Patents Examined by Henry R. Jiles
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Patent number: 4738975Abstract: The compound of the formula ##STR1## wherein R.sup.1 is hydrogen, fluorine, methoxy or trifluoromethyl, R.sup.2 is a C.sub.1-8 alkyl, R.sup.3 is a C.sub.1-8 alkyl which may be fluorinated, and n is 0 or 1, or a pharmacologically acceptable salt thereof is useful for prevention and treatment of digestive ulcers (e.g. gastric ulcer, duodenal ulcer) and gastritis.Type: GrantFiled: June 18, 1986Date of Patent: April 19, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Akira Nohara, Yoshitaka Maki
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Patent number: 4739057Abstract: A process for converting organic hydroxyl-containing compounds to halides which comprises reacting the hydroxyl-containing compound with a phosphorushalide reagent of formula: R.sub.n PX.sub.5-n wherein n is selected from 1, 2 and 3; R is selected from the group consisting of C-6 to C-10 aryl and substituted aryl wherein the substituents are selected from the group consisting of straight and branched chain alkyl, alkoxy, and haloalkyl, halogen, sulfonate and mixtures thereof; and X is a halogen. It is preferred to carry out the reaction in the presence of an arylphosphorusoxydihalide solvent. The use of an arylphosphorustetrahalide and particularly phenylphosphorustetrachloride is preferred. The arylphoshorustetrahalide can be prepared in situ by contacting a solution of the corresponding arylphosphorusdihalide in an arylphosphorusoxydihalide solvent with a halogen. The process can further comprise the step of heating the reaction mixture. Maintaining a reaction temperature of from about 0.degree. C.Type: GrantFiled: June 30, 1986Date of Patent: April 19, 1988Assignee: Stauffer Chemical Co.Inventors: Andrea Leone-Bay, Elliott Bay, Peter E. Timony
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Patent number: 4739106Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 19, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Nobuo Harada
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Patent number: 4739065Abstract: Thienopyridinone derivatives of the general formula: ##STR1## in which Y represents hydrogen or a lower alkyl group and X represents: a hydroxy, lower alkanoyloxy, lower alkoxy unsubstituted or substituted by a hydroxy, lower alkoxy, di-(lower alkyl)-amino, piperidino, pyrrolidino, morpholino or N-(lower alkyl)-piperazino group,a group of formula: ##STR2## in which R' and R", which are the same or different, each represent hydrogen or a lower alkyl, W represents hydrogen or a lower alkyl radical or a vinyl or ethynyl group and Z represents hydrogen or a lower alkyl radical,a phenyl radical unsubstituted or substituted by an atom of fluorine, chlorine, bromine or iodine or by a hydroxy, lower alkoxy or nitro group,a group of formula: ##STR3## in which Z has the same meaning as above, an amino, lower alkylamino or --NHCOOZ group in which Z has the same meaning as above and pharmaceutically acceptable salts thereof.They possess antibactericidal properties.Type: GrantFiled: January 5, 1987Date of Patent: April 19, 1988Assignee: SanofiInventors: Louis Giral, Marc Puygrenier, Jacques Bompart
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Patent number: 4738967Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in which A is lower alkylene andR.sup.2 is di(lower) alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino(lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 23, 1986Date of Patent: April 19, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Youichi Shiokawa, Masayuki Kato, Nobukiyo Konishi, Atsushi Akahane
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Patent number: 4738803Abstract: Derivatives having the general formula: ##STR1## in which the various radicals, A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.Type: GrantFiled: August 22, 1986Date of Patent: April 19, 1988Inventors: Bernard Roques, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Patent number: 4739050Abstract: This invention relates to 2-arylbenzothiazine derivatives of the formula[I] and salts thereof, process of preparation and therapeutic drug comprising them for circulatory diseases, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, lower alkyl, hydroxy, lower alkoxy, acyloxy, tetrahydropyranyloxy, halogen, nitro, amino, lower alkylamino or ##STR2## and the lower alkoxy group may be substituted by halogen, formyl, lower alkoxy or epoxy;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, hydroxy, lower alkoxy, mercapto, lower alkylthio, arylthio, halogen, cyano, formyl-lower alkyl, lower alkoxy-lower alkyl or ##STR3## R.sup.5,R.sup.6,R.sup.7 and R.sup.Type: GrantFiled: November 4, 1986Date of Patent: April 19, 1988Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Iwao Jun-ichi, Iso Tadashi, Oya Masayuki
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Patent number: 4738968Abstract: The present invention relates to a 1,8-naphthyridine derivative of the formula ##STR1## wherein X is a fluorine or chlorine atom, and R is a hydrogen atom, or a methyl or ethyl group;and esters thereof and salts thereof are processes for preparation thereof. These compounds show excellent anti-bacterial activity and are useful antibacterial agents.Type: GrantFiled: February 12, 1986Date of Patent: April 19, 1988Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Jun-ichi Matsumoto, Junji Nakano, Katsumi Chiba, Shinichi Nakamura
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Patent number: 4738976Abstract: A novel ketene S,S-acetal derivative which is useful as an antimycotic agent and an agricultural chemical of fungicidal, plant growth regulating or insecticidal properties represented by the general formula (I): ##STR1## wherein R represents a hydrogen atom; an alkyl group having 1 to 8 carbon atoms; a cycloalkyl group having 3 to 6 carbon atoms; a methylene group; a lower alkenyl group; a lower alkyl group substituted by a halogen atom, a cyano group, a lower alkoxyl group, a lower alkylthio group; a carbamoyl group, an acyl group, or an alkenoyloxy group; a phenyl group represented by ##STR2## (in which R.sub.Type: GrantFiled: October 8, 1986Date of Patent: April 19, 1988Assignee: Nihon Nohyaku Co., Ltd.Inventors: Akira Seo, Hideo Kanno, Nobu Hasegawa, Yukio Miyagi, Akira Nishimura, Shigeo Konaka, Tetsuto Ohmi, Yukimi Munechika, Matazaemon Uchida, Kenichi Ikeda
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Patent number: 4737514Abstract: Compounds of formula (I) ##STR1## wherein n is 0, 1 or 2;one or R.sup.1 and R.sup.2 is hydrogen and the other is selected from carbamoyl, N-C.sub.1-4 alkylcarbamoyl, N,N-di-C.sub.1-4 alkylcarbamoyl, carbamimidoyl, N.sup.1 -C.sub.1-4 alkylcarbamimidoyl, N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1 -C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl and imidazolin-2-yl (optionally substituted by one or more C.sub.1-4 alkyl groups); andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula--NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen, C.sub.1-4 alkyl and hydroxy C.sub.Type: GrantFiled: January 2, 1986Date of Patent: April 12, 1988Assignee: Burroughs Wellcome Co.Inventors: Morton Harfenist, Charles T. Joyner, Darryl J. Heuser
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Patent number: 4737510Abstract: Novel bioactive metabolites from the Caribbean sponge Agelas coniferin are disclosed. These compounds are generically referred to as halopyrroles. They exhibit antiviral and antibacterial properties, and, thus, are useful for various non-therapeutic and therapeutic purposes.Type: GrantFiled: September 30, 1986Date of Patent: April 12, 1988Assignee: The Board of Trustees of The University of IllinoisInventor: Kenneth L. Rinehart, Jr.
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Patent number: 4737511Abstract: Novel imidazolylphenylpyrrol-2-ones are described as having cardiovascular properties especially as cardiotonic agents in the treatment of congestive heart failure. Pharmaceutical formulations containing such compounds are also described.Type: GrantFiled: November 3, 1986Date of Patent: April 12, 1988Assignee: Schering A.G.Inventors: Paul W. Erhardt, Alfred A. Hagedorn, III, John W. Lampe
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Patent number: 4737458Abstract: The present invention provides aminopyrazolinones of the general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 6 carbon atoms and together containing at most 8 carbon atoms.The present invention also provides a process for the preparation of these new aminopyrazolinones and reagents containing them. In addition, the present invention is concerned with the use of these new aminopyrazolinones as a color coupler for the detection of hydrogen peroxide.Type: GrantFiled: August 8, 1986Date of Patent: April 12, 1988Assignee: Boehringer Mannheim GmbHInventors: Hans-Georg Batz, Rupert Herrmann, Joachim Siedel
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Patent number: 4737506Abstract: This invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate derivative represented by the following general formula (I): ##STR1## wherein R means an imidazolyl or pyridyl group, R.sub.1 denotes a hydrogen or halogen atom or a nitro or trifluoromethyl group, R.sub.2 is a lower alkyl group, X is CH or N, A means a lower alkylene group, ##STR2## B being a lower alkylene or O-lower alkylene group, ##STR3## R.sub.4 being a hydrogen atom or lower alkyl group, or ##STR4## m denotes a number of 1-3, and n stands for 1 or 2. The derivative has vasodilative effects, hyperkinemic effects, platelet aggregation inhibitory effects, thromboxane A.sub.2 formation inhibitory effects and so on, and are hence useful as a pharmaceutical product such as vasodilator, antihypertensive, antithrombotic agent, antiarteriosclerotic agent or the like.Type: GrantFiled: April 7, 1986Date of Patent: April 12, 1988Assignee: Kowa Co., Ltd.Inventors: Noboru Shimizu, Hiroyuki Ishiwata, Tomio Ohta, Hiroshi Ishihama, Yasumi Uchida
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Patent number: 4736028Abstract: A process for the preparation of a 2-cyanamino-4,6-dialkoxy-1,3,5-triazine of the formula ##STR1## in which R.sup.1 and R.sup.2 are each alkoxy, which comprises reacting ##STR2## with Na.sub.2 N--CN to produce ##STR3## acidifying that to produce ##STR4## and reacting that with at least twice the molar amount of R.sup.2 Na in the presence of a diluent, then adding water and acidifying the mixture.The intermediates are new and the known end products can be used to synthesize herbicides.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Bayer AktiengesellschaftInventor: Hans-Jochem Riebel
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Patent number: 4735950Abstract: This invention relates to 1,3-dihydro-6-methyl-7-hydroxy-furo-(3,4-c)-pyridine derivatives of the general formula I ##STR1## wherein each of A.sub.1 and A.sub.2 independently represents various hydrocarbon groups and therapeutically acceptable addition salts thereof; to a process for the preparation of the same comprising oxidizing the secondary alcohol .alpha..sup.4, 3-o-isopropylidene-1-methyl-5-(1-hydroxy-1-A.sub.1)-methyl pyridine by any usual technique, reacting the resultant ketone with a compound of the general formula XA.sub.2 wherein X stands for Br or I in the presence of magnesium in diethyl ether at the boil and treating the resultant tertiary alcohol with an acidic agent to provoke breaking of the isopropylidene ring and 3,4-cyclisation; and to pharmaceutical compositions containing these derivatives useful for example in diuresis.Type: GrantFiled: March 30, 1987Date of Patent: April 5, 1988Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S)Inventor: Andre Esanu
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Patent number: 4735965Abstract: The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks.Type: GrantFiled: May 28, 1986Date of Patent: April 5, 1988Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Gabor Kovacs, Geza Galambos, Istvan Tomoskozi, Karoly Kanai, Peter Gyory, Peter Kormoczy, Istvan Stadler, Laszlo Szekeres, Gyula Papp, Eva Udvary, Pal Hadhazy, Jeno Marton, Gyorgy Dorman
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Patent number: 4735949Abstract: Disubstituted 7-pyrrolidinoquinoline- and -naphthyridine-3-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.Type: GrantFiled: June 22, 1987Date of Patent: April 5, 1988Assignee: Warner-Lambert CompanyInventors: John M. Domagala, Susan E. Prugh, Joseph P. Sanchez, Marjorie S. Solomon
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Patent number: 4736036Abstract: A process is disclosed for the manufacture of quinolinic acid by oxidizing quinoline with ruthenium tetraoxide in the presence of hypochlorite solution in which a certain amount of base is added prior to the inception of the oxidation reaction. The disclosed process provides greatly improved yields of high purity quinolinic acid.Type: GrantFiled: August 8, 1983Date of Patent: April 5, 1988Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 4736031Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1986Date of Patent: April 5, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata