Plural Rings In Alcohol Moiety Patents (Class 560/107)
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Patent number: 5750577Abstract: Novel medicinally-useful compounds are provided herein. These compounds include isomeric cyclic tetramers of formaldehyde and 1-naphthol, and the derivatives or analogues of such cyclic tetramers, and linear oligomers of chromotropic acid, or its derivatives or analogues with naphthalene.Type: GrantFiled: December 5, 1996Date of Patent: May 12, 1998Assignee: Seabright Corporation LimitedInventor: Paris Georghiou
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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: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5670673Abstract: An improved method for isolating taxol and certain clinically important analogues of taxol from a crude extract of a naturally occurring Taxus species comprising treating the extract by reverse phase liquid chromatography on an adsorbent, causing the taxol and the taxol analogues to be adsorbed on the adsorbent, and recovering taxol and the natural analogues of taxol from the adsorbent by elution with an elutant. The compounds thus isolated in pure form are taxol, taxol-7-xyloside, 10-deacetyltaxol, 10-deacetyltaxol-7-xyloside, cephalomannine, cephalomannine-7-xyloside, 10-deacetylcephalomannine-7-xyloside, baccatin III, 10-deacetylbaccatin III, baccatin VI, brevitaxane A, and taxiflorine.Type: GrantFiled: May 5, 1995Date of Patent: September 23, 1997Assignee: University of FloridaInventor: Koppaka V. Rao
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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: 5643948Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes of the phorbol-, resiniferonol- and ingenol-classes.Type: GrantFiled: September 13, 1993Date of Patent: July 1, 1997Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5604256Abstract: Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.Type: GrantFiled: December 14, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company, LimitedInventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
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Patent number: 5550246Abstract: Synthetic calicheamicin mimics employ alternative activation triggers and trigger cites and include tithers for conjugation to DNA targeting systems.Type: GrantFiled: September 7, 1994Date of Patent: August 27, 1996Assignee: The Scripps Research InstituteInventors: K. C. Nicolaou, Emmanuel N. Pitsinos
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Patent number: 5523320Abstract: N-methyldeacetylcolchiceinamide derivatives represented by the formula ##STR1## wherein R denotes a residue obtained by removing COOH from a C.sub.3 -C.sub.7 sugar carboxylic acid, and hydroxyl groups present in the residue may properly be protected with a protecting group for a hydroxyl group.The N-methyldeacetylcolchiceinamide derivatives have less toxicity and strong effect for inhibiting proliferation of tumor cells, and are expected to be used as a carcinostatic.Type: GrantFiled: January 3, 1995Date of Patent: June 4, 1996Assignee: Ohgen Research Laboratories, Ltd.Inventor: Kiyoshi Akiyama
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Patent number: 5514825Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 10 carbons; R.sub.2 and R.sub.3 are hydrogen, or alkyl of 1 to 6 carbons and the substituted ethynyl group occupies either the 2 or the 3 position of the tetrahydronaphthalene nucleus; m is an integer having the value of 0-3; o is an integer having the value 0-4; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.2 groups; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.Type: GrantFiled: December 29, 1994Date of Patent: May 7, 1996Assignee: Allergan, Inc.Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5475120Abstract: An improved method for isolating taxol and certain clinically important analogues of taxol from a crude extract of a naturally occuring Taxus species comprising treating the extract by reverse phase liquid chromatography on an adsorbent, causing the taxol and the taxol analogues to be absorbed on the adsorbent, and recovering taxol and the natural analogues of taxol from the adsorbent by elution with an elutant. The compounds thus isolated in pure form are taxol, taxol-7- xyloside, 10-deacetyltaxol, 10-deacetyltaxol-7-xyloside, cephalomannine, cephalomannine-7-xyloside, 10-deacetylcephalomannine-7-xyloside, baccatin III, 10-deacetylbaccatin III, baccatin VI, brevitaxane A, and taxiflorine.Type: GrantFiled: November 2, 1994Date of Patent: December 12, 1995Assignee: University of FloridaInventor: Koppaka V. Rao
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Patent number: 5412134Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, diphenylsilane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.Type: GrantFiled: May 26, 1992Date of Patent: May 2, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Janak Singh, Gregory S. Bisacchi, Richard H. Mueller
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Patent number: 5382598Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.Type: GrantFiled: September 24, 1993Date of Patent: January 17, 1995Assignees: Imperial Chemical Industries PLC, Imperial Chemical HouseInventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5380916Abstract: An improved method for isolating certain clinically important taxane derivatives from the crude extract of a naturally occurring Taxus species comprising treating the extract by reverse phase liquid chromatography on an adsorbent; causing the taxane derivatives to be adsorbed on the adsorbent; and recovering the taxane derivatives from the adsorbent by elution with an elutant. The taxane derivatives thus isolated in pure form are taxol, taxol-7-xyloside, 10-deacetyitaxol, 10-deacetyltaxol-7-xyloside, cephalomannine, cephalomannine-7-xyloside, 10-deactylcephalomannine-7-xyloside, baccatin III, 10-deacetylbaccatin III, baccatin VI, and brevitaxane A.Type: GrantFiled: July 16, 1992Date of Patent: January 10, 1995Assignee: University of FloridaInventor: Koppaka V. Rao
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Patent number: 5374376Abstract: Disclosed are herein optically active aromatic compounds represented by the formula (I): ##STR1## wherein X represents --COO-- or --OCO--; Y represents --COO--, --OCO-- or --O--; R.sub.2 represents an alkyl or alkoxyalkyl group having 1 to 20 carbon atoms unsubstituted or substituted by a halogen atom; R.sub.1 represents an alkyl group having 3 to 20 carbon atoms;Z represents ##STR2## wherein p represents a number of 1 to 5 and * indicates an asymmetric carbon atom; l and k each represents a number of 1 or 2; m and s each represents a number of 0 or 1, which are useful as a liquid crystal.Type: GrantFiled: September 21, 1993Date of Patent: December 20, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Isao Kurimoto, Shoji Toda, Masayoshi Minai, Shigeaki Chika, Koichi Fujisawa, Kiyoshi Imamura
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Patent number: 5340498Abstract: A novel anti-ferroelectric liquid crystal of the formula (I), ##STR1## wherein: is an integer of 3 to 8,each of X and Y is independently a hydrogen atom or a fluorine atom,Z is --CF.sub.3, --CH.sub.3 or --C.sub.2 H.sub.5,q is 0 or 5,m is 0 or 1,n is an integer of 2 to 8, andC* is an asymmetric carbon, provided that when m is 0, q is 0 and n is an integer of 4 to 8 and that when m is 1, q is 5 and z is --CF.sub.3,and use of tile above liquid crystal as a liquid crystal display device.Type: GrantFiled: August 19, 1993Date of Patent: August 23, 1994Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Yoshihisa Arai, tomoyuki Yui, Yoshihiro Gocho
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Patent number: 5326786Abstract: Compounds represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent a hydrogen atom or a protective group for a hydroxyl group, or R.sub.1 and R.sub.2 combine to represent a protective group for hydroxyl groups, andR.sub.3 represents CH.sub.3 O-- or CH.sub.3 NH--.These compounds exhibit a strong effect to inhibit proliferation of cancer cells and are expected to be used as a carcinostatic agent.Type: GrantFiled: April 23, 1993Date of Patent: July 5, 1994Assignee: Ohgen Research Laboratories Ltd.Inventor: Kiyoshi Akiyama
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Patent number: 5321044Abstract: 15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.Type: GrantFiled: May 4, 1992Date of Patent: June 14, 1994Assignee: SRI InternationalInventors: Richard H. Peters, Masato Tanabe
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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: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5275757Abstract: Novel anti-ferroelectric liquid crystal compounds represented by the following general formula (I) and a liquid crystal display element wherein such a compound is used. ##STR1## Ph represents a phenylene group, R represents a straight-chain alkyl group having 6 to 10 carbon atoms,X represents an oxygen atom or a single bond provided that when X is an oxygen atom, L is an integer of 5 to 8, m is 1 and n is an integer of 1 to 7, or L and m are zero (0) and n is an integer of 6 to 8, and when X is a single bond,L is an integer of 5 to 8, m is 1 and n is an integer of 1 to 7, andC* represents an asymmetric carbon atom.Type: GrantFiled: December 4, 1992Date of Patent: January 4, 1994Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Hiroshi Mineta, Tomoyuki Yui, Takahiro Matsumoto
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Patent number: 5258544Abstract: Disclosed is a process for the preparation of 2-aryl-1-cyclohexene-1-carboxaldehydes from 1-arylcyclohexenes which are intermediates for trans-6-[(2-arylsubstituted cycloalkenyl and substituted cycloalkyl)alkenyl and alkyl]-3,4,5,6-tetrahydro-2H-pyran-2-ones.Type: GrantFiled: March 5, 1991Date of Patent: November 2, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Laurence W. Reilly, Jr., Ching T. Tsuei, Walter Rodriquez, Thomas Goetzen
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Patent number: 5238602Abstract: Compounds of the formula ##STR1## wherein n stands for the number 0 or 1; the rings A.sup.1, A.sup.2 and A.sup.3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; X.sup.1 represents a single covalent bond, --COO--, --OOC--, --CH.sub.2 CH.sub.2 --, p--C.sub.6 H.sub.4 --, --CH.sub.2 CH.sub.2 --p-- C.sub.6 H.sub.4 --, --CH.sub.2 CH.sub.2 --p--C.sub.6 H.sub.4 --CH.sub.2 CH.sub.2 -- or, insofar as the rings A.sup.1 and A.sup.2 represent 1,4-phenylene, also --NON--; R.sup.2 represents 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or alkenyloxy, with the proviso that the oxygen atom in alkenyloxy is linked with a saturated carbon atom; and R.sup.1 signifies 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or, insofar as R.sup.2 represents alkenyloxy, also alkyl, their manufacture, as well as liquid crystalline mixtures and the use for electro-optical purposes.Type: GrantFiled: May 26, 1987Date of Patent: August 24, 1993Assignee: Hoffmann La Roche Inc.Inventors: Martin Petrzilka, Martin Schadt
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Patent number: 5231221Abstract: Compounds of the formula ##STR1## can advantageously be prepared by reacting compounds the formula II ##STR2## in which the substituents R.sup.1 -R.sup.4 have the meanings given, with the anhydride of the formula III ##STR3## in the presence of dimethyl sulfoxide and the acid corresponding to the anhydride of the formula III.Type: GrantFiled: March 18, 1991Date of Patent: July 27, 1993Assignee: Hoechst AktiengesellschaftInventors: Winfried Hertzsch, Gerhard Jahne
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Patent number: 5209867Abstract: Novel derivatives of aromatic carboxylic acid esters which are useful as a dopant for liquid crystal compositions, and smectic liquid crystal compositions containing at least one of said derivatives.Type: GrantFiled: December 30, 1991Date of Patent: May 11, 1993Assignee: Sharp Kabushiki KaishaInventors: Mitsuhiro Koden, Tomoaki Kuratate, Fumiaki Funada
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Patent number: 5137653Abstract: This invention provides a novel alkanoyl ester compound represented by general formula (I): ##STR1## (wherein A is of --, --O--, ##STR2## B is ##STR3## l and m are 1 or 2 provided that both are not simultaneously 2, k and n are an integer of 1 or more, respectively, provided that k>n, and R is an alkyl group), a liquid crystal composition containing this compound, a novel alkanoylphenyl compound or a novel alkanoylbiphenyl compound as an intermediate for the production of the above compound, and a method of producing the same. These novel alkanoyl ester compounds are excellent in the stability against light and the like and can take a liquid crystal state at a wide temperature range. Particularly, these compounds form liquid crystals of ferroelectricity having a large spontaneous polarization and a fast response rate by introducing an optically active group into the compound, so that they develop a very excellent effect as a starting material for optoelectronics and its related elements.Type: GrantFiled: October 18, 1991Date of Patent: August 11, 1992Assignee: Nippon Mining Co., Ltd.Inventors: Toshihiro Hirai, Atsushi Yoshizawa, Isa Nishiyama, Mitsuo Fukumasa, Nobuyuki Shiratori, Akihisa Yokoyama
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Patent number: 5128479Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A 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: January 29, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5124070Abstract: Disclosed are herein optically active ester derivatives represented by the formula (I): ##STR1## (wherein R.sub.1 represents an alkyl group having 3 to 20 carbon atoms; R.sub.2 represents an optically active alkyl or alkoxyalkyl group having 3 to 15 carbon atoms optionally substituted by halogen atoms; Y represents --O--, --COO-- or --OCO--; X represents --COO-- or --OCO--; l represents a number of 1 or 2; k and m each represents a number of 0 or 1; n represents a number of 1 to 6), preparation processes therefor, liquid crystal materials containing such ester derivatives as active ingredient, and a light switching element using said liquid crystal materials as liquid crystal element.Type: GrantFiled: August 28, 1989Date of Patent: June 23, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Isao Kurimoto, Shoji Toda, Masayoshi Minai, Takeshi Tani, Chizu Kawakami, Koichi Fujisawa, Kiyoshi Imamura
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Patent number: 5116867Abstract: Chemicals are disclosed which are useful for inhibiting the actions of adenosine in mammals, comprising: L-propranolol, or D-propranolol, or alprenolol and derivatives thereof for parenteral or topical administration are disclosed for purposes of achieving desired circulating concentrations in the range of 10 nanogram to 10 milligrams per kilogram.D-Propranolol is of special interest because it is relatively inactive as a .beta.-adrenergic blocking agent. Specific uses of D-propranolol include the treatment of asthma, chronic obstructive pulmonary disease, A-V node conduction disturbances; apnea of preterm infants, pulmonary hypertension, headaches, migraine, and in attention-deficit disorder. D-Propranolol might also be used as a substitute for xanthines in beverages to produce a feeling of well being, awakeness, awareness and increased performance.Type: GrantFiled: June 30, 1989Date of Patent: May 26, 1992Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: David C. Klein, Olga Nikodijevic
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 5105020Abstract: The invention concerns a cycloalkane derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted banzoyl; andR.sup.2 and R.sup.3 together form a (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: December 22, 1989Date of Patent: April 14, 1992Assignees: Imperial Chemistries Industries PLC, ICI PharmaInventor: Jean-Marc M. M. Girodeau
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Patent number: 5098602Abstract: This invention provides a novel halogen-containing ester compound represented by the following general formula (I): ##STR1## (wherein R is an alkyl group, A is selected from a single bond, --O--, --COO-- and --CO--, both of X and Y are halogen atoms or either one of X and Y is a halogen atom and the other is a hydrogen atom, each of m and n is 0 or 1, m+n=0 or 1, each of k and l is an integer of 1 or more, provide k<l), a liquid crystal composition and a light switching element each containing the above compound as well as a novel fluorophenol compound represented by the following general formula (II): ##STR2## (wherein each of k and l is an integer of 1 or more, provided k<l) as an intermediate for the synthesis of the above ester compound and a method of producing the same.Type: GrantFiled: May 2, 1989Date of Patent: March 24, 1992Assignee: Nippon Mining Co., Ltd.Inventors: Toshihiro Hirai, Atsushi Yoshizawa, Isa Nishiyama, Mitsuo Fukumasa, Nobuyuki Shiratori, Akihisa Yokoyama
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Patent number: 5091558Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.Type: GrantFiled: March 6, 1987Date of Patent: February 25, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
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Patent number: 5091565Abstract: New poly-dicarboxylic acid anhydrides, which are suitable as bio-degradable matrix materials for the controlled release of medicinal agents in humans.Type: GrantFiled: August 21, 1990Date of Patent: February 25, 1992Assignee: Sandoz Ltd.Inventor: Gerd Ziegast
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Patent number: 5089657Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein:R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are selected from the group consisting of hydrogen, R.sup.4 and -C(O)W, whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.Type: GrantFiled: March 11, 1987Date of Patent: February 18, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti
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Patent number: 5079245Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.Type: GrantFiled: July 5, 1989Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
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Patent number: 5064564Abstract: The present invention discloses an optically active compound represented by the following general formula (I): ##STR1## wherein R.sup.1 represents an alkyl, alkoxyl, or alkoxyalkanoyloxy group which has 1 to 18 carbon atoms and may be substituted with fluorine, chlorine, or cyano group; R.sup.2 represents an alkyl group having 1 to 18 carbon atoms; ##STR2## m is 0 or 1; Y represents a single bond, --CH.sub.2 O--, or --COO--; Z represents a single bond or --COO--; and C* and C** each independently represents an asymmetric carbon atom of the (R) and (S) configuration, an intermediate therefor being represented by the following general formula (II): ##STR3## wherein R.sup.2 represents an alkyl group having 1 to 18 carbon atoms, n is 0 or 1, and C* and C** each independently represents an asymmetric carbon atom of the (R) or (S) configuration, a process for producing the intermediate, and a liquid-crystal compound using the optically active compound.Type: GrantFiled: December 20, 1990Date of Patent: November 12, 1991Assignees: Dainippon Ink and Chemicals, Inc., Sagami Chemical Research CenterInventors: Sadao Takehara, Takeshi Kuriyama, Toru Fujisawa, Kayoko Nakamura, Tamejiro Hiyama, Kusumoto, Tetsuo, Akiko Nakayama
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Patent number: 5053525Abstract: Mevinolin-like compounds in which the lactone is opened and the hydroxyl function produced thereby is replaced by an oxo function are potent HMG-CoA reductase inhibitors possessing one less asymmetric center.Type: GrantFiled: February 13, 1986Date of Patent: October 1, 1991Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Gerald E. Stokker
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Patent number: 5051409Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.Type: GrantFiled: November 1, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5051527Abstract: The invention lies in novel ferroelectric liquid crystal compounds particularly represented by the general formulae, having a good responsibility in relation to the applied electric field and a wide range of phase transition points inclusive of the room temperature so as to be useful alone as the liquid crystal material but also to be mixed with other liquid crystal compounds for expanding the phase transition points to a desired range and making the response speed of the liquid crystal composition faster. ##STR1## In the formulae, m and n are same or different with each other and represent an integral of 1-20.Type: GrantFiled: February 28, 1989Date of Patent: September 24, 1991Assignee: Showa Shell Sekiyu K.K.Inventors: Yoshiichi Suzuki, Takashi Hagiwara, Hiroyuki Mogamiya
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Patent number: 5030764Abstract: Novel styryl-tetrahydronaphthalene and indane derivatives useful for treating neoplasms and dermatoses.Type: GrantFiled: October 15, 1990Date of Patent: July 9, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
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Patent number: 5030765Abstract: The present invention is concerned with novel tetrahydronaphthalene and indane derivatives of the formula ##STR1## useful as for combatting dermatoses as well as neoplasmas.Type: GrantFiled: October 16, 1990Date of Patent: July 9, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
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Patent number: 5030654Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 19, 1989Date of Patent: July 9, 1991Assignee: Pfizer Inc.Inventors: Ian T. Barnish, John C. Danilewicz, Keith James, Gillian M. R. Samuels, Nicholas K. Terrett, Michael T. Williams, Martin J. Wythes
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Patent number: 5026899Abstract: The invention relates to novel 2-acyl-1,3-cyclohexanediones and the oxime ethers thereof with herbicidal and plant growth regulating properties.The novel 2-acyl-1,3-cyclohexanediones and the oxime ethers thereof are of the formula I ##STR1## wherein A is a 2- or 7-membered alkylene bridge, or a 3- to 7-membered alkenylene bridge which may be mono- or polyunsaturated,n is 0, 1 or 2,R.sub.1 is C.sub.1 -C.sub.4 alkyl or benzyl,R.sub.2 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; or is C.sub.3 -C.sub.6 cycloalkyl; or phenyl, benzyl or phenylethyl, the phenyl ring of each of which may be substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, cyano or nitro,X is oxygen or a radical --NOR.sub.3, andR.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.Type: GrantFiled: December 13, 1989Date of Patent: June 25, 1991Assignee: Ciba-Geigy CorporationInventor: Hans Tobler
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Patent number: 5025017Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.Type: GrantFiled: September 28, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5021453Abstract: Compounds of formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: June 6, 1990Date of Patent: June 4, 1991Assignee: Merck & Co., Inc.Inventors: Henry Joshua, Kenneth E. Wilson, Michael S. Schwartz, Ta J. Lee, Gerald E. Stokker
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Patent number: 5004817Abstract: Compounds having the formula (I): ##STR1## wherein: M is an alkali or alkaline-earth metal or a C.sub.1 -C.sub.18 alkyl group;X is a group selected from --CH.sub.2 --, --CO--, --CH.sub.2 --CO--, --CH(CH.sub.3)--CO--,p is 0 or 1;Ar is a simple or condensed aromatic ring or Ar represents two or more aromatic nuclei bonded either by a simple bond or by an --O--, --S--, --SO.sub.2 --, --SO--, --CO--, --CS--, or --NH-- group;y is H or CH.sub.3 ;m is 1 when Y=--CH.sub.3, or an integer from 1 to 5 (including both values) when Y=H; n is a number ranging from 1 to 500 (including both values); andZ is H; a C.sub.1 -C.sub.18 alkyl; benzyl; glycidyl; acetyl; allyl; --CO--NH--R or --CO--NH--R.sub.1 --NCO group.Type: GrantFiled: February 27, 1989Date of Patent: April 2, 1991Assignee: Montefibre, S.p.A.Inventors: Catia Bastioli, Salvatore Garlisi, Dario Fornara, Vittorio Bellotti
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4979805Abstract: A ferroelectric liquid crystal composition containing an optically active mesomorphic compound represented by the following formula (I) or (II): ##STR1## wherein R.sub.1 and R.sub.2 are respectively an alkyl, and C with * represents an asymmetric carbon atom. The mesomorphic compound provides the ferroelectric liquid crystal composition with an extended operational life in a liquid crystal device.Type: GrantFiled: December 1, 1989Date of Patent: December 25, 1990Assignee: Canon Kabushiki KaishaInventors: Kazuo Yoshinaga, Kazuharu Katagiri
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Patent number: 4976887Abstract: A compound represented by formula: ##STR1## In the formula, Ar represents ##STR2## and each of Ra and Rb independently represents an optically non-active alkyl group or an optically active group having an asymmetric carbon atom. Either Ra or Rb is the optically active group. X represents ##STR3## Each of l and m represents 0 or 1.Type: GrantFiled: November 23, 1988Date of Patent: December 11, 1990Assignee: Kabushiki Kaisha ToshibaInventors: Kohki Takatoh, Masanori Sakamoto, Kazuyuki Sunohara