The Six-membered Hetero Ring Is Unsubstituted Or Alkyl Substituted Only Patents (Class 546/166)
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Patent number: 6034242Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CO.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.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.Type: GrantFiled: October 2, 1998Date of Patent: March 7, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 6005111Abstract: A method for forming a color image comprises the step of developing an image-wise exposed silver halide color photographic photosensitive material at the presence of a 6-aminotetrahydroquinoline color developing agent which is the following compound or its analoge. According to this method, the rapid process can be attained and an image of a low fog density can be obtained.Type: GrantFiled: January 30, 1998Date of Patent: December 21, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Masato Taniguchi, Kiyoshi Morimoto, Keizo Kimura, Kazumi Nii, Shigeo Hirano
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Patent number: 5994546Abstract: Disclosed are 4-(N,N-dialkylamino)aniline compounds having a 4-N substituent which is a polyethyleneoxy group and which forms a condensed ring with benzene ring, such as aniline compounds having the following structure, a processing composition containing such a compound and a method for forming a color image with the processing solution. The aniline compound is useful as a color developing agent capable of having a low fog density and sufficient yellow and cyan image densities and suitable for the rapid process.Type: GrantFiled: February 11, 1998Date of Patent: November 30, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
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Patent number: 5977125Abstract: Compounds of the formula ##STR1## and compounds of the formula ##STR2## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.Type: GrantFiled: May 6, 1997Date of Patent: November 2, 1999Assignee: Eisai Co., Ltd.Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
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Patent number: 5942620Abstract: Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.Type: GrantFiled: July 1, 1998Date of Patent: August 24, 1999Assignee: ConjuChem, Inc.Inventors: Alexander Krantz, Alan M. Ezrin, Yonghong Song
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Patent number: 5908849Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.Type: GrantFiled: February 13, 1998Date of Patent: June 1, 1999Assignee: Alcon Laboratories, Inc.Inventors: Mark Hellberg, Pete Delgado, Jon C. Nixon
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Patent number: 5856490Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: January 5, 1999Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5840733Abstract: Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.Type: GrantFiled: July 1, 1996Date of Patent: November 24, 1998Assignee: RedCell, Canada, Inc.Inventors: Alexander Krantz, Alan M. Ezrin, Yonghong Song
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Patent number: 5830897Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: November 3, 1998Assignees: G. D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5792761Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##Type: GrantFiled: August 8, 1997Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Adel M. Naylor-Olsen, Randall W. Hungate, Joseph P. Vacca
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Patent number: 5767129Abstract: The present invention relates to novel substituted quinolines and isoquinolines and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also included. The compounds are useful in treating pain, cerebral ischemia, and other cerebrovascular disorders.Type: GrantFiled: August 13, 1996Date of Patent: June 16, 1998Assignee: Warner-Lambert CompanyInventor: Po-Wai Yuen
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Patent number: 5739134Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: April 14, 1998Assignee: Janssen Pharmacetuica N.V.Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
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Patent number: 5723633Abstract: A pyran derivative has a structure ofR.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle.A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer.Type: GrantFiled: December 20, 1995Date of Patent: March 3, 1998Assignee: Canon Kabushiki KaishaInventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
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Patent number: 5708174Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.Type: GrantFiled: April 11, 1995Date of Patent: January 13, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
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Patent number: 5686616Abstract: A novel process for preparing an optically active amine by asymmetric hydrogenation of an imine compound, such as an imine compound prepared by condensing benzylamine and acetophenone, in the presence of a catalytic amount of an iridium-optically active phosphine complex and benzylamine or a benzylamine derivative. The present invention provides an optically active amine of high optical purity.Type: GrantFiled: March 14, 1996Date of Patent: November 11, 1997Assignee: Takasago International CorporationInventors: Kazuhide Tani, Tsuneaki Yamagata, Yasutaka Kataoka, Hidenori Kumobayashi
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Patent number: 5676884Abstract: Nonlinear optical (NLO) compositions are disclosed which contain polar disulfone-functionalized molecules (PDFMs) incorporated in a polymeric material. when aligned noncentrosymmetrically in the polymeric material, the PDFMs generate a second-order NLO response. There is also disclosed: a method of preparing a NLO composition; novel PDFMs and novel polymers; and a new process for preparing PDFMs.Type: GrantFiled: November 20, 1996Date of Patent: October 14, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: George V. Tiers, Robert J. Koshar, Louis M. Leichter
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5658904Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: June 6, 1995Date of Patent: August 19, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5616729Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.Type: GrantFiled: December 27, 1988Date of Patent: April 1, 1997Assignee: Board of Governors of Wayne State UniversityInventors: Arthur P. Schaap, Hashem Akhavan-Tafti
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Patent number: 5599819Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is thienyl, furyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 2, 1995Date of Patent: February 4, 1997Assignee: AllerganInventor: Roshantha A. S. Chandraratna
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Patent number: 5596012Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO--or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.Type: GrantFiled: May 24, 1995Date of Patent: January 21, 1997Assignee: Sterling winthrop Inc.Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Chakrapani Subramanyam, Lee H. Latimer, Eric P. Lodge
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Patent number: 5561141Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.Type: GrantFiled: May 25, 1995Date of Patent: October 1, 1996Assignee: American Cyanamid CompanyInventors: Dennis Powell, Rolf Paul, William A. Hallett, Dan M. Berger, Minu D. Dutia
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Patent number: 5478845Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.Type: GrantFiled: May 23, 1994Date of Patent: December 26, 1995Assignee: Novo Nordisk A/SInventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
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Patent number: 5457103Abstract: Compounds of the general formula (I): ##STR1## in which R represents: a hydrogen atom, ora radical --OR'in which R' is as defined in the description.Type: GrantFiled: August 18, 1993Date of Patent: October 10, 1995Assignee: Adir et CompagnieInventors: Yves Rolland, Guy Lewin, Jean-Paul Vilaine, Albert Lenaers, Catherine Thollon
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Patent number: 5420281Abstract: A photographic material is disclosed comprising a support, at least one silver halide emulsion layer, and optionally one or more non-photosensitive hydrophylic layer(s), characterized in that at least one of said emulsion layer(s) and/or non-photosensitive layer(s) contains a triphenylmethane dye, absorbing around 670 nm, represented by general formula (ID) : ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen unsubstituted or substituted alkyl, or unsubstituted or substituted aryl,R.sup.3 represents an electron-withdrawing group, and the substance contains at least two water-solubilizing groups,and X.sup.- represents an anion, or an intramolecular anionic group.The triphenylmethane dyes can serve as filter dye, acutance dye, or anti-halation dye. The claimed photographic materials are especially suited for exposure by a laser diode emitting at 670 nm.Type: GrantFiled: August 31, 1994Date of Patent: May 30, 1995Assignee: AGFA-Gevaert, N.V.Inventors: Eric Kiekens, Paul Callant, Roland Claes
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Patent number: 5391741Abstract: There are described a novel squarylium compound represented by the formula (I): ##STR1## and an optical information recording medium using the squarylium compound in the recording layer.Type: GrantFiled: April 23, 1993Date of Patent: February 21, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Ikuo Shimizu, Hiroshi Toyoda, Yukiyoshi Ito, Tsutomu Sato
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Patent number: 5382590Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.Type: GrantFiled: July 8, 1992Date of Patent: January 17, 1995Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5371266Abstract: Methine transfer dyes have the formula ##STR1## where L is a bridge member which does not permit any conjugation of .pi.-electrons between Z and Y,X is cyano, C.sub.1 -C.sub.6 -alkoxycarbonyl or C.sub.1 -C.sub.6 -monoalkylcarbamoyl, wherein alkyl may in each case be interrupted by oxygen atoms, or is C.sub.5 -C.sub.7 -cycloalkoxycarbonyl, C.sub.5 -C.sub.7 -monocycloalkylcarbamoyl, phenoxycarbonyl or monophenylcarbamoyl, andY and Z are each independently of the other aminophenylene, which may be benzo-fused, or heterocyclyl.Type: GrantFiled: February 18, 1994Date of Patent: December 6, 1994Assignee: BASF AktiengesellschaftInventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
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Patent number: 5359076Abstract: The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) ##STR1## wherein R and R.sup.1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R.sup.Type: GrantFiled: December 9, 1992Date of Patent: October 25, 1994Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasushi Kohno, Katsuya Awano, Takayoshi Ishizaki, Eisuke Kojima, Shinji Kudoh, Yasuhiko Sakoe, Koji Saito
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Patent number: 5332822Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein X is S or --CH.sub.2 --; m is 0, 1 or 2 when X is --S-- or m is 0 when X is --CH.sub.2 --; n is 1, 2 or 3; R.sup.1 and R.sup.2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 5- to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R.sup.3 is heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 24, 1992Date of Patent: July 26, 1994Assignee: Bristol-Myers Squibb CompanyInventor: Raj N. Misra
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Patent number: 5281600Abstract: An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, halogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.Type: GrantFiled: August 14, 1992Date of Patent: January 25, 1994Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Eisuke Kojima, Shizuyoshi Fujimori, Katsuya Awano
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Patent number: 5272156Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or aketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 were m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 28, 1992Date of Patent: December 21, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5246606Abstract: Novel substituted tetrahydroquinoline compounds of the formula I ##STR1## are described, in which R.sub.1 is C.sub.1-18 alkyl or together with R.sub.8 1,4-butylene, R.sub.2 and R.sub.3, independently of one another, are C.sub.1-18 alkyl, phenyl or phenyl-C.sub.1-4 alkyl or together tetra-, penta- or hexamethylene, R.sub.4 is hydrogen, halogen, nitro, C.sub.1-24 alkyl or a group of the formula --O--R.sub.5, R.sub.5 is hydrogen, C.sub.1-18 alkyl or benzyl, R.sub.6 and R.sub.7, independently of one another, are hydrogen, C.sub.1-18 alkyl, C.sub.2-18 alkyl which is interrupted by --S-- or --O--, or are phenyl or phenyl-C.sub.1-4 alkyl or together C.sub.4-11 alkylene, R.sub.8 is hydrogen, C.sub.1-18 alkyl or together with R.sub.1 1,4-butylene, and n is 1,2 or 3. The compounds are suitable as stabilisers, in particular as antioxidants for organic materials.Type: GrantFiled: January 27, 1992Date of Patent: September 21, 1993Assignee: Ciba-Geigy CorporationInventor: Samuel Evans
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Patent number: 5243051Abstract: The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.Type: GrantFiled: June 26, 1992Date of Patent: September 7, 1993Assignee: Shionigi & Co., Ltd.Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
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Patent number: 5234926Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-2; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 15, 1991Date of Patent: August 10, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5220027Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## wherein X represents ##STR2## R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group, an alkoxyl group, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group, ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom or an alkyl group which may be substituted by a hydroxyl group; R.sub.7 represents a hydrogen atom, an alkyl group, an alkyoxyl group, a hydroxyl group, a halogen atom, a nitro group, a cyano group, ##STR4## wherein -A represents ##STR5## and R and R' represent independently a hydrogen atom or an alkyl group; and R.sub.10 to R.sub.12 represent independently a hydrogen atom or an alkyl group, a process for producing such compounds, and a medium for recording optical information using these compounds.Type: GrantFiled: April 12, 1991Date of Patent: June 15, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5218120Abstract: Quinolinemethine dyes suitable for use in a thermal transfer process have the formula ##STR1## where R.sup.1 is fluorine, chlorine or bromine,R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.3 is hydrogen, fluorine, chlorine or bromine, andK is the radical of an aniline derivative.Type: GrantFiled: September 16, 1991Date of Patent: June 8, 1993Assignee: BASF AktiengesellschaftInventors: Ruediger Sens, Karl-Heinz Etzbach
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Patent number: 5210200Abstract: A dye compound of a general formula (I): ##STR1##where R.sub.1 represents a hydrogen atom, or a substituent; R.sub.2 and R.sub.3 independently represent a substituent; X represents a nitrogen atom or --C(R.sub.5).dbd.; R.sub.5 represents a substituent; and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group as bonded to the nitrogen atom in the formula via an unsaturated carbon atom, which dye compound is fast to heat and light and is useful for color image formation and as a filter dye; and a thermal transfer dye donating material having a dye donating layer containing a thermal transferring dye on a support, where the thermal transferring dye is represented by: ##STR2##where X.sup.2 represents --N.dbd., or --C(R.sup.22).dbd.; R.sup.21, R.sup.22, R.sup.23 and R.sup.24 independently represent a hydrogen atom, or a non-metallic substituent; R.sup.25, R.sup.26, R.sup.27 and R.sup.Type: GrantFiled: November 27, 1991Date of Patent: May 11, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Yasuhiro Shimada, Hisashi Mikoshiba, Hideo Usui
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Patent number: 5189188Abstract: Compounds of the general formula ##STR1## in which the symbols have the meaning given in the description, are highly suitable as color formers in recording materials based on acid developers. They give deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness.Type: GrantFiled: October 31, 1990Date of Patent: February 23, 1993Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5183827Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 18, 1991Date of Patent: February 2, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5149817Abstract: The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.Type: GrantFiled: February 15, 1991Date of Patent: September 22, 1992Assignee: Shionogi & Co., Ltd.Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
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Patent number: 5136054Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.Type: GrantFiled: April 12, 1990Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5122611Abstract: A method for producing an azomethine or indoaniline series dye, which comprises oxidatively condensing an active methylene- or methine-containing compound, except those containing a sulfonic or carboxylic acid group, and p-phenylenediamine, except those containing a sulfonic or carboxylic acid group, in the presence of methylene chloride as a solvent under a basic condition.Type: GrantFiled: August 23, 1990Date of Patent: June 16, 1992Assignee: Fuji Photo Film Co., Ltd.Inventors: Mitsugu Tanaka, Hisashi Mikoshiba
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Patent number: 5100904Abstract: A novel prolinal derivatives of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.Type: GrantFiled: June 5, 1990Date of Patent: March 31, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5097034Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.Type: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5028708Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.Type: GrantFiled: April 8, 1988Date of Patent: July 2, 1991Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 4963566Abstract: A hydroquinoline compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, A, l, m and n are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing same are disclosed. The compound is useful as an antiulcer agent.Type: GrantFiled: March 27, 1987Date of Patent: October 16, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru Uchida, Seiji Morita, Masatoshi Chihiro
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Patent number: 4956372Abstract: An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.Type: GrantFiled: September 27, 1988Date of Patent: September 11, 1990Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Eisuke Kojima, Shizuyoshi Fujimori, Katsuya Awano
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Patent number: 4929732Abstract: Compounds useful as additives for lubricants, hydraulic oils and metal-working fluids include those of formula IV ##STR1## where R.sup.1 and R.sup.2 are independently alkyl or substituted aryl, R.sup.3 and R.sup.13 are independently hydrogen or methyl, R.sup.6 is alkyl, alkenyl, aralkyl or substituted benzyl, and R.sup.15 and R.sup.16 are independently hydrogen, alkyl, aryl or aralkyl.Type: GrantFiled: February 2, 1989Date of Patent: May 29, 1990Assignee: Ciba-Geigy CorporationInventors: Hans R. Meier, Samuel Evans
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Patent number: 4922020Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## B is a group of the formula: ##STR3## when B is of Formula III, X is of Formula III;when B is of Formula IV,X is selected from H, phenyl, substituted phenyl, naphthyl, substituted naphthyl, thienyl, substituted thienyl, thiazol-5-yl and substituted thiazol-5-yl in which the substituents are selected from NR.sup.7 R.sup.8, NO.sub.2, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyl, halogen, cyano and phenyl;each Q is independently selected from H, C.sub.1-4 -alkyl, phenyl and benzyl;and wherein each benzene ring in Formulae II, III and IV has no further substituents or carries 1 or 2 further substituents selected from halogen, C.sub.1-4 -alkyl and C.sub.1-4 -alkoxy.The compound is suitable for use as a charge transport material in organic photoconductors, as a charge control agent in electroreprographic toners and as a color former in pressure sensitive recording materials.Type: GrantFiled: March 17, 1988Date of Patent: May 1, 1990Assignee: Imperial Chemical Industries PLCInventors: Peter Gregory, Nigel Hughes