or CONR.sup.3 R.sup.4, said alkylene always containing at least two carbon atoms separating the nitrogen atom of the urea from any SO.sub.2 NR.sup.1 R.sup.2 or SO.sub.2 NR.sup.3 R.sup.4 ;R.sup.1 and R.sup.2 are the same or different and selected from hydrogen, 5-6 C cycloalkyl, lower alkoxy, phenyl, benzyl, and straight or branched 1-6 C alkyl, optionally monosubstituted with hydroxy, lower alkoxy, SO.sub.2 NR.sup.3 R.sup.4, or CONR.sup.3 R.sup.4 ; R.sup.1 and R.sup.2 may also together form a 4-5 C alkylene; and R.sup.3 and R.sup.4 are the same or different and selected from hydrogen or lower alkyl, or R.sup.3 and R.Type: GrantFiled: September 6, 1983Date of Patent: September 23, 1986Assignee: Aktiebolaget LeoInventors: Jan-Inge L. Carlsson, Herta G. Jensen Petersen, Anders R. Stamvik
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Patent number: 4610819Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.Type: GrantFiled: September 19, 1984Date of Patent: September 9, 1986Assignee: A. H. Robins Company, Inc.Inventors: Young S. Lo, Albert D. Cale, Jr.
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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: 4532339Abstract: A process for purifying an aminosulfenylcarbamate derivative represented by the formula (I) ##STR1## wherein Ar is ##STR2## and R.sup.1 and R.sup.2 are the same or different and are each C.sub.1-8 alkyl, C.sub.3-6 cycloalkyl, benzyl which is unsubstituted or substituted with halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy, phenyl which is unsubstituted or substituted with halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy, --X--COOR.sup.3 or --Y--CN (in which X and Y are each straight-chain or branched-chain alkylene and R.sup.3 is C.sub.1-8 alkyl or C.sub.3-6 cycloalkyl), R.sup.1 and R.sup.2, when taken together, represent a 5- or 6-membered heterocyclic ring which may contain a sulphur or oxygen atom, the process comprising bringing a solution of the unreacted carbamate-containing aminosulfenylcarbamate derivative of the formula (I) in a water-insoluble organic solvent into contact with an aqueous alkali solution or a mixture of alkali, water and a water-soluble organic solvent.Type: GrantFiled: March 2, 1984Date of Patent: July 30, 1985Assignee: Otsuka Kagaku Yakuhin Kabushiki KaishaInventor: Hisashi Takao
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Patent number: 4500662Abstract: Polysubstituted .alpha.-aminoacetamides of the formula ##STR1## wherein R.sup.1 is tert-alkyl; R.sup.4 is alkyl, phenyl, substituted phenyl, cycloalkyl, piperidinyl, tetraalkylpiperidinyl or an alkylene (.alpha.-aminoacetamide). These compounds are prepared by first reacting an .alpha.-haloacetamide with a base to form an .alpha.-lactam intermediate which in turn is reacted with a primary amine. The compounds are useful as stabilizers of polymeric materials against ultraviolet light degradation.Type: GrantFiled: September 29, 1982Date of Patent: February 19, 1985Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4496542Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclic and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.Type: GrantFiled: April 13, 1983Date of Patent: January 29, 1985Assignee: USV Pharmaceutical CorporationInventors: Jerry W. Skiles, Raymond D. Youssefyeh, John T. Suh, Howard Jones
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Patent number: 4492801Abstract: A one-step process for the preparation of N-substituted (meth)acrylamides from the reaction of a (meth)acrylate ester and an amine over a catalytic amount of a metal alkoxide catalyst is described. These catalysts, such as stannous dimethoxide, lead dimethoxide, zinc dimethoxide, copper dimethoxide and bismuth tributoxide give high selectivity to the N-substituted (meth)acrylamides and little selectivity of the Michael adduct propionate ester, which would predominate in the absence of these catalysts. Also, these catalysts are less costly than organo metal catalysts commonly used.Type: GrantFiled: February 28, 1983Date of Patent: January 8, 1985Assignee: Texaco Inc.Inventors: Edward E. McEntire, Kathy B. Sellstrom, Edward C. Y. Nieh, David R. Livingston
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Patent number: 4479002Abstract: Carbamate-carbamoyl fluoride compounds are useful intermediates for the production of insecticidal bis-carbamate compounds.Type: GrantFiled: December 1, 1975Date of Patent: October 23, 1984Assignee: Union Carbide CorporationInventor: Wei C. Liang
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Patent number: 4473694Abstract: Process for the synthesis of hindered polysubstituted .alpha.-amino acetamides which comprises first reacting an .alpha.-haloacetamide with a base to form an intermediate .alpha.-lactam which in turn is reacted with a primary or secondary amine. The product thus obtained can comprise a multifunctional compound having one or more hindered amino moieties. These compounds are highly effective as UV stabilizers in a variety of plastics, especially the alpha monoolefins.Type: GrantFiled: September 29, 1982Date of Patent: September 25, 1984Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4435330Abstract: Amphoteric branched sulfatobetaines of the formula ##STR1## wherein R.sub.f is perfluoroalkyl or perfluoroxyperfluoroalkyl; R.sub.1 is a direct bond or a divalent connecting group; R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5, R.sub.6 and R.sub.7 are independently lower alkyl, and R.sub.6 may additionally represent aralkyl, and R.sub.6 and R.sub.7 taken together with the nitrogen to which they are attached may also represent piperidino or morpholino and R.sub.5, R.sub.6 and R.sub.7 taken together may also represent pyridyl, acridyl or quinolyl and salts thereof, their preparation and use as surfactants are disclosed.Type: GrantFiled: December 29, 1982Date of Patent: March 6, 1984Assignee: Ciba-Geigy CorporationInventor: Robert A. Falk
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Patent number: 4432985Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl; R.sub.1 is --OR.sub.2 or --NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 independently of one another denote hydrogen or loweralkyl; n is 0 or 1; R.sub.4 and R.sub.5 independently of one another denote loweralkyl or together form a 5 or 6 membered cycloalkyl substituted by hydrogen or loweralkyl, and together with the nitrogen atom, form a ring; and pharmaceutically acceptable salts thereof and their use as anticonvulsant agents in a method of controlling convulsions or seizures.Type: GrantFiled: March 15, 1982Date of Patent: February 21, 1984Assignee: Abbott LaboratoriesInventors: Alex M. Nadzan, George R. Granneman