Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
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Patent number: 5101033Abstract: N-(2,2,6,6,-tetraalkyl-4-piperidinyl)amide-hydrazides of dicarboxylic acids contain a light stabilizing group, a heat stabilizing group, and a reactive hydrazide functionality in the same molecule. The reactive stabilizers are prepared by reacting 4-amino-2,2,6,6-tetraalkylpiperidines with diesters (or mono ester acid chlorides) of dicarboxylic acids or dialkyl itaconates followed by hydrazinolysis of the ester group of the intermediate mono esteramide. The compounds are useful for introducing permanent heat and light stability to coreactive polymers or copolymers. They are also useful in the stabilization of inert polymeric systems against the degradative effects of heat and light when merely mixed with, rather than reacted with, the polymers for which stabilization is sought.Type: GrantFiled: November 27, 1990Date of Patent: March 31, 1992Assignee: Atochem North America, Inc.Inventors: Robert T. Kazmierczak, Ronald E. MacLeay
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Patent number: 5075337Abstract: Deuterated 2-alkylaminoacetamide compounds are described having the alpha carbon of the alkyl side chain of the compounds substituted by one or two deuterium atoms. These compounds have pharmacokinetic properties which enable treatment of CNS diseases with lower toxic effects. These compounds are also useful in evaluating the metabolic fate of non-deuterated counterpart compounds. Of particular interest are compounds of Formula I: ##STR1## wherein X is deutero or hydrido; wherein R.sup.1 is selected from alkyl and aralkenyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and alkyl; wherein each of R.sup.1, R.sup.2 and R.sup.3 having a substitutable position may be substituted with one or more halo radicals; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 26, 1989Date of Patent: December 24, 1991Assignee: G. D. Searle & Co.Inventors: Alex A. Cordi, Philippe Janssens de Varebeke, Hugo Gorissen
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Patent number: 5075302Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.Type: GrantFiled: March 9, 1990Date of Patent: December 24, 1991Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5069812Abstract: A novel multifunctional bleach/builder precursor molecule is disclosed which is useful in various detergent compositions.Type: GrantFiled: December 10, 1990Date of Patent: December 3, 1991Assignee: Lever Brothers CompanyInventors: Robert W. R. Humphreys, Bijan Harirchian, Frans L. M. Smeets
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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: 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: 5041546Abstract: Heterocyclic (poly)peroxycarboxylic acids having a N-amidic heteroatom, which have the formula:R--(CH.sub.2).sub.m --R' (I)wherein:R and R', alike or different from each other, represent hydrogen atoms or a group: ##STR1## with the proviso that at least one of R and R' shall be different from H, and wherein the other symbols have the following meaning:R" represents a hydrogen atom or any other substituent non-reactive in the presence of the active oxygen of the peroxycarboxylic group and/or under the preparation conditions;m represents a number between 1 to 12;n represents a number selected from 0, 1 and 2;p represents a number between 1 and 3;their process of preparation and their use as bleaching agents.Type: GrantFiled: June 14, 1989Date of Patent: August 20, 1991Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5030729Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, O.degree., CN, NO, cyanomethyl, C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -alkenyl or C.sub.3 -C.sub.12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C.sub.7 -C.sub.12 -aralkyl, C.sub.1 -C.sub.12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C.sub.2 -C.sub.6 -alkyl or 2,3-dihydroxypropyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.5 -C.sub.18 -cycloalkyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aryalkyl, R.sub.3 is C.sub.6 -C.sub.18 -aryl or a group of the formula (II) ##STR2## in which R.sub.1 is as defined above, n is an integer from 1 to 4 and R.sub.4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.Type: GrantFiled: March 1, 1990Date of Patent: July 9, 1991Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Valerio Borzatta
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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: 5017721Abstract: A new process for preparing oxalyl- and oxamyl-hydrazides which comprises contacting oxamide or diacetyloxamide with the corresponding hydrazine derivative of formulaR.sub.1 R.sub.2 N--NHR.sub.3wherein R.sub.1 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, aryl, or aryl-alkyl group, R.sub.2 is a hydrogen atom or an optionally substituted alkyl group, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom represent a saturated heterocyclic ring, and R.sub.3 is a hydrogen atom or an optionally substituted alkyl group.Type: GrantFiled: April 21, 1989Date of Patent: May 21, 1991Assignee: Enichim ANIC S.p.A.Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
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Patent number: 5017693Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of target cell an agent free of its targeting molecular carrier.Type: GrantFiled: December 19, 1989Date of Patent: May 21, 1991Assignee: NeoRx CorporationInventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
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Patent number: 5017702Abstract: Useful stabilizers for organic material, in particular plastics and paints, and metal ion deactivators are amides of the formula ##STR1## where R.sup.1 and R.sup.2 are singly methyl or together tetramethylene or pentamethylene, R.sup.3 is hydrogen, alkyl, alkoxycarbonyl, alkanoyl, benzyl, hydroxyethyl, cyanomethyl or aminomethyl, n is 1, 2 or 3 and--when n is 1--R.sup.4 is hydrogen and R.sup.5 is --CO--R.sup.6 is H, alkyl, cycloalkyl, aralkyl, phenoxyalkyl, aryl, a 5- or 6-membered heterocycle, alkoxy, aryloxy, cycloalkyloxy, phenylalkoxy, carbamoyl or --SO.sub.2 --R.sup.8 where R.sup.8 is alkyl or phenyl or ##STR2## is a phthalimide group or--when n is 2--R.sup.4 is H and R.sup.5 is --CO--Z--CO-- where Z is a chemical bond, C.sub.1 -C.sub.8 -alkylene, oxaalkylene, phenylene, cyclohexylene, biphenylene, biphenylene oxide, dioxyphenylene, diaminophenylene, diaminocyclohexylene, 1-.OMEGA.-diiminoalkylene or a 2-valent heterocycle or ##STR3## is a pyromellimide group or--when n is 3--R.sup.4 is H and R.sup.Type: GrantFiled: July 6, 1989Date of Patent: May 21, 1991Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
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Patent number: 5015678Abstract: The Michael addition products of N-hydroxy hindered amines with alpha,beta-unsaturated carbonyl compounds including derivatives of esters, amids, imides and anhydrides are effective stabilizers for protecting organic polymers from the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: May 14, 1991Assignee: Ciba-Geigy CorporationInventors: Raymond Seltzer, James P. Galbo, Ramanathan Ravichandran
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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Patent number: 4983738Abstract: N-(2,2,6,6-tetraalkyl-4-piperidinyl)amide-hydrazides of dicarboxylic acids contain a light stabilizing group, a heat stabilizing group, and a reactive hydrazide functionality in the same molecule. The reactive stabilizers are prepared by reacting 4-amino-2,2,6,6-tetraalkylpiperidines with diesters (or mono ester acid chlorides) of dicarboxylic acids or dialkyl itaconates followed by hydrazinolysis of the ester group of the intermediate mono esteramide. The compounds are useful for introducing permanent heat and light stability to coreactive polymers or copolymers. They are also useful in the stabilization of inert polymeric systems against the degradative effects of heat and light when merely mixed with, rather than reacted with, the polymers for which stabilization is sought.Type: GrantFiled: February 13, 1989Date of Patent: January 8, 1991Assignee: Atochem North America, Inc.Inventors: Robert T. Kazmierczak, Ronald E. Mac Leay
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Patent number: 4983737Abstract: Ethylenically unsaturated compounds containing 1-hydroxycarbyloxy-2,2,6,6-tetramethylpiperidine moieties represent reactable stabilizers which may be homopolymerized or copolymerized with other ethylenically saturated monomers to form non-migrating, light stabilizers which are very effective in stabilizing polyolefins and other polymer substrates against the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: January 8, 1991Assignee: Ciba-Geigy CorporationInventors: Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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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: 4976889Abstract: 4-Formylaminopiperidine derivatives of the formula (I) ##STR1## where n is 1 or 2, R.sup.1 to R.sup.4 are each alkyl or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 are tetra- or pentamethylene, R.sup.5 is hydrogen or alkyl, R.sup.6 is hydrogen, unsubstituted or substituted alkyl, alkenyl, aralkyl or acyl, and, when n is 1, Y is hydrogen, unsubstituted or substituted alkyl, alkenyl, cycloalkyl, bicycloalkyl, aralkyl, aryl, alkyl containing heterocyclic radicals, or ##STR2## or, when n is 2, Y is alkylene, cycloalkylene, aralkylene or arylene or is alkylene which is interrupted by oxygen, nitrogen, sulfur or a 5-membered or 6-membered heterocyclic structure, and their acid addition salts have very good stabilizing properties in plastics.Type: GrantFiled: November 14, 1988Date of Patent: December 11, 1990Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
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Patent number: 4972009Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.Type: GrantFiled: August 18, 1989Date of Patent: November 20, 1990Assignee: Ciba-Geigy CorporationInventors: Joseph Suhadolnik, Ramanathan Ravichandran
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Patent number: 4970307Abstract: A process for formation of a base from a base precursor, which comprises decomposing the base precursor in the presence of a catalyst. The base precursor has the following formula (I) or (II):(R.sup.1 --C.tbd.C--CO.sub.2 H).sub.x .multidot.B (I)R.sup.2 (--C.tbd.C--CO.sub.2 H).sub.2 .multidot.B.sub.y (II)wherein R.sup.1 is a monovalent group selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aryl group, a heterocyclic group, an aralkyl group, an acyl group, an alkoxycarbonyl group, carbamoyl, --CO.sub.2 M (M is an alkali metal) and --CO.sub.2 H.B, each of which may have one or more substituent groups; R.sup.Type: GrantFiled: August 13, 1987Date of Patent: November 13, 1990Assignee: Fuji Photo Film Co., Ltd.Inventors: Keiji Takeda, Jiro Tsukahara, Kozo Sato
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Patent number: 4952574Abstract: Certain 2,5-disubstituted N-(2-piperidylmethyl)benzamides, wherein one substituent is 2,2,2-trifluoroethyoxy, and pharmaceutically acceptable acid-addition salts thereof, are active as antiarrhythmic agents.Type: GrantFiled: September 26, 1988Date of Patent: August 28, 1990Assignee: Riker Laboratories, Inc.Inventor: Elden H. Banitt
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Patent number: 4940727Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as anti-hypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##Type: GrantFiled: October 6, 1988Date of Patent: July 10, 1990Assignee: Merck & Co., Inc.Inventors: Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta J. Lee, Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker
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Patent number: 4927925Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, O.sup.., CN, NO, cyanomethyl, C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -alkenyl or C.sub.3 -C.sub.12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C.sub.7 -C.sub.12 -aralkyl, C.sub.1 -C.sub.12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C.sub.2 -C.sub.6 -alkyl or 2,3-dihydroxypropyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.5 -C.sub.18 -cycloalkyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aralkyl, R.sub.3 is C.sub.6 -C.sub.18 -aryl or a group of the formula (II) ##STR2## in which R.sub.1 is as defined above, n is an integer from 1 to 4 and R.sub.4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.Type: GrantFiled: October 13, 1988Date of Patent: May 22, 1990Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Valerio Borzatta
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Patent number: 4925974Abstract: A process for the production of a blocked urea group-containing polyisocyanate from a partially blocked polyisocyanate and polyamine, comprising the steps of:(i) reacting a partially blocked polyisocyanate, said polyisocyanate being made substantially free of monomeric polyisocyanate, by vacuum thin layer evaporation with a primary polyamine, secondary polyamine, or mixtures thereof, in relative proportions such that the ratio of isocyanate groups to amino groups is in the range from about 1:1 to 1.3:1, and(ii) isolating said urea group-containing polyisocyanate by wherein the vacuum boiling point of said polyisocyanate is lower than the deblocking temperature of said urea group-containing polyisocyanate.Type: GrantFiled: September 16, 1988Date of Patent: May 15, 1990Assignee: Huels AktiengesellschaftInventor: Rainer Gras
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Patent number: 4920116Abstract: N-(aminoalkyl)-substituted(N or C alkyl)-aryl-4-(methylsylfonylamino)benzamides of the formula ##STR1## wherein R is C.sub.1 -C.sub.4 straight chain alkyl, one of R.sub.1, R.sub.2 and R.sub.3 is a phenyl or naphthyl group and the others are hydrogen, --NR.sub.4 R.sub.5 is a secondary or teritary amino group, X and X.sub.1 are hydrogen or alkyl and n is 0 or 1, are useful as antiarrhythmic agents in the treatment of cardiac arrhythmias especially as combination Class I/Class III agents.Type: GrantFiled: December 13, 1988Date of Patent: April 24, 1990Assignee: Schering A.G.Inventors: Thomas K. Morgan, Jr., Klaus Nickisch
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Patent number: 4904714Abstract: Tetraalkylpiperidinyl substituted uracil derivatives are disclosed which can be represented by the formula ##STR1## wherein each R' is independently an alkyl radical, n is 1 or 2 and R is a substituted or unsubstituted aliphatic radical, cycloaliphatic radical, aromatic radical or aromatic-aliphatic radical.These derivatives are useful as UV light stabilizers in synthetic resins.Type: GrantFiled: December 5, 1988Date of Patent: February 27, 1990Assignee: Olin CorporationInventors: Robert J. Raynor, Francis W. Migliaro, Jr.
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4871739Abstract: There are disclosed certain 2-substituted-4-substituted 6H-7,8-dihydrothiapyrano[3,2-d]pyrimidines which have oral hypoglycemic activity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed. The compounds are also .beta.-adrenergic blocking agonists or .alpha.-adrenergic blocking agents and act as ocular antihypertensives and are useful for the treatment of glaucoma and other eye disorders.Type: GrantFiled: January 21, 1987Date of Patent: October 3, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Richard L. Tolman, Mu T. Wu
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Patent number: 4871858Abstract: An amine is reached with dimethyformamioe in the presence of a solid catalyst to produce a formamide corresponding to the amine. The solid catalyst includes an oxide of metals belonging to Groups III, IV and V of the Periodic Table.Type: GrantFiled: December 7, 1987Date of Patent: October 3, 1989Assignee: Japan Tobacco Inc.Inventors: Hajime Matsushita, Makoto Shibagaki, Kyoko Takahashi
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Process for introducing a thiocarboxylic ester group at the orthoposition of phenols or phenylamines
Patent number: 4857645Abstract: A process for introducing thiocarboxylic ester at ortho-position of phenols or phenylamines which comprises reacting a phenyl compound having group or optionally substituted amino or cyclic amino group, of which at least one ortho-position is vacant, with C.sub.1 -C.sub.5 alkyl thiocyanate, C.sub.7 -C.sub.13 aralkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and hydrolyzing the resultant product under acidic conditions is provided, and said process is useful in the synthesis of medicinals, pesticides and dyes.Type: GrantFiled: November 5, 1987Date of Patent: August 15, 1989Assignee: Shionogi & Co., Ltd.Inventors: Adachi Makoto, Hiromu Matsumura, Tsutomu Sugasawa -
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: 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: 4816585Abstract: Tetraalkylpiperidinyl substituted uracil derivatives are disclosed which can be represented by the formula ##STR1## wherein each R' is independently an alkyl radical, n is 1 or 2 and R is a substituted or unsubstituted aliphatic radical, cycloaliphatic radical, aromatic radical or aromatic-aliphatic radical.These derivatives are useful as UV light stabilizers in synthetic resins.Type: GrantFiled: October 2, 1987Date of Patent: March 28, 1989Assignee: Olin CorporationInventors: Robert J. Raynor, Francis W. Migliaro, Jr.
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Patent number: 4808582Abstract: Compounds of formula: ##STR1## wherein: Ar is an aromatic group; R and R.sub.1 are H or CH.sub.3 ; A represents a nitrogenized heterocyclic radical; B is OH or forms with the adjacent CO group, either an amido group, or a carbonyloxy group; R.sub.2 and R.sub.3 are H or alkyl; m=0 or 1; and n=0, 1, 2 or 3.These compounds are useful as drugs having stimulating, protecting and/or correcting activities of the cerebral functions.Type: GrantFiled: March 19, 1987Date of Patent: February 28, 1989Assignee: Delalande S.A.Inventors: Alain Y. Platel, Guy R. Bourgery, Patrick G. Guerret
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Patent number: 4803234Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, O.sup.., CN, NO, cyanomethyl, C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -alkenyl or C.sub.3 -C.sub.12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C.sub.7 -C.sub.12 -aralkyl, C.sub.1 -C.sub.12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C.sub.2 -C.sub.6 -alkyl or 2,3-dihydroxypropyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.5 -C.sub.18 -cycloalkyl, C.sub.6 -Chd 18-aryl or C.sub.7 -C.sub.18 -aralkyl, R.sub.3 is C.sub.6 -C.sub.18 -aryl or a group of the formula (II) ##STR2## in which R.sub.1 is as defined above, n is an integer from 1 to 4 and R.sub.4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.Type: GrantFiled: January 29, 1987Date of Patent: February 7, 1989Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Valerio Borzatta
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Patent number: 4785107Abstract: The novel phenol derivatives of the general formula (I) ##STR1## where R is hydrogen, straight-chain or branched C.sub.1 -C.sub.8 -alkyl or cycloalkyl, A is a bridge member and B is a radical of the formula ##STR2## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and T.sup.1 independently of one another are each hydrogen, C.sub.1 -C.sub.8 -alkyl, halogen, CN, COOT.sup.2 or CONHT.sup.2, with the proviso that one or more of the radicals R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and T.sup.1 are halogen, CN, COOT.sup.2 and CONHT.sup.2 and T.sup.2 is C.sub.1 -C.sub.8 -alkyl, are useful for stabilizing organic material, in particular polyolefins, to degradation by oxidation.Type: GrantFiled: June 12, 1986Date of Patent: November 15, 1988Assignee: BASF AktiengesellschaftInventors: Reinhard Helwig, Peter Neumann, Herbert Bender, Alexander Aumueller, Hubert Trauth
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Patent number: 4774332Abstract: A compopund containing one or more units of formula I ##STR1## in which R.sub.1 is --CH.sub.2 C.sub.1-4 alkyl or --CH.sub.3 or both groups R.sub.1 form --(CH.sub.2).sub.5 --;R.sub.2 is --CH.sub.2 C.sub.1-4 alkyl or --CH.sub.3 or both groups R.sub.2 form --(CH.sub.2).sub.5 --;R.sub.3 is furylmethyl, unsubstituted C.sub.1-18 alkyl; C.sub.1-4 alkyl monosubstituted by phenyl, the phenyl group of which is unsubstituted or substituted by 1 to 3 groups selected from --OH and C.sub.1-8 alkyl; C.sub.2-8 alkyl monosubstituted by C.sub.1-4 alkoxy; phenyl, unsubstituted or substituted by 1 to 3 groups selected from C.sub.1-8 alkyl and --OH; or cyclohexy, unsubstituted or monosubstituted by C.sub.1-8 alkyl or --OH.These compounds are useful as light stabilizers for polymeric material.Type: GrantFiled: July 11, 1986Date of Patent: September 27, 1988Assignee: Sandoz, Ltd.Inventor: Lajos Avar
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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: 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: 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: 4716187Abstract: both R.sub.1 's and CH.sub.3 or together form --CH.sub.2).sub.5 ;both R.sub.2 's are CH.sub.3 or together form --CH.sub.2).sub.5 ;R.sub.3 has a significance of R, independently of R, except for oxygen;X is --O--, --NH-- or ##STR2## m is an integer from 1 to 4 inclusive; R.sub.4 is a saturated or unsaturated aliphatic group unsubstituted or substituted by one or two groups selected from --OH and C.sub.1-4 alkoxy and which can be interrupted by an oxygen or sulphur atom; or an aromatic group unsubstituted or substituted by one or two groups selected from --OH, C.sub.1-4 alkyl and C.sub.1-4 alkoxy are useful as U.V. light stabilizers in polymeric organic compounds.Type: GrantFiled: March 15, 1985Date of Patent: December 29, 1987Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4707507Abstract: Water-soluble or dispersible 2,2,6,6-tetramethylquaternary ammonium halides are provided, effective as stabilizers to increase the resistance to deterioration when exposed to light of synthetic resins, and having the formula: ##STR1## wherein: R.sub.1, R.sub.3 and R.sub.4 are alkyl having from one to about twelve carbon atoms;n is 1 or 2;when n is 1, R.sub.2 is alkyl having from one to about twelve carbon atoms; andwhen n is 2, R.sub.2 is alkylene having from one to about twelve carbon atoms; andX is halogen as well as stabilizer compositions and synthetic resin compositions containing the same.Type: GrantFiled: September 4, 1986Date of Patent: November 17, 1987Assignee: Adeka Argus Chemical Co., Ltd.Inventors: Mitsuo Akutsu, Mitsuharu Kanai
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Patent number: 4695600Abstract: These compounds are useful as light stabilizers in polymeric systems. ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are organic radicals.Type: GrantFiled: June 17, 1986Date of Patent: September 22, 1987Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4690708Abstract: A herbicide of the formula: ##STR1## in which: Z is N or CX',W, Y, Y', X, Z' and X' represent H, a halogen atom, NO.sub.2, CN or a polyhalogenoalkyl, alkyl or alkoxy group,R.sup.2 represents H, halogen, substituted alkyl, allyl, propargyl, CN, NR.sup.4 R.sup.5, C(X.sup.2)R.sup.7, C(X.sup.2)X.sup.3 R.sup.8, C(X.sup.2)NR.sup.4 R.sup.5, SO.sub.2 F, SO.sub.2 OR.sup.8, SO.sub.2 NR.sup.4 R.sup.5 or P(X.sup.2)R.sup.9 R.sup.10,R.sup.1 is halogen, X.sup.2 R.sup.3 or NR.sup.4 R.sup.5,R.sup.3 is optionally substituted alkyl or is allyl or propargyl,R.sup.4, R.sup.7 and R.sup.8 represent H, alkyl, cycloalkyl, phenyl, allyl, propargyl or the like,R.sup.5 represents R.sup.4, a cation or OR.sup.6, R.sup.6 being H, a cation or alkyl,X.sup.2 and X.sup.3 are O or S,R.sup.9 and R.sup.10 are H, alkyl, OH, OM or R.sup.1, andM is a cation.Type: GrantFiled: July 11, 1984Date of Patent: September 1, 1987Assignee: Rhone-Poulenc AgrochimieInventors: Alain Chene, Guy Borrod
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Patent number: 4678638Abstract: This invention relates to amino hexahydropyridines, and to the preparation and use thereof as corrosion inhibitors.Type: GrantFiled: April 28, 1986Date of Patent: July 7, 1987Assignee: Petrolite CorporationInventors: Benjamin T. Outlaw, Bernardus A. Oude Alink
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Patent number: 4666967Abstract: The invention provides polyurethanes and polyisocyanurate having incorporated therein a flame retardant amount of a salt formed by reaction between dimethyl methyl phosphonate, monomethyl methyl phosphonate or methyl phosphonic acid, and a compound of the general formula (I). ##STR1## in which X is O, S or NH, R.sup.1 is H, alkyl with 1 to 4 carbon atoms, alkenyl of up to 4 carbon atoms, CN, CONH.sub.2 or NH.sub.2, R.sup.2 is H, alkyl with 1 to 4 carbon atoms or alkenyl of up to 4 carbon atoms or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring of up to 6 carbon atoms which may optionally contain another hetero atom and R is H, an alkyl group with 1 to 8 carbon atoms, an aryl group with 6 to 10 carbon atoms, a cycloalkyl group with 5 to 12 carbon atoms or a heterocyclic group with up to 9 ring carbon atoms, or, together with R.sup.1 forms an alkylene chain of 3 to 10 carbon atoms, or R is a group NHR.sup.3 wherein R.sup.Type: GrantFiled: January 22, 1986Date of Patent: May 19, 1987Assignee: Ciba-Geigy CorporationInventors: Norman Richardson, deceased, Brian G. Clubley, Richard J. Dellar
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Patent number: 4652297Abstract: This invention relates to a new class of organic chemical compounds. More particularly, this invention is concerned with amido and hydrazido derivatives of N-phosphinothioylmethylglycine esters. This class of compounds has been found to be useful as herbicides.Type: GrantFiled: February 25, 1982Date of Patent: March 24, 1987Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4629739Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.Type: GrantFiled: September 23, 1985Date of Patent: December 16, 1986Assignee: Schering A.G.Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
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Patent number: 4607104Abstract: 2,2,6,6-tetraalkyl-4-piperidylamines are produced by reacting an amine with a 2,2,6,6-tetraalkyl-4-piperidone in the presence of a catalyst selected from the group consisting of platinum, nickel and cobalt, employing a reaction medium comprising (a) between about 10 and 100 weight percent water and (b) between 0 and about 90 weight percent of a polar organic compound selected from the group consisting of C.sub.1 -C.sub.10 aliphatic alcohols and C.sub.2 -C.sub.6 aliphatic glycols.Type: GrantFiled: July 11, 1985Date of Patent: August 19, 1986Assignee: Uniroyal Chemical Company, Inc.Inventors: Russell E. Malz, Jr., Harold Greenfield
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Patent number: RE33495Abstract: The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of .[.3-substituted-4-(phenylamino)piperidine.]. .Iadd.3-substituted-4-anilino piperidine .Iaddend.compounds or their substituted derivatives.Type: GrantFiled: September 27, 1989Date of Patent: December 18, 1990Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Savernak