Plural Rings In Phenolic Moiety Patents (Class 560/138)
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Patent number: 6316616Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: April 22, 1998Date of Patent: November 13, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Publication number: 20010034370Abstract: A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.Type: ApplicationFiled: February 28, 2001Publication date: October 25, 2001Inventors: Kunio Kosaka, Toshitsugu Miyazaki, Toshio Yokoi
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Patent number: 6284918Abstract: The present invention provides a compound of the formula wherein when X is S; R is selected from the group consisting of CH3, CH2CH3, CH2Ph, (CH2)2Ph, (CH2)2CH3, (CH2)3CH3, (CH2)4CH3, CH2)5CH3, (CH2)6CH3, (CH2)2O(CH2)3CH3, CH2HC═CH(CH2)3CH3, CH2C≡C(CH2)3CH3, CH2C≡C(CH2)2CH3, CH2C≡CCH2CH3, CH2C≡CCH3, CH2C≡CH, CH2C≡C(CH2)4CH3, CH2C≡C(CH2)5CH3, CH2C≡C(CH2)6CH3, (CH2)2C≡C(CH2)2CH3, CH(Ch3)C≡C(CH2)3CH3, (CH2)6I, (CH2)6Br, (CH2)5Br, (CH2)5COOH and (CH2)5OCOCH3, and R′ is selected from the group consisting of CH3, CF3, CH2Cl, CH2Br, CH2CH3, NH2, and OSO2CH3; wherein when R is CH3, R′ can not be CH3 or CH2Cl; wherein when R is CH2CH3, R′ can not be CH3; wherein when X is Se, R is (CH2)6CH3, and R′ is CH3 or a pharmaceutically acceptable salt or hydrate thereof; and wherein when X is O, R is CH2C≡C(CH2)3CH3, and R′ is CH3 or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: April 6, 1999Date of Patent: September 4, 2001Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Amit S. Kalgutkar
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Patent number: 6242638Abstract: The present invention relates to novel aromatic cyanate ester compounds containing at least two rings linked by a group containing an unsaturated group. The present invention further relates to compositions and prepolymers of said novel aromatic cyanate ester compounds. The present invention further relates to a process for preparing said compounds and cured articles resulting from curable mixtures thereof.Type: GrantFiled: March 12, 1999Date of Patent: June 5, 2001Assignee: Vantico Inc.Inventors: Bor-Sheng Lin, Michael James Amone
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Patent number: 6225499Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting a N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.Type: GrantFiled: July 14, 1997Date of Patent: May 1, 2001Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6215029Abstract: A process for the preparation of halohydroxydiphenyl compounds useful for protecting organic materials and articles from microorganisms, of the formula by acylation of a halogenated benzene compound (first stage), etherification of the acylated compound with a halogenated phenol compound (second stage), oxidation of the etherified compound (third stage) and hydrolysis of the oxidized compound in a fourth stage, according to the following reaction scheme: in which R1 and R2 independently of one another are F, Cl or Br; R3 and R4 independently of one another are hydrogen; or C1-C4alkyl; m is 1 to 3; and n is 1 or 2.Type: GrantFiled: June 9, 1999Date of Patent: April 10, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: Urs Burckhardt, Armando Di Teodoro, Werner Hölzl, Dieter Reinehr, Rudolf Zink, Hanspeter Sauter, Uwe Gronde
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Patent number: 6147250Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.Type: GrantFiled: May 14, 1998Date of Patent: November 14, 2000Assignee: AtheroGenics, Inc.Inventor: Patricia K. Somers
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Patent number: 6133279Abstract: Herein disclosed are therapeutic agents for renal diseases and organ preservatives containing a compound represented by the general formula (1): ##STR1## wherein X represents an oxygen atom or a group represented by the general formula (2): ##STR2## where n represents an integer from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group, R.sub.3 represents a lower alkyl group, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or an optionally substituted alkyl group, and R.sub.6 further represents a formyl, carboxyl, lower alkoxycarbonyl or optionally substituted carbamoyl group, or R.sub.3 and R.sub.4 may be taken together to form a five-membered ring, or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group, provided that when the five-membered ring formed by R.sub.3 and R.sub.4 and the benzene ring form benzofuran or benzo[b]thiophene, R.sub.6 is absent.Type: GrantFiled: December 17, 1998Date of Patent: October 17, 2000Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Osamu Cynshi, Yoshiaki Takashima, Kunio Tamura, Akira Ishikawa, Yoshiaki Kato
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Patent number: 6127423Abstract: The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: July 31, 1998Date of Patent: October 3, 2000Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade, Andreas Ding
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Patent number: 6100429Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene.Type: GrantFiled: June 16, 1999Date of Patent: August 8, 2000Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6066757Abstract: A stilbene compound is disclosed which has the following general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each stand for hydrogen, an alkyl group or an acyl group and Ar.sup.1 and Ar.sup.2 each stand for a monovalent homocyclic aromatic group. The stilbene compound may be incorporated into a photoconducting layer of an electrophotographic photoconductor as a charge transporting material. A process for the production of the stilbene compound is also disclosed.Type: GrantFiled: January 20, 1998Date of Patent: May 23, 2000Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tomoyuki Shimada
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Patent number: 6040339Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.Type: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 6013836Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.Type: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 5998499Abstract: A liquid crystalline compound, a polymeric product formed by polymerization of the liquid crystalline compound, a dental composition including the liquid crystalline compound and method of using the dental composition. Polymerization of the liquid crystalline compound results in an low volume percent shrinkage and a high conversion to polymer. The composition of the invention is useful for dental adhesive, primer, cement, pit and fissure sealant and restorative.Type: GrantFiled: October 7, 1996Date of Patent: December 7, 1999Assignee: Dentsply G.m.b.H.Inventors: Joachim E. Klee, Holger Frey, Dirk Holter, Rolf Mulhaupt
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Patent number: 5925674Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.Type: GrantFiled: October 26, 1995Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
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Patent number: 5880314Abstract: The present invention can provide cosmetic formulations comprising hydrochalcone compounds of the general formula (I): ##STR1## in which R.sup.1 to R.sup.4 are each independently H or --COR, and R is an alkyl group having 1-20 carbon atoms as effective components, which are highly effective in suppressing pigment deposition and depigmenting the skin and which are very safe to the skin and highly stable during storage.Type: GrantFiled: July 18, 1997Date of Patent: March 9, 1999Assignee: Mitsui Chemicals, Inc.Inventors: Tatsuro Shinomiya, Hiroko Kaminaga, Shohei Nozaki, Masahiro Sakamoto, Shigeharu Morimoto
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Patent number: 5874611Abstract: A hydroquinone derivative (I) represented by the following formula: ##STR1## wherein R.sup.1 is a hydrogen atom, acetyl group or benzoyl group, such hydroquinone derivative being useful as an intermediate for chroman derivatives useful as a blood sugar-lowering agent.Type: GrantFiled: July 1, 1996Date of Patent: February 23, 1999Assignee: Eisai Chemical Co., Ltd.Inventors: Kimio Hamamura, Chiaki Seki, Masayuki Konishi
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Patent number: 5808139Abstract: Non-steroidal compounds which are high affinity, high specificity ligands for progesterone receptors are disclosed. The compounds include synthetic derivatives of cyclocymopol and its diastereomers, spectroscopically and chromatographically pure (3R)-cyclocymopol monomethyl ether, which functions as a progesterone receptor antagonist, and spectroscopically and chromatographically pure (3S)-cyclocymopol monomethyl ether, which functions as a progesterone receptor agonist. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by progesterone receptors and for treating patients requiring progesterone receptor agonist or antagonist therapy.Type: GrantFiled: September 8, 1994Date of Patent: September 15, 1998Assignees: Ligand Pharmaceuticals Incorporated, The Regents of the University of CaliforniaInventors: I. Charles Pathirana, Christina S. Berger, Robert B. Stein, William Fenical, Todd K. Jones, Lawrence G. Hamann, Michael G. Johnson, Luc Farmer
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Patent number: 5808137Abstract: The present invention relates to the use of some natural or synthetic chalcones and the esters thereof with straight or branched aliphatic acids, saturated and unsaturated, containing up to 22 carbon atoms in the therapy and prevention of the uterus, ovary and breast tumors, as well as the formulations containing them. Chalcones such as isocordoin, cordoin, 2-hydroxyderricin, 2',4'-dihydroxychalcone, 4,2',4'-trihydroxychalcone have a marked affinity to the estrogen receptors of type II and an antiproliferative activity on uterus, ovary and breast tumor cell lines. These molecules proved to be useful both in therapy and in the prevention of such tumors.Type: GrantFiled: June 12, 1997Date of Patent: September 15, 1998Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Salvatore Mancuso, Franco Delle Monache
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Patent number: 5798348Abstract: The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of an estrogen and a fatty acid wherein the estrogen is estrone, diethylstilbestrol, estriol, estradiol or ethinyl estradiol and the fatty acid is oleic, linoleic, linolenic, stearic, palmitic, palmitoleic or arachidonic acids. The fatty-acid monoesters mimic the function of estrone monooleate, as a signal that informs the brain of the size of fat tissue mass. In preferred pharmaceutical and/or cosmetic compositions for intravenous injection the monoester is incorporated in a lipidic suspension, prepared from lipoproteins or from liposome components, such as soy oil and egg phospholipids. When administered to rats with a 15% of total adipose tissue, they produce weight reduction of about 10%, by a new and unexpected mechanism. They are useful for the treatment of obesity and/or overweight in mammals, with the advantages of high efficacy and low toxicity.Type: GrantFiled: October 30, 1996Date of Patent: August 25, 1998Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventor: Maria Alemany
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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
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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
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Patent number: 5624961Abstract: Novel benzylaminoethoxybenzene derivatives of the formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, a lower hydroxyalkyl, a lower alkoxyalkyl, an allyl or a benzyl; R.sup.2 is a hydrogen atom, a lower alkyl, a lower acyl, an allyl or a benzyl; R.sup.3 is a hydrogen atom, a lower alkyl, a lower alkoxyalkyl, a lower dialkylaminoalkyl or a lower acyl; and R.sup.4 is a hydrogen atom, a halogen atom, a lower alkoxy, an amino, a lower acylamino, a hydroxy, a lower acyloxy, a lower acyl, a carboxy or a lower alkoxycarbonyl, salts thereof and solvates thereof. An .alpha..sub.1 -adrenoceptor blocker obtained from this compound has a strong .alpha..sub.1 -adrenoceptor blocking effect and causes less side effects such as orthostatic hypotension.Type: GrantFiled: December 11, 1995Date of Patent: April 29, 1997Assignee: Japan Tobacco Inc.Inventors: Masakazu Ban, Kiyotaka Shinoda, Mitsuru Takahashi, Shuhei Deguchi, Hiroaki Taguchi, Takeo Katsushima
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Patent number: 5597390Abstract: A di- or tri-ester polyether unsaturated acid amine reaction product effective as a fuel additive for reducing intake valve deposits and octane requirement increase, as well as controlling combustion chamber deposits, in gasoline engines is disclosed together with fuel compositions and methods of making and using the same. Also disclosed are compositions and methods for dispersing deposits in lubricating oil products.Type: GrantFiled: September 25, 1995Date of Patent: January 28, 1997Assignee: Ethyl CorporationInventor: John T. Loper
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Patent number: 5563129Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.Type: GrantFiled: April 24, 1995Date of Patent: October 8, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5484935Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.3 are each C.sub.1-4 alkyl or C.sub.1-4 alkyl-carbonyl, and R.sup.2 is carboxy, tetrazolyl, C.sub.1-4 alkyl-sulphonamido or --CR.sup.4 R.sup.5 CO.sub.2 H where R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl; provided that when R.sup.1 and R.sup.3 are both methyl and when R.sup.1 and R.sup.3 are both methylcarbonyl, R.sup.2 is not carboxy; and salts and esters thereof.Type: GrantFiled: August 11, 1994Date of Patent: January 16, 1996Assignee: Lilly Industries LimitedInventors: Peter T. Gallagher, Terence A. Hicks, William M. Owton
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Patent number: 5447659Abstract: Disclosed are novel active benzene derivatives represented by the general formula (I): ##STR1## (wherein X represents --CCO--, --OCO--, --CH.sub.2 C-- or --OCH.sub.2 --; A represents a hydrogen atom, a halogen atom or an alkyl or alkoxyl group having 1 to 20 carbon atoms; R represents an alkyl group having 1 to 20 carbon atoms; l and m each represents a number of 1 or 2, n represents a number of 0 or 1, but when n is 0 the sum of l and m is 3 or less; and * indicates asymmetric carbon atom), a process for producing the same, liquid-crystalline substances containing said derivatives as active ingredient, and optical switching elements utilizing the liquid crystal compositions containing said liquid-crystalline substances.Type: GrantFiled: May 31, 1994Date of Patent: September 5, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Masayoshi Minai
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Patent number: 5420334Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting famesyl-protein transferase and the famesylation of the oncogene protein Ras.Type: GrantFiled: April 4, 1994Date of Patent: May 30, 1995Assignee: Merck & Co., Inc.Inventors: Sheo B. Singh, Gerald F. Bills, Russell B. Lingham, Isabel Martin, Keith C. Silverman, Jack L. Smith
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Patent number: 5384425Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.Type: GrantFiled: October 7, 1993Date of Patent: January 24, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5347041Abstract: Monomers containing two diacetylene segments each of which is connected on one end through a spacer segment to a central mesogen segment, and on the other end to an additional spacer segment, are topochemically polymerized in a molecularly ordered phase to produce homogeneous molecular composites. A preferred monomer embodiment comprises a compound of the formulaH--(CH.sub.2).sub.m --C.tbd.C--C.tbd.C--(CH.sub.2).sub.n --CO--O--R.sub.1 --O--CO--(CH.sub.2).sub.n --C.tbd.C--C.tbd.C--(CH.sub.2).sub.m Hwhere m and n are the number of repeating units, and R.sub.1 is a biphenylene mesogen.Type: GrantFiled: June 16, 1993Date of Patent: September 13, 1994Assignee: Edison Polymer Innovation CorporationInventor: Jerome B. Lando
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Patent number: 5344963Abstract: A process for the production of substituted vinylbenzenes of the general formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 C atoms, R.sub.1 is hydrogen or an acetyl group and R.sub.2 is hydrogen, a lower alkyl group having 1 to 4 C atoms or a benzyl group. A trialkylhydroquinone is cyclized with an aldehyde to an acetal and the latter is pyrolized to the end product. The substituted vinylbenzenes are valuable intermediate products in the synthesis of antioxidants.Type: GrantFiled: April 8, 1993Date of Patent: September 6, 1994Assignee: Lonza Ltd.Inventors: Aleksander Warm, David Laffan
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Patent number: 5322639Abstract: The carboxylic acid ester compound of the invention is represented by the following formula [I]: ##STR1## wherein R is an alkyl group of 3-20 carbon atoms; n is 0 or 1; at least one of A.sup.1, A.sup.2 and A.sup.3 is a group having tetralin structure, and the residual groups of A.sup.1, A.sup.2 and A.sup.3 are each independently a group having specific aromatic cyclic structure such as a phenylene group and a biphenyl group; Y.sup.1 and Y.sup.2 are each independently a group selected from the group consisting of --COO--, --CH.sub.2 CH.sub.2 -- and --CH.sub.2 O--; Q.sup.1 is a group selected from the group consisting of --CH.sub.3, --CF.sub.3, --C.sub.2 H.sub.5 and --C.sub.2 F.sub.5 ; and q is an integer of 4 to 12.This carboxylic acid ester compound may be used as an antiferroelectric liquid crystal material, and also be used as a liquid crystal composition by using other liquid crystal material in combination.Type: GrantFiled: April 14, 1993Date of Patent: June 21, 1994Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Junichi Kawabata, Hideo Yamaoka, Yuuichirou Tatsuki, Shinichi Nishiyama
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Patent number: 5306837Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.Type: GrantFiled: July 15, 1993Date of Patent: April 26, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Gregory S. Bisacchi, Toomas Mitt
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Patent number: 5296508Abstract: The invention relates to novel farnesylated tetrahydro-naphthalenols, that inhibit HMGR activity which results in a decrease in serum total cholesterol, a decrease in LDL cholesterol levels, and inhibition of LDL oxidation. The farnesylated tetrahydro-naphthalenols of the present invention are thus useful for cholesterol/lipid lowering in cases of hypercholesterolemia, hyperlipidemia, and atherosclerosis.Type: GrantFiled: December 23, 1992Date of Patent: March 22, 1994Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5283352Abstract: Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.Type: GrantFiled: December 7, 1992Date of Patent: February 1, 1994Assignee: Orion-yhtyma OyInventors: Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo J. Pystynen
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Patent number: 5281626Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.Type: GrantFiled: September 26, 1991Date of Patent: January 25, 1994Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
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Patent number: 5274174Abstract: A method for producing 4-acetoxystyrene by heating 4-acetoxyphenylmethylcarbinol, with an acid catalyst, at a temperature of from about 85.degree. C. to about 300.degree. C. under a pressure of from about 0.1 mm HgA to about 760 mm HgA for from about 0.2 minutes to about 10 minutes. The process also provides for the solventless (neat) hydrogenation of 4-acetoxyacetophenone to produce 4-acetoxyphenylmethylcarbinol. The reaction proceeds by heating at 54.degree. C. to 120.degree. C. with an excess of hydrogen in the presence of a Pd/C or activated nickel such as Raney Nickel catalyst in the absence of a solvent. The 4-acetoxyphenylmethylcarbinol may then be dehydrated to 4-acetoxystyrene. The later may be polymerized to poly(4-acetoxystyrene) and hydrolyzed to poly(4-hydroxystyrene).Type: GrantFiled: June 10, 1993Date of Patent: December 28, 1993Assignee: Hoechst Celanese CorporationInventors: Bakulesh N. Shah, Dung Q. Tran, Donna L. Keene
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Patent number: 5274179Abstract: Photoinitiators having at least one terminal fluoroalkyl moiety are useful for photopolymerizing and photocuring fluorinated as well as non-fluorinated monomers, especially fluorinated acrylic monomers.Type: GrantFiled: April 6, 1993Date of Patent: December 28, 1993Assignee: AlliedSignal Inc.Inventor: Chengjiu Wu
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Patent number: 5274175Abstract: A method for producing 4-acetoxystyrene by heating 4-acetoxyphenylmethylcarbinol, with an acid catalyst, at a temperature of from about 85.degree. C. to about 300.degree. C. under a pressure of from about 0.1 mm HgA to about 760 mm HgA for from about 0.2 minutes to about 10 minutes. The process also provides for the solventless (neat) hydrogenation of 4-acetoxyacetophenone to produce 4-acetoxyphenylmethylcarbinol. The reaction proceeds by heating at 54.degree. C. to 120.degree. C. with an excess of hydrogen in the presence of a Pd/C or activated nickel such as Raney Nickel catalyst in the absence of a solvent. The 4-acetoxyphenylmethylcarbinol may then be dehydrated to 4-acetoxystyrene. The later may be polymerized to poly(4-acetoxystyrene) and hydrolyzed to poly(4-hydroxystyrene).Type: GrantFiled: June 10, 1993Date of Patent: December 28, 1993Assignee: Hoechst Celanese CorporationInventors: Bakulesh N. Shah, Dung Q. Tran, Donna L. Keene
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Patent number: 5274176Abstract: A process for the production of substituted vinylbenzenes of the general formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 C atoms, R.sub.1 is hydrogen or an acetyl group and R.sub.2 is hydrogen, a lower alkyl group having 1 to 4 C atoms or a benzyl group. A trialkylhydroquinone is cyclized with an aldehyde to an acetal and the latter is pyrolized to the endproduct. The substituted vinylbenzenes are valuable intermediate products in the synthesis of antioxidants.Type: GrantFiled: October 21, 1992Date of Patent: December 28, 1993Assignee: Lonza Ltd.Inventors: Aleksander Warm, David Laffan
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Patent number: 5262439Abstract: The invention provides a class of water-soluble probucol derivatives having one or more ester groups replacing the phenyl hydroxyl groups of the probucol molecule. Some derivatives have polar or charged functionalities such as carboxylic acid groups, amino groups, aldehyde groups and amide groups located on the ester groups. Some of these compounds are spontaneously hydrolyzable in typical biological milieus. The present invention also provides method of treating an animal with probucol by administering a water-soluble probucol prodrug to the animal.Type: GrantFiled: April 30, 1992Date of Patent: November 16, 1993Assignee: The Regents of the University of CaliforniaInventor: Sampath Parthasarathy
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Patent number: 5246965Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.Type: GrantFiled: September 17, 1992Date of Patent: September 21, 1993Assignee: Ciba-GeigyInventor: Alan J. Main
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Patent number: 5235068Abstract: Acylaromatic compounds ##STR1## (Q: aromatic compound residue; R: straight, branched or cyclic aliphatic group, aromatic group or araliphatic group) are prepared in high yield by a reaction, in the presence of a boron trifluoride complex catalyst, of an aromatic compound with ##STR2## (X: H, Cl, Br; Y: Cl, Br) or with RCOOH in the presence of (XYCHCO).sub.2 O.Type: GrantFiled: July 21, 1992Date of Patent: August 10, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Masayoshi Minai, Michitada Kondo, Yuji Ueda, Seiichi Kai, Takayuki Higashii
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Patent number: 5214192Abstract: Diacetoxyatene compounds are obtained by reacting a perborate such as sodium perborate monohydrate or tetrahydrate and acetic acid with an iodoarene compound under mild conditions, such as 40 to 50.degree. C. The iodoarene can be further substituted by a wide range of substituents, such as halo, nitro, alkyl, alkoxy or carbosylic acid, in any position around the nucleus, except that electron withdrawing substituents occupy meta positions only. The invention process thus enables a wide range of substituted diacetoxyarene compounds to be produced using widely available and easily handled materials under mild operating conditions.Type: GrantFiled: October 2, 1991Date of Patent: May 25, 1993Assignee: Interox Chemicals LimitedInventors: Alexander McKillop, Duncan Kemp
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Patent number: 5210278Abstract: A process for preparing a substituted styrene by reacting a bisarylalkyl ether in the presence of an acid catalyst is disclosed. The process is preferably used for the preparation of 4-acetoxystyrene from 4,4'-(oxydiethylidene)bisphenol diacetate and 4-methoxystyrene from 4,4'-(oxydiethylidene)bisphenol dimethyl ether. A process for preparing a bisarylalkyl ether by reacting a corresponding arylalkanol in the presence of an acid catalyst is also disclosed.Type: GrantFiled: August 25, 1992Date of Patent: May 11, 1993Assignee: Hoechst Celanese CorporationInventors: Mohammad Aslam, Brad L. Smith, George Kvakovszky
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Patent number: 5166218Abstract: Tertiary and secondary amines of the formulas ##STR1## and ##STR2## wherein n is the integer 1 or 2,R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.Type: GrantFiled: August 12, 1991Date of Patent: November 24, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5142095Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 17, 1989Date of Patent: August 25, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5135940Abstract: Compounds of the Formulae: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 20, 1991Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Joshua Rokach, Rejean Fortin, Christiane Yoakim, Yvan Guindon
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Patent number: RE35060Abstract: Photoinitiators having at least one terminal fluoroalkyl moiety are useful for photopolymerizing and photocuring fluorinated as well as non-fluorinated monomers, especially fluorinated acrylic monomers.Type: GrantFiled: June 2, 1994Date of Patent: October 10, 1995Assignee: AlliedSignal Inc.Inventor: Chengjiu Wu
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Patent number: RE36849Abstract: Anisotropic compounds of the formula (1) specified in claim 1 are suitable, owing to their low .DELTA..epsilon./.epsilon..perp. values for liquid crystal displays which have high information densities of for examples up to 10.sup.6 image dots and accordingly need to be highly multiplexible; compared with known compounds they offer improved application properties and are relatively simple to synthesize.Type: GrantFiled: April 1, 1993Date of Patent: September 5, 2000Assignee: Merck Patent GmbHInventors: Hans P. Schad, Stephen M. Kelly, Eike Poetsch, Reinhard Hittich, Georg Weber