Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
  • Patent number: 5101033
    Abstract: 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: Grant
    Filed: November 27, 1990
    Date of Patent: March 31, 1992
    Assignee: Atochem North America, Inc.
    Inventors: Robert T. Kazmierczak, Ronald E. MacLeay
  • Patent number: 5075337
    Abstract: 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: Grant
    Filed: July 26, 1989
    Date of Patent: December 24, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Alex A. Cordi, Philippe Janssens de Varebeke, Hugo Gorissen
  • Patent number: 5075302
    Abstract: 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: Grant
    Filed: March 9, 1990
    Date of Patent: December 24, 1991
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5069812
    Abstract: A novel multifunctional bleach/builder precursor molecule is disclosed which is useful in various detergent compositions.
    Type: Grant
    Filed: December 10, 1990
    Date of Patent: December 3, 1991
    Assignee: Lever Brothers Company
    Inventors: Robert W. R. Humphreys, Bijan Harirchian, Frans L. M. Smeets
  • Patent number: 5051511
    Abstract: 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: Grant
    Filed: February 14, 1990
    Date of Patent: September 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Raymond Seltzer, Roland A. E. Winter, Peter J. Schirmann
  • Patent number: 5041545
    Abstract: 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: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5041546
    Abstract: 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: Grant
    Filed: June 14, 1989
    Date of Patent: August 20, 1991
    Assignee: Ausimont S.r.l.
    Inventors: Carlo Venturello, Claudio Cavallotti
  • Patent number: 5030729
    Abstract: 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: Grant
    Filed: March 1, 1990
    Date of Patent: July 9, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Valerio Borzatta
  • Patent number: 5025005
    Abstract: 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: Grant
    Filed: July 23, 1990
    Date of Patent: June 18, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
  • Patent number: 5017721
    Abstract: 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: Grant
    Filed: April 21, 1989
    Date of Patent: May 21, 1991
    Assignee: Enichim ANIC S.p.A.
    Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
  • Patent number: 5017693
    Abstract: 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: Grant
    Filed: December 19, 1989
    Date of Patent: May 21, 1991
    Assignee: NeoRx Corporation
    Inventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
  • Patent number: 5017702
    Abstract: 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: Grant
    Filed: July 6, 1989
    Date of Patent: May 21, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
  • Patent number: 5015678
    Abstract: 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: Grant
    Filed: February 14, 1990
    Date of Patent: May 14, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Raymond Seltzer, James P. Galbo, Ramanathan Ravichandran
  • Patent number: 4996316
    Abstract: 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: Grant
    Filed: December 24, 1988
    Date of Patent: February 26, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
  • Patent number: 4983738
    Abstract: 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: Grant
    Filed: February 13, 1989
    Date of Patent: January 8, 1991
    Assignee: Atochem North America, Inc.
    Inventors: Robert T. Kazmierczak, Ronald E. Mac Leay
  • Patent number: 4983737
    Abstract: 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: Grant
    Filed: February 14, 1990
    Date of Patent: January 8, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
  • Patent number: 4978699
    Abstract: 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: Grant
    Filed: October 24, 1988
    Date of Patent: December 18, 1990
    Assignee: Atochem North America, Inc.
    Inventors: Robert T. Kazmierczak, Ronald E. MacLeay
  • Patent number: 4976889
    Abstract: 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: Grant
    Filed: November 14, 1988
    Date of Patent: December 11, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
  • Patent number: 4972009
    Abstract: 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: Grant
    Filed: August 18, 1989
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran
  • Patent number: 4970307
    Abstract: 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: Grant
    Filed: August 13, 1987
    Date of Patent: November 13, 1990
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keiji Takeda, Jiro Tsukahara, Kozo Sato
  • Patent number: 4952574
    Abstract: 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: Grant
    Filed: September 26, 1988
    Date of Patent: August 28, 1990
    Assignee: Riker Laboratories, Inc.
    Inventor: Elden H. Banitt
  • Patent number: 4940727
    Abstract: 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: Grant
    Filed: October 6, 1988
    Date of Patent: July 10, 1990
    Assignee: 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
  • Patent number: 4927925
    Abstract: 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: Grant
    Filed: October 13, 1988
    Date of Patent: May 22, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Valerio Borzatta
  • Patent number: 4925974
    Abstract: 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: Grant
    Filed: September 16, 1988
    Date of Patent: May 15, 1990
    Assignee: Huels Aktiengesellschaft
    Inventor: Rainer Gras
  • Patent number: 4920116
    Abstract: 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: Grant
    Filed: December 13, 1988
    Date of Patent: April 24, 1990
    Assignee: Schering A.G.
    Inventors: Thomas K. Morgan, Jr., Klaus Nickisch
  • Patent number: 4904714
    Abstract: 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: Grant
    Filed: December 5, 1988
    Date of Patent: February 27, 1990
    Assignee: Olin Corporation
    Inventors: Robert J. Raynor, Francis W. Migliaro, Jr.
  • Patent number: 4889953
    Abstract: 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: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4871739
    Abstract: 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: Grant
    Filed: January 21, 1987
    Date of Patent: October 3, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Richard L. Tolman, Mu T. Wu
  • Patent number: 4871858
    Abstract: 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: Grant
    Filed: December 7, 1987
    Date of Patent: October 3, 1989
    Assignee: Japan Tobacco Inc.
    Inventors: Hajime Matsushita, Makoto Shibagaki, Kyoko Takahashi
  • Patent number: 4857645
    Abstract: 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: Grant
    Filed: November 5, 1987
    Date of Patent: August 15, 1989
    Assignee: Shionogi & Co., Ltd.
    Inventors: Adachi Makoto, Hiromu Matsumura, Tsutomu Sugasawa
  • Patent number: 4845090
    Abstract: 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: Grant
    Filed: September 24, 1985
    Date of Patent: July 4, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Heinz Gries, Ulrich Niedballa, Hanns-Joachim Weinmann
  • Patent number: 4824884
    Abstract: 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: Grant
    Filed: August 12, 1987
    Date of Patent: April 25, 1989
    Assignee: Pennwalt Corporation
    Inventors: Ronald E. MacLeay, Robert T. Kazmierczak
  • Patent number: 4816585
    Abstract: 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: Grant
    Filed: October 2, 1987
    Date of Patent: March 28, 1989
    Assignee: Olin Corporation
    Inventors: Robert J. Raynor, Francis W. Migliaro, Jr.
  • Patent number: 4808582
    Abstract: 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: Grant
    Filed: March 19, 1987
    Date of Patent: February 28, 1989
    Assignee: Delalande S.A.
    Inventors: Alain Y. Platel, Guy R. Bourgery, Patrick G. Guerret
  • Patent number: 4803234
    Abstract: 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: Grant
    Filed: January 29, 1987
    Date of Patent: February 7, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Valerio Borzatta
  • Patent number: 4785107
    Abstract: 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: Grant
    Filed: June 12, 1986
    Date of Patent: November 15, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Helwig, Peter Neumann, Herbert Bender, Alexander Aumueller, Hubert Trauth
  • Patent number: 4774332
    Abstract: 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: Grant
    Filed: July 11, 1986
    Date of Patent: September 27, 1988
    Assignee: Sandoz, Ltd.
    Inventor: Lajos Avar
  • Patent number: 4762829
    Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: August 9, 1988
    Assignee: Eisai Co., Ltd.
    Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
  • Patent number: 4742058
    Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: May 3, 1988
    Assignee: Eisai Co., Ltd.
    Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
  • Patent number: 4737518
    Abstract: 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: Grant
    Filed: September 12, 1986
    Date of Patent: April 12, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
  • Patent number: 4716187
    Abstract: 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: Grant
    Filed: March 15, 1985
    Date of Patent: December 29, 1987
    Assignee: Sandoz Ltd.
    Inventor: Lajos Avar
  • Patent number: 4707507
    Abstract: 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: Grant
    Filed: September 4, 1986
    Date of Patent: November 17, 1987
    Assignee: Adeka Argus Chemical Co., Ltd.
    Inventors: Mitsuo Akutsu, Mitsuharu Kanai
  • Patent number: 4695600
    Abstract: 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: Grant
    Filed: June 17, 1986
    Date of Patent: September 22, 1987
    Assignee: Sandoz Ltd.
    Inventor: Lajos Avar
  • Patent number: 4690708
    Abstract: 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: Grant
    Filed: July 11, 1984
    Date of Patent: September 1, 1987
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Alain Chene, Guy Borrod
  • Patent number: 4678638
    Abstract: This invention relates to amino hexahydropyridines, and to the preparation and use thereof as corrosion inhibitors.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: July 7, 1987
    Assignee: Petrolite Corporation
    Inventors: Benjamin T. Outlaw, Bernardus A. Oude Alink
  • Patent number: 4666967
    Abstract: 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: Grant
    Filed: January 22, 1986
    Date of Patent: May 19, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Norman Richardson, deceased, Brian G. Clubley, Richard J. Dellar
  • Patent number: 4652297
    Abstract: 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: Grant
    Filed: February 25, 1982
    Date of Patent: March 24, 1987
    Assignee: Monsanto Company
    Inventors: John E. Franz, Robert J. Kaufman
  • Patent number: 4629739
    Abstract: 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: Grant
    Filed: September 23, 1985
    Date of Patent: December 16, 1986
    Assignee: Schering A.G.
    Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
  • Patent number: 4607104
    Abstract: 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: Grant
    Filed: July 11, 1985
    Date of Patent: August 19, 1986
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Russell E. Malz, Jr., Harold Greenfield
  • Patent number: RE33495
    Abstract: 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: Grant
    Filed: September 27, 1989
    Date of Patent: December 18, 1990
    Assignee: BOC, Inc.
    Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Savernak