Phenoxazines (including Hydrogenated) Patents (Class 544/102)
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Patent number: 5654298Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.Type: GrantFiled: April 16, 1991Date of Patent: August 5, 1997Assignee: Imperial Chemical IndustriesInventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
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Patent number: 5631371Abstract: The present invention involves a method for the preparation of substituted 3-(phenylimino)-3 H-phenothiazines or phenoxazines which method involves reacting phenothiazine or phenoxazine with an aromatic amine in the presence of periodic acid as coupling agent.Type: GrantFiled: November 22, 1995Date of Patent: May 20, 1997Assignee: Bayer CorporationInventor: Michael L. Bloczynski
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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: 5519134Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.Type: GrantFiled: January 11, 1994Date of Patent: May 21, 1996Assignee: Isis Pharmaceuticals, Inc.Inventors: Oscar L. Acevedo, Normand Hebert
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Patent number: 5504211Abstract: A polyalky-piperidinyl-containing .beta.-aminoacrylic ester derivative represented by the formula I ##STR1## is useful in stabilizing plastic and paints against light, oxygen and heat.Type: GrantFiled: May 31, 1994Date of Patent: April 2, 1996Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Alfred Krause, Hubert Trauth
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Patent number: 5502177Abstract: A compound having the structure: ##STR1## wherein R.sup.1 is an oligonucleotide;a is 1 and b is 0;A is C or CH;X is S, O, NH or NCH.sub.2 R.sup.6 ;Z is taken together with A to form an aryl ring structure comprising 6 ring atoms wherein the aryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R.sup.6 or .dbd.O;R.sup.6 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, NO.sub.2, N(R.sup.3).sub.2, C.tbd.N or halo, or an R.sup.6 is taken together with an adjacent Z group R.sup.6 to complete a phenyl ring; andR.sup.3 is a protecting group or H; and tautomers, solvates and salts thereof.Type: GrantFiled: September 17, 1993Date of Patent: March 26, 1996Assignee: Gilead Sciences, Inc.Inventors: Mark D. Matteucci, Robert J. Jones, Kuei-Ying Lin
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Patent number: 5498542Abstract: Disclosed is an electrode suitable for the electrochemical regeneration of the co-enzymes NADH and NADPH. The electrode has imparted on its surface a mediator function which is a 3-methylene-3H-phenothiazine or a 3-methylene-3H-phenoxazine compound.Type: GrantFiled: September 29, 1994Date of Patent: March 12, 1996Assignee: Bayer CorporationInventors: Paul F. Corey, Matthew K. Musho
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Patent number: 5451337Abstract: Dye transfer inhibiting systems are disclosed, comprising an enzyme exhibiting peroxidase activity, a hydrogen peroxide source, an additional oxidizable substrate, and a accelerator preferably having the formula ##STR1## wherein X is S or O and R.sub.1 is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or --CH.sub.2 CH.sub.2 COOHDetergent compositions containing the dye transfer inhibition system and typical detergent ingredients are also disclosed. More effective and efficient dye transer inhibition of fugitive dyes is achieved by using the dye transfer inhibition system as an detergent additive or in a detergent composition matrix.Type: GrantFiled: May 31, 1994Date of Patent: September 19, 1995Assignee: The Procter & Gamble Co.Inventors: Don K. K. Liu, Andre C. Convents
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Patent number: 5371081Abstract: Disclosed are compounds useful in potentiating the cytotoxic effect of chemotherapeutic agents, the compounds having the formula: ##STR1## and pharmacologically acceptable salts thereof, wherein R is --H or --[C(O)].sub.a --(CH.sub.2).sub.b --A, a is 0-1 and b is 0-6 provided that a and b are not both zero; and A is selected from the group consisting of--NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms, and either or both of R.sub.1 and R.sub.2 are optionally substituted with --OH; ##STR2## wherein X and Y are independently alkylene having 1 to 4 carbon atoms, and Z is --O--, --N(R.sub.3)--, or --CH(R.sub.4)--, wherein R.sub.3 and R.sub.4 are each hydrogen or alkyl having 1 to 4 carbon atoms optionally substituted with a hydroxyl group;halide; and trihalomethyl.Type: GrantFiled: September 24, 1993Date of Patent: December 6, 1994Assignee: St. Jude Children's Research HospitalInventors: Peter J. Houghton, Julie K. Horton, Kuntebommanahalli N. Thimmaiah
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Patent number: 5364854Abstract: Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.Type: GrantFiled: June 3, 1993Date of Patent: November 15, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Franco Heidempergher, Claudio Arrigoni, Carla Caccia
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Patent number: 5319074Abstract: A metal-free dyestuff of the formula ##STR1## and metal complex thereof wherein: Fb=the radical of a dyestuff selected from the group consisting of mono- or polyazo, anthraquinone, phthalocyanine, formazan, dioxazine and triphenylmethane radicals,B and B'=a direct bond or an aliphatic or aromatic bridge member to a ring C atom of an aromatic-carbocyclic ring or to a ring C or N atom or an aromatic-heterocyclic ring in Fb,X=CH.dbd.CH.sub.2 or CH.sub.2 CH.sub.2 --Y, whereinY=OSO.sub.3 H, SSO.sub.3 H, OCOCH.sub.3, OPO.sub.3 H.sub.2, OSO.sub.2 CH.sub.3, SCN, NHSO.sub.2 CH.sub.3 --, Cl, Br, F, OCOC.sub.6 H.sub.5, OSO.sub.2 --C.sub.6 H.sub.4 CH.sub.3, ##STR2## R=H or C.sub.1 -C.sub.4 -alkyl, which is optionally be substituted by halogen, hydroxy, cyano, C.sub.1 -C.sub.4 -alkoxy, carboxyl, sulpho or sulphato,Z=a fiber-reactive radical of the formula ##STR3## wherein M=H, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -thioalkyl, F or CF.sub.Type: GrantFiled: January 24, 1992Date of Patent: June 7, 1994Assignee: Bayer AktiengesellschaftInventors: Wolfram Reddig, Karl-Josef Herd, Ernst Kysela
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Patent number: 5308766Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.Type: GrantFiled: June 10, 1991Date of Patent: May 3, 1994Assignee: The Regents of the University of CaliforniaInventors: Edward A. Dennis, William N. Washburn
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Patent number: 5304645Abstract: The present invention provides resorufin derivatives of the general formulae: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which can be the same or different, are hydrogen, halogen, carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups or lower alkyl or lower alkoxy radicals, which can be substituted by carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups, and wherein R.sup.4 and R.sup.5 can together also represent an anellated aromatic residue, Z is a bridge member, A is the residue of a ligand and n is a whole number of from 1 to 200.The present invention also provides processes for the preparation of these resorufin derivatives, as well as intermediates for the preparation thereof.Type: GrantFiled: March 28, 1991Date of Patent: April 19, 1994Assignee: Boehringer Mannheim GmbHInventors: Christian Klein, Hans-Georg Batz, Rupert Herrmann
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Patent number: 5242805Abstract: The claimed invention relates to a substrate for evaluating glycosidic enzymes comprising a resorufin derivative of the general formula: ##STR1## wherein Gly is a carbohydrate bonded to resorufin by a glycosidic linkage; where at least one of substituents R.sub.1, R.sub.2, R.sub.4, R.sub.6, R.sub.8, and R.sub.9 is a lipophilic residue of the formula --L(CH.sub.2).sub.n CH.sub.3, where n is greater than 3 and less than 22, and where L is a methylene --CH.sub.2 --, an amide --NHCO--, a sulfonamide --NHSO.sub.2 --, a carboxamide --CONH--, a carboxylate ester --COO--, a urethane --NHCOO--, a urea --NHCONH--, or a thiourea --NHCSNH--; andwhere the remainder of substituents R.sub.1, R.sub.2, R.sub.4, R.sub.6, R.sub.8, and R.sub.9, which may be the same or different, are hydrogen, halogen, or other lipophilic residues, which may be the same or different, containing from about 1 to about 22 carbon atoms of the formula --L'(CH.sub.2).sub.m CH.sub.3, where m is less than 22, and where L' is a methylene --CH.sub.Type: GrantFiled: August 23, 1991Date of Patent: September 7, 1993Assignee: Molecular Probes, Inc.Inventors: John J. Naleway, Yu-zhong Zhang, Richard P. Haugland
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5208332Abstract: An optical probe enables the study of enzyme activity by absorbance spectroscopy or by sensitive fluorescence methods. In particular, the probe provides the ability to monitor the activity of cytochrome P-450.sub.scc enzyme, the rate limiting enzyme for steroid biosynthesis. Located on the inner mitochondrial membrane, P-450.sub.scc catalyzes the conversion of cholesterol to pregnenolone and isocapraldehyde by sequential oxidations of the cholesterol side chain. The fluorogenic probe includes a cholesterol-like steroid linked to a chromophore through a linking group. The chromophore is selected to have little optical response when linked to the steroid substrate and an enhanced optical response when cleaved from the substrate and linking group. Thus, a fluorescent anion that can be optically detected is generated by the side-chain cleavage reaction during steroidogenesis.Type: GrantFiled: December 20, 1991Date of Patent: May 4, 1993Assignee: The United States of America as represented by the United States Department of EnergyInventors: Babetta L. Marrone, Daniel J. Simpson, Clifford J. Unkefer, Thomas W. Whaley
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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: 5091527Abstract: The present invention provides phospholipase substrates of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R is a hydrgen atom or an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety, X is the residue of an aromatic hydroxy or thiol compound and each Y, independently of one another, is an oxygen or sulphur atom and Z is --SO.sub.3.sup..crclbar. or a radical of the general formula: ##STR2## wherein R.sup.1 can be a hydrogen atom or a radical of the general formula --(CH.sub.2).sub.n NR.sub.3.sup.2, in which n is 2, 3 or 4 and R.sup.2 is a hydrogen atom or a methyl radical, or is an inositol or serine (--CH.sub.2 --CH(NH.sub.2)--COOH) or glycerol residue.The present invention also provides a process for the optical determination of phospholipases using these substrates, as well as a reagent containing them.Type: GrantFiled: March 2, 1989Date of Patent: February 25, 1992Assignee: Boehringer Mannheim GmbHInventors: Martina Junius, Ulrich Neumann, Herbert von der Eltz
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Patent number: 5084459Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.Type: GrantFiled: October 25, 1989Date of Patent: January 28, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi, Noriko Higuchi
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Patent number: 5082938Abstract: Enhanced branched chain hydroxyl compounds are provided of formulaY--(Z).sub.1-6wherein Y is the residue of a nucleophile devoid of conjugated divalent linking moieties, and each Z is a poly(oxyalkylene) moiety having a molecular weight of from about 200-10,000 and containing at least one glycidol residue, wherein at least one of the primary oxy sites of said glycidol residue is linked preferably directly to a first epoxide residue of three or more carbons, and wherein said first epoxide residue is linked through a secondary oxy site preferably directly to a second epoxide reside having a primary terminal hydroxyl.Type: GrantFiled: March 1, 1990Date of Patent: January 21, 1992Assignee: Milliken Research CorporationInventors: Edward W. Kluger, David J. Moody
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Patent number: 5073634Abstract: Basic dyes of the formulaChr.sup..sym.[FeCl.sub.4 ].sup..crclbar.where Chr.sup.a is a dye cation are useful for dyeing acrylonitrile polymers or acid-modified polyesters.Type: GrantFiled: May 1, 1990Date of Patent: December 17, 1991Assignee: BASF AktiengesellschaftInventors: Johannes P. Dix, Guenter Hansen, Hellmut Kast
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Patent number: 5030721Abstract: Novel N-acetyl-.beta.-D-glucosamine derivatives represented by the following formula: ##STR1## wherein R represents a hydrogen atom or an acyl group; and X represents a nitrogen atom or an oxide of nitrogen, are disclosed. The glucosamine derivatives are useful for determination of N-acetyl-.beta.-D-glucosaminidase in body fluids as an index of renal diseases.Type: GrantFiled: February 2, 1989Date of Patent: July 9, 1991Assignee: Kikkoman CorporationInventors: Kouichi Kasai, Shoichi Tokutake, Nobuyuki Yamaji
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Patent number: 5026848Abstract: A heteroaryloxyalkylheterocyclic derivative of the Formula I:R--(CH.sub.2).sub.n --O--R.sup.1 Iis provided wherein:R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a non-fused or fused substituted azole, azine, furyl or polycyclic hydrocarbon.Type: GrantFiled: March 27, 1989Date of Patent: June 25, 1991Assignee: Synphar Laboratories IncorporatedInventors: Mohsen Daneshtalab, Dai Q. Nguyen, Chan M. Ha, Hiep T. Luu, Laurence M. Tempest, Ronald G. Micetich
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Patent number: 4990625Abstract: A process for synthesizing an N,N-disubstituted hydrazone comprises carrying out nitrozation by adding an aqueous solution of sodium nitrite to a solution having one part by weight of an N,N-disubstituted amine dissolved in 3 to 30 parts by weight of an organic acid, then reducing the nitrozated product to an N,N-disubstituted hydrazine by adding a reducing agent to the mixture containing the nitrozated product, and thereafter adding to the mixture containing the N,N-disubstituted hydrazine a carbonyl compound of the formula: ##STR1## wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group which may have a substituent, B represents a hydrogen atom, an alkyl group, an aryl group or an aromatic heterocyclic group, which may have a substituent, thereby performing condensation of the N,N-disubstituted hydrazine with the carbonyl compound.Type: GrantFiled: December 5, 1989Date of Patent: February 5, 1991Assignee: Canon Kabushiki KaishaInventors: Tetsuo Arita, Minoru Mabuchi, Shoji Umehara, Kiyoshi Sakai
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Patent number: 4954630Abstract: The present invention provides resorufin derivatives of the general formulae: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which can be the same or different, are hydrogen, halogen, carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups or lower alkyl or lower alkoxy radicals, which can be substituted by carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups, and wherein R.sup.4 and R.sup.5 can together also represent an anellated aromatic residue, Z is a bridge member, A is the residue of a ligand and n is a whole number of from 1 to 200.The present invention also provides processes for the preparation of these resorufin derivatives, as well as intermediates for the preparation thereof.Type: GrantFiled: July 24, 1986Date of Patent: September 4, 1990Assignee: Boehringer Mannheim GmbHInventors: Christian Klein, Hans-Georg Batz, Rupert Herrmann
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Patent number: 4952707Abstract: Chemiluminescent 1,2-dioxetane compounds are disclosed in which the molecule is stabilized at the 3-position on the dioxetane ring against decomposition prior to the molecule's coming in contact with a labile group-removing substance (e.g., an enzyme that will cleave the labile group to cause the molecule to decompose to form at least one light-emitting fluorophore) and substituted at the 4-position on the dioxetane ring with a fused polycyclic ring-containing fluorophore moiety bearing a labile ring substituent whose point of attachment to the fused polycyclic ring, in relation to this ring's point(s) of attachment to the dioxetane ring, is such that the total number of ring atoms separating these points of attachment, including the ring atoms at the points of attachment, is an odd whole number. These odd pattern substituted compounds decompose to emit light of greater intensity and of a different wavelength than that emitted by the corresponding even pattern substituted isomers.Type: GrantFiled: June 30, 1988Date of Patent: August 28, 1990
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Patent number: 4912258Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.Type: GrantFiled: February 5, 1988Date of Patent: March 27, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans-Georg Batz, Rupert Herrmann
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Patent number: 4910195Abstract: Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.Type: GrantFiled: October 29, 1987Date of Patent: March 20, 1990Assignee: Green Cross CorporationInventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
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Patent number: 4900822Abstract: Reagents for the determination of hydrolase comprises compounds of the formula ##STR1## wherein Z is an organic or inorganic acid residue or a sugar residue, A is an organic or inorganic acid residue, and B is an organic acid residue. Each of R.sup.2 and R.sup.5, is hydrogen, halogen or lower alkyl. Each of R.sup.1, R.sup.3, R.sup.4 and R.sup.6, is hydrogen, halogen, cyano, lower alkyl, lower alkoxy, carboxyl, lower alkoxycarbonyl, carboxy lower alkyl or lower alkoxycarbonyl lower alkyl, or carboxamido groups optional substituted once or twice, or a radical of the formula--COO--(CH.sub.2 CH.sub.2 O).sub.n --R.sup.7in which R.sup.7 is hydrogen or lower alkyl and n is a number from 1 to 4. Additionally, R.sup.6 can be sulpho or nitro.Type: GrantFiled: December 21, 1987Date of Patent: February 13, 1990Assignee: Boehringer Mannheim GmbHInventors: Herbert von der Eltz, Hans-Joachim Guder, Klaus Muhlegger
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Patent number: 4888335Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine, Z is alkylene, alkenylene, oxygen or a sulfur atom and W is an oxygen or a sulfur atom.Type: GrantFiled: July 25, 1988Date of Patent: December 19, 1989Assignee: McNeilab, Inc.Inventors: Richard J. Mohrbacher, Philip P. Grous
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Patent number: 4864024Abstract: A new leuco dye is capable of developing into a colored dye which has an absorption band in the near infrared region. The new leuco dye has the following formula (I): ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently is hydrogen, an alkyl group, an aralkyl group, a cycloalkyl group or an aryl group; each of X.sup.1 and X.sup.2 independently is oxygen, sulfur or --NR.sup.4 -- (R.sup.4 has the same meaning as for R.sup.1, R.sup.2 and R.sup.3); each of the rings A to E independently is benzene ring or naphthalene ring and may have one or more substituent groups; and each of R.sup.1 to R.sup.4 may have one or more substituent groups. A recording material containing the leuco dye is also disclosed.Type: GrantFiled: February 10, 1988Date of Patent: September 5, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Sato, Toru Harada
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Patent number: 4861775Abstract: Streptomyces spec. DSM 3813 produces novel compounds with a basic phenoxazinone structure, which have an antifungal and antiviral action and can be used as lipoxygenase inhibitors.Type: GrantFiled: August 25, 1987Date of Patent: August 29, 1989Assignee: Hoechst AktiengesellschaftInventors: Axel Zeeck, Sabine Breiding-Mack, Susanne Grabley, Hartmut Voelskow, Gerhard Seibert
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Patent number: 4859667Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.Type: GrantFiled: January 14, 1987Date of Patent: August 22, 1989Assignee: Merck Frosst Canada, Inc.Inventors: Cheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
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Patent number: 4847376Abstract: The present invention provides a lipase substrate of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R and R.sub.1, which can be the same or different, each signify an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety and wherein one of R and R.sub.1 can also be a hydrogen atom, X is the residue of an aromatic hydroxy or thiol compound, and each Y and Z, independently from each other, is --S-- or --O--, Z also --CH.sub.2 --.The present invention also provides a process and a reagent for the optical determination of lipase.Type: GrantFiled: May 1, 1986Date of Patent: July 11, 1989Assignee: Boehringer Mannheim GmbHInventors: Ulrich Neumann, Martina Junius, Hans-Georg Batz
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Patent number: 4831190Abstract: There are disclosed 2,4,5-Trifluoro-3-hydroxybenzoic acid represented by the following formula (I): ##STR1## and a salt thereof and a process for preparing the same. Further, there is disclosed a process for preparing 3,5,6-trifluoro-4-hydroxyphthalic acid, which is employed for preparing the above compound.Type: GrantFiled: November 27, 1987Date of Patent: May 16, 1989Assignee: UBE Industries, Ltd.Inventors: Kikuo Ataka, Masayoshi Oku
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Patent number: 4803269Abstract: 4-Monosubstituted and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.Type: GrantFiled: August 14, 1987Date of Patent: February 7, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
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Patent number: 4775754Abstract: Oxazine, thiazine and diazine leuco dyes are synthesized through a reaction using a dicyclohexylcarbodiimide adduct. The adducts are themselves novel compounds.Type: GrantFiled: October 7, 1987Date of Patent: October 4, 1988Assignee: Minnesota Mining and Manufacturing CompanyInventors: Kim M. Vogel, Roger A. Mader
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Patent number: 4774331Abstract: A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.Type: GrantFiled: August 21, 1987Date of Patent: September 27, 1988Assignee: Shionogi & Co., Ltd.Inventors: Makoto Adachi, Hiromu Matsumura, Tsutomu Sugasawa
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Patent number: 4741765Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: April 3, 1987Date of Patent: May 3, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4719097Abstract: The present invention provides phosphates of resorufin derivatives of the general formulae: ##STR1## wherein R.sup.2 and R.sup.5, which can be the same or different, are hydrogen or halogen atoms or lower alkyl radicals, R.sup.1, R.sup.3, R.sup.4 and R.sup.6, which can be the same or different, are hydrogen or halogen atoms, cyano or carboxy groups or lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy lower alkyl or lower alkoxycarbonyl lower alkyl radicals or carboxamide groups which are optionally mono- or disubstituted or radicals of the general formula --COO--(CH.sub.2 CH.sub.2 O).sub.n --R.sup.7, R.sup.7 being a hydrogen atom or a lower alkyl radical and n being a whole number of from 1 to 4, and wherein R.sup.6 can additionally also be a sulphonyl or nitro group, Y is a nitrogen atom or an N.fwdarw.O group and M and M', which can be the same or different, are hydrogen atoms or alkali metal, alkaline earth metal or ammonium ions.Type: GrantFiled: September 26, 1986Date of Patent: January 12, 1988Assignee: Boehringer Mannheim GmbHInventors: Klaus Muhlegger, Herbert von der Eltz
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Patent number: 4710570Abstract: Azine redox dyes and their corresponding dyes of the formula: ##STR1## in which: X is O, S, NR.sup.2,Z completes a fused aromatic of heterocyclic ring system,n is 0 or 1 to allow one R.sup.1 ring substituent,Q represents CR.sup.4 R.sup.5 in which at least one of R.sup.4 and R.sup.5 is an electronegative group or R.sup.4 and R.sup.5 may complete a ring, orwhen X is S Q may represent NR.sup.3 in which R.sup.3 is an aromatic or heterocyclic group.The leuco dyes are useful as dye generators in pressure sensitive, thermographic or photothermographic imaging systems.Type: GrantFiled: September 30, 1985Date of Patent: December 1, 1987Assignee: Minnesota Mining and Manufacturing CompanyInventor: Tran V. Thien
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Patent number: 4707473Abstract: 4-Monosubstitued and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.Type: GrantFiled: May 30, 1986Date of Patent: November 17, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
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Patent number: 4666907Abstract: Phenothiazine derivatives and analogs thereof having the Formula I are useful as inhibitors of the biosynthesis of mammalian leukotrienes. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation, and are useful as cytoprotective agents.Type: GrantFiled: September 26, 1986Date of Patent: May 19, 1987Assignee: Merck Frosst Canada, Inc.Inventors: Rejean Fortin, Cheuk K. Lau, Yvan Guindon, Joshua Rokach, Christiane Yoakim
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Patent number: 4667032Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.Type: GrantFiled: October 10, 1985Date of Patent: May 19, 1987Assignee: Merck Frosst Canada, Inc.Inventors: Cheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
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Patent number: 4620010Abstract: A process is provided to a unique preparation of carboalkoxy substituted or unsubstituted benzoxazole compounds from an amino-phenol compound.Type: GrantFiled: March 29, 1984Date of Patent: October 28, 1986Assignee: USV Pharmaceutical Corp.Inventors: Shou-Nan Ueng, Frederick A. Golec, Jr.
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Patent number: 4608399Abstract: The invention relates to stabilizer-containing reactive components for the production of polyurethane foams having little or no tendency towards core discoloration which are characterized by a stabilizing addition of monomeric and/or oligomeric derivatives of the diphenylamine series, including the phenothiazine series. The invention also relates to new stabilizers of the diphenylamine and/or phenothiazine series and to a process for their production, characterized in that aromatic amines of the diphenylamine and/or phenothiazine series are reacted with bifunctional halogen derivatives, diols, bis-ethers or bis-esters or with bis-olefins formed therefrom at elevated temperatures in the presence of strong acids and the amines are optionally further alkylated.Type: GrantFiled: October 18, 1985Date of Patent: August 26, 1986Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Buysch, Hans-Walter Illger, Karl H. Dorner
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Patent number: 4565834Abstract: The invention relates to stabilizer-containing reactive components for the production of polyurethane foams having little or no tendency towards core discoloration which are characterized by a stabilizing addition of monomeric and/or oligomeric derivatives of the diphenylamine series, including the phenothiazine series. The invention also relates to new stabilizers of the diphenylamine and/or phenothiazine series and to a process for their production, characterized in that aromatic amines of the diphenylamine and/or phenothiazine series ae reacted with bifunctional halogen derivatives, diols, bis-ethers or bis-esters or with bis-olefins formed therefrom at elevated temperatures in the presence of strong acids and the amines are optionally further alkylated.Type: GrantFiled: September 17, 1984Date of Patent: January 21, 1986Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Buysch, Hans-Walter Illger, Karl H. Dorner
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Patent number: 4540523Abstract: Cationic styryl dyestuffs of the formula ##STR1## in which A.sup.1 is an alkyleneoxy or alkyleneamino radical,D.sup.1 is a direct bond or divalent radical,An is an anion, andthe terminal phenyl ring is unsubstituted or substituted by CN, alkyl or alkoxy. The compounds are suitable for dyeing, enscribing and printing paper for dyeing and printing synthetic fibres, especially made of polyacrylonitrile, acid-modified polyesters or polyamides.Type: GrantFiled: October 17, 1980Date of Patent: September 10, 1985Assignee: Bayer AktiengesellschaftInventor: Hermann Beecken
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Patent number: 4500527Abstract: Unsaturated heterocyclic dihydropyridines of the formula: ##STR1## wherein the substituents defined herein have been found to have useful antihypertensive activity.Type: GrantFiled: June 22, 1983Date of Patent: February 19, 1985Assignee: USV Pharmaceutical CorporationInventors: Bernard Loev, James R. Shroff, Rohit Desai
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Patent number: 4430452Abstract: The invention relates to stabilizer-containing reactive components for the production of polyurethane foams having little or no tendency towards core discoloration which are characterized by a stabilizing addition of monomeric and/or oligomeric derivatives of the diphenylamine series, including the phenothiazine series. The invention also relates to new stabilizers of the diphenylamine and/or phenothiazine series and to a process for their production, characterized in that aromatic amines of the diphenylamine and/or phenothiazine series are reacted with bifunctional halogen derivatives, diols, bis-ethers or bis-esters or with bis-olefins formed therefrom at elevated temperatures in the presence of strong acids and the amines are optionally further alkylated.Type: GrantFiled: July 6, 1982Date of Patent: February 7, 1984Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Buysch, Hans-Walter Illger, Karl H. Dorner