Tricyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/150)
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Patent number: 6225050Abstract: Cyanine and related dyes, such as merocyanine, styryl and oxonol dyes, are strongly light-absorbing and highly luminescent. Cyanine and related dyes having functional groups make them reactive with amine, hydroxy and sulfhydryl groups are covalently attached to proteins, nucleic acids, carbohydrates, sugars, cells and combinations thereof, and other biological and nonbiological materials, to make these materials fluorescent so that they can be detected. The labeled materials can then be used in assays employing excitation light sources and luminescence detectors. For example, fluorescent cyanine and related dyes can be attached to amine, hydroxy or sulfhydryl groups of avidin and to antibodies and to lectins. Thereupon, avidin labeled with cyanine type dyes can be used to quantify biotinvlated materials and antibodies conjugated with cyanine-type dyes can be used to detect and measure antigens and haptens. In addition, cyanine-conjugated lectins can be used to detect specific carbohydrate groups.Type: GrantFiled: November 12, 1996Date of Patent: May 1, 2001Assignee: Carnegie Mellon UniversityInventor: Alan S. Waggoner
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Patent number: 6225330Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: May 1, 2001Assignees: Synaptic Pharmaceutical Corporation, Novartis AGInventors: Mohammad R. Marzabadi, Wai C. Wong, Walter Schilling, Stewart A. Noble
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Patent number: 6207689Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.Type: GrantFiled: February 9, 2000Date of Patent: March 27, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
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Patent number: 6187801Abstract: The invention relates to polycyclic thiazole systems and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: February 10, 2000Date of Patent: February 13, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jähne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
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Patent number: 6159996Abstract: Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and a process for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: July 12, 1999Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Karl Geisen, Hans Jochen Lang
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Patent number: 6107318Abstract: A compound of Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein n is an integer between 2 and 6 and R.sub.1 is a methyl group or a group ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, methoxy, methylsulfonyl, or one of R.sub.2, R.sub.3 and R.sub.4 together with another one of the three substituents forms a --O--CH.sub.2 --O-- bridge. The asterisk marks an asymmetric carbon atom.Type: GrantFiled: December 6, 1999Date of Patent: August 22, 2000Assignee: Zambon Group S.p.A.Inventors: Felice Pocchiari, Claudio Masotto, Paolo Cavalleri, Stefania Montanari, Francesco Santangelo
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Patent number: 6090833Abstract: Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I ##STR1## wherein the radicals may have various meanings. The compounds are particularly useful as anorectics.Type: GrantFiled: September 29, 1999Date of Patent: July 18, 2000Assignee: Aventis Pharma Deutschand GmbHInventors: Gerhard Jaehne, Heiner Glombik, Karl Geisen, Martin Bickel
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Patent number: 6057318Abstract: The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N;Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene;Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.Type: GrantFiled: May 20, 1998Date of Patent: May 2, 2000Assignee: SanofiInventors: Andre Bernat, Jean-Marc Herbert, Gerard Valette
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Patent number: 5834499Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.Type: GrantFiled: August 26, 1996Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
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Patent number: 5733648Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: March 31, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5705498Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.Type: GrantFiled: May 4, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plc.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5665887Abstract: A novel methine compound is disclosed, which contains a rhodanine ring substituted with a linear or branched alkyl, alkenyl, or alkynyl group containing at least one carboxyl group and at least one ester bond, amide bond, or ether bond. The methine compound has excellent stability and dyeing power.Type: GrantFiled: August 9, 1996Date of Patent: September 9, 1997Assignee: Fuji Photo Film Co., Ltd.Inventor: Toyohisa Oya
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Patent number: 5599825Abstract: There are provided methine compounds having the following structure and their analogs, with a high solubility and are usefull as an active ingredient for pharmaceutical composition for treatment of cancer: ##STR1##Type: GrantFiled: April 12, 1995Date of Patent: February 4, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
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Patent number: 5587482Abstract: The present invention is directed to a dye suitable for spectral sensitization of a photographic element. Specifically, the dye is a compound having the structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each independently represents H; halogen; alkyl of 1-6 carbons; aryl of 6-24 carbons; alkoxy of 1-6 carbons; carbonyl; or sulfonate; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 taken together represent the atoms necessary to complete a six-membered carbocylic ring;R.sup.5 represents hydrogen, alkyl of 1-6 carbons or aryl of 6-24 carbons;R.sup.6, R.sup.7, and R.sup.8 independently represent alkyl 1-6 carbons; aryl of 6-24 carbons; or any pair of R.sup.6, R.sup.7 and R.sup.8 taken together represent a five- or six-member heterocyclic ring;X represents O, S, CH.dbd.CH, Se, Te or N--R.sup.10 ;Y represents O, S, or N--R.sup.9 ;Z represents O, S or Se;R.sup.9 represents alkyl of 1-6 carbons; or an aryl of 6-24 carbons;R.sup.Type: GrantFiled: March 7, 1996Date of Patent: December 24, 1996Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich M. Fabricius, Ralf H. Harms, James J. Welter
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Patent number: 5569766Abstract: A method for detecting a component of an aqueous liquid comprising adding to the liquid a luminescent dye selected from the group consisting of cyanine, merocyanine and styryl dyes containing at least one sulfonic acid or sulfonate group attached to an aromatic nucleus and reacting the dye with the component. The labeled component is then detected by an optical detection method.Type: GrantFiled: November 29, 1993Date of Patent: October 29, 1996Assignee: Carnegie Mellon UniversityInventors: Alan S. Waggoner, Lauren A. Ernst, Ratnakar B. Mujumdar
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Patent number: 5565479Abstract: Condensed thiazole derivatives useful as 5-HT.sub.3 receptor agonists are provided and can be represented by the following formula (I) or a pharmaceutically acceptable salt thereof, a process for the production thereof and a pharmaceutical composition thereof: ##STR1## wherein R, A, L.sub.1, L.sub.2, L, and R.sup.1 -R.sup.Type: GrantFiled: April 28, 1995Date of Patent: October 15, 1996Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Iwaoka, Hiroyuki Koshio, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
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Patent number: 5559240Abstract: A silver halide photographic light-sensitive material contains a methine compound represented by the following formula: ##STR1## wherein Y.sup.1 is a group which is clearable by a nucleophile; Z.sup.1 is --O--, --S-- or other; Z.sup.2 is --S--; A and B are each independently hydrogen, halogen, alkyl, aryl or a heterocyclic group; A and B may be linked to each other to form an unsaturated aliphatic ring or an aromatic ring; and Q.sup.1 is a methine or polymethine group which may have a heterocyclic group. A novel methine compound is also disclosed.Type: GrantFiled: December 6, 1994Date of Patent: September 24, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Ken Kawata, Tadashi Ikeda
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Patent number: 5527914Abstract: Methine compounds are described, which can be represented by general formula [Ic]: ##STR1##Type: GrantFiled: May 3, 1994Date of Patent: June 18, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Takanori Hioki, Tadashi Ikeda
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Patent number: 5519136Abstract: A radiation-sensitive compound has the general formula ##STR1## wherein A represents the ring members required to complete a 5- or 6-membered heterocyclic ring which may optionally be fused to an optionally substituted aromatic nucleus,B represents H, acryl, aroyl, heterocyclyl carbonyl or ##STR2## R represents an optionally substituted alkyl group, E and G, which may be the same or different, each represents H or CH.sub.p X.sub.3-p,J and K, which may be the same or different, each represents an aryl or heterocyclic group, which may optionally include a substitutent additional to E or G,X represents Cl or Br, andm, n and p, which may be the same or different, each represents an integer equal to 0, 1 or 2.The compound can be used to form radiation sensitive compositions for the production of radiation sensitive plates in lithographic printing plate manufacture.Type: GrantFiled: May 22, 1992Date of Patent: May 21, 1996Inventor: John R. Wade
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Patent number: 5514809Abstract: A novel silver halide photographic material is disclosed, which comprises at least one methine dye represented by the following formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2 each represents an atomic group required for the formation of a 5- or 6-membered nitrogen-containing heterocyclic nucleus; R.sub.1 represents an alkyl, aryl or heterocyclic group; R.sub.2 and R.sub.3 each represents an alkyl group, with the proviso that at least one of R.sub.2 and R.sub.3 represents an alkyl group substituted by an alkoxy or aryloxy group; L.sub.1, L.sub.2, L.sub.3, L.sub.4, L.sub.5, L.sub.6, and L.sub.7 each represents a methine group which may be substituted or unsubstituted; n.sub.1 and n.sub.2 each represents an integer 0 or 1; M represents a charge neutralizing ion; and m represents 0 or a higher number required for the neutralization of electric charge in the dye.Type: GrantFiled: August 22, 1994Date of Patent: May 7, 1996Assignee: Fuji Photo Film Co., Ltd.Inventor: Takashi Kato
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Patent number: 5486616Abstract: A method for detecting a component of an aqueous liquid comprising adding to the liquid a luminescent dye selected from the group consisting of cyanine, merocyanine and styryl dyes containing at least one sulfonic acid or sulfonate group attached to an aromatic nucleus and reacting the dye with the component. The labeled component is then detected by an optical detection method.Type: GrantFiled: November 29, 1993Date of Patent: January 23, 1996Assignee: Carnegie Mellon UniversityInventors: Alan S. Waggoner, Lauren A. Ernst, Ratnakar B. Mujumdar
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Patent number: 5480874Abstract: The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein the variables are as defined in the specification. The derivative of the invention has excellent hypolipidemic and hypoglycemic activities and little side effects and hence is useful as therapeutic and prophylactic agents for hyperlipidemic diseases and diabetes and as a therapeutic agent for cataract.Type: GrantFiled: January 12, 1995Date of Patent: January 2, 1996Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Yasuo Shoji, Yoshihiko Tsuda, Kazuhiko Tsutsumi, Yasuhide Inoue
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Patent number: 5476945Abstract: A methine compound represented by the following formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2 each represent a non-metallic atomic group necessitated for forming a five-membered or six-membered, nitrogen-containing heterocyclic ring, R.sub.1 and R.sub.2 each represent an alkyl group, X represents an inorganic anion, k represents a number necessitated for adjusting the electric charge of the molecule to zero, and n represents 0 or 1; with the proviso that when n is 1, the five-membered or six-membered, nitrogen-containing heterocyclic ring formed by Z.sub.2 is cationic, k is not zero and X represents chloride ion. The compound is useful as a spectral sensitizing dye and an antitumor agent.Type: GrantFiled: October 19, 1993Date of Patent: December 19, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Akihiko Ikegawa, Toshinao Ukai, Masayuki Kawakami
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Patent number: 5466813Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.Type: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
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Patent number: 5461162Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.Type: GrantFiled: July 27, 1994Date of Patent: October 24, 1995Assignee: Merck & Co., Inc.Inventors: Guo-Jie Ho, David J. Mathre
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Patent number: 5409835Abstract: Fluorescent, calcium-binding probe compounds having visible-light excitation and emission wavelengths, and a method of usage for these probe compounds in making wavelength-ratiometric or intensity-ratiometric measurements of calcium ion concentration in samples. The probe compounds generally relate to a heterocyclic part as bonded to a Ca.sup.2+ binding unit, namely, BAPTA, via an ethylenically unsaturated group; preferred examples of the heterocyclic group include benzothiazole, naphthothiazole, thiaflavin, indolenine, chloroindolenine, methoxybenzothiazole, and methoxyindolenine.Type: GrantFiled: December 30, 1992Date of Patent: April 25, 1995Assignee: The University of Maryland at BaltimoreInventors: Joseph R. Lakowicz, Engin U. Akkaya
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Patent number: 5329006Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.Type: GrantFiled: September 6, 1991Date of Patent: July 12, 1994Assignee: Ciba-Geigy CorporationInventors: Hans Baumann, Ian J. Fletcher
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Patent number: 5326876Abstract: A process for preparing an alkyl sulfonate derivative comprises causing a nitrogen-containing heterocyclic compound represented by the following formula (1): ##STR1## wherein X represents --O--, --S--, --NR.sup.1 --, --Se--, --Te-- or --CR.sup.2 R.sup.3 --, in which each of R.sup.1, R.sup.2 and R.sup.3 independently represents a hydrogen atom or a lower alkyl group, Y represents a hydrogen atom, a mercapto group, an arylthio group, an aralkyl group, a sulfo group, a halogen atom, an alkyl group, an alkylthio group, an alkylsulfonyloxy group or an arylsulfonyloxy group and each of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represents a hydrogen atom, an alkyl group, an aryl group, an alkoxy group which may be substituted with a sulfo group, an aryloxy group, an alkylthio group, a haloalkyl group, a halogen atom, a cyano group, a carboxy group or a sulfo group, otherwise R.sup.4 and R.sup.5, R.sup.6 and R.sup.6, R.sup.6 and R.sup.7 and R.sup.7 and R.sup.Type: GrantFiled: March 12, 1993Date of Patent: July 5, 1994Assignee: Fuji Photo Film Co., Ltd.Inventor: Ken Kawata
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Patent number: 5294709Abstract: Methine compounds represented by the following general formula (Ia) or (Ib); ##STR1## wherein CYA represents atoms having a cyanine chromogen structure, MER represents atoms having a merocyanine chromogen structure, L represents a divalent linkage group composed of an atom or atoms containing at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Het represents a group containing a 5- to 7-membered hetero ring containing at least one nitrogen atom, l.sub.1 represents 1 or 2, l.sub.2 represents 0 or 1, and l.sub.3 represents 1, 2 or 3. Methine dyes using same are also disclosed.Type: GrantFiled: January 14, 1993Date of Patent: March 15, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Toshinao Ukai, Yoshio Inagaki
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Patent number: 5250695Abstract: Disclosed are sulfonate and phosphonate salts of tetrazolium compounds whose enhanced solubility in various solvents renders them particularly suitable for use as redox indicators in dry reagent, diagnostic test systems.Type: GrantFiled: June 15, 1992Date of Patent: October 5, 1993Assignee: Miles Inc.Inventors: Joel M. Blatt, Robert P. Hatch
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Patent number: 5250517Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.Type: GrantFiled: May 4, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 5250692Abstract: A water-soluble methine compound represented by the following general formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents a non-metallic atomic group required for forming a 5-membered or 6-membered nitrogen-containing heterocyclic ring; R.sub.1 and R.sub.2, which may be the same or different, each represents an alkyl group; Q.sub.1 and Q.sub.2 each represents an atomic group required, in combination, for forming a 4-thiazolidinone ring, a 5-thiazolidinone ring, a 4-imidazolidinone ring, a 4-oxazolidinone ring, a 5-oxazolidinone ring, a 5-imidazolidinone ring or a 4-dithiolanone ring; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5, which may be the same or different, each represents a methine group; R represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group; m represents 1 or 2; i and h each represents 0 or 1; l represents 1 or 2; and j and k each represents 0, 1, 2 or 3.Type: GrantFiled: April 18, 1991Date of Patent: October 5, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Koya, Toshinao Ukai, Haruo Takei
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Patent number: 5216166Abstract: Cyanine dyes are disclosed having a nucleus of the formula: ##STR1## wherein; A and B are independently selected from the group consisting of heterocyclic ring nuclei and heterocyclic fused ring nuclei so as to complete a cyanine dye,m and n independently have values of 0, 1, 2 or 3 with the proviso that 2.ltoreq.m+n.ltoreq.4,R is selected from the group consisting of hydrogen, alkyl groups and aryl groups, each of which groups may be substituted, andQ represents those non-metallic atoms necessary to complete a nucleus selected from the group consisting of heterocyclic ring nuclei, carbocyclic ring nuclei, heterocyclic fused ring nuclei and carbocyclic fused ring nuclei.Type: GrantFiled: June 19, 1991Date of Patent: June 1, 1993Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ronald W. Burrows, Kevin P. Hall
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Patent number: 5204467Abstract: Photopolymerizable compositions containing photoinitiator systems that absorb in the visible are disclosed.Type: GrantFiled: December 20, 1991Date of Patent: April 20, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventor: William K. Smothers
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Patent number: 5189049Abstract: Compounds of formula ##STR1## in which R.sub.1 represents H, an alkyl or a substituted alkyl, R.sub.2 represents H or alkyl and R.sub.3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R.sub.2 and R.sub.3 considered together represent the group ##STR2## which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases.Use of these compounds as medicaments.No figure.Type: GrantFiled: December 5, 1990Date of Patent: February 23, 1993Assignee: SanofiInventors: Daniel Frehel, Danielle Gully, Gerard Valette, Jean-Pierre Bras
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Patent number: 5149819Abstract: Squarylium compounds having the following formula (I), ##STR1## and an optical information recording medium comprising a substrate, and a recording layer formed on the substrate, comprising a squarylium compound having formula (II) are disclosed: ##STR2##Type: GrantFiled: May 1, 1991Date of Patent: September 22, 1992Assignees: Ricoh Company, Ltd., Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Satoh, Ikuo Shimizu, Yukiyoshi Ito
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Patent number: 5137909Abstract: An indole derivative represented by the general formula (I) ##STR1## wherein R is hydrogen, lower alkyl having 1 to 6 carbons, carboxymethyl, or substituted or unsubstituted aralkyl; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 may be the same with or different from each other and are hydrogen, halogen, lower alkyl having 1 to 6 carbons, lower alkoxy having 1 to 6 carbons, acyl, substituted or unsubstituted amino, nitro, hydroxy, acyloxy, substituted or unsubstituted aralkyl, substituted or unsubstituted aryloxy, or substituted or unsubstituted aralkyloxy, or a combination of R.sup.2 and R.sup.3 may be methylenedioxy;R.sup.5 is hydrogen, lower alkyl having 1 to 6 carbons, or substituted or unsubstituted aralkyl; R and R.sup.4, or R.sup.1 and R.sup.5 may form together a six-membered ring constituted of methylene chains which may contain a heteroatom;R.sup.6 and R.sup.Type: GrantFiled: May 14, 1990Date of Patent: August 11, 1992Assignee: Kyorin Seiyaku Kabushiki KaishaInventors: Hidehiko Miura, Naoki Harano, Yasuo Takano, Toshiro Mochizuki, Yoshinori Takahashi, deceased, Takashi Nagayama
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Patent number: 4970318Abstract: Acyl derivatives of 2-aminobenzothiazole and alkylated analogs thereof as antitumor agents.Type: GrantFiled: April 12, 1989Date of Patent: November 13, 1990Assignee: Pfizer Inc.Inventors: Rodney C. Schnur, Anton F. J. Fliri
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Patent number: 4966828Abstract: Disclosed is a compound of the general formula ##STR1## wherein L=H or CO--(R.sup.1).sub.n (CX.sub.3).sub.m, M=alkylene, alkenylene, Q=S, Se, O, dialkylmethylene, alken-1,2-ylene, 1,2-phenylene or N-R, with M+Q together forming 3 or 4 ring members, R=alkyl, aralkyl or alkoxyalkyl, R.sup.1 is an aromatic group and X=Cl, Br or I, with n=O and m=1 or n=1 and m=1 or 2. The compounds, on exposure, eliminate HX and form free radicals and are therefore highly effective as acid donors and free radical initiators for photochemical processes.Type: GrantFiled: September 13, 1984Date of Patent: October 30, 1990Assignee: Hoechst AktiengesellschaftInventors: Reinhard Doenges, Hans Ruckert, Ulrich Geissler, Hartmut Steppan
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Patent number: 4946960Abstract: Perester compounds suitable for causing the polymerisation of addition polymerisable compounds on exposure to radiation have the general formulae ##STR1##Type: GrantFiled: October 9, 1987Date of Patent: August 7, 1990Assignee: Vickers PLCInventors: John R. Wade, Rodney M. Potts, Michael J. Pratt
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Patent number: 4946955Abstract: A method for preparation of polycyclic 1,3-thiazolidines is described. The method comprises reacting a fluoride ion source, in a solvent, with an onium salt synthesized by the reaction of a nitrogenous heteroaromatic compound with a halomethyl trimethylsilylmethyl sulfide, the halomethyl trimethylsilylmethyl sulfide being selected from the group consisting of chloromethyl trimethylsilylmethyl sulfide, bromomethyl trimethylsilylmethyl sulfide, or iodomethyl trimethylsilylmethyl sulfide.Type: GrantFiled: September 9, 1988Date of Patent: August 7, 1990Assignee: Toray Silicone Company LimitedInventor: Akira Hosomi
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Patent number: 4929623Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.Type: GrantFiled: June 16, 1988Date of Patent: May 29, 1990Assignee: Eisai Co., Ltd.Inventors: Shinya Abe, Mitsuaki Miyamoto, Masayuki Tanaka, Kozo Akasaka, Kenji Hayashi, Tetsuya Kawahara, Satoshi Katayama, Yoshinori Sakuma, Takeshi Suzuki, Isao Yamatsu
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Patent number: 4877876Abstract: This invention provides an indenothiazole derivative and a process for manufacturing the same. The said indenothiazole derivative is represented by the following formula: ##STR1## wherein X and Y are identical with, or different from, each other and are each a hydrogen atom, halogen atom, low alkyl group or low alkoxy group; n is an integer of from 0 to 4; R.sub.1 is a hydrogen atom, low alkyl group, unsubstituted or substituted phenyl group; R.sub.2 is a low alkyl group, cycloalkyl group, low alkoxyl group, unsubstituted or substituted phenoxy group, unsubstituted or substituted phenyl group, alkenyl group, heterocyclic group or cycloamino group; R.sub.3 is a hydrogen atom, low alkyl group or acyl group; and R.sub.2 and R.sub.3 may be combined to form a cycloamino group. Further, this invention also provides a tautomer of the compound represented by the above formula (Ia), wherein all the symbols are as defined above except that R.sub.3 is limited to a hydrogen atom.Type: GrantFiled: August 31, 1987Date of Patent: October 31, 1989Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Masayoshi Tsuji, Akira Nakagawa, Hisataka Inoue, Terumi Hachiya, Yoshihiro Tanoue, Kouichi Ikesue, Masaru Saita, Takenobu Mizoguchi, Testsuo Aoki, Hironobu Sato, Kanji Nodo
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Patent number: 4874866Abstract: Compounds containing an aromatic ring portion fused with a tellurazolium or derivative tellurazole, tellurazoline (including tellurazolinylidene), or tellurazolinium ring portion are disclosed together with processes and intermediates for their preparation. With properly selected pendant groups these tellurazolium and derivatives compounds can be usefully employed as dyes, antifoggants or stabilizers, nucleating agents, latent image keeping addenda, or speed or contrast altering addenda in silver halide photographic systems.Type: GrantFiled: October 3, 1985Date of Patent: October 17, 1989Assignee: Eastman Kodak CompanyInventors: Wolfgang H. H. Gunther, Ronald E. Leone, Rosemary Przyklek
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Patent number: 4732984Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --O--, --NH--, ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.7 is 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl or phenyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, trifluoromethyl, cyano, nitro or halo, with the proviso that when R.sup.1 and R.sup.2 taken together represent ##STR3## then R.sup.7 is other than 2-pyridinyl, 2-pyrimidinyl or substituted pyrimidin-2-yl;Z is --(CH.sub.2).sub.Type: GrantFiled: August 5, 1986Date of Patent: March 22, 1988Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Scott J. Childress
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Patent number: 4727154Abstract: Process for the preparation of benzothiazoles of the formula (1) ##STR1## wherein R denotes an alkyl.sub.C.sbsb.1.sub.-C.sbsb.6 or an a kenyl.sub.C.sbsb.2.sub.-C.sbsb.6 group which can be substituted by alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, acyl, phenyl, chlorophenyl, bromophenyl, alkyl.sub.C.sbsb.1.sub.-C.sbsb.4 phenyl, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4 -phenyl or nitrophenyl groups or halogen atoms, or denotes a phenyl group which can be substituted by alkyl.sub.C.sbsb.1.sub.-C.sbsb.4, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, carboxyl-, --COO-alkyl.sub.C.sbsb.1.sub.-C.sub.4, cyano or nitro or halogen atoms, and X and Y each denote a hydrogen or halogen atom or an alkyl.sub.C.sbsb.1.sub.-C.sbsb.4, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.Type: GrantFiled: July 31, 1986Date of Patent: February 23, 1988Assignee: Hoechst AktiengesellschaftInventor: Theodor Papenfuhs
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Patent number: 4609738Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atom, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6-membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.Type: GrantFiled: September 30, 1982Date of Patent: September 2, 1986Assignee: Ciba-Geigy CorporationInventor: Peter Mockli
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Patent number: 4599410Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.Type: GrantFiled: February 19, 1985Date of Patent: July 8, 1986Assignee: Eastman Kodak CompanyInventor: Wolfgang H. H. Gunther
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Patent number: RE37094Abstract: Compounds of formula in which R1 represents H, an alkyl or a substituted alkyl, R2 represents H or alkyl and R3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R2 and R3 considered together represent the group which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases. Use of these compounds as medicaments. No figure.Type: GrantFiled: September 11, 1995Date of Patent: March 13, 2001Assignee: SanofiInventors: Daniel Fréhel, Danielle Gully, Gérard Valette, Jean-Pierre Bras