Unsaturated Carbocyclic Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding (e.g., Quinophthalones, Etc.) Patents (Class 546/173)
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Patent number: 6335449Abstract: The present invention relates a process for producing the quinoline derivative (3) via the nitrile compound (1) obtained by reacting the aldehyde compound represented by formula (2) with diethyl cyanomethylphosphonate and its intermediate (1).Type: GrantFiled: January 23, 2001Date of Patent: January 1, 2002Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshio Ohara, Mikio Suzuki, Yoshinobu Yanagawa, Yasutaka Takada
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Patent number: 6262269Abstract: The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: wherein R1, R2, R3, R4, R5, R6, R7, R9, and Y, have the meanings provided.Type: GrantFiled: February 3, 1998Date of Patent: July 17, 2001Assignee: Trega Biosciences, Inc.Inventors: Thomas K. Hayes, Behrouz Forood, John S. Kiely
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Patent number: 6258824Abstract: The present invention relates to compounds of formula 1 and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering compounds of formula 1 to the mammal. The invention also relates to intermediates and methods useful in synthesizing compounds of formula 1.Type: GrantFiled: February 9, 2000Date of Patent: July 10, 2001Assignee: Pfizer Inc.Inventor: Bingwei V. Yang
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Patent number: 6222047Abstract: The invention relates to the preparation of pyrocarbonic acid diesters by an improved process and to the novel pyrocarbonic acid diesters prepared according to said process as well as to the use thereof. The core of the invention is a process for the preparation of a pyrocarbonic acid diester of formula (I) wherein R1 and R1′ are each independently of the other branched or straight-chain C1-C24alkyl, C3-C24alkenyl, C3-C24alkynyl, C4-C12cycloalkyl, C4-C12cycloalkenyl or C7-C24aralkyl, each of which is unsubstituted or substituted by one or more than one substituent which is inert under the reaction conditions, by reacting at least one ester carbonate of formula (II) with 40-50 mol % of a sulfochloride of formula (IV) in the presence of 0.Type: GrantFiled: January 13, 1998Date of Patent: April 24, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: John Zambounis, VĂ©ronique Hall-Goulle
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Patent number: 6221604Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: February 7, 2000Date of Patent: April 24, 2001Assignee: PE CorporationInventors: Krishna G. Upadhya, Steven M. Menchen, Weiguo Zhen
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Patent number: 6194450Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: July 23, 1998Date of Patent: February 27, 2001Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
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Patent number: 6166006Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: December 17, 1998Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6165944Abstract: 4-(3-Heterocyclyl-1-benzoyl)pyrazoles of the formula I ##STR1## where: R.sup.1 and R.sup.3 are each hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, N-alkylaminosulfonyl, N,N-dialkyl)aminosulfonyl, N-alkylsulfonylamino, N-haloalkylsulfonylamino, N-alkyl-N-alkylsulfonylamino or N-alkyl-N-haloalkylsulfonylamino;R.sup.2 is a 5- or 6-membered heterocyclyl radical with or without substitution which comprises 1 to 4 identical or different hetero atoms from the following group: oxygen, sulfur or nitrogen;R.sup.4 is hydrogen, halogen or alkyl;R.sup.5 is substituted pyrazole which is attached in position 4;and agriculturally useful salts thereof; processes for preparing the 4-(3-heterocyclyl-1-benzoyl)pyrazoles; compositions comprising them; and the use of these derivatives or these compositions comprising them for controlling undesirable plants.Type: GrantFiled: June 16, 1998Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Ernst Baumann, Stefan Engel, Guido Mayer, Joachim Rheinheimer, Matthias Witschel, Ulf Misslitz, Oliver Wagner, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6130238Abstract: The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: October 10, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6114349Abstract: Substituted quinoline derivatives, processes for their preparation, and their use.Compounds of the formula I ##STR1## and their tautomeric forms, of the formula Ia ##STR2## in which m, n and the substituents X and R.sup.1 to R.sup.5 have the meanings mentioned, have an action against viruses.Type: GrantFiled: March 3, 1999Date of Patent: September 5, 2000Assignee: Hoechst AktiengesellschaftInventors: Reinhard Kirsch, Jorg-Peter Kleim, Gunther Riess, Bernd Rosenstock, Manfred Rosner, Irvin Winkler
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Patent number: 6093821Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: July 25, 2000Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L. F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 6084120Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.Type: GrantFiled: June 22, 1998Date of Patent: July 4, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jawad Alzeer, Jacques Chollet, Christian Hubschwerlen, Hugues Matile, Robert George Ridley
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Patent number: 6069151Abstract: Compounds of the formula ##STR1## have therapeutic utility, as inhibitors of phosphodiesterase IV and TNF release.Type: GrantFiled: June 17, 1998Date of Patent: May 30, 2000Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, John Gary Montana, Alan Findlay Haughan, Verity Margaret Sabin
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Patent number: 6057336Abstract: The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: October 2, 1998Date of Patent: May 2, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
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Patent number: 6051360Abstract: Dyestuffs represented by the below-described formula (1), that is, dyestuffs formed of a chromophoric nucleus and a bisphenol introduced therein have excellent solubility in solvents and binder resins, and can provide color filters having excellent transmittance characteristics and durability. ##STR1## wherein Dye represents a chromophoric nucleus, X represents a direct bond or a divalent connecting group, R.sup.1 to R.sup.10 and n are defined with the provision that one of R.sup.9 and R.sup.10 has 3 or more carbon atoms.Type: GrantFiled: December 31, 1997Date of Patent: April 18, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Akio Karasawa, Hisato Itoh
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Patent number: 6031106Abstract: A process for preparing pyridyl-substituted N-phenylhydroxylamines by catalytic hydrogenation of the corresponding nitro compounds in the presence of an N-substituted morpholine compound and rearrangement of the hydroxylamine compounds obtained to pyridyl-4-fluoraniline compounds is described.Type: GrantFiled: September 14, 1998Date of Patent: February 29, 2000Assignee: BASF AktiengesellschaftInventors: Albrecht Harreus, Norbert Gotz, Michael Rack, Heinz Isak, Peter Schafer
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Patent number: 6025378Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: June 18, 1998Date of Patent: February 15, 2000Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5968952Abstract: The present invention is concerned with compounds of formula (I), ##STR1## the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)-aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2 and R.sup.3 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxy-C.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.Type: GrantFiled: April 29, 1998Date of Patent: October 19, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Patrick Rene Angibaud, Gerard Charles Sanz, David William End
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Patent number: 5955614Abstract: Compounds of the general formula (I) or tautomeric forms thereof ##STR1## wherein Ar.sub.1 and Ar.sub.2 independently of one another denote radicals to complete optionally substituted carbocyclic aromatic rings, B denotes an optionally substituted alkylene group or a radical of the formula ##STR2## wherein r represents a number from 1 to 4, the ends of which are in each case bonded to an aromatic C atom of the two radicals Ar.sub.1 and Ar.sub.2, andX.sub.1 and X.sub.2 independently of one another represent a radical of the formulae chosen from the group consisting of ##STR3## these being in each case located in the ring such that the ##STR4## or the ##STR5## group is adjacent to the C--C double bond, wherein Y, Z, R.sub.a and R.sub.b have the meaning, given in the description, are outstandingly suitable for bulk dyeing of plastics.Type: GrantFiled: August 28, 1997Date of Patent: September 21, 1999Assignee: Bayer AktiengesellschaftInventors: Dietmar Kalz, Dieter Arlt, Karl-Heinz Reinhardt
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Patent number: 5952345Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives 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. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: June 9, 1997Date of Patent: September 14, 1999Assignee: Allergan Sales, Inc.Inventors: Elliot 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
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Patent number: 5948597Abstract: Dyes suitable for use in the fabrication of color filters are described which contain one or more photopolymerizable substituents preferably represented by the following formula:D-(A-Yn.sup.1)n.sup.2 (1)where D represents a chromophoric nucleus, A denotes a connecting group, Y means the photopolymerizable group, .sub.n.sup.1 is 1-10,000, and .sub.n.sup.2 stands for an integer of 1-10. Also described are photosensitive resist resin compositions containing the dyes as well as color filters fabricated by curing the photosensitive resist resin compositions.Type: GrantFiled: June 1, 1998Date of Patent: September 7, 1999Assignee: Mitsui Chemicals, Inc.Inventors: Hisato Itoh, Akio Karasawa, Kenichi Sugimoto
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Patent number: 5932592Abstract: A compound represented by the general formula: ##STR1## wherein Y represents a nitrogen atom or C-G (G represents a carboxyl group which may be esterified); ring R is a nitrogen-containing unsaturated heterocyclic group which may be substituted for; each of rings A and B may have a substituent; n represents an integer from 1 to 4; k represents the integer 0 or 1, or a salt thereof, which serves well as an anti-inflammatory agent, particularly a therapeutic agent for arthritis.Type: GrantFiled: October 21, 1997Date of Patent: August 3, 1999Assignee: Takeda Chemical Ind., Ltd.Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
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Patent number: 5872130Abstract: Described herein are mevalonolactone derivatives having a quinoline ring of formula (I) ##STR1## wherein the R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z variables are described therein.Type: GrantFiled: December 19, 1990Date of Patent: February 16, 1999Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 5866579Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: April 11, 1997Date of Patent: February 2, 1999Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, T. G. Murali Dhar, Charles Gluchowski
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Patent number: 5856336Abstract: A compound of the formula ##STR1## Z=--CH(OH)--CH.sub.2 --CH(OH)--CH.sub.2 --COO.1/2Ca have HMG--CoA inhibiting effects, making them useful as inhibitors of cholesterol biosynthesis. The compound may be prepared as a pharmaceutical for reducing hyperlipidemia, hyperlipoproteinemia or atherosclerosis.Type: GrantFiled: May 15, 1992Date of Patent: January 5, 1999Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 5856337Abstract: 2-Arylquinolines represented by formula (1): ##STR1## wherein R.sup.1, R.sup.3 to R.sup.9 each represents hydrogen, halogen, lower alkyl, cyclic lower alkyl, aryl, aralkyl, alkoxy or --C.sub.m F.sub.2m+1 ; R.sup.2 represents hydrogen, halogen, lower alkyl, cyclic lower alkyl, aryl, aralkyl, alkoxy, --C.sub.n F.sub.2n+1 or --CH.sub.2 Q, in which Q represents a monovalent organic group obtained by eliminating from an organic compound having --NH-- the hydrogen atom bonded to the nitrogen, or halogen; X represents halogen or hydrogen; Y represents nitro or amino which may be protected with a protecting group; and m and n each represents an integer of from 1 to 6; and processes for producing the 2-arylquinolines.Type: GrantFiled: January 24, 1997Date of Patent: January 5, 1999Assignees: Asahi Glass Co., Ltd., The Green Cross CorporationInventors: Takashi Okazoe, Yoshitomi Morizawa
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Patent number: 5854259Abstract: Described herein are mevalonolactone derivatives having a quinoline ring of formula (I) ##STR1## wherein the R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z variables are described therein.Type: GrantFiled: November 19, 1992Date of Patent: December 29, 1998Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 5852039Abstract: The present invention provides a pharmaceutical composition for inhibiting bone resorption or for preventing or treating osteoporosis which comprises a quinoline or quinazoine derivative as an active ingredient.Type: GrantFiled: January 15, 1997Date of Patent: December 22, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Atsuo Baba
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Patent number: 5795889Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.Type: GrantFiled: February 9, 1995Date of Patent: August 18, 1998Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
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Patent number: 5783522Abstract: Substituted 2-phenylpyridines I ##STR1## R.sup.1,R.sup.3 =H, halogen, alkyl, haloalkyl, alkoxyalkyl, alkoxy, alkoxyalkoxy, OH, haloalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, SH, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, CHO, CN, CO.sub.2 H, alkoxycarbonyl, alkoxyalkoxycarbonyl, haloalkoxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxyalkylcarbonyl, CONH.sub.2, alkyl-aminocarbonyl, dialkylaminocarbonyl, pyrrolidinyl-carbonyl piperidylcarbonyl, morpholinylcarbonyl, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, pyrrolidinyl, piperidinyl, morpholinyl, alkylcarbonylamino, haloalkylcarbonylamino, alkylsulfonylamino;R.sup.2 =halogen, CN, NO.sub.2, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio; orR.sup.1 +R.sup.2 or R.sup.2 +R.sup.3 =trimethylene or tetramethylene chain;R.sup.Type: GrantFiled: January 11, 1996Date of Patent: July 21, 1998Assignee: BASF AktiengesellschaftInventors: Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hartmann Koenig, Ralf Klintz, Peter Muenster, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5780634Abstract: Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.Type: GrantFiled: October 27, 1995Date of Patent: July 14, 1998Assignees: The Green Cross Corporation, Asahi Glass Co., Ltd.Inventors: Yoshihisa Inoue, Hajime Ebisu, Naomichi Ishida, Norifumi Nakamura, Jun Sasaki, Takashi Okazoe, Yoshitomi Morizawa, Arata Yasuda, Shuzhong Wang, Tomoko Ito
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Patent number: 5770602Abstract: A compound represented by the general formula: ##STR1## wherein Y represents a nitrogen atom or C--G (G represents a carboxyl group which may be esterified); ring R is a nitrogen-containing unsaturated heterocyclic group which may be substituted for; each of rings A and B may have a substituent; n represents an integer from 1 to 4; k represents the integer 0 or 1, or a salt thereof, which serves well as an anti-inflammatory agent, particularly a therapeutic agent for arthritis.Type: GrantFiled: May 8, 1995Date of Patent: June 23, 1998Assignee: Takeda Chemical IndustriesInventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
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Patent number: 5767277Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.Type: GrantFiled: January 7, 1997Date of Patent: June 16, 1998Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5753675Abstract: Quinoline analogs of mevalonolactone of the following formula are useful as anti-cholesterol synthesis agents: ##STR1## where the substituents are as defined in the specification.Type: GrantFiled: March 23, 1990Date of Patent: May 19, 1998Assignee: Novartis Pharmaceuticals CorporationInventor: Sompong Wattanasin
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Patent number: 5714488Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.Type: GrantFiled: September 17, 1996Date of Patent: February 3, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
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Patent number: 5695684Abstract: A mesomorphic compound represented by a formula (I) containing a quinoline-2,6-diyl skeleton is suitable as a component for a liquid crystal composition providing improved response characteristics and a high contrast. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of electrode plates. The liquid crystal device may preferably be used as a display panel constituting a liquid crystal apparatus providing good display characteristics.Type: GrantFiled: March 27, 1995Date of Patent: December 9, 1997Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
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Patent number: 5691322Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have a quinoline or a pyridine anchor attached by means of a linker to a binding domain sidechain, which compounds inhibit the enzyme 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: E.R. Squibb & Sons, Inc.Inventor: Jeffrey Adam Robl
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Patent number: 5688810Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 5674880Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.4)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Celltech Therapeutics LimitedInventors: Ewan Campbell Boyd, Michael Anthony William Eaton, Graham John Warrellow
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Patent number: 5663348Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.Type: GrantFiled: July 19, 1995Date of Patent: September 2, 1997Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5650410Abstract: This invention provides an anti-inflammatory agent, particularly an agent for treating arthritis, containing a quinoline or quinazoline derivative or a salt thereof ##STR1## wherein Y is a nitrogen atom or C--G in which G is an optionally esterified carboxyl group;R.sup.1 and R.sup.2 are each independently a hydrogen atom, optionally substituted hydrocarbon group or optionally substituted heterocyclic group, or R.sup.1 and R.sup.2 are linked together to form a saturated ring;each of the ring A and ring B may optionally be substituted;n is an integer of 1 to 4; andk is 0 or 1.This invention also provides a novel quinoline or quinazoline derivative having anti-inflammatory activity.Type: GrantFiled: April 17, 1995Date of Patent: July 22, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
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Patent number: 5650514Abstract: The present invention relates to 3-substituted quinoline-5-carboxylic acid derivatives and processes for their preparation.Type: GrantFiled: July 17, 1995Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Michael Negele, Karl-Heinz Wahl, Jan-Bernd Lenfers, Samir Samaan
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Patent number: 5641789Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof, wherein X.sup.1, Ar, X, Y.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and n are defined below, which are inhibitors of the production of leukotrienes and/or blockers of leukotriene receptors, methods for preparing said compounds and intermediates useful in the preparation thereof, pharmaceutical compositions thereof methods of treatment therewith. The compounds of the above formula are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related diseases in mammals.Type: GrantFiled: March 31, 1995Date of Patent: June 24, 1997Assignee: Pfizer Inc.Inventor: Anthony Marfat
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Patent number: 5622964Abstract: Methods of treating asthma are provided which methods comprise administering to a mammal in need of such treatment an effective amount of a compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 have any of the meanings given in the specification.Type: GrantFiled: August 18, 1995Date of Patent: April 22, 1997Assignee: Zeneca LimitedInventors: Cyrus J. Ohnmacht, Jr., Diane A. Trainor, Janet M. Forst, Mark M. Stein, Robert J. Harris
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Patent number: 5607953Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: November 23, 1994Date of Patent: March 4, 1997Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5565571Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difiuorophenyl]-2-oxazolid inone.Type: GrantFiled: April 28, 1994Date of Patent: October 15, 1996Assignee: The Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5563154Abstract: Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 1, 1995Date of Patent: October 8, 1996Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5561143Abstract: This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: May 22, 1995Date of Patent: October 1, 1996Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Robert A. Groneberg, John R. Regan, Kent W. Neuenschwander, Anthony C. Scotese
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Patent number: 5559248Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH.dbd.CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.c is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl and these compounds are useful in preventing and treating skin disorders.Type: GrantFiled: April 5, 1995Date of Patent: September 24, 1996Assignee: Bristol-Myers Squibb Co.Inventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
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Patent number: 5541323Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.Type: GrantFiled: January 18, 1995Date of Patent: July 30, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls