Patents Examined by E. Bernhardt
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Patent number: 5187277Abstract: Disclosure is made of a compound of the formula: ##STR1## and pharmaceutically acceptable salts thereof. A salt, for instance, the dihydrochloride is usable as a compound which exhibits psychotropic and antiemetic effect.Type: GrantFiled: August 23, 1991Date of Patent: February 16, 1993Inventors: Igor V. Komissarov, Vladimir I. Dulenko, Valentin N. Voschula, Nikolai A. Kharin, Sergei V. Naletov, Alexandr B. Mamonov
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Patent number: 5185332Abstract: New heterocyclic compounds of formula I ##STR1## In which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 --group; R.sub.1 and R.sub.2 independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrgen or lower alkyl or R.sub.1 and R.sub.2 together form a susbtituted or unsubstituted 5 or 6 membered ring which may contain 1 to 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 means independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.Type: GrantFiled: March 15, 1991Date of Patent: February 9, 1993Assignee: Orion-yhtyma OyInventors: Heimo O. Haikala, Erkki J. Honkanen, Kari K. Lonnberg, Pentti T. Nore, Jarmo J. Pystynen, Anne M. Luiro, Aino K. Pippuri
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Patent number: 5183891Abstract: A method for the preparation of compounds of the formula ##STR1## wherein X represents a group of the formula OR.sub.1 or NR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 independently represent H or an organic group that forms a stable covalent bond with the N or O of said X; Y is H or an organic group that forms a stable ester with the adjacent COO group; R is an alkyl or aryl group optionally substituted with one or more stable organic substituents; each R.sub.3 independently represents a stable organic group; and n is an integer from 0 to 3;the method using new intermediates of the formula ##STR2## wherein R.sub.3 and Y have the foregoing meanings; W is either F or Cl;and R.sub.9 is a hydrocarbon such as a C.sub.1 -C.sub.4 alkyl or alkenyl group.Type: GrantFiled: November 9, 1989Date of Patent: February 2, 1993Assignees: Orsan, OrsemInventors: Jeffrey Labovitz, William J. Guilford, Lawrence Fang, Yi Liang
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Patent number: 5182280Abstract: The present invention relates to novel compounds derived from benzimidazole, characterized in that they correspond to the formula I, or their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical,n may have the values 0 or 1,m may have the values 2 to 4,X, Y, Z and W, equal or different, represents a nitrogen atom or a carbon atom bonded to a hydrogen atom, a halogen or another alkyl, aryl, alkoxycarbonyl, carboxy, hydroxyl, sulfonic and alkylsulfonic radical. The present invention relates also to the treatment of various allergic disorders caused by histamine.Type: GrantFiled: July 25, 1991Date of Patent: January 26, 1993Assignee: Laboratorios Del Dr. Esteve, S. A.Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
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Patent number: 5182285Abstract: A cell-protective composition for preventing or treating of a peptic ulcer due to topical endogenous lesion of gastric or duodenal mucous membrane comprises as a physiologically active component the cyclo-(1-alanyl-amino-1-cyclopentanecarbonyl)cyclodipeptide. The subject composition is designated for administration by oral or parenteral route. It is substantially non-toxic and well tolerated, and acts beneficially, even at low dosage level.Type: GrantFiled: April 6, 1990Date of Patent: January 26, 1993Assignee: Spojene Podniky Pro Zdravotnickou VyrobuInventors: Evzen Kasafirek, Vaclav Plaisner, Libuse Korbova, Jirj Kohout, Jirina Cizkova, Ivan Krejci, Arnost Pospisil, Milan Pesak, Antonin Sturc, Jiri Krepelka, Antonin Dlabac, Jiri Vanzura
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Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
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Patent number: 5180728Abstract: A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl,R.sup.4 is imidazolyl, which may have alkyl or imino-protective group as substituents, or pyridyl,A is lower alkylene, andis single bond or double bond, and pharmaceutically acceptable salts thereof, having 5-HT antagonism.Type: GrantFiled: August 27, 1990Date of Patent: January 19, 1993Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Kiyotaka Ito, Hisashi Takasugi
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Patent number: 5177239Abstract: A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal.dbd.Cl,Br,I) with an alkoxide of the structure ##STR2## wherein M is an alkali metal and R.sup.2c is lower alkyl. The resulting phosphonic acid ester is an intermediate in preparing a squalene synthetase inhibitor which is used for inhibiting cholesterol biosynthesis.Type: GrantFiled: July 17, 1989Date of Patent: January 5, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Janak Singh, Richard H. Mueller
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Patent number: 5177077Abstract: A disubstituted piperazine compound having the formula I ##STR1## wherein R.sup.1 is thienyl or phenyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.2 is thienyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.3 is C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl which all may be substituted with hydroxy, oximino or keto in any position giving a stable tertiary amine or R.sup.3 is C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl which in any position may be substituted as above, but is terminally substituted with phenoxy, phenyl, thienyl, furyl, methoxy or --CN and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.Type: GrantFiled: July 11, 1991Date of Patent: January 5, 1993Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Erling Guddal, Erik Nielsen
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Patent number: 5175167Abstract: Hetarylalkenes of the general formula I ##STR1## where Ar is hetaryl,A is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.3 -alkyl or unsubstituted or monosubstituted, disubstituted or trisubstituted aryl or aralkyl, ##STR2## Z is whereR is hydrogen, C.sub.2 -C.sub.4 -acyl, unsubstituted or substituted benzoyl, C.sub.1 -C.sub.4 -alkylsulfonyl, unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted phenylsulfonyl or a radical R.sup.1,R.sup.1 is C.sub.1 -C.sub.4 -alkyl or unsubstituted or substituted phenyl or benzyland Hal is fluorine, chlorine, bromine or iodine,and B is unsubstituted or substituted mononuclear or dinuclear aryl, aralkyl or hetaryl,and their N-oxides and addition salts, the preparation of these substances, intermediates for this purpose and the preparation thereof, fungicides containing hetarylalkenes and a corresponding method for controlling harmful fungi.Type: GrantFiled: February 8, 1991Date of Patent: December 29, 1992Assignee: BASF AktiengesellschaftInventors: Bernhard Zipperer, Manfred Lauer, Norbert Goetz, Thomas Zierke, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5175304Abstract: Polyetherimide oligomers having crosslinking end cap moieties which provide improved solvent-resistance to cured composites are generally represented by the formula: ##STR1## wherein X=--O-- or --S--; ##STR2## n=1 or 2; ##STR3## E=allyl or methallyl; R=a trivalent C.sub.(6-13) aromatic organic radical;R.sub.1 =any of lower alkyl, lower alkoxy, aryl, or substituted aryl;R'=a divalent C.sub.(6-30) aromatic organic radical;j=0, 1, or 2; andG=--CH.sub.2 --, --O--, --S--, or --SO.sub.2 --Blends generally comprise substantially equimolar amounts of the oligomers and a comparable, compatible, noncrosslinking, etherimide polymer of substantially the same backbone. The crosslinkable oligomers are made by reacting substituted phthalic anhydrides with hydroxyaryl amines and suitable crosslinking end cap reactants, or by self-condensation of phthalimide salts followed by capping the polymers.Type: GrantFiled: May 10, 1990Date of Patent: December 29, 1992Assignee: The Boeing CompanyInventors: Clyde H. Sheppard, Hyman R. Lubowitz
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Patent number: 5173484Abstract: An antibacterially active quinolone or naphthyridonecarboxylic acid derivative of the formula ##STR1## in which R.sup.1 stands for various organic radical,R.sup.2 stands for hydrogen, alkyl having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl,R.sup.3 stands for hydrogen or amino,R.sup.4 stands for a radical of the formula ##STR2## A stands for N or C-R.sup.5, whereinR.sup.5 stands for hydrogen, halogen methyl, cyano or nitro or else together with R.sup.1 can form a bridge of the structure ##STR3## or a pharmaceutically utilizable hydrate, acid addition salt, alkali metal salt, alkaline earth metal salt, silver salt or guanidinium salt of the carboxylic acid when R.sup.2 is hydrogen.Type: GrantFiled: May 14, 1991Date of Patent: December 22, 1992Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5171747Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;D is an oxygen atom or a NOR group, wherein R.dbd.H or C.sub.1 -C.sub.4 alkyl;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group; andR'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain,useful as drugs.Type: GrantFiled: October 16, 1990Date of Patent: December 15, 1992Assignee: Delalande S.A.Inventors: Francois X. Jarreau, Vincenzo Rovei, Jean-Jacques Koenig, Alain R. Schoffs
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Patent number: 5169955Abstract: A process for producing a 2-hydroxyquinoxaline which may be substituted with one or more substituents selected from the group consisting of halogen, lower alkyl and lower alkoxy, which comprises reacting o-phenylenediamine which may be substituted with one or more substituents selected from the group consisting of halogen, lower alkyl and lower alkoxy with glyoxylic acid in a lower aliphatic alcohol solvent without using a catalyst is disclosed. By the process according to the present invention, the 2-hydroxyquinoxaline derivatives can be obtained at a high purity and a high yield without using any catalyst.Type: GrantFiled: February 21, 1991Date of Patent: December 8, 1992Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hisabumi Kobayashi, Hiroshi Maruyama, Shuji Kawata, Sadahiko Noda
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Patent number: 5169853Abstract: Fluorinated 1- cyclopropyl-7-(substituted-pyridinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxy lic acids of the formula ##STR1## wherein R is hydrogen, R' and R" are hydrogen or fluoro, and Z is 3- or 4-pyridinyl substituted by alkyl groups or substituted alkyl groups, are superior antibacterial agents. They are prepared via a coupling reaction between the corresponding esters (R=alkyl) having a halo group in the 7-position and a substituted (trialkylstannyl)-pyridine.Type: GrantFiled: September 9, 1991Date of Patent: December 8, 1992Assignee: Sterling Drug Inc.Inventors: George Y. Lesher, Baldev Singh, Michael Reuman, Sol J. Daum
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Patent number: 5166205Abstract: The present invention relates to novel derivatives of 1-diphenylmethyl piperazinyl, characterized in that they correspond to the general formula I, and their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical,n may have the values 2 to 4,X, Y, Z and W, equal or different, represent a nitrogen atom or a carbon atom linked to a hydrogen atom, a halogen or to another alkyl, aryl, carboxyalkyl, carbonyl, hydroxyl, sulfonyl and alkylsulfonyl radical.The present invention also relates to the process of preparing these compounds and their use for the manufacture of medicaments intended for prophylaxis and for the treatment of various allergic disorders caused by histamine.Type: GrantFiled: July 25, 1991Date of Patent: November 24, 1992Assignee: Laboratorios Del Dr. Esteve, S. A.Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
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Patent number: 5164391Abstract: The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula ##STR1## wherein M is --CONH--NHR.sup.1 group, --CONH--OR.sup.2 group, ##STR2## in which R.sup.1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphthyl radical, a substituted naphthyl group, a pyridyl radical, a furyl radical or a thienyl radical, R.sup.2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R.sup.3 and R.sup.4 are the same or different independently, each being a phenyl radical, or an aralkyl group, or R.sup.3 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.4 and a possible nitrogen or oxygen atom, R.sup.5 forms a substituted or non-substituted saturated heterocyclic ring together with R.sup.6 and a possible nitrogen or oxygen atom, R.sup.Type: GrantFiled: September 13, 1990Date of Patent: November 17, 1992Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Noboru Tomiya, Kiichi Sawai, Kenji Miura, Toshinao Usui, Yasuaki Kondo, Yukiya Tanaka, Shigeyoshi Nakamura, Tsunemasa Suzuki, Motohide Hayashi
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Patent number: 5162320Abstract: Compounds of formula I are described, ##STR1## wherein: R.sub.1 and R.sub.2, that can be the same or different, are hydrogen or acyl groups;R.sub.3 and R.sub.4, that can be the same or different, are hydrogen or optionally substituted alkyl groups.The compounds of formula I are prepared by oxydation of the compounds of formula II: ##STR2## wherein the groups R'.sub.1, R'.sub.2, R'.sub.3 and R'.sub.4 have the same meanings as R.sub.1, R.sub.2, R.sub.3 and R.sub.4 or groups convertible to the latter.The compounds of formula I have remarkable antitumor activity.Type: GrantFiled: October 25, 1990Date of Patent: November 10, 1992Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Francis Johnson, Ernesto Menta, Silvano Spinelli, Sergio Tognella
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Patent number: 5157182Abstract: A dehydrocyclization process is described for producing polynuclear organic compounds by contacting a starting organic material having at least one ring moiety comprising at least two adjacent ring carbon atoms each bonded to an independently selected monovalent radical comprising at most about eight carbon atoms provided at least one of the monovalent hydrocarbon radicals comprises more than one carbon atom with a crystalline copper aluminum borate catalyst. The preferred catalyst comprises at least one member selected from the group consisting of (a) crystalline copper aluminum borate and (b) zero valent copper on a support comprising at least one member selected from the group consisting of Al.sub.4 B.sub.2 O.sub.9 and the crystalline copper aluminum borate, the zero valent copper on the support being formed by the reduction of the crystalline copper aluminum borate.Type: GrantFiled: June 19, 1991Date of Patent: October 20, 1992Assignee: Amoco CorporationInventors: Patrick E. McMahon, Larry C. Satek
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Patent number: 5153203Abstract: Antibacterial quinolone derivatives represented by the following formula and salts thereof are disclosed. ##STR1## wherein R.sup.1 meawns a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted phenyl group, R.sup.2 denotes a hydrogen atom or a carboxyl-protecting group, R.sup.3 represents a hydrogen or halogen atom or an amino, mono- or di-(lower alkyl)amino, hydroxyl or lower alkoxyl group, X is a hydrogen or halogen atom, Y means a nitrogen atom or a group C-R.sup.4 in which R.sup.4 is a hydrogen or halogen atom or a lower alkyl or lower alkoxyl group or is a group ##STR2## which forms a ring together with R.sup.1 (i.e., the asterisked carbon atoms are linked to the N(1) atom of the quinolone skeleton), and A denotes a specific N-containing group. Preparation processes of the quinolone derivatives and antibacterial agents containing the same are also disclosed.Type: GrantFiled: March 30, 1990Date of Patent: October 6, 1992Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Takashi Yatsunami, Hitodshi Yamamoto, Yasuhiro Kuramoto, Norihiro Hayashi, Akira Yazaki, Satoshi Inoue, Shuichiro Noda, Hirotaka Amano