Patents Examined by James H. Turnipseed
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Patent number: 4992550Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.Type: GrantFiled: April 6, 1989Date of Patent: February 12, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4992448Abstract: There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1,2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: October 24, 1989Date of Patent: February 12, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
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Patent number: 4988809Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: February 21, 1990Date of Patent: January 29, 1991Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
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Patent number: 4988698Abstract: This invention relates to new 2(1H)-quinolinone compounds having the formula: ##STR1## wherein R.sup.1 is a imidazopyridyl, thiazolyl, indolyl, dihydroindolyl, imidazolyl, benzimidazolyl, quinolyl, isoquinolyl, quinazolinyl, dihydroisoquinolyl, tetrahydroimidazopyridyl or tetrahydroquinolyl, each of which may be substituted with substituents(s) selected from the group consisting of lower alkyl, halogen, lower alkoxy, lower alkylthio, ar(lower)alkoxy, cyano, nitro, amino, lower alkylamino, acylamino, hydroxy and oxo,R.sup.2 is hydrogen, lower alkyl or halogen,A is a single bond or a group of the formula selected from the group consisting of: ##STR2## and --X--CO--, in which X is a single bond or lower alkylene andX.sup.1 is lower alkylene, anda heavy solid line means a single or a double bond,and its pharmaceutically acceptable salt. Said compounds are used in the therapeutic treatment of heart diseases and hypertension in human beings and other animals.Type: GrantFiled: November 13, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Kiyotaka Ito, Hisashi Takasugi
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Patent number: 4987134Abstract: The present invention relates to thienylpiperazines of the general formula I ##STR1## in which R.sup.1 denotes hydrogen or double-bonded oxygen and R.sup.2 denotes hydrogen or double-bonded oxygen, with R.sup.1 and R.sup.2 not both having the same meaning, as well as the pharmaceutically tolerated salts thereof, process for the preparation thereof, the use thereof, and pharmaceuticals containing these and the preparation thereof.Type: GrantFiled: March 16, 1990Date of Patent: January 22, 1991Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler, Bernd Jablonka, Jeffery Troke
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Patent number: 4985441Abstract: The invention relates to quinazoline derivatives which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl or halogenoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH-- or --CO.NR.sup.3 --, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is hydrogen or alkyl, cycloalkyl, alkenyl or alkynyl each of up to 6 carbon atoms; orY is a group of the formula --A--Y.sup.1 in which A is alkylene of up to 6 carbon atoms and Y.sup.1 includes hydroxy, amino and cyano, and alkoxy, alkylamino and alkylthio each of up to 6 carbon atoms.Type: GrantFiled: April 3, 1990Date of Patent: January 15, 1991Assignees: Imperial Chemical Industries plc, National Research Development Corp.Inventors: Leslie R. Hughes, John Oldfield, Stephen J. Pegg
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Patent number: 4983607Abstract: A quinolinone derivative which is a compound of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 are each, independently of one another, a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical;R.sub.3 is a hydrogen atom or a (C.sub.1-4)alkyl radical;R.sub.4 is an unsubstituted or substituted naphthyl, tetrahydronaphthyl, benzyl, phenyl, pyridyl, isoquinolyl or benzoyl radical; and X and Y are each a hydrogen atom or together form a bond; or a pharmaceutically acceptable acid addition salt thereof and, when X and Y are each a hydrogen atom, the diastereoisomers and enantiomers thereof.Type: GrantFiled: October 10, 1989Date of Patent: January 8, 1991Assignee: SynthelaboInventors: Philippe Manoury, Daniel Obitz, Michel Peynot, Jonathan Frost
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Patent number: 4983623Abstract: The invention relates to derivatives of cyclic amino acids of the general formula ##STR1## in which R.sup.1 denotes hydrogen, alkyl, alkenyl or (subst.) aryl,R.sup.2 is hydrogen, alkyl, hydroxyl, alkoxy, (subst.) aryl, (subst.) aryloxy or (subst.) aroyl, or R.sup.1 and R.sup.2 together represent (subst.) benzylidene, or R.sup.1 and R.sup.2, together with the carbon atom carrying them, represent (subst.) cycloalkyl, R.sup.3 denotes hydrogen, hydroxymethyl, formyl, (subst.) alkenyl, (subst.) carboxycarbonyl, (subst.) carbamoylcarbonyl or (subst.) trifluoromethylcarbonyl, A represents a cyclic amino acid, X denotes oxygen, imino or N-alkylimino, m is 0-5 and n is 0 or 1, to a process for the preparation thereof, to agents containing them, and to the use thereof.Type: GrantFiled: December 13, 1988Date of Patent: January 8, 1991Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Franz Hock
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Patent number: 4983613Abstract: This invention relates to isoquinoline acetic acids and acetyl carbamates and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.Type: GrantFiled: April 21, 1989Date of Patent: January 8, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 4981966Abstract: The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.Type: GrantFiled: January 10, 1989Date of Patent: January 1, 1991Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvari nee Debreczy, Agnes Horvath, Maria Balogh, Gabor Kovacs, Tamas Szuts, Peter Ritli, Judit Sipos, Aniko Pajor
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Patent number: 4981853Abstract: The compounds of this invention are heterocyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N-R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N-R.sup.4, and n is 1 to 3 when X is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.Type: GrantFiled: November 14, 1989Date of Patent: January 1, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 4981981Abstract: The novel sesquiterpene epoxides trans-(Z)-1-methyl-4-(1,5-dimethyl-1,4-hexadienyl)-1,2-epoxycyclohexane and cis-(z)-1-methyl-4-(1,5-dimethyl-1,4-hexadienyl)-1,2-expoxycyclohexane have been isolated from N. viridula adult males, and have been successfully synthesized. The compounds are useful for the production of synthetic sex attractants for N. viridula and its parasitoids.Type: GrantFiled: March 14, 1988Date of Patent: January 1, 1991Assignees: The United States of America as represented by the Secretary of Agriculture, The Trustees of the University of PennsylvaniaInventors: Jeffrey R. Aldrich, James E. Oliver, Kyriacos C. Nicolaou, Brian E. Marron
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Patent number: 4981854Abstract: Antibacterially active and animal growth promoting novel 1-aryl-4-quinolone-3-carboxylic acids of the formula ##STR1## in which X is halogen or nitro,X.sup.2 is halogen,R is optionally substituted phenyl, andA is halogen or optionally substituted piperazine or pyrrolidine,or pharmaceutically useable hydrates, acid additions salts, alkali metal, alkaline earth metal, silver or guanidinium salts thereof, and/or esters thereof.Type: GrantFiled: November 6, 1989Date of Patent: January 1, 1991Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4981856Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, arylalkyl, halogeno, hydroxy or mercapto, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl or alkynyl, or substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents;wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;wherein R.sup.4 is hydrogen or alkyl;wherein R.sup.5 is hydrogen or alkyl; andwherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, phenyl, halogeno, nitro, cyano or amino, or substituted alkyl, alkoxy or alkylthio;provided that at least one of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is other than hydrogen;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.Type: GrantFiled: April 12, 1990Date of Patent: January 1, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4980351Abstract: The present invention are novel 3-aminopropoxyaryl derivatives, compositions and methods of use thereof for treating congestive heart failure, coronary heart disease, or myocardial ischemia.Type: GrantFiled: November 4, 1987Date of Patent: December 25, 1990Assignee: Warner-Lambert CompanyInventors: Hubert G. K. Barth, Ila Sircar
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Patent number: 4980353Abstract: Antibacterially active and animal growth promoting novel 1-aryl-4-quinolone-3-carboxylic acids of the formula ##STR1## in which X is halogen or nitro,X.sup.2 is halogen,R is optionally substituted phenyl, andA is halogen or optionally substituted piperazine or pyrrolidine,or pharmaceutically useable hydrates, acid additions salts, alkali metal, alkaline earth metal, silver or guanidinium salts thereof, and/or esters thereof.Type: GrantFiled: May 13, 1986Date of Patent: December 25, 1990Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4980359Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl; R.sub.2 is hydrogen and R.sub.3 is hydrogen or C.sub.1-4 alkyl, or R.sub.2 and R.sub.3 together represent an additional bond as indicated by the dotted line; R.sub.4 is hydrogen, C.sub.1-4 alkyl or phenyl; R.sub.5 is methoxy or ethoxy; R.sub.6 is hydrogen, hydroxy, C.sub.1-4 alkoxy, hydroxy-(C.sub.2-4 alkoxy) or (C.sub.1-4 alkoxy)-(C.sub.2-4 alkoxy); R.sub.7 and R.sub.8 are each independently C.sub.1-4 alkoxy or (C.sub.1-4 alkoxy)-(C.sub.2-4 alkoxy); and R.sub.9 is hydrogen or halogen,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular as bronchodilators, eosinophil accumulation and/or activation inhibiting agents and in the treatment of prophylactic treatment of obstructive or inflammatory airways diseases.Type: GrantFiled: April 10, 1990Date of Patent: December 25, 1990Assignee: Sandoz Ltd.Inventors: Klaus Hasspacher, Reto Naef
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Patent number: 4980470Abstract: Quinolonecarboxylic acid derivatives of the following formula: ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.Type: GrantFiled: January 16, 1987Date of Patent: December 25, 1990Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Kuniyoshi Masuzawa, Seigo Suzue, Keiji Hirai, Takayoshi Ishizaki
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Patent number: 4980471Abstract: The 2-piperazinones are made by reacting a 1-cyano-1-hydroxyalkane with ethylenediamine or a substituted ethylenediamine in aqueous solution. The process to make the 2-piperazinones suitable as a regenerable sulfur dioxide absorbing medium requires that the cyano compound be present in at least a molar equivalent amount to the diamine and that the resulting 2-piperazinone product be sparged with an inert gas.Type: GrantFiled: October 6, 1989Date of Patent: December 25, 1990Assignee: The Dow Chemical CompanyInventors: Steven H. Christiansen, David A. Wilson, Dane Chang
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Patent number: 4978753Abstract: A 7-phenylpyrimido[1,2-a][1,4]benzodiazepin-3(5H)-ones of the formula II: ##STR1## wherein R.sub.o is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, --COOR in which R is alkyl defined as above, ##STR2## in which n is a number of 1 to 4, R.sub.6 and R.sub.7 are hydrogen or alkyl defined as above or together ##STR3## is selected from the group consisting of pyrrolidino, piperidino, morpholino, and 4-methylpiperazino, and --CH.sub.2 OH; wherein R.sub.1 is selected from the group consisting of hydrogen, hydroxy, acetoxy, propionoxy, succinyloxy, and alkyl esters thereof; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.Type: GrantFiled: November 2, 1989Date of Patent: December 18, 1990Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz