Tricyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/249)
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Patent number: 5663337Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.Type: GrantFiled: May 25, 1995Date of Patent: September 2, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5625062Abstract: The present invention provides a novel process for the production of organic solvent soluble squaraine dyes. More specifically, the invention describes how a difficult to prepare tetrahydroxy squaraine intermediate can be prepared in an organic solvent system in the presence of water. This intermediate can then be esterified in pyridine to form the soluble squaraine dye which can then be easily isolated from the reaction mixture. The invention also provides the dyes prepared according to this method.Type: GrantFiled: May 29, 1996Date of Patent: April 29, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: Roger A. Mader, William D. Ramsden, Terence D. Spawn, Daniel E. Saddoris
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Patent number: 5597823Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an .alpha.-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.Type: GrantFiled: June 5, 1995Date of Patent: January 28, 1997Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, Steven W. Elmore, James F. Kerwin, Jr., Suzanne A. Lebold, Edmund L. Lee, Kevin B. Sippy, Karin R. Tietje, Michael D. Wendt
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Patent number: 5574039Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.Type: GrantFiled: September 22, 1994Date of Patent: November 12, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
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Patent number: 5563144Abstract: This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.Type: GrantFiled: June 6, 1995Date of Patent: October 8, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Dominique Damour, Richard Labaudiniere, Jean-luc Malleron, Serge Mignani
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Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5464809Abstract: Fungicidal new 2-methoximinocarboxylic esters of the general formula (I) ##STR1## in which Ar represents one of the radicals ##STR2## and A represents one of the radicals --CH.sub.2 --; ##STR3## where Y represents one of the radicals ##STR4## --O--CH.sub.2 --; --CH.sub.2 --O--; --S--CH.sub.2 --; ##STR5## --SO.sub.2 --CH.sub.2 --; --O--; --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --,n represents the number 0 or 1,R represents alkyl, halogenoalkyl, alkenyl, halogenoalkenyl, or represents optionally substituted cycloalkyl, or represents optionally substituted aryl or represents optionally substituted heteroaryl, and, moreover, in the event that n is 0, also represents halogen, andX.sup.1, X.sup.2, X.sup.3 and X.sup.4 independently of one another in each case represent hydrogen, halogen, hydroxyl or methoxy, but where, in the event that X.sup.2 represents bromine, X.sup.3 does not simultaneously represent hydroxyl or methoxy.Type: GrantFiled: September 12, 1994Date of Patent: November 7, 1995Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann
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Patent number: 5439916Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.Type: GrantFiled: August 31, 1990Date of Patent: August 8, 1995Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Edmund J. Sybertz
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Patent number: 5401745Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: March 28, 1995Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: 5326872Abstract: This invention relates to a process for preparing asymmetric isoindoline pigments of the formula ##STR1## in which R.sup.1 is an electron-withdrawing group, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, or aryl, and R.sup.4 R.sup.5 R.sup.6 and R.sup.7 are independently hydrogen, halogen, alkyl, alkoxy, or aryloxy. The process employs an initial reaction of a 1,2-dicyanobenzene with an alcohol in an organic medium in the presence of a base. The resultant imino-isoindoline intermediate composition reacts without isolation with a cyanomethylene compound NC--CH.sub.2 -R.sup.1 to form a partly condensed product that is then condensed, optionally without isolation, in the presence of water with barbituric acid or a derivative thereof to form the asymmetric isoindoline pigment.Type: GrantFiled: March 6, 1992Date of Patent: July 5, 1994Assignees: Miles Inc., Bayer AktiengesellschaftInventors: Barbara J. Wagner, Bernd Kaletta
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Patent number: 5316906Abstract: Novel fluorescent precipitating substrates made from a class of fluorophores, generally including quinazolinones (quinazolones), benzimidazoles, benzothiazoles, benzoxazoles, quinolines, indolines, and phenanthridines, having the general formula: ##STR1## where carbon atoms of --C.sup.1 .dbd.C.sup.2 -- are further joined so as to complete a first 5- or 6-membered aromatic ring which may contain at least one of the hetero atoms N, O or S,where carbon atoms of --C.sup.4 --N.dbd.C.sup.3 -- are further joined so as to complete a second 5- or 6-membered aromatic ring that contains at least the nitrogen between C.sup.3 and C.sup.4 and may contain at least one additional hetero atom N, O or S,where the first and second aromatic rings may be joined by a 5- or 6-membered bridging ring that contains at least the C.sup.2 from the first aromatic ring and the C.sup.Type: GrantFiled: August 23, 1991Date of Patent: May 31, 1994Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Yu-zhong Zhang, Stephen T. Yue, Ewald Terpetschnig, Nels A. Olson, John J. Naleway, Karen D. Larison, Zhijian Huang
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Patent number: 5288866Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.Type: GrantFiled: October 14, 1992Date of Patent: February 22, 1994Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5241068Abstract: Compounds of the formulae ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1 and Y.sup.1 have the stated meanings, processes for their preparation and their use.Type: GrantFiled: August 21, 1991Date of Patent: August 31, 1993Assignee: Bayer AktiengesellschaftInventors: Christina Diblitz, Hans Hochstetter
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Patent number: 5227461Abstract: High performance composites can be made from linear or multidimensional oligomer or blends that include unsaturated hydrocarbon crosslinking functionalities linked to a benzenetriyl or pyrimidine radical on the terminal ends of the polymeric backbones of the oligomers. The oligomers are made by condensing benzenetriyl or pyrimidine-based end-cap monomers of the formulas: ##STR1## wherein R.sub.1 =lower alkyl, lower alkoxy, aryl, aryloxy, substituted alkyl, substituted aryl, halogen, or mixtures thereof;j=0, 1, or 2;G=--CH.sub.2 --, --O--, --S--, --SO--, --CO--, --CHR--, --CR.sub.2 --, or --SO.sub.2 --;T=methallyl or allyl;Me=methyl;R=hydrogen, lower alkyl, or phenyl;Ph=phenyl; ##STR2## Q=--NH.sub.2, --COX, --NO.sub.2, or --COOH, with suitable polymeric precursors.Type: GrantFiled: September 30, 1992Date of Patent: July 13, 1993Assignee: The Boeing CompanyInventors: Hyman R. Lubowitz, Clyde H. Sheppard
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Patent number: 5147568Abstract: N-Allyl and N-methylene-thio substituted 2,3-dihydroperimidine compounds are very effective antioxidant stabilizers for organic material subject to oxidative or thermal degradation, particularly for lubricant compositions.Type: GrantFiled: October 28, 1991Date of Patent: September 15, 1992Assignee: Ciba-Geigy CorporationInventors: John J. Luzzi, David H. Steinberg
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Patent number: 5124326Abstract: A pharmaceutically efficacious pteridine compound of formula I: ##STR1## wherein A denote a bridging hydrocarbon group containing 1 to 8 carbon atoms and containing a ##STR2## group directly bonded to the phenyl group and one of the methylene radicals of the bridging A group is optionally replaced by --O--; R.sub.1 is hydrogen, a cycloalkyl group with up to 7 carbon ring atoms, or an alkyl group having 1 to 6 carbon atoms, benzyl, or aryl; R.sub.2 is hydrogen or an alkyl group having 1 to 6 carbon atoms, or wherein R.sub.1 and R.sub.2 together form a five- or six-membered heterocyclic group which optionally contains additional hetero atoms selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R.sub.3 ' is hydrogen, an optionally substituted alkyl group having 1 to 3 carbon atoms, carboxyl, hydroxyl or R.sub.3 and R.sub.Type: GrantFiled: April 20, 1990Date of Patent: June 23, 1992Assignee: Roehm GmbH Chemische FabrikInventors: Ernst Mutschler, Angelika Christner, Ingrid Hofmann
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Patent number: 5097029Abstract: Processes for preparing 2,3-dihydro-1,3-dialkyl-2,2-dialkyl perimidines and N,N'-dialkyl-1,8-naphthalene diamines are disclosed. The 2,3-dihydro-1,3-dialkyl-2,2-dialkyl perimidines are prepared by alkylating 2,3-dihydro-2,2-dialkyl perimidines with an alkylating agent in a water miscible organic solvent at room temperature to 80.degree. C. in the presence of water and an inorganic base. N,N'-dialkyl-1,8-naphthalene diamines are prepared by hydrolyzing the 2,3-dihydro-1,3-dialkyl-2,2-dialkyl perimidines with strong aqueous acid in an aqueous organic solvent and removing a ketone by-product and the aqueous organic solvent by codistillation.Type: GrantFiled: August 6, 1990Date of Patent: March 17, 1992Assignee: Hercules IncorporatedInventor: Paul J. Shannon
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Patent number: 5084457Abstract: This invention is compounds of the formula: ##STR1## and a method of treating cognitive and related neuronal behavioral problems in mammals using the compounds.Type: GrantFiled: July 23, 1990Date of Patent: January 28, 1992Assignee: American Cyanamid CompanyInventors: William J. Fanshawe, Joseph W. Epstein, Jeremy I. Levin
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Patent number: 5070086Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.Type: GrantFiled: June 15, 1990Date of Patent: December 3, 1991Assignee: Schering CorporationInventor: Richard Friary
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Patent number: 5037834Abstract: 1-Substituted-6-fluoro-7-heterocyclic-1,4-dihydroquino-1-(or dihydronaphthyridin)-4-one carboxylic acids have antibacterial properties. The 7-heterocyclic group is a bicyclic group, one of the rings of which is saturated and the other ring of which is unsaturated.Type: GrantFiled: August 1, 1989Date of Patent: August 6, 1991Assignee: Pfizer Inc.Inventors: Katherine E. Brighty, John A. Lowe, III, Paul R. McGuirk
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Patent number: 4906630Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.Type: GrantFiled: October 11, 1988Date of Patent: March 6, 1990Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4895981Abstract: A process is described for improving the photochemical stability of dyeings on polyester fibre materials by means of UV absorbers of the formula ##STR1## in which R is alkyl, alkoxy, halogen or hydroxyl, R.sub.1 is alkyl, R.sub.2 is hydrogen, halogen, alkyl, alkylamino, hydroxyalkylamino, aralkylamino, alkoxyalkylamino, alkenyl, alkoxy, alkoxy which is substituted by hydroxyl, carboxyl or C.sub.2 -C.sub.5 alkoxycarbonyl, alkenyloxy, phenyl or phenyl which is substituted by halogen, alkyl, hydroxy-C.sub.1 -C.sub.4 alkyl, alkenyloxy, alkoxy, hydroxyl or carboxy-C.sub.1 -C.sub.4 alkoxy, m is 0 or 1 and n is 0, 1 or 2, and also novel compounds of the formula (1) in which m and n are both 0 and R.sub.2 is alkylamino, hydroxyalkylamino, aralkylamino or alkoxyalkylamino.Type: GrantFiled: March 24, 1989Date of Patent: January 23, 1990Assignee: Ciba-Geigy CorporationInventors: Gerhard Reinert, Kurt Burdeska
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Patent number: 4847364Abstract: Methine-azo compounds of the formula ##STR1## in which A is the complement to a heterocyclic 5- or 6-membered ring which has a quaternized N atom as a ring member, which can contain further hetero atoms and which can be substituted or/and be fused with carbocyclic or heterocyclic rings,R is hydrogen, cyano or C.sub.2 --C.sub.3 -alkylene which is bonded to an N atom of ring A to form a 5- or 6-membered ring,B is substituted or unsubstituted phenylene or naphthylene,X.sup..crclbar. is an anion andKK is the radical of an open-chain coupling component which contains active methylene groups, except that, if A is the complement to a pyridinium ring, KK cannot be the radical of acetoacetanilide which is unsubstituted or alkyl-substituted in the aniline ring.They are suitable for use as dyes for dyeing and printing cationically dyeable substrates, in particular paper.Type: GrantFiled: June 16, 1987Date of Patent: July 11, 1989Inventor: Peter Mockli
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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: 4814335Abstract: In one aspect, compounds having antiviral activity and having the general formula: ##STR1## wherein each R.sup.2, independently, is H or lower (fewer than 6 carbon atoms) alkyl; each R.sup.3, independently, is H or lower alkyl; R.sup.0 is H or lower alkyl; R.sup.1 is H or lower alkyl; 1.ltoreq.n.ltoreq.11; n-2.ltoreq.m.ltoreq.2n; 0.ltoreq.p.ltoreq.3; z is 0 or 1; and p.ltoreq.1.ltoreq.2p; each n, m, p, and q being selected so that the sp.sup.3 valence shell of each carbon atom in each ring is filled; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 23, 1987Date of Patent: March 21, 1989Assignee: Biomeasure, IncorporatedInventor: Sun H. Kim
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Patent number: 4785101Abstract: Benzodiazinone-pyridazinone and -hydroxypyrazolyl compounds possess cardiotonic activity and are included in therapeutic cardiotonic compositions useful in methods for increasing cardiac contractility and for the treatment of congestive heart failure.Type: GrantFiled: June 17, 1987Date of Patent: November 15, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4769378Abstract: Certain 5-phenyl-5H-indeno[1,2-d]pyrimidines, their pharmaceutical formulations, and their use in methods for inhibiting aromatase and treating or preventing estrogen-dependent diseases.Type: GrantFiled: March 31, 1986Date of Patent: September 6, 1988Assignee: Eli Lilly and CompanyInventors: Kenneth S. Hirsch, C. David Jones, Eriks V. Krumkalns, Donald G. Saunders
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Patent number: 4764512Abstract: This invention relates to substituted benzodiazinone-pyridone compounds and their use as cardiotonic agents including methods for increasing cardiac contractility, pharmaceutical compositions including the same and methods for the preparation thereof.Type: GrantFiled: August 27, 1986Date of Patent: August 16, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Bruce F. Molino, Henry F. Campbell, Donald E. Kuhla, William L. Studt
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Patent number: 4725685Abstract: Isoindoline compounds of the formula (I) ##STR1## and their metal complexes of the formula (II) ##STR2## where (in formulae (I) and (II)) X and Y are each hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy, alkoxycarbonyl, alkylsulfonyl, alkanoylamino, carbamyl, nitro, benzoylamino or N-phenylcarbamyl, or X and Y together form a radical of a fused benzene ring, T is fluorine, chlorine or bromine, Z is nitro, carbamyl, alkanoylamino, alkoxy, alkyl or phenyl, n and n' are each 0, 1, 2, 3 or 4, p and p' are each 0 or 1, the sums (n+p) and (n'+p') are each not more than 4, and Me is a divalent cation of a transition metal, of zinc or of cadmium, are useful pigments or coloring polymers, printing inks and finishes.Type: GrantFiled: November 25, 1985Date of Patent: February 16, 1988Assignee: BASF AktiengesellschaftInventor: Wolfgang Lotsch
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Patent number: 4678499Abstract: 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: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4625026Abstract: In one aspect, compounds having antiviral activity and having the general formula: ##STR1## wherein each R.sup.2, independently, is H or lower (fewer than 6 carbon atoms) alkyl; each R.sup.3, independently, is H or lower alkyl R.sup.0 is H or lower alkyl, R.sup.1 is H or lower alkyl; 1.ltoreq.n.ltoreq.11; n-2.ltoreq.m.ltoreq.2n; 0.ltoreq.p.ltoreq.3; z is 0 or 1; and p.ltoreq.q.ltoreq.2p; each n, m, p and q being selected so that the sp.sup.3 valence shell of each carbon atom in each ring is filled; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 13, 1983Date of Patent: November 25, 1986Assignee: Biomeasure, Inc.Inventor: Sun H. Kim
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Patent number: 4599413Abstract: A compound prepared by reacting at least one aromatic or aliphatic polyamine compound having at least two amine groups, which are separated by no more than one carbon atom, with at least one carbonyl-containing compound selected from the group consisting of aldehydes and ketones, wherein said polyamine compound is selected from:aliphatic polyamines having 2-20 carbon atoms corresponding to the formula: ##STR1## wherein A is a direct carbon-carbon bond or --CH.sub.2 -- and R.sub.3 and R.sub.Type: GrantFiled: December 15, 1983Date of Patent: July 8, 1986Assignee: Hexcel CorporationInventors: Richard J. Moulton, John D. Neuner
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Patent number: 4581172Abstract: Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.Type: GrantFiled: April 25, 1984Date of Patent: April 8, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Ado Kaiser, Frank Kienzle
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Patent number: 4560688Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3, or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optional double bond, R.sup.2 being absent if the double bond is present, and Y is substiuted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.Type: GrantFiled: February 8, 1984Date of Patent: December 24, 1985Assignee: Schering CorporationInventor: Frank J. Villani
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Patent number: 4465758Abstract: Described are 1,3-diaza-9-thia-anthracene-2,4-diones of the general formula (II) ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are identical or different and individually each denotes a hydrogen or halogen atom, an alkyl, alkoxy, carboxyl or alkoxy-carbonyl group,R.sup.2 denotes an alkoxy, carboxyl or alkoxy-carbonyl group, ortwo of the groups R.sup.1, R.sup.2, R.sup.3, and R.sup.4 together form a condensed aromatic radical.These compounds are used as photoinitiators in photopolymerizable recording materials and have an increased sensitivity in the spectral range between 425 and 480 nm.Type: GrantFiled: August 29, 1983Date of Patent: August 14, 1984Assignee: Hoechst AktiengesellschaftInventors: Rainer Wingen, Klaus Horn, Walter Lutz
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Patent number: 4464457Abstract: The present invention relates to novel 10-phenyl-1,3,9-triazaanthracenes and to a photopolymerizable mixture which contains, as the essential components,(a) a polymeric binder(b) a polymerizable compound having at least two terminal, ethylenically unsaturated groups and a boiling point of more than 100.degree. C., and(c) a 10-phenyl-1,3,9-triazaanthracene as the photoinitiator.Type: GrantFiled: August 29, 1983Date of Patent: August 7, 1984Assignee: Hoechst AktiengesellschaftInventors: Dieter Bosse, Rainer Wingen, Klaus Horn, Walter Lutz
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Patent number: 4428953Abstract: Novel pleuromutilin derivatives of formula I, ##STR1## in which R.sub.1 is ethyl or vinyl,m is 0 or 1, andR.sub.2 is a heterocyclic radical, in which a 5- or 6-membered, unsaturated or saturated heterocyclic ring containing one or more hetero atoms selected from oxygen, sulphur and nitrogen, is attached to the --S(CH.sub.2).sub.m --group,provided that when m is 0, R.sub.2 is other than pyridyl,their production and use as antimicrobial agents are described.Type: GrantFiled: March 8, 1982Date of Patent: January 31, 1984Assignee: Sandoz, Ltd.Inventors: Heinz Berner, Friederike Turnowsky, Georg Laber, Johannes Hildebrandt
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Patent number: 4328223Abstract: The invention includes new 2-amino-3a,4,5,6-tetrahydro-perimidines and method for their preparation from corresponding racemacic compounds. Also included in the invention are pharmaceutical compositions containing said 2-amino-3a,4,5,6-tetrahydro-perimidines and methods for the use of said compounds and compositions.Type: GrantFiled: April 5, 1979Date of Patent: May 4, 1982Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Hildegard E. Mayer, Annedore Mayer, Andrea Mayer, Heinz Ziemann, Kurt Stoepel
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Patent number: 4294964Abstract: The present invention is directed to certain 2-aryl-1H-perimidines as immunosuppressive agents.Type: GrantFiled: February 28, 1980Date of Patent: October 13, 1981Assignee: Eli Lilly and CompanyInventor: Ken Matsumoto
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Patent number: 4224326Abstract: The present invention is directed to certain 2-aryl-1H-perimidines as immunosuppressive agents.Type: GrantFiled: September 21, 1978Date of Patent: September 23, 1980Assignee: Eli Lilly and CompanyInventor: Ken Matsumoto
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Patent number: 4134981Abstract: Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.Type: GrantFiled: October 27, 1977Date of Patent: January 16, 1979Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Leonard J. Czuba, Hans-Jurgen E. Hess, Saul B. Kadin
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Patent number: 4128643Abstract: (2-Amino-4-quinazolinyl)-quanidines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the defined meanings, and their physiologically tolerable acid addition salts, process for preparing these compounds, pharmaceutical preparations containing them and their use as medicines.Type: GrantFiled: May 26, 1977Date of Patent: December 5, 1978Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Hans G. Alpermann, Karl Geisen, Norbert Kothe, Walter Ried
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Patent number: 4125724Abstract: An improved and novel process is provided for the reduction of isocyanate groups in organic compounds to formamide groups by catalytic hydrogenation with a noble metal catalyst. The process allows preparation of formamides in consistently high yields from all types of isocyanates.Type: GrantFiled: October 6, 1977Date of Patent: November 14, 1978Assignee: Bristol-Myers CompanyInventor: Henry G. Howell
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Patent number: 4122274Abstract: A novel series of optionally substituted 3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-ones is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.Type: GrantFiled: May 25, 1977Date of Patent: October 24, 1978Assignee: Bristol-Myers CompanyInventor: Peter Frederick Juby
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Patent number: 4120962Abstract: Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.Type: GrantFiled: April 11, 1977Date of Patent: October 17, 1978Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Leonard J. Czuba, Hans-Jurgen E. Hess, Saul B. Kadin
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Patent number: 4113637Abstract: Alkyl-guanidino heterocyclic compound produced by alkylation with a halogenated hydrocarbon of the general formula RX.sub.n, of a guanidino-heterocyclic compound (A) of general formula: ##STR1## in which R is substantially a hydrocarbon radical containing about 10 to 200 carbon atoms, X is a halogen atom and n is 1 or 2; Y is an oxygen atom, --O--, a sulfur atom --S--, a --NH-- group, or a --CONH-- group in which the carbon atom is directly bound to the benzene ring, R' and R" are each a hydrogen atom, an alkyl radical having from 1 to 10 carbon atoms, or a --Z--Ar group in which Z is a divalent atom or group and Ar is a substituted or unsubstituted aromatic radical, R' and R" being capable of forming together, when they are in ortho position, an aliphatic or aromatic cycle fused to the benzene ring.Type: GrantFiled: August 1, 1977Date of Patent: September 12, 1978Assignee: Institut Francais du PetroleInventors: Choua Cohen, Bernard Sillion