Chalcogen Bonded Directly To The Carbocyclic Ring Of The Bicyclo Ring System (e.g., Tocopherols, Etc.) Patents (Class 549/408)
-
Patent number: 6140505Abstract: A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO.sub.3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0.degree. C. to about 75.degree. C., cooling, if necessary, to a temperature of from about -25.degree. C. to about 65.degree. C. and then adding oxalyl halide.Type: GrantFiled: May 19, 1998Date of Patent: October 31, 2000Assignee: G. D. Searle & Co.Inventors: Sastry A. Kunda, Leo J. Letendre, Gary A. De Crescenzo
-
Patent number: 6136985Abstract: The present invention provides CLA esters and uses thereof. More particularly, the present invention provides a composition for topical use comprising CLA esters and a topical carrier. In addition, the present invention specifically provides tocopheryl CLA esters, ascorbyl CLA esters and retinyl CLA esters.Type: GrantFiled: December 21, 1998Date of Patent: October 24, 2000Assignee: DCV, Inc.Inventor: James R. Millis
-
Patent number: 6107349Abstract: This invention pertains to the novel combination of Vitamin E, evening primrose oil and B-complex vitamins as a treatment for patients afflicted with psoriasis. It is postulated that the above compounds act synergistically to provide the cofactors required for normal skin production and repair in psoriatic patients.Type: GrantFiled: April 16, 1998Date of Patent: August 22, 2000Inventor: Philip R. Mantynen
-
Patent number: 6096907Abstract: A process for preparing chromanol derivatives of the formula I ##STR1## where n is from 1 to 10,R.sup.1, R.sup.2,R.sup.3, R.sup.4 independently of one another are hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.18 aralkyl, C.sub.7 -C.sub.18 alkylaryl, C.sub.1 -C.sub.22 acyl, or a group protecting the hydroxyl,by reduction of the corresponding 4-oxochromanol derivatives of the formula II ##STR2## comprises reacting the 4-oxochromanol derivatives of the formula II with metallic zinc in the presence of an acid or an acid mixture.Compounds of the formula I having C.sub.1 -C.sub.22 acyl as radical R.sup.5 can also be prepared by the above-described reduction of the compounds of the formula II with hydrogen as radical R.sup.5 and simultaneous or subsequent esterification.Type: GrantFiled: September 14, 1999Date of Patent: August 1, 2000Assignee: BASF AktiengesellscahftInventors: Kai-Uwe Baldenius, Bernhard Bockstiegel, Hagen Jaedicke, Detlef Ruff, Carsten Siedenbiedel, Rainer Sturmer
-
Patent number: 6093836Abstract: The present invention relates to a novel 1,3-diphenylpropane derivative having an inhibitory activity against tyrosinase represented by the following formula (I): ##STR1## in which - - represents double or single bond,R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl,R.sub.2 represents C.sub.1 -C.sub.5 alkyl or C.sub.1 -C.sub.5 alkoxyalkyl, orR.sub.1 and R.sub.2 together represent a 5 to 6 membered heterocycle which can be substituted by C.sub.1 -C.sub.5 alkyl and which contains oxygen as the hetero atom,R.sub.3 represents hydrogen or C.sub.1 -C.sub.7 alkyl,R.sub.4 represents hydrogen, hydroxy, or oxo, andR.sub.5 and R.sub.6 mindependently of one another represent hydrogen or C.sub.1 -C.sub.5 alkyl.Type: GrantFiled: November 6, 1998Date of Patent: July 25, 2000Assignee: LG Chemical Ltd.Inventors: Young Ho Rhee, Kyung Ae Kim, Hyun Ho Lee, Jong Kwon Choi, Sang Hwa Lee
-
Patent number: 6077659Abstract: An improved process is disclosed for photodynamically inactivating viruses in red blood cell containing compositions by adding vitamin E or a derivative thereof, such as Trolox, to the red blood cell and photosensitizer containing composition prior to irradiation. Addition of vitamin E or derivative thereof is protective of the red blood cells but not the viruses to be inactivated. Cells irradiated in this manner exhibit reduced leakage of potassium ion, and reduced loss of negative charges from the cell membrane compared to cells treated in the absence of vitamin E or derivative. Red blood cells sterilized by this method are better preserved during storage and their life-time in the circulation in vivo is enhanced.Type: GrantFiled: November 16, 1994Date of Patent: June 20, 2000Assignee: New York Blood Center, Inc.Inventors: Ehud Ben-Hur, Shanti Rywkin, Bernard Horowitz
-
Patent number: 6066745Abstract: A process for the manufacture of d,1-.alpha.-tocopherol by the acid catalyzed condensation of trimethylhydroquinone with isophytol is provided, in which the condensation is carried out in the presence of not more than about 0.4 weight percent, based on the weight of isophytol, of a sulfur-containing acid catalyst such as sulfuric acid, methanesulphonic acid, ethanesulphonic acid, trifluoromethanesulphonic acid, p-toluenesulphonic acid, fluorosulphonic acid and mixtures thereof, and in a solvent which is ethylene or propylene carbonate or a mixture of both carbonates, or a mixture of one or both of the carbonates and a non-polar solvent.Type: GrantFiled: March 31, 1999Date of Patent: May 23, 2000Assignee: Roche Vitamins Inc.Inventors: Marcel Baak, Werner Bonrath, Paul Kreienbuhl
-
Patent number: 6066731Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of .delta.-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-.gamma.-tocopherols.Type: GrantFiled: March 22, 1996Date of Patent: May 23, 2000Assignee: Roche Vitamins Inc.Inventors: Robert Karl Muller, Heinz Schneider
-
Patent number: 6001554Abstract: Multiple micro-encapsulations of a high concentration oleophilic substance using heat to set the primary particle renders the composition suitable for the production of free-flowing powders or beadlets. Microencapsulation involves forming an emulsion out of the oleophilic substance and a polymer, and then use heat setting and/or cross-linking the polymer encapsulates the oleophilic composition. This process is then repeated with a second polymer or third polymer, and with or without cross-linked via the same or different mechanism to further protect the oleophilic substance.Type: GrantFiled: January 16, 1998Date of Patent: December 14, 1999Assignee: Roche Vitamins Inc.Inventors: Stasia Boyle, Kuei-Tu Chang
-
Patent number: 5977073Abstract: A composition and method for its use in treatment of an immune disorder in a mammal. The composition includes, in relative amounts, between 50 and 3000 mg of a purified compound selected from oxidized and unoxidized gamma-L-glutamyl-L-cysteinylglycine, gamma-L-glutamyl-L-cysteine, N-acetyl-L-cysteine, N-acetyl-L-cysteine-glycine, and any other pharmaceutically active compound which directly enhances the level of gamma-L-glutamyl-L-cysteinylglycine in a mammal, and any salt or ester of said compound, between 50 and 3000 mg purified L-glutamine, between 50 and 10,000 mg purified vitamin C, between 50 and 500 mg purified vitamin E, between 10 and 100 mg purified Beta-carotene, and between 1 and 25 mg purified vitamin B.sub.6.Type: GrantFiled: June 6, 1991Date of Patent: November 2, 1999Assignee: Life Sciences' Technologies, Inc.Inventor: F. Mahnaz Khaled
-
Patent number: 5973169Abstract: Process for the preparation of ipriflavone consisting in the following steps:a) reaction of 2,4-dihydroxy-phenyl-benzyl-ketone of formula (II) with ethyl orthoformate in dimethylformamide as solvent and in the presence of a catalyst consisting of morpholine, to yield 7-hydroxyisoflavone of formula (III),b) separation of product (III) from the reaction residue,c) alkylation of product (III) from step b) with isopropyl halide to obtain ipriflavone, wherein:I. step a) is carried out at a temperature ranging from 115 to 120.degree. C. using a 2,4-dihydroxy-phenyl-benzyl-ketone (II) weight/solvent volume (w/v) ratio lower than 1:4;II. step b) consists in the precipitation of the corresponding salt with dicyclohexylamine of formula (IV).The process yields 7-hydroxyisoflavone (III) in high yields within short reaction times (2 h max.) and ipriflavone with impurity .ltoreq.0.1%.Type: GrantFiled: February 22, 1999Date of Patent: October 26, 1999Assignee: Erregierre S.p.A.Inventor: Massimo Ferrari
-
Patent number: 5958954Abstract: 2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula ##STR1## where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.Type: GrantFiled: December 24, 1997Date of Patent: September 28, 1999Assignee: Allergan Sales, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
-
Patent number: 5922757Abstract: New methods are described for the treatment of viral hepatitis C involving the administration of vitamin E and other compounds with antioxidant properties. Treatment with high doses of vitamin E is effective in treating chronic hepatitis C in patients refractory to interferon. In addition, new methods are described for the treatment of hepatic fibrosis and hepatic conditions manifesting hepatic fibrosis involving the administration of butylated hydroxytoluene and a metabolite of pentoxifylline, 1-?3-carboxypropyl!-3, 7-dimethylxanthine.Type: GrantFiled: September 30, 1996Date of Patent: July 13, 1999Assignee: The Regents of the University of CaliforniaInventor: Mario Chojkier
-
Patent number: 5922889Abstract: Isochromans and their derivatives have been chemically synthesized. These compounds possess significant phytotoxic activity which may be used as a biodegradable contact herbicide. The synthetic method allows for economic production of these herbicides.Type: GrantFiled: June 21, 1996Date of Patent: July 13, 1999Assignee: The United States od America as Represented by the Secretary of AgricultureInventors: Horace G. Cutler, George Majetich, Xinrong Tian, Paul Spearing
-
Patent number: 5917060Abstract: A process for the preparation of chromanyl derivatives of the formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.8 -alkyl, aryl, aralkyl, Si(R.sup.4).sub.3, C(.dbd.O)R.sup.4 or C.sub.1 -C.sub.4 -alkoxymethyl,R.sup.2 and R.sup.3 are hydrogen or C.sub.1 -C.sub.3 -alkyl, andR.sup.4 is C.sub.1 -C.sub.8 -alkyl or aryl,which comprises decarboxylating 5-carboxychromanyl derivatives of the formula II ##STR2## where the substituents R.sup.1 to R.sup.3 are as defined above and 5-carboxylchromanyl derivatives of the formula II.Type: GrantFiled: December 17, 1997Date of Patent: June 29, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Rosenau, Wolf-Dieter Habicher
-
Patent number: 5912362Abstract: High-purity isochroman compounds can be obtained in high yields according to a simple and economical process for preparing isochroman compounds, comprising the step of adding an aquesous solution of formaldehyde having a concentration of 40 to 70 wt. % to a complex of an arylalkanol represented by the following general formula (II) with a Friedel-Crafts catalyst to cyclize the arylalkanol: ##STR1## wherein R.sub.1 and R.sub.2 each stands for a hydrogen atom, a lower alkyl group or a lower alkoxyl group, or alternatively R.sub.1 and R.sub.2 are respectively bonded to adjacent carbon atoms with mutual bonding of R.sub.1 and R.sub.2 together with the carbon atoms respectively bonded to R.sub.1 and R.sub.2 to form a benzene ring, a naphthalene ring, or a C.sub.5 or C.sub.6 cycloalkane or cycloalkene which may have 1 to 6 lower alkyl groups; and R.sub.3 stands for a hydrogen atom or a lower alkyl group.Type: GrantFiled: November 10, 1997Date of Patent: June 15, 1999Assignee: Kao CorporationInventors: Shigeyoshi Tanaka, Masayuki Oku, Junji Koshino
-
Patent number: 5908940Abstract: The present invention relates to processes for obtaining Tocol products, such as tocotrienols, tocopherols and tocotrienol-like compounds from plant sources in high yields. More particularly, this invention relates to processes for stabilizing and recovering Tocol products from plant materials, such as cereals, grains and grain oils. The Tocol products recovered according to this invention are useful in pharmaceutical compositions, food formulations and dietary supplements. These compositions, formulations and supplements advantageously lower the blood level of low density lipoproteins and total serum cholesterol in humans and animals.Type: GrantFiled: January 5, 1996Date of Patent: June 1, 1999Assignee: Lipogenics, Inc.Inventors: Ronald H. Lane, Kenneth W. Becker, Asaf A. Qureshi, D. Michael Wells
-
Patent number: 5886197Abstract: A process is provided for the preparation of .alpha.-tocopherol. According to the process, a condensation reaction between trimethylhydroquinone and a specific phytol derivative or isophytol is conducted in the presence of any one of the following solvents:(i) a carbonate ester,(ii) a lower fatty acid ester represented by the following formula:R.sup.1 COOR.sup.2wherein R.sup.1 means a lower alkyl group having 1-4 carbon atoms and R.sup.2 means a lowe alkyl group having 1-5 carbon atoms with the proviso that methyl acetate and ethyl acetate are excluded;(iii) a mixed solvent of a nonpolar solvent and a lower alcohol having 1-5 carbon atoms; and(iv) a mixed solvent of the nonpolar solvent and the lower fatty acid ester.Type: GrantFiled: April 3, 1997Date of Patent: March 23, 1999Assignee: Eisai Co., Ltd.Inventors: Noriyasu Hirose, Hiroshi Inoue, Toshio Matsunami, Takashi Yoshimura, Kouzou Morita, Yuh Horikawa, Noriyoshi Iwata, Norio Minami, Kenji Hayashi, Chiaki Seki
-
Patent number: 5871766Abstract: This invention is directed to a method for inhibiting the occurrence of a major vascular event in a subject whereby a subject is administered beta-carotene and/or vitamin E, either alone or in combination. Beta-carotene and/or vitamin E is administered such that the subject's risk of experiencing a major vascular event is thereby reduced. In another preferred embodiment, beta-carotene in combination with aspirin is particularly effective.The invention further includes pharmaceutical compositions comprising beta-carotene in combination with vitamin E.Type: GrantFiled: December 21, 1994Date of Patent: February 16, 1999Assignee: Brigham and Women's HospitalInventor: Charles H. Hennekens
-
Patent number: 5869703Abstract: Disclosed herein are nonionic vitamin E or polyethoxylated vitamin E derivatives represented by the following formula (I) and a method for the preparation thereof, and polymeric amphiphilic vesicles made therefrom. ##STR1## wherein, n is an integer from 0 to 30, inclusive;A is --CH.sub.2 --CH(CH.sub.3)-- or --CH.dbd.C(CH.sub.3)--;B is --CH.sub.3 at the 5-, 7- or 8- position;m is 1, 2, or 3; andR is residue of acrylate or methacrylate derivatives represented by the following formula (II); ##STR2## wherein, R.sub.1 is H or CH.sub.3.Type: GrantFiled: October 28, 1997Date of Patent: February 9, 1999Assignee: Pacific CorporationInventors: Young Dae Kim, Jung No Lee, Won Chae Kim, Young Hyun Kim, Min Ki Kim, Myoung Su Ku, Iw Han Cho
-
Patent number: 5846988Abstract: Compounds useful as cytoprotective agents are disclosed. The compounds possess dual activity, containing a phenolic portion selected to have antioxidant or free radical scavenging properties and a thiazolidine-4-carboxylate portion selected for its potential to act as a cysteine prodrug.Type: GrantFiled: October 20, 1997Date of Patent: December 8, 1998Assignee: Alcon Laboratories, Inc.Inventor: Mark R. Hellberg
-
Patent number: 5821264Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.Type: GrantFiled: September 24, 1996Date of Patent: October 13, 1998Assignee: LipoGenics, Inc.Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
-
Patent number: 5817766Abstract: Novel benzpyran derivatives and the use of these derivatives in producing novel anti-cannabinoid antibodies are disclosed. Also disclosed is the use of these antibodies as reagents in improved immunoassays for tetrahydrocannabinol metabolites in biological fluid samples.Type: GrantFiled: April 5, 1995Date of Patent: October 6, 1998Assignee: Roche Diagnostic Systems, Inc.Inventors: Raymond Albert Hui, Steven Mark Rosen, Salvatore Joseph Salmone
-
Patent number: 5811083Abstract: Novel tocopherol derivatives useful for regulating skin aging and other skin disorders, as well as compositions containing the derivatives and methods for their use are described. The tocopherol derivative is tocopherol-cysteamine. Such types of skin atrophy to be treated the thinning of the epidermis and/or general degradation of the dermis often characterized by hyperplasia and structural disorganization. Such skin maladies include but are not limited to dry skin, severe dry skin, terosis, dandruff, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses and age-related skin changes.Type: GrantFiled: March 26, 1996Date of Patent: September 22, 1998Assignee: Estee Lauder, Inc.Inventors: Edward Pelle, Daniel H. Maes
-
Patent number: 5801179Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.Type: GrantFiled: June 2, 1997Date of Patent: September 1, 1998Assignee: Janssen Pharmaceutica, NVInventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
-
Patent number: 5795981Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: December 16, 1996Date of Patent: August 18, 1998Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
-
Patent number: 5767290Abstract: The present invention relates to a process for preparing protected amines or amino acids. The invention furthermore relates to the use of tocopheryl radicals or radicals derived therefrom as protective groups for amines and amino acids, and to compounds obtained in this process as intermediates and to processes for preparing dipeptides and oligopeptides.Type: GrantFiled: February 26, 1997Date of Patent: June 16, 1998Assignee: BASF AktiengesellschaftInventors: Thomas Rosenau, Wolf-Dieter Habicher, Chen-Loung Chen
-
Patent number: 5750516Abstract: This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).Type: GrantFiled: September 30, 1996Date of Patent: May 12, 1998Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Masayuki Nakamura, Kazumi Ogata, Takahiro Sakaue, Noriko Saito, Masahito Iemura
-
Patent number: 5744617Abstract: A process for the preparation of substituted phenols, in particular, the condensation of phenols having one or more alkyl substituents with a butadiene derivative comprising at least six carbon atoms, in particular myrcene and/or .beta.-springene is disclosed. The cyclization, in the form of chromans, of the products obtained during this condensation and their hydrogenation in order to prepare vitamin E is also disclosed.Type: GrantFiled: May 10, 1996Date of Patent: April 28, 1998Assignee: Rhone-Poulenc Nutrition AnimaleInventors: Jean-Erick Ancel, Hugues Bienayme, Pierre Meilland
-
Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
-
Patent number: 5719180Abstract: Described herein is a chroman derivative represented by the following formula: ##STR1## wherein X represents H, --CH.sub.2 OH, --CHO, --COOH, --COOCH.sub.3, --CH.dbd.NOH, --CONH.sub.2, --COCH.sub.3, --CH(OH)CH.sub.3, Br, or CN; Y represents a hydroxyl group which may optionally be protected; R represents an alkyl group, alkenyl group, or aralkyl group; provided that, where X is hydrogen atom, R is an alkyl group, alkenyl group, or aralkyl group each having 16 or more carbon atoms; and a vitamin E-like active medicament comprising said derivative as an active ingredient.Type: GrantFiled: August 12, 1996Date of Patent: February 17, 1998Assignee: Koichi ShudoInventors: Koichi Shudo, Masashi Akaike
-
Patent number: 5695689Abstract: .alpha.- and/or .beta.-tocopherol (vitamin E), optionally in combination with octylated diphenylamines, is combined with a polyether polyol having a molecular weight of from about 300 to about 10,000 to stabilize that polyether polyol. Polyether polyols which are stabilized in this manner are particularly useful in the production of polyurethanes and polyurethane foams with a reduced tendency toward discoloration.Type: GrantFiled: September 20, 1995Date of Patent: December 9, 1997Assignee: Bayer AktiengesellschaftInventors: Pramod Gupta, Hansjurgen Rabe
-
Patent number: 5672722Abstract: A silver halide color photographic material comprising a support having thereon at least one layer containing at least one compound represented by formula (A) ##STR1## wherein the definition of R.sub.a1, R.sub.a2, R.sub.a3, Z, Y, m and n is described in the specification.Type: GrantFiled: June 7, 1995Date of Patent: September 30, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Nobuo Seto, Yasuhiro Yoshioka, Masakazu Morigaki
-
Patent number: 5663389Abstract: The present invention refers to compounds having a benzopyranic structure of general formula I ##STR1## wherein R represents a hydrogen atom or an acyl group, useful as intermediates in the synthesis of vitamin E and of other compounds having benzopyranic structure endowed with properties inhibiting the formation of organic peroxides and therefore having antioxidizing activity, and to the process for their preparation.Type: GrantFiled: March 6, 1996Date of Patent: September 2, 1997Assignee: Alfa Wassermann S.p.A.Inventors: Goffredo Rosini, Claudia Baldazzi, Silvano Piani
-
Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
-
Patent number: 5656750Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu
-
Patent number: 5650404Abstract: This invention provides a therapeutic composition for pancreatitis which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl. The pharmaceutical composition of this invention can be used with advantage in the prevention and treatment of pancreatitis.Type: GrantFiled: July 18, 1995Date of Patent: July 22, 1997Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Shinya Ogino, Sachiko Matsuura, Rie Nagao
-
Patent number: 5627205Abstract: New substituted phenoxyisobutyric acids and esters that can be used as medicaments and correspond to the formula: ##STR1## wherein X, A, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the description.Those compounds and their physiologically tolerable salts can be used therapeutically.Type: GrantFiled: August 3, 1995Date of Patent: May 6, 1997Assignee: Adir Et CompagnieInventors: Gilbert Regnier, Claude Guillonneau, Jean-Paul Vilaine, Albert Lenaers, Christine Breugnot
-
Patent number: 5606080Abstract: Tocopherol derivatives of the following formula (I) or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.l and R.sub.2 are the same or different and each represents hydrogen or methyl; R.sub.3 represents an .alpha.-amino acid, .omega.-amino acid, or peptide bonding via the N terminus thereof, except that in the case of cysteine or glutathione which has a thiol group, bonding via the thiol group, are water-soluble and can be expected to be of use as a cerebral function-improving drug and an anticataract drug. Moreover, these compounds are of value as an UV-absorber, a skin care ingredient, or a stabilizer for other cosmetic ingredients.Type: GrantFiled: May 11, 1995Date of Patent: February 25, 1997Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Hidetoshi Nakao
-
Patent number: 5596095Abstract: The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion of R--SO.sub.3 --H to R'--SO.sub.3 --H, wherein R and R' are different organic radicals. Also disclosed is a method of increasing the bioavailability of drugs with a sulfonic acid functional group by protecting the sulfonic acid functional group as a substituted neopentyl sulfonate ester which has a masked heteroatom nucleophile. The masked nucleophile can be liberated in vivo, resulting in removal of the neopentyl protecting group and regeneration of the parent drug.Type: GrantFiled: May 12, 1995Date of Patent: January 21, 1997Assignee: Procept, Inc.Inventors: John C. Roberts, Raymond J. Patch
-
Patent number: 5591772Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.Type: GrantFiled: August 15, 1994Date of Patent: January 7, 1997Assignee: Lipogenics, Inc.Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
-
Patent number: 5556996Abstract: Compounds of the formula ##STR1## wherein all the symbols in the formula are as defined in the specification, have retinoid-like activity.Type: GrantFiled: December 29, 1994Date of Patent: September 17, 1996Assignee: AllerganInventors: Richard L. Beard, Roshantha A. Chandraratna
-
Patent number: 5554642Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 22, 1995Date of Patent: September 10, 1996Assignee: Adir et CompagnieInventors: Michel Langlois, Pierre Renard, G erard Adam
-
Patent number: 5538847Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T.sub. 1/2 kinetics of the chemiluminescent reaction, as well as the signal intensity, or quantum yield of the chemiluminescent reaction, can be altered by selection of an electron-withdrawing or an electron-donating group Z, at positions on the aromatic substituent other than those adjacent the point of attachment to the dioxetane. Signal strength can further be enhanced by recognized chemiluminescent enhancers.Type: GrantFiled: May 7, 1993Date of Patent: July 23, 1996
-
Patent number: 5534536Abstract: Fused phenol compounds of the formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 each, independently, is H, halogen, trifluoromethyl, cyano, (substituted) alkyl, alkoxy, cycloalkyl, COOH, COOR.sup.6 (in which R.sup.6 is C1-6 alkyl), alkenyl or R.sup.1 and R.sup.2, taken together, is --CH.dbd.CH--CH.dbd.CH--, when R.sup.1 and R.sup.2 are ortho to each other; A is alkylene, alkenylene, oxyalkylene or ##STR2## (in which m is 1-6); B is a monocyclic hetero ring containing a nitrogen atom; G is --OR.sup.3A or --NR.sup.3B R.sup.3C (in which R.sup.3A, R.sup.3B and R.sup.3C each, independently, is H, alkyl, acyl, or alkoxyalkyl); R.sup.4 and R.sup.5 each, independently, is H, alkyl, or R.sup.4, R.sup.5 together with the carbon atom to which they are attached represent C4-7 cycloalkyl; and n is 1-3; non-toxic salts thereof, non-toxic acid addition salts thereof, and hydrates thereof.The compounds of the formula (I) have inhibitory activities on TXA.sub.Type: GrantFiled: August 23, 1994Date of Patent: July 9, 1996Assignee: Ono Pharmaceuticals Co. Ltd.Inventors: Shuichi Ohuchida, Fumio Nambu, Masaaki Toda
-
Patent number: 5523319Abstract: The present application relates to novel compounds of the benzo-heterocycle family as well as to processes for their preparation and to the intermediate compounds obtained.Type: GrantFiled: May 31, 1995Date of Patent: June 4, 1996Assignee: Lore LInventors: Guy Solladie, Dominique Boeffel, Jean Maignan
-
Patent number: 5495026Abstract: A phenol, a formaldehyde and an unsaturated compound having carbon-carbon double bond are reacted in the presence of a secondary amine and an acid at a temperature of 100.degree. to 250.degree. C., to give a chroman.Type: GrantFiled: September 13, 1994Date of Patent: February 27, 1996Assignee: Kuraray Company Ltd.Inventors: Eriko Fukumoto, Masahiro Torihara, Yoshin Tamai
-
Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
-
Patent number: 5480645Abstract: Hydroxyamines N-acyl derivatives with benzochroman or 2,3-dihydrobenzofuran carboxy acids and relative pharmaceutical composition for the therapeutic treatment of those CNS, vascular, cardiovascular, dermatologic and ophthalmic pathologies wherein it is important to associate an inflammatory modulation effect to an antioxidant activity.Type: GrantFiled: December 29, 1993Date of Patent: January 2, 1996Assignee: LifeGroup S.p.A.Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
-
Patent number: 5464872Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.Type: GrantFiled: January 18, 1995Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Michel Langlois, Pierre Renard, Gerard Adam