Polycyclo Ring System Having Oxazine Ring As At Least One Of The Cyclos Patents (Class 544/73)
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Patent number: 6165941Abstract: A substituted 2-phenylpyridine of the formula I ##STR1## where Ar is ##STR2## and the N-oxides of I and the agriculturally utilizable salts of I where these exist. Use: herbicides; desiccation/defoliation of plants.Type: GrantFiled: January 11, 1996Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventors: Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hartmann Koenig, Ralf Klintz, Peter Muenster, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 6030973Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinediones of the general formula (I), their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: August 17, 1998Date of Patent: February 29, 2000Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6013647Abstract: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams.Type: GrantFiled: March 5, 1998Date of Patent: January 11, 2000Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Steffen Wittmann, Ute Moellmann, Rolf Reissbrodt
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Patent number: 6011031Abstract: Novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them; methods for preparing the antidiabetic compounds and their uses.Type: GrantFiled: December 2, 1997Date of Patent: January 4, 2000Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Chennaveerappa Bajji, Shivaramayya Kalchar, Sekar Reddy Alla, Rajagopalan Ramanujam, Reeba Kannimel Vikramadithyan
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Patent number: 5985871Abstract: Compounds having a certain benzoxazine ring system and their precursors are disclosed which are useful for enhancing synaptic responses mediated by AMPA receptors. Also disclosed are methods for preparing such compounds, and methods for their use in treating subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: December 24, 1997Date of Patent: November 16, 1999Assignee: Cortex Pharmaceuticals, Inc.Inventors: Gary A. Rogers, Christopher Marrs
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Patent number: 5973144Abstract: Benzoxazine monomers, oligomers and polymers are desirably modified by adding pendant functional groups to either the amine or phenolic reactants. These pendant functional groups can be activated at temperatures generally from about 25.degree. C. to about 300.degree. C. to form chemical bonds between said benzoxazine monomers, oligomers and polymers. The additional chemical bonds increase the thermal stability of benzoxazine polymers such that they can withstand higher use temperature, act as more effective flame barriers, or result in higher amounts of char if used as a precursor to high temperature (600-1000.degree. C. reaction condition) chars.Type: GrantFiled: October 3, 1997Date of Patent: October 26, 1999Inventor: Hatsuo Ishida
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Patent number: 5728693Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##Type: GrantFiled: June 25, 1996Date of Patent: March 17, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas Martin Stevenson
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Patent number: 5726172Abstract: This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.Type: GrantFiled: January 6, 1997Date of Patent: March 10, 1998Assignee: Merck & Co., Inc.Inventors: Michelle A. Sparks, Roger M. Freidinger, Debra S. Perlow, Peter D. Williams
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Patent number: 5705639Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.Type: GrantFiled: September 21, 1995Date of Patent: January 6, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Patent number: 5543086Abstract: Novel squarylium dyestuffs are formed by condensing one molecular equivalent of squaric acid with two molecular equivalents of a heterocyclic intermediate of the formula ##STR1## in which X is an optionally substituted ethylene or o-phenylene group; Y is an optionally substituted methylene or imino group, oxygen, sulfur, selenium or (if X is ethylene) a direct bond; and R.sub.1 through R.sub.5 are various substituents or (except for R.sub.2 and R.sub.5) hydrogen. A preferred class of dyestuffs are those formed from intermediates in which Y is methylene or a direct bond, the former including 7-acylaminotetrahydroquinolines and the latter including 6-acylaminoindolines. Thus, two molecular equivalents of each of 1-methyl-7-acetamido-1,2,3,4-tetrahydroquinoline and 6-acetamido-1,2,3, 3-tetramethylindoline were condensed with one molecular equivalent of squaric acid to produce respective dyes each having an absorption maximum substantially coincident with the ruby-laser wavelength of 694 nm.Type: GrantFiled: November 30, 1989Date of Patent: August 6, 1996Assignee: Gentex CorporationInventors: Robert C. Bertelson, Robert A. Sallavanti
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Patent number: 5466689Abstract: A compound represented by the formula ##STR1## wherein X is hydrogen or a substituent; R.sup.1 is an optionally substituted hydrocarbon residue; R.sup.2 and R.sup.3 are respectively hydrogen or a substituent; and ----- shows a single bond or a double bond, or a pharmacologically acceptable acid addition salt thereof, has an analgesic action and is useful as a medicine.Type: GrantFiled: February 2, 1994Date of Patent: November 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuo Yamamoto, Takayuki Doi, Kaneyoshi Kato
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Patent number: 5391482Abstract: The present invention is concerned with the use of 1-arylsemicarbazides of the general formula:Ar--NH--NH--CON.sub.2wherein Ar is an aryl radical optionally substituted by alkyl, alkoxy or halogen, for the stabilization of an enzyme substrate from which, by enzymatic hydrolysis, a leuko coloured material can be formed which, in turn, can be reacted by an oxidation agent to give a colored material. The present invention also provides a corresponding stabilizing process and a diagnostic agent containing such a stabilizer.Type: GrantFiled: December 21, 1990Date of Patent: February 21, 1995Assignee: Boehringer Mannheim GmbHInventor: Dieter Mangold
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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: 5281571Abstract: The invention herein relates to titled compounds having the structure ##STR1## wherein the R.sub.1 -(R.sub.4).sub.n members are as defined in the claims. Characteristic features of these compounds are the haloalkyl R.sub.2 radical and cyclization of two R.sub.4 members at the meta and para positions of the phenyl ring to form a substituted benzoxazinone ring fused to the phenyl or benzthiazinone ring. Such compounds are useful as active ingredients in herbicidal compositions to control undesirable weeds in various crops.Type: GrantFiled: September 25, 1991Date of Patent: January 25, 1994Assignee: Monsanto CompanyInventors: Scott S. Woodard, Bruce C. Hamper, Kurt Moedritzer, Michael D. Rogers, Deborah A. Mischke, Gerard A. Dutra
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Patent number: 5275653Abstract: In order to improve the application properties, in particular the rheological and coloristic properties, and the gloss behavior and the flocculation stability of dioxazine pigments in acrylic varnishes, the surface of the base pigment is modified by coating with sulfo-containing dioxazine derivatives, which in most cases have been converted into the corresponding metal salts, into specific salt-like derivatives derived therefrom or, if desired, into cyclic ammonium compounds. Such a modification of the base pigment, i.e. production of the pigment preparations according to the invention by adding the specific dispersant, can take place at the stage of the pigment synthesis, during a comminution process of the coarse-crystalline crude pigment, by addition to the already finely divided crude pigment in the course of a subsequent solvent finish treatment or by mechanical mixing of the two essential components, pigment and dispersant.Type: GrantFiled: March 20, 1992Date of Patent: January 4, 1994Assignee: Hoechst AktiengesellschaftInventors: Erwin Dietz, Manfred Urban
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Patent number: 5266695Abstract: The compounds are of the class of multi-functional benzoxazine compounds, useful in forming carbon-carbon composites by means of the pyrolysis of carbon fibers impregnated with such compounds.Type: GrantFiled: October 5, 1992Date of Patent: November 30, 1993Assignee: Edison Polymer Innovation CorporationInventor: Hatsuo Ishida
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Patent number: 5252734Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 - alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.Type: GrantFiled: February 5, 1992Date of Patent: October 12, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5246929Abstract: Thiazine (or oxazine) derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.Type: GrantFiled: January 31, 1991Date of Patent: September 21, 1993Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Masakatsu Ozeki, Shin-ichi Kodato, Kousuke Yasuda, Yukitsuka Kudo, Kayoko Maeda
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Patent number: 5214038Abstract: This invention relates to compounds of the formula ##STR1##whereinR.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen or loweralkyl; andR.sub.3 is hydrogen, loweralkyl, halogen, nitro, amino, hydroxy, loweralkoxy, benzyloxy or ##STR2##where R.sub.4 is hydrogen or loweralkyl and R.sub.5 is loweralkyl, aryl or arylloweralkyl, or R.sub.4 and R.sub.5 taken together form a heterocyclic ring selected from the group consisting of ##STR3##whereinR.sub.6 is hydrogen, loweralkyl, aryl or arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful for alleviating depression and various memory dysfunctions characterized by a cholinergic or adrenergic deficit, such as Alzheimer's Disease.Type: GrantFiled: April 15, 1991Date of Patent: May 25, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
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Patent number: 5211885Abstract: A novel class of squarylium infrared absorbing dyes is disclosed which are prepared by the condensation of squaric acid with a benzoxazinone. The dyes are unique in that they possess the desirable properties of squarylium dyes in general along with a narrow band of peak absorbency greater than 1000.Because of their stability to laser beams, the dyes are particularly useful in ocular products for eye protection against lasers.Type: GrantFiled: June 17, 1991Date of Patent: May 18, 1993Assignee: Steadfast Inc.Inventor: Charles M. Zepp
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Patent number: 5185333Abstract: A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.Type: GrantFiled: June 26, 1991Date of Patent: February 9, 1993Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takeshi Kawakita, Takanobu Kuroita, Takemi Fukuda, Ryuhei Iezawa
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Patent number: 5108483Abstract: Herbicidal nitrogen-containing N-aryl-heterocycles of the formula ##STR1## in which Het represents a heterocycle of the formula ##STR2## X.sup.1 represents oxygen, a --CH.sub.2 -- group or an ##STR3## X.sup.2 represents nitrogen or a CH group, Z.sup.1 represents oxygen or sulphur andn represents the number 0 or 1.Type: GrantFiled: September 28, 1990Date of Patent: April 28, 1992Assignee: Bayer AktiengesellschaftInventors: Franz Kunisch, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5109135Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.Type: GrantFiled: August 13, 1991Date of Patent: April 28, 1992Assignee: Sterling Drug Inc.Inventors: Thomas E. D'Ambra, Malcolm R. Bell
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Patent number: 5097027Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.Type: GrantFiled: October 5, 1990Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5030728Abstract: A molecule capable of forming stable complexes with urea, guanidine or amidine compounds and the acid addition salts thereof comprises a nucleus of heterocyclic rings.Type: GrantFiled: June 2, 1989Date of Patent: July 9, 1991Assignee: The Research Foundation State University of New YorkInventor: Thomas W. Bell
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Patent number: 4977260Abstract: Process for preparing mono-, bi- and tricyclic amino acids, intermediates of this process, and a process for preparing same.The invention relates to a process for preparing compounds of the formula I ##STR1## in which R stands for hydrogen, alkyl or aralkyl and R.sup.1 to R.sup.5 are identical or different radicals, (substituted) alkyl, cycloalkyl or (substituted) aryl or in which the pairs of radicals R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5 together with the carbon atom(s) supporting them form a mono- or bicyclic ring system and the other radicals are hydrogen, by treating a compound of the formula II ##STR2## in which R and R.sup.1 to R.sup.5 have the abovoementioned meaning and R.sup.6 and R.sup.7 denote alkyl or aralkyl or together with the nitrogen atom supporting them form a heterocycle which can additionally contain an oxygen atom, with a reducing agent.Type: GrantFiled: April 10, 1989Date of Patent: December 11, 1990Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach
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Patent number: 4977265Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.Type: GrantFiled: May 15, 1990Date of Patent: December 11, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
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Patent number: 4973693Abstract: Novel pentacyclic compounds having antimicrobial and antitumor activity and a process for preparing the same. The pentacyclic compounds are also usefual as intermediates in the production of known tetracyclic antitumor compounds.Type: GrantFiled: September 1, 1989Date of Patent: November 27, 1990Inventors: Shunsuke Goto, Tohru Fukuyama
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Patent number: 4968797Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 30, 1987Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
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Patent number: 4939140Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.Type: GrantFiled: October 27, 1988Date of Patent: July 3, 1990Assignee: Pfizer Inc.Inventors: Eric R. Larson, Banavara L. Mylari
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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: 4897223Abstract: Color-forming agents of the general formula ##STR1## wherein X denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkoxycarbonyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino,Q denotes cyano, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-aryl-carbamoyl, acyl, alkoxysulphonyl, aralkoxysulphonyl, sulphamoyl, N-alkylsulphamoyl, N,N-dialkylsulphamoyl, alkylsulphonyl, arylsulphonyl or aralkylsulphonyl andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused on to the rings A, B, C and D, and the cyclic and acyclic radicals and the rings A, B, C and D can carry further substituents, are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: March 1, 1988Date of Patent: January 30, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar, Roderich Raue
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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: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4835270Abstract: Compounds of the formula ##STR1## wherein Z.sup.1 denotes hydrogen, alkyl, cycloalkyl or ##STR2## R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl, heteroalkyl or heteryl,X.sup.1, X.sup.2 and X.sup.3 denote hydrogen, halogen, alkyl, cycloalkyl, aryl, alkanoylamino, aroylamino or heteryl, and at least one of these radicals denotes NH.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,Y.sup.1, Y.sup.2 and Y.sup.3 denote hydrogen, alkyl, cycloalkyl, aralkyl, aryl or heteryl andY.sup.1 +Y.sup.2 denote the remaining members of a 5-membered or 6-membered ring which optionally contains further hetero-atoms,are outstandingly suitable as colour-forming agents for pressure-sensitive, heat-sensitive and electrosensitive recording materials with an acid developer. Deep copies which are fast to light are obtained.Type: GrantFiled: December 18, 1988Date of Patent: May 30, 1989Assignee: Bayer AktiengesellschaftInventor: Horst Berneth
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Patent number: 4831141Abstract: The invention relates to chromogenic 3,1-benzoxazines of the formula ##STR1## wherein X.sup.1 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl, chlorine or OY.sup.1,X.sup.2 denotes NY.sup.2 Y.sup.3,X.sup.3 denotes OY.sup.4 or NY.sup.5 Y.sup.6,R.sup.1 -R.sup.3 independently of one another denote hydrogen, C.sub.1 -C.sub.4 -alkyl, chlorine, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -mono- or -dialkylamino, orR.sup.1 together with Y.sup.2,R.sup.2 or R.sup.3 together with Y.sup.4 or Y.sup.5, orR.sup.2 and R.sup.3 simultaneously with Y.sup.5 and Y.sup.6 denote a 2 to 4-membered bridge which can contain one oxygen atom or one nitrogen atom and can carry up to 4 methyl groups, and whereinR.sup.1 and R.sup.3 simultaneously represent hydrogen only if R.sup.2 with Y.sup.4 or Y.sup.5 forms one of the abovementioned bridges,R.sup.4 denotes hydrogen, methyl or chlorine,Y.sup.1 and Y.sup.4 independently of one another denote C.sub.1 -C.sub.4 -alkyl, cyclohexyl or benzyl and Y.sup.2, Y.sup.3, Y.sup.5 and Y.sup.Type: GrantFiled: June 1, 1987Date of Patent: May 16, 1989Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Gert Jabs
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Patent number: 4831027Abstract: The invention relates to new imidazo-benzoxazinones of formula ##STR1## wherein the substituents are defined herein below, which compounds are useful in the treatment of cardiovascular disorders.Type: GrantFiled: October 5, 1987Date of Patent: May 16, 1989Assignee: Dr. Karl Thomae GmbHInventors: Berthold Narr, Norbert Hauel, Klaus Noll, Joachim Heider, Manfred Psiorz, Andreas Bomhard, Jacques van Meel, Willi Diederen
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Patent number: 4822791Abstract: This invention relates to pharmaceutical compositions of compounds of the general formula: ##STR1## wherein R.sup.1 is an aryl group or a substituted aryl group wherein the substituent is halogen, hydroxy, C.sub.(1-6) lower alkoxy, C.sub.(1-6) lower alkylenedioxy, halo C.sub.(1-6) lower alkyl, cyano, nitro, mono- or di-C.sub.(1-6) alkylamino or C.sub.(1-6) lower alkanoylamino; or a 5-membered or 6-membered C.sub.(1-6) alkyl substituted or unsubstituted heterocyclic group containing a heteroatom selected from oxygen, nitrogen, and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, and R.sup.2 and R.sup.2' are, independently, hydrogen, halogen, nitro, C.sub.(1-6) lower alkyl or C.sub.(1-6) lower alkoxy. These compounds have been found to exhibit hyaluronidase inhibiting activity, anti-allergic activity and anti-ulcerous activity.Type: GrantFiled: March 2, 1988Date of Patent: April 18, 1989Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
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Patent number: 4812569Abstract: Chromogenic phthalides of the general formula ##STR1## wherein R.sub.1 and R.sub.2 independently of one another denote hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl or are linked to the ring A or B respectively in the o-position to the nitrogen and then represent the remaining members of a partially or fully hydrogenated heterocyclic 5-membered or 6-membered ring which can contain a further heteroatom from the series O, S, N--R.sub.1 or N--R.sub.2,X.sub.1, X.sub.2, X.sub.3 and X.sub.4 independently of one another denote hydrogen, halogen, alkyl, alkenyl, aralkyl, cycloalkyl, aryl, hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylmercapto, arylmercapto, aralkylmercapto, alkylsulphonyl, alkoxycarbonyl or nitro or X.sub.1 +X.sub.2, X.sub.2 +X.sub.3 or X.sub.3 +X.sub.4 denote a fused benzene ring,Z.sub.1 and Z.sub.Type: GrantFiled: February 27, 1987Date of Patent: March 14, 1989Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 4806541Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.Type: GrantFiled: September 22, 1986Date of Patent: February 21, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
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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: 4777253Abstract: A process for producing racemic or optically active compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 to C.sub.6 alkyl or benzyl; and Z is amino or substituted amino.Also disclosed are intermediates useful in the process and methods for producing the intermediates.Type: GrantFiled: April 25, 1986Date of Patent: October 11, 1988Assignee: Abbott LaboratoriesInventors: Lester A. Mitscher, Daniel T. Chu
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Patent number: 4754034Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicals X.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 21, 1985Date of Patent: June 28, 1988Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
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Patent number: 4748175Abstract: The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.Type: GrantFiled: December 30, 1986Date of Patent: May 31, 1988Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara RtInventors: Endre Kasztreiner, Gyorgy Rabloczky, Nandor Makk, Gyorgy Cseh, Maria Kuhar nee Kurthy, Eszter Diesler, Laszlo Jaszlits, Laszlo Sebestyen, Janos Wellmann, Aniko Tegdes, Judit Sarossy nee Kincsesy, Peter Matyus, Andras Varro, Laszlo Szam, Sarolta Vegvari nee Gyurki
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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: 4727140Abstract: 4,4-Diaryl-2-oxobenzo-3,1-oxazines of the general formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,at least one of the radicals X.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring B,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl or aryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further heteroatoms or Y.sup.1 +Y.sup.Type: GrantFiled: October 21, 1985Date of Patent: February 23, 1988Assignee: Bayer AktiengesellschaftInventors: Karlheinrich Meisel, Horst Berneth
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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: 4701512Abstract: The adducts of isocyanates wtih benzoxazolones or benzoxazinediones are novel compounds which may be employed as blocked isocyanates and are particularly useful as latent, epoxide curing agents. At typical epoxide curing temperatures, the isocyanate is oxirane or hydroxyl reactive and the benzoxazole or benzoxazinedione acts like a di- or trifunctional phenol, respectively.Type: GrantFiled: October 29, 1985Date of Patent: October 20, 1987Assignee: The Dow Chemical CompanyInventor: Theodore L. Parker
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Patent number: 4695633Abstract: Chromogenic 4,4-diaryl-dihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 independently of one another represent hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,and whereinat least one of the radicals X.sup.1, X.sup.2 or X.sup.3 represents NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl, hetaralkyl or hetaryl,Y.sup.1, Y.sup.2 and Y.sup.3 independently of one another denote hydrogen, alkyl, cycloalkyl, aralkyl or aryl or the remaining members of a 5-membered or 6-membered ring which reaches to one of the benzene-C atoms in the o-position and optionally contains further hetero-atoms, orY.sup.1 +Y.sup.Type: GrantFiled: May 17, 1985Date of Patent: September 22, 1987Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack