The Six-membered Hetero Ring Is Unsubstituted Or Alkyl Substituted Only Patents (Class 546/166)
  • Patent number: 6034242
    Abstract: 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: Grant
    Filed: October 2, 1998
    Date of Patent: March 7, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 6005111
    Abstract: 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: Grant
    Filed: January 30, 1998
    Date of Patent: December 21, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Masato Taniguchi, Kiyoshi Morimoto, Keizo Kimura, Kazumi Nii, Shigeo Hirano
  • Patent number: 5994546
    Abstract: 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: Grant
    Filed: February 11, 1998
    Date of Patent: November 30, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
  • Patent number: 5977125
    Abstract: 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: Grant
    Filed: May 6, 1997
    Date of Patent: November 2, 1999
    Assignee: 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
  • Patent number: 5942620
    Abstract: 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: Grant
    Filed: July 1, 1998
    Date of Patent: August 24, 1999
    Assignee: ConjuChem, Inc.
    Inventors: Alexander Krantz, Alan M. Ezrin, Yonghong Song
  • Patent number: 5908849
    Abstract: 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: Grant
    Filed: February 13, 1998
    Date of Patent: June 1, 1999
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark Hellberg, Pete Delgado, Jon C. Nixon
  • Patent number: 5856490
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: January 5, 1999
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5840733
    Abstract: 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: Grant
    Filed: July 1, 1996
    Date of Patent: November 24, 1998
    Assignee: RedCell, Canada, Inc.
    Inventors: Alexander Krantz, Alan M. Ezrin, Yonghong Song
  • Patent number: 5830897
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 3, 1998
    Assignees: G. D. Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5792761
    Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, Adel M. Naylor-Olsen, Randall W. Hungate, Joseph P. Vacca
  • Patent number: 5767129
    Abstract: 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: Grant
    Filed: August 13, 1996
    Date of Patent: June 16, 1998
    Assignee: Warner-Lambert Company
    Inventor: Po-Wai Yuen
  • Patent number: 5739134
    Abstract: 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: Grant
    Filed: April 13, 1995
    Date of Patent: April 14, 1998
    Assignee: 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
  • Patent number: 5723633
    Abstract: 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: Grant
    Filed: December 20, 1995
    Date of Patent: March 3, 1998
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
  • Patent number: 5708174
    Abstract: 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: Grant
    Filed: April 11, 1995
    Date of Patent: January 13, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
  • Patent number: 5686616
    Abstract: 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: Grant
    Filed: March 14, 1996
    Date of Patent: November 11, 1997
    Assignee: Takasago International Corporation
    Inventors: Kazuhide Tani, Tsuneaki Yamagata, Yasutaka Kataoka, Hidenori Kumobayashi
  • Patent number: 5676884
    Abstract: 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: Grant
    Filed: November 20, 1996
    Date of Patent: October 14, 1997
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: George V. Tiers, Robert J. Koshar, Louis M. Leichter
  • Patent number: 5658904
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: August 19, 1997
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5616729
    Abstract: 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: Grant
    Filed: December 27, 1988
    Date of Patent: April 1, 1997
    Assignee: Board of Governors of Wayne State University
    Inventors: Arthur P. Schaap, Hashem Akhavan-Tafti
  • Patent number: 5599819
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: February 4, 1997
    Assignee: Allergan
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5596012
    Abstract: 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: Grant
    Filed: May 24, 1995
    Date of Patent: January 21, 1997
    Assignee: 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
  • Patent number: 5561141
    Abstract: 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: Grant
    Filed: May 25, 1995
    Date of Patent: October 1, 1996
    Assignee: American Cyanamid Company
    Inventors: Dennis Powell, Rolf Paul, William A. Hallett, Dan M. Berger, Minu D. Dutia
  • Patent number: 5478845
    Abstract: 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: Grant
    Filed: May 23, 1994
    Date of Patent: December 26, 1995
    Assignee: Novo Nordisk A/S
    Inventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
  • Patent number: 5457103
    Abstract: 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: Grant
    Filed: August 18, 1993
    Date of Patent: October 10, 1995
    Assignee: Adir et Compagnie
    Inventors: Yves Rolland, Guy Lewin, Jean-Paul Vilaine, Albert Lenaers, Catherine Thollon
  • Patent number: 5420281
    Abstract: 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: Grant
    Filed: August 31, 1994
    Date of Patent: May 30, 1995
    Assignee: AGFA-Gevaert, N.V.
    Inventors: Eric Kiekens, Paul Callant, Roland Claes
  • Patent number: 5391741
    Abstract: 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: Grant
    Filed: April 23, 1993
    Date of Patent: February 21, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Ikuo Shimizu, Hiroshi Toyoda, Yukiyoshi Ito, Tsutomu Sato
  • Patent number: 5382590
    Abstract: 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: Grant
    Filed: July 8, 1992
    Date of Patent: January 17, 1995
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
  • Patent number: 5371266
    Abstract: 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: Grant
    Filed: February 18, 1994
    Date of Patent: December 6, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
  • Patent number: 5359076
    Abstract: 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: Grant
    Filed: December 9, 1992
    Date of Patent: October 25, 1994
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Katsuya Awano, Takayoshi Ishizaki, Eisuke Kojima, Shinji Kudoh, Yasuhiko Sakoe, Koji Saito
  • Patent number: 5332822
    Abstract: 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: Grant
    Filed: December 24, 1992
    Date of Patent: July 26, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventor: Raj N. Misra
  • Patent number: 5281600
    Abstract: 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: Grant
    Filed: August 14, 1992
    Date of Patent: January 25, 1994
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Eisuke Kojima, Shizuyoshi Fujimori, Katsuya Awano
  • Patent number: 5272156
    Abstract: 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: Grant
    Filed: October 28, 1992
    Date of Patent: December 21, 1993
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5246606
    Abstract: 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: Grant
    Filed: January 27, 1992
    Date of Patent: September 21, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Samuel Evans
  • Patent number: 5243051
    Abstract: 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: Grant
    Filed: June 26, 1992
    Date of Patent: September 7, 1993
    Assignee: Shionigi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
  • Patent number: 5234926
    Abstract: 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: Grant
    Filed: November 15, 1991
    Date of Patent: August 10, 1993
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5220027
    Abstract: 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: Grant
    Filed: April 12, 1991
    Date of Patent: June 15, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
  • Patent number: 5218120
    Abstract: 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: Grant
    Filed: September 16, 1991
    Date of Patent: June 8, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Ruediger Sens, Karl-Heinz Etzbach
  • Patent number: 5210200
    Abstract: 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: Grant
    Filed: November 27, 1991
    Date of Patent: May 11, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Yasuhiro Shimada, Hisashi Mikoshiba, Hideo Usui
  • Patent number: 5189188
    Abstract: 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: Grant
    Filed: October 31, 1990
    Date of Patent: February 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5183827
    Abstract: 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: Grant
    Filed: July 18, 1991
    Date of Patent: February 2, 1993
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5149817
    Abstract: 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: Grant
    Filed: February 15, 1991
    Date of Patent: September 22, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
  • Patent number: 5136054
    Abstract: 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: Grant
    Filed: April 12, 1990
    Date of Patent: August 4, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
  • Patent number: 5122611
    Abstract: 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: Grant
    Filed: August 23, 1990
    Date of Patent: June 16, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Mitsugu Tanaka, Hisashi Mikoshiba
  • Patent number: 5100904
    Abstract: 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: Grant
    Filed: June 5, 1990
    Date of Patent: March 31, 1992
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
  • Patent number: 5097034
    Abstract: 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: Grant
    Filed: May 14, 1991
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5028708
    Abstract: 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: Grant
    Filed: April 8, 1988
    Date of Patent: July 2, 1991
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
  • Patent number: 5008276
    Abstract: 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: Grant
    Filed: October 17, 1988
    Date of Patent: April 16, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 4963566
    Abstract: 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: Grant
    Filed: March 27, 1987
    Date of Patent: October 16, 1990
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Uchida, Seiji Morita, Masatoshi Chihiro
  • Patent number: 4956372
    Abstract: 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: Grant
    Filed: September 27, 1988
    Date of Patent: September 11, 1990
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Eisuke Kojima, Shizuyoshi Fujimori, Katsuya Awano
  • Patent number: 4929732
    Abstract: 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: Grant
    Filed: February 2, 1989
    Date of Patent: May 29, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans R. Meier, Samuel Evans
  • Patent number: 4922020
    Abstract: 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: Grant
    Filed: March 17, 1988
    Date of Patent: May 1, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter Gregory, Nigel Hughes