Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/447)
  • Patent number: 5756498
    Abstract: 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: Grant
    Filed: January 11, 1996
    Date of Patent: May 26, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5750565
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: May 12, 1998
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 5747518
    Abstract: 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: Grant
    Filed: April 3, 1996
    Date of Patent: May 5, 1998
    Assignee: 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
  • Patent number: 5739140
    Abstract: 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: Grant
    Filed: October 23, 1996
    Date of Patent: April 14, 1998
    Assignee: Monsanto Company
    Inventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
  • Patent number: 5728696
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5712393
    Abstract: 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: Grant
    Filed: November 24, 1995
    Date of Patent: January 27, 1998
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5710173
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: January 20, 1998
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Asaad S. Nematalla, Gerald McMahon
  • Patent number: 5698581
    Abstract: 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: Grant
    Filed: April 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5688817
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: November 18, 1997
    Assignee: Centre Int'l. De Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5681966
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 28, 1997
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
  • Patent number: 5652250
    Abstract: 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: Grant
    Filed: November 21, 1995
    Date of Patent: July 29, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Franco Buzzetti, Angelo Crugnola, Antonio Longo, Maria Gabriella Brasca, Dario Ballinari
  • Patent number: 5646153
    Abstract: 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: Grant
    Filed: May 11, 1995
    Date of Patent: July 8, 1997
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
  • Patent number: 5635527
    Abstract: 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: Grant
    Filed: February 6, 1996
    Date of Patent: June 3, 1997
    Assignee: The Green Cross Corporation
    Inventors: 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
  • Patent number: 5627198
    Abstract: 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: Grant
    Filed: December 4, 1995
    Date of Patent: May 6, 1997
    Assignee: Hafslund Nycomed Pharma Aktiengesellschaft
    Inventors: Peter Esch, Robertson Towart, Franz Rovenszky
  • Patent number: 5602119
    Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: February 11, 1997
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5571810
    Abstract: 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: Grant
    Filed: April 13, 1995
    Date of Patent: November 5, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Nobukiyo Konishi, Katsuya Nakamura
  • Patent number: 5567723
    Abstract: 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: Grant
    Filed: July 5, 1995
    Date of Patent: October 22, 1996
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./Ltee
    Inventors: Mark A. Dekeyser, Derek J. McPhee, Paul T. McDonald
  • Patent number: 5567721
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: October 22, 1996
    Assignee: Centre International de Recherches Dermatologiques
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5554633
    Abstract: 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: Grant
    Filed: January 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Martin R. Teall
  • Patent number: 5552430
    Abstract: 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: Grant
    Filed: May 2, 1995
    Date of Patent: September 3, 1996
    Assignee: 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
  • Patent number: 5543433
    Abstract: 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: Grant
    Filed: June 3, 1994
    Date of Patent: August 6, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
  • Patent number: 5506259
    Abstract: 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: Grant
    Filed: July 27, 1994
    Date of Patent: April 9, 1996
    Assignee: Zambon Group S.p.A.
    Inventors: Gabriele Norcini, Francesco Santangelo
  • Patent number: 5506263
    Abstract: 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: Grant
    Filed: December 14, 1994
    Date of Patent: April 9, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5482966
    Abstract: 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: Grant
    Filed: June 13, 1994
    Date of Patent: January 9, 1996
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Thomas G. C. Bird, Patrick Ple
  • Patent number: 5472956
    Abstract: 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: Grant
    Filed: January 21, 1994
    Date of Patent: December 5, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5420164
    Abstract: 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: Grant
    Filed: May 3, 1993
    Date of Patent: May 30, 1995
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tadashi Mishina, Kanou Harada, Joji Yasuoka, Hidenobu Kushuhara, Noriyoshi Izumi
  • Patent number: 5416110
    Abstract: 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: Grant
    Filed: July 30, 1993
    Date of Patent: May 16, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5413997
    Abstract: 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: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5399585
    Abstract: 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: Grant
    Filed: August 30, 1993
    Date of Patent: March 21, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5387594
    Abstract: 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: Grant
    Filed: August 4, 1992
    Date of Patent: February 7, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5326759
    Abstract: 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: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5321042
    Abstract: 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: Grant
    Filed: October 8, 1992
    Date of Patent: June 14, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Mittendorf, Franz Kunisch, Manfred Plempel
  • Patent number: 5317021
    Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: May 31, 1994
    Assignee: ONO Pharmaceutical Co., Ltd.
    Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
  • Patent number: 5314891
    Abstract: 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: Grant
    Filed: September 10, 1992
    Date of Patent: May 24, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5306727
    Abstract: 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: Grant
    Filed: April 30, 1993
    Date of Patent: April 26, 1994
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5298515
    Abstract: 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: Grant
    Filed: October 6, 1992
    Date of Patent: March 29, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Schubert, Reiner Kober, Gerhard Hamprecht, Hubert Sauter, Uwe Kardorff, Christoph Kuenast
  • Patent number: 5292771
    Abstract: 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: Grant
    Filed: October 8, 1992
    Date of Patent: March 8, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: 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
  • Patent number: 5288750
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: February 22, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
  • Patent number: 5270301
    Abstract: 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: Grant
    Filed: May 7, 1990
    Date of Patent: December 14, 1993
    Assignee: ICI Americas Inc.
    Inventor: Donald J. Wolanin
  • Patent number: 5196410
    Abstract: 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: Grant
    Filed: September 11, 1991
    Date of Patent: March 23, 1993
    Assignee: Pfizer Inc.
    Inventors: Michael L. Francoeur, Russell O. Potts
  • Patent number: 5190961
    Abstract: 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: Grant
    Filed: August 2, 1991
    Date of Patent: March 2, 1993
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
  • Patent number: 5185363
    Abstract: 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: Grant
    Filed: September 30, 1991
    Date of Patent: February 9, 1993
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Daniel J. Kerkman, Jonathan G. Martin, Andrew O. Stewart, James B. Summers
  • Patent number: 5162364
    Abstract: 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: Grant
    Filed: June 11, 1991
    Date of Patent: November 10, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5153225
    Abstract: 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: Grant
    Filed: April 9, 1991
    Date of Patent: October 6, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 5145867
    Abstract: 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: Grant
    Filed: April 6, 1990
    Date of Patent: September 8, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: John C. Ellory, Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Wulf Merkel
  • Patent number: 5130331
    Abstract: 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: Grant
    Filed: October 9, 1990
    Date of Patent: July 14, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfons Pascual
  • Patent number: 5128367
    Abstract: 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: Grant
    Filed: August 31, 1990
    Date of Patent: July 7, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Wierzbicki, Jacqueline Bonnet, Martine Brisset, Yannis Tsouderos
  • Patent number: 5118681
    Abstract: 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: Grant
    Filed: July 28, 1989
    Date of Patent: June 2, 1992
    Assignee: Rohm and Haas Company
    Inventors: David R. Amick, Katherine E. Flynn, Cherylann Schieber
  • Patent number: 5116848
    Abstract: 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: Grant
    Filed: March 30, 1988
    Date of Patent: May 26, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5112868
    Abstract: 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: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar