Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/447)
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Patent number: 5756498Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.In accordance with the present invention, compounds of Formula (I) are disclosed ##STR1## wherein the substituents are as defined in the specification.Type: GrantFiled: January 11, 1996Date of Patent: May 26, 1998Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5750565Abstract: Tetrahydrofurans tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: May 31, 1995Date of Patent: May 12, 1998Assignee: Cytomed, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 5747518Abstract: The substituted thiophene derivative of the invention which is represented by the general formula (1) has a broad disease spectrum for a pathogenic fungus of various crops, exhibits an excellent controlling effect on disease such as gray mold, powdery mildew and rust in particular, and is also effective for a resistant fungus of conventional fungicides which has become a serious problem, and consequently is useful for an agricultural and horticultural fungicide.Type: GrantFiled: April 3, 1996Date of Patent: May 5, 1998Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Yukihiro Yoshikawa, Kanji Tomiya, Hiroyuki Katsuta, Hideo Kawashima, Osamu Takahashi, Shunichi Inami, Yuji Yanase, Junro Kishi, Hitoshi Shimotori, Naofumi Tomura
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Patent number: 5739140Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.Type: GrantFiled: October 23, 1996Date of Patent: April 14, 1998Assignee: Monsanto CompanyInventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
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Patent number: 5728696Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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Patent number: 5710173Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.Type: GrantFiled: June 7, 1995Date of Patent: January 20, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Asaad S. Nematalla, Gerald McMahon
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Patent number: 5698581Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 7, 1995Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5681966Abstract: Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: June 7, 1995Date of Patent: October 28, 1997Assignee: Cytomed, Inc.Inventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
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Patent number: 5652250Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 21, 1995Date of Patent: July 29, 1997Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Angelo Crugnola, Antonio Longo, Maria Gabriella Brasca, Dario Ballinari
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Patent number: 5646153Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.Type: GrantFiled: May 11, 1995Date of Patent: July 8, 1997Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5627198Abstract: The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.Type: GrantFiled: December 4, 1995Date of Patent: May 6, 1997Assignee: Hafslund Nycomed Pharma AktiengesellschaftInventors: Peter Esch, Robertson Towart, Franz Rovenszky
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5571810Abstract: This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: April 13, 1995Date of Patent: November 5, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Nobukiyo Konishi, Katsuya Nakamura
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Patent number: 5567723Abstract: Compounds having the structural formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl; R.sup.1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.1 -C.sub.4 haloalkyl and nitro; and R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkoxyalkyl. The compounds of this invention are effective for controlling mites and nematodes.Type: GrantFiled: July 5, 1995Date of Patent: October 22, 1996Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Mark A. Dekeyser, Derek J. McPhee, Paul T. McDonald
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Patent number: 5567721Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: October 22, 1996Assignee: Centre International de Recherches DermatologiquesInventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5552430Abstract: The present invention is concerned with antiretroviral (e.g. anti-HIV-1) compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifluoromethyl; R.sup.4 is trifluoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical --Alk--R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.Type: GrantFiled: May 2, 1995Date of Patent: September 3, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Marc G. C. Verdonck, Paul A. J. Janssen
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Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5506259Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.Type: GrantFiled: July 27, 1994Date of Patent: April 9, 1996Assignee: Zambon Group S.p.A.Inventors: Gabriele Norcini, Francesco Santangelo
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Patent number: 5506263Abstract: Benzyl derivatives of the formula I ##STR1## where A is CH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B is OH, alkylthio, alkoxy or alkylamino,U, V, W are hydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' is hydrogen or alkyl andR is hydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.Type: GrantFiled: December 14, 1994Date of Patent: April 9, 1996Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5482966Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: June 13, 1994Date of Patent: January 9, 1996Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5472956Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.Type: GrantFiled: January 21, 1994Date of Patent: December 5, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Richard F. Borch, James P. Schmidt
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Patent number: 5420164Abstract: A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.Type: GrantFiled: May 3, 1993Date of Patent: May 30, 1995Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tadashi Mishina, Kanou Harada, Joji Yasuoka, Hidenobu Kushuhara, Noriyoshi Izumi
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Patent number: 5416110Abstract: Benzyl derivatives of the formula I ##STR1## where A isCH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B isOH, alkylthio, alkoxy or alkylamino,U, V, W arehydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' ishydrogen or alkyl andR ishydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.Type: GrantFiled: July 30, 1993Date of Patent: May 16, 1995Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5399585Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.Type: GrantFiled: August 30, 1993Date of Patent: March 21, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
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Patent number: 5387594Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: August 4, 1992Date of Patent: February 7, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5321042Abstract: The invention relates to the use of substituted tetrahydrothiophenes, some of which are known, as medicaments, in particular as antimycotic agents, to new active substances and to processes for their preparation.Type: GrantFiled: October 8, 1992Date of Patent: June 14, 1994Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Franz Kunisch, Manfred Plempel
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Patent number: 5317021Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.Type: GrantFiled: November 4, 1992Date of Patent: May 31, 1994Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
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Patent number: 5314891Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: September 10, 1992Date of Patent: May 24, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, Keith Oldham, David Waterson
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Patent number: 5306727Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.Type: GrantFiled: April 30, 1993Date of Patent: April 26, 1994Assignee: Research Corporation Technologies, Inc.Inventors: Richard F. Borch, James P. Schmidt
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Patent number: 5298515Abstract: Abstract of the Disclosure: N-Hetaryl-2-nitroanilines Ia and Ib ##STR1## (R.sup.1 =H, halogen, C.sub.1 -C.sub.4 -alkoxy; R.sup.2 =NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -haloalkyl; R.sup.3 =NO.sub.2, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; R.sup.4 =CO--R.sup.5,CO--OR.sup.5, SO.sub.2 R.sup.5 with R.sup.5 =C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl or naphthyl; Q=H, alkali metal or alkaline earth metal ion, substituted or unsubstituted ammonium ion, phosphonium, sulfonium or sulfoxonium ion, one equivalent of a transition metal cation; Het=thienyl, thiazolyl, isothiazolyl or thiadiazolyl, each of which is linked via a ring carbon to the basic element, which can be fused to a non-aromatic C.sub.5 -C.sub.8 -ring and/or can additionally carry on each other carbon one of the following: CN, SCN, NO.sub.2, halogen, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, substituted or unsubstituted phenyl, naphthyl, benzyl or thienyl, CO--R.sup.5, CO--OR.sup.5, NR.sup.6 R.sup.7 ; R.Type: GrantFiled: October 6, 1992Date of Patent: March 29, 1994Assignee: BASF AktiengesellschaftInventors: Juergen Schubert, Reiner Kober, Gerhard Hamprecht, Hubert Sauter, Uwe Kardorff, Christoph Kuenast
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Patent number: 5292771Abstract: Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.Type: GrantFiled: October 8, 1992Date of Patent: March 8, 1994Assignee: Orion-yhtyma OyInventors: Reijo J. Backstrom, Erkki J. Honkanen, Jarmo J. Pystynen, Anne M. Luiro, Paivi A. Aho, Inge-Britt Y. Linden, Erkki A. O. Nissinen, Pentti Pohto
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Patent number: 5288750Type: GrantFiled: January 31, 1991Date of Patent: February 22, 1994Assignee: Orion-yhtyma OyInventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
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Patent number: 5270301Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.Type: GrantFiled: May 7, 1990Date of Patent: December 14, 1993Assignee: ICI Americas Inc.Inventor: Donald J. Wolanin
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Patent number: 5196410Abstract: A transdermal flux enhancing pharmaceutical composition for transdermal administration to a human or lower animal subject comprising a safe and effective amount of pharmacologically active compound or a prodrug thereof, an aqueous solvent system comprising from about 15 to 75% by volume of one or more water miscible solvents, and a penetration enhancer selected from certain 1-alkylazacycloheptan-2-ones and cis-olefin compounds of the formulaCH.sub.3 (CH.sub.2).sub.x CH.dbd.CH(CH.sub.2).sub.y R.sup.3where R.sup.3 is CH.sub.2 OH, CH.sub.2 NH.sub.2 or COR.sup.4 and R.sup.4 is OH or (C.sub.1 -C.sub.4)alkoxy, x and y are each an integer from 3 to 13 and the sum of x and y is from 10 to 16; methods for their use in treating various illnesses in a human or lower animal by transdermal administration of said composition.Type: GrantFiled: September 11, 1991Date of Patent: March 23, 1993Assignee: Pfizer Inc.Inventors: Michael L. Francoeur, Russell O. Potts
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5185363Abstract: Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5- and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.Type: GrantFiled: September 30, 1991Date of Patent: February 9, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Daniel J. Kerkman, Jonathan G. Martin, Andrew O. Stewart, James B. Summers
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Patent number: 5162364Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.Type: GrantFiled: June 11, 1991Date of Patent: November 10, 1992Assignee: Adir et CompagnieInventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
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Patent number: 5153225Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: April 9, 1991Date of Patent: October 6, 1992Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5145867Abstract: Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, processes for the preparation thereof and the use thereof as medicines.Compounds I ##STR1## R(1) hydrogen, (C.sub.1 -C.sub.4)-alkyl and Na, K, NH.sub.4, Ca, Mg, R(2) and R(3) hydrogen, alkyl groups which can also be linked together in a ring,X oxygen, sulfur, SO, SO.sub.2, NR(6) [with R(6)=hydrogen-alkyl], CH.sub.2, CO, or a bond,R(4) phenyl, thienyl, which are unsubstituted or substitutedR(5) hydrogen, (C.sub.1 -C.sub.4)-alkyl,n 1, 2, 3 or 4,where the naphthyl system is unsubstituted or substituted like the phenyl radical of R(4),and where X and R(4) together can also be Cl are medicaments for treating sickle-cell anemia.Type: GrantFiled: April 6, 1990Date of Patent: September 8, 1992Assignee: Hoechst AktiengesellschaftInventors: John C. Ellory, Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Wulf Merkel
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Patent number: 5130331Abstract: The novel substituted 3-thienylthioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.4 alkyl substituted by a C.sub.3 -C.sub.6 cycloalkyl radical, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.3 -C.sub.6 cycloalkyl substituted by a C.sub.1 -C.sub.4 alkyl radical; R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl, or phenyl substituted by from 1 to 3 radicals from the group halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.6 haloalkyl having from 1 to 9 halogen atoms; Z is a group --NH--CS--NH--, --N .dbd.C(SR.sub.5)--NH-- or --N.dbd.C.dbd.N--; and R.sub.5 is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.5 alkenyl; with the proviso that at least one of the radicals R.sub.2, R.sub.3 and R.sub.4 is other than hydrogen; and the salts of compounds of formula I in which Z is the group --N.dbd.C(SR.sub.5 )--NH--, have valuable pesticidal properties.Type: GrantFiled: October 9, 1990Date of Patent: July 14, 1992Assignee: Ciba-Geigy CorporationInventor: Alfons Pascual
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Patent number: 5128367Abstract: New divalent metal salts of 2-[N,N-di(carboxymethyl)amino]-3-cyano-4-carboxymethylthiophene-5-carboxyl ic acid, which can be used therapeutically especially in the treatment of bone diseases, cutaneous and vascular ageing, hepatic diseases and dental diseases.Type: GrantFiled: August 31, 1990Date of Patent: July 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Jacqueline Bonnet, Martine Brisset, Yannis Tsouderos
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Patent number: 5118681Abstract: S-beta-dicarbonyl substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carries, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.Type: GrantFiled: July 28, 1989Date of Patent: June 2, 1992Assignee: Rohm and Haas CompanyInventors: David R. Amick, Katherine E. Flynn, Cherylann Schieber
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Patent number: 5116848Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.Type: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar