Patents Examined by Paul M. Coughlan, Jr.
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Patent number: 4548818Abstract: Compounds having activity against chronic obstructive airway disease or cardiac disease, characterized by the formula ##STR1## wherein R.sup.1 is n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexylmethyl, and R.sup.2 is hydrogen or methyl, provided that R.sup.2 is methyl when R.sup.1 is n-propyl, n-butyl or isobutyl, or a physiologically acceptable salt thereof.Type: GrantFiled: November 23, 1981Date of Patent: October 22, 1985Inventors: Per G. Kjellin, Carl G. A. Persson
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Patent number: 4520194Abstract: A 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin derivative of the formula; ##STR1## wherein R.sub.3 is hydrogen or a residue of a nucleophilic compound; R.sub.2 NH is an amino group which may optionally be protected, pharmaceutically acceptable salt or ester thereof, is found to have excellent anti-bacterial activity against a broad spectrum of bacteria inclusive of gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae and Citrobacter freundii. Thus, this compound may be used for an antibacterial agent in therapeutical purposes.Type: GrantFiled: July 6, 1978Date of Patent: May 28, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
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Patent number: 4518754Abstract: Novel imido copolymers are prepared by copolymerizing:[i] a bis-maleimide of the structural formula: ##STR1## [ii] an olefinically unsaturated comonomer copolymerizable therewith. The subject copolymers are applicable to the production of a variety of useful shaped articles, coatings, laminates, foams, and the like.Type: GrantFiled: May 30, 1979Date of Patent: May 21, 1985Assignee: Rhone-Poulenc IndustriesInventors: Jean L. Locatelli, Bernard Rollet
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Patent number: 4518755Abstract: Novel imido copolymers are prepared by copolymerizing:[i] a bis-maleimide of the structural formula: ##STR1## with [ii] a (meth)acrylic acid amide.The subject copolymers are applicable to the production of a variety of useful shaped articles, coatings, laminates, foams, and the like.Type: GrantFiled: May 30, 1979Date of Patent: May 21, 1985Assignee: Rhone-Poulenc IndustriesInventors: Jean L. Locatelli, Bernard Rollet
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Patent number: 4517361Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula -SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.Type: GrantFiled: March 31, 1983Date of Patent: May 14, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuo Numata, Isao Minamida, Masayoshi Yamaoka, Mitsuru Shiraishi, Toshio Miyawaki
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Patent number: 4515788Abstract: This invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen or lower alkyl, andR.sup.4 is lower alkyl, lower alkoxy, acyloxymethyl, lower alkylthiomethyl, lower alkoxymethyl, halogen, lower alkenyl or hydrogen,and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 27, 1982Date of Patent: May 7, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi, Hideaki Yamanaka
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Patent number: 4515795Abstract: A pharmaceutical composition containing as an essential ingredient a compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is an .omega.- or (.omega.-1)-hydroxyalkyl group having from 5 to 8 carbon atoms in which the hydroxy group is separated from the xanthine nucleus by at least 2 carbon atoms, radicals R.sub.1 and R.sub.3 which are no hydroxyalkyl group, are hydrogen or methyl and equal or different, and R.sub.2 is said hydroxyalkyl group or methyl, a compound of formula (I) and a pharmaceutical product for treatment of diseases involving insufficiency of cerebral blood flow.Type: GrantFiled: March 4, 1977Date of Patent: May 7, 1985Assignee: Hoechst AktiengesellschaftInventors: Heinz-Joachim Hinze, Alfons Soder, Kurt Popendiker
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Patent number: 4515945Abstract: N-alkyl-4-(4-pyridinyl)isatoic anhydrides are prepared by alkylating a 4-(4-pyridinyl)isatoic anhydride, suitably in the presence of sodium hydride and N,N-dimethylformamide. The products are particularly useful in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.Type: GrantFiled: August 15, 1983Date of Patent: May 7, 1985Assignee: Ethyl CorporationInventors: Paul F. Ranken, Thomas J. Walter
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Patent number: 4515789Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.Type: GrantFiled: April 7, 1983Date of Patent: May 7, 1985Assignee: Bayer AktiengesellschaftInventors: Karl G. Metzger, Wilfried Schrock, Dieter Habich, Paul Naab, Hans-Joachim Zeiler
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Patent number: 4515956Abstract: A process has been discovered for selective preparation of isomers and enantiomers of 2,2-dimethyl-3-(2,2-dihalovinyl)cyclopropane carboxylic acids. In this process an adduct of an alkyl 3,3-dimethyl-4-pentenoate and a substituted 2-oxazolidone is reacted with a substituted dihalomethane compound. The resulting compound is cyclized, dehydrohalogenated and hydrolyzed to yield the desired product. These cyclopropane carboxylic acids are useful precursors for pyrethroid insecticides.Type: GrantFiled: August 13, 1984Date of Patent: May 7, 1985Assignee: The Dow Chemical CompanyInventor: William A. Kleschick
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Patent number: 4514403Abstract: A hydrouracil compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein A represents --CH.dbd.CH--CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, and R represents hydrogen or methyl. Such compounds are useful as analgesics.Type: GrantFiled: September 17, 1981Date of Patent: April 30, 1985Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Chiaki Tashiro, Takeshi Kawakita, Ichiro Horii, Koretake Anami
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Patent number: 4509972Abstract: Compounds of the formula ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types, and salts thereof. The compounds as well as their salts are useful as herbicides.Type: GrantFiled: March 28, 1983Date of Patent: April 9, 1985Assignee: Celamerck GmbH & Co. KGInventors: Rudolf Mengel, Ludwig Schroder, Werner Stransky, Gerbert Linden, Gerhart Schneider, Sigmund Lust
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Patent number: 4510138Abstract: An antibacterial composition is provided consisting of a 7-[2-(2-aminothiazol)-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin compound of the formula ##STR1## wherein R.sub.2 NH is amino or a protected amino group, n is an integer of 1 to 3 and R is a di-C.sub.1-3 alkylamino, carboxyl or sulfo group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: September 29, 1982Date of Patent: April 9, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
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Patent number: 4507293Abstract: The invention relates to novel cephem compounds, of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 15, 1983Date of Patent: March 26, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi, Toshiyuki Chiba, Kiyoshi Tsuji
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Patent number: 4507298Abstract: The invention relates to new 6-{4-(.omega.-(1-imidazolyl)-alkyl)-phenyl}-3-oxo-2,3,4,5-tetrahydro-pyrid azines having the general formula I ##STR1## and acid addition salts thereof, and to a process for the treatment of inflammatory, atherosclerotic and thromboembolic diseases especially in humans.Type: GrantFiled: July 12, 1982Date of Patent: March 26, 1985Assignee: A. Nattermann & Cie GmbHInventors: Hans-Heiner Lautenschlager, Gerd Hilboll, Hugo Friehe, Josef P. Lohr
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Patent number: 4507299Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.1-3 alkyl substituted amino; heteroaryl; formyl C.sub.2-4 alkenyl; or C.sub.2-4 alkenyl; andR.sup.2 is straight or branched C.sub.Type: GrantFiled: December 27, 1982Date of Patent: March 26, 1985Assignee: Merck & Co., Inc.Inventor: David B. R. Johnston
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Patent number: 4506076Abstract: The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5, --NHCO--R.sup.5, or ##STR2## R.sup.5 is aryl or heterocyclic, either of which may be substituted, R.sup.6 is hydrogen or lower alkyl, andA is lower alkylene, or a salt thereof.Type: GrantFiled: April 29, 1981Date of Patent: March 19, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
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Patent number: 4504481Abstract: The invention relates to new benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.Type: GrantFiled: December 27, 1983Date of Patent: March 12, 1985Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Edit Toth, Jozsef Torley, Eva Palosi, Szabolcs Szeberenyi, Laszlo Szporny, Sandor Gorog, Istvan Hajdu
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Patent number: 4504478Abstract: An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen, 1-6C alkoxy or 1-6C alkylthio; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.5 ; R.sup.4 and R.sup.5 are a variety of radicals described in the specification; --A-- is of the formula II or III: ##STR2## in which R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.Type: GrantFiled: September 7, 1982Date of Patent: March 12, 1985Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Frederic H. Jung, Gareth M. Davies
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Patent number: 4503221Abstract: The process for preparing cephalosporanic acid derivatives ##STR1## and salts thereof with bases as well as solvates thereof, comprising reacting a compound of the formula II: ##STR2## wherein R.sub.3 represents hydrogen or an amino protecting group and R.sub.2 represents hydrogen, an easily removable ester group or other carboxyl protecting group, with a compound of formula IIIa, ##STR3## wherein R.sub.1 represents hydrogen, an easily removable ester group or other carboxyl protecting group, and R.sub.4 is a 2-benzothiazol group and salts thereof with bases, and if required removing any ester group or protecting group.Type: GrantFiled: June 20, 1983Date of Patent: March 5, 1985Assignee: Sandoz Ltd.Inventors: Hans Fliri, Helmut Hamberger