Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/68)
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5563250Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.Type: GrantFiled: May 13, 1994Date of Patent: October 8, 1996Assignee: NeoRx CorporationInventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
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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: 5527926Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.Type: GrantFiled: June 6, 1995Date of Patent: June 18, 1996Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
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Patent number: 5508439Abstract: There are provided perfluoroalkanoyl aminonitrile intermediates and their use in a facile and efficient synthesis of 2-perfluoroalkyl-3-oxazolin-5-one. Said oxazolinone is a key intermediate in the preparation of insecticidal, acaricidal and nematocidal pyrrole compounds.Type: GrantFiled: April 24, 1995Date of Patent: April 16, 1996Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5495018Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.Type: GrantFiled: December 8, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5495031Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar aprotic solvent. The resulting compounds are useful as antibiotics.Type: GrantFiled: September 13, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5480997Type: GrantFiled: May 12, 1994Date of Patent: January 2, 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: 5480902Abstract: There are provided fungicidal thienyl- and furylpyrrole compounds of formula I ##STR1## Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestation and disease.Type: GrantFiled: August 31, 1993Date of Patent: January 2, 1996Assignee: American Cyanamid CompanyInventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan
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Patent number: 5464834Abstract: New N-substituted N'-heterobicyclic piperazines corresponding to the general formula I: ##STR1## wherein: R represents: ##STR2## D represents a single bond, except when R represents naphthyl, or a hydrocarbon chain having 1 to 8 carbon atoms inclusive which is straight-chain or branched by a gem-dimethyl; andA-B represents: --(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.3 --O--, or --CO--CH.dbd.CH--,as well as their possible stereoisomers, epimers, and pharmaceutically-acceptable acid addition salts thereof; and medicinal products containing the same, useful in the treatment of a disorder requiring a 5-HT.sub.1A receptor antagonist.Type: GrantFiled: June 11, 1993Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Jean-Michel Rivet
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Patent number: 5457085Abstract: The invention relates to (1S,aRS)-2-chloro-N-(2,4-dimethyl-3-thienyl)-N-(2-metho1xy-1-methylethyl)a cetamide, a novel method of preparation, herbicidal compositions comprising said compound and methods of combatting weeds employing said compound.Type: GrantFiled: September 21, 1994Date of Patent: October 10, 1995Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Reynold Chollet, Stefan Blarer, Thomas Vettiger
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Patent number: 5442059Abstract: The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 13, 1992Date of Patent: August 15, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5434151Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines 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.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: August 24, 1992Date of Patent: July 18, 1995Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5424373Abstract: Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.Type: GrantFiled: June 28, 1994Date of Patent: June 13, 1995Assignee: Ciba-Geigy CorporationInventors: Peter Flury, Martin Roth, Sameer H. Eldin
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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: 5395946Abstract: The invention related to a method of preparing a protein or a proteinaceous material labelled with a metalradionuclide and intended for diagnostic or therapeutic application, by reacting a protein or a proteinaceous material with an agent for coupling the radionuclide to the protein or the proteinaceous material, a protein conjugate being formed, and by then complexing the radionuclide with the conjugate thus formed to a radionuclide complex.Type: GrantFiled: August 7, 1990Date of Patent: March 7, 1995Inventors: Wilhelmus T. Goedemans, Karel J. Panek
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Patent number: 5358938Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines 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.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: July 13, 1992Date of Patent: October 25, 1994Assignee: CytoMed, Inc.Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5352831Abstract: Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.Type: GrantFiled: July 14, 1992Date of Patent: October 4, 1994Assignee: Ciba-Geigy CorporationInventors: Peter Flury, Martin Roth, Sameer H. Eldin
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Patent number: 5344843Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.Type: GrantFiled: March 13, 1992Date of Patent: September 6, 1994Assignee: Hoffman-La Roche Inc.Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
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Patent number: 5328902Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 13, 1992Date of Patent: July 12, 1994Assignee: American Cyanamid Co.Inventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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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: 5326911Abstract: Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formulaM.sup.1 OR.sup.1 (III)where the radicals R.sup.1 to R.sup.4, M.sup.1 and X.sup..crclbar. have the meaning given in the description. The alcoholates are employed in highly active form with an effective content of 98-100% M.sup.1 OR.sup.1.Type: GrantFiled: July 20, 1992Date of Patent: July 5, 1994Assignee: Bayer AktiengesellschaftInventors: Heinz-Ulrich Blank, Helmut Kraus, Gerhard Marzolph, Nikolaus Muller
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Patent number: 5298661Abstract: Charge transporting materials having general formula (I): ##STR1## R.sup.1 represents hydrogen; an unsubstituted or substituted alkyl group; an alkoxyl group having 1 to 4 carbon atoms; a thioalkoxyl group having 1 to 4 carbon atoms; an aryloxy group; an aralkyl group; a nitro group; an unsubstituted or substituted aryl group; a halogen; an amino group; an unsubstituted or substituted dialkylamino group; R.sup.2 represents hydrogen; an unsubstituted or substituted alkyl group; an alkoxyl group having 1 to 4 carbon atoms; or a halogen; R.sup.3 represents hydrogen; an alkyl group having 1 to 4 carbon atoms; an alkoxyl group having 1 to 4 carbon atoms; a halogen; a dialkylamino group; an amino group; a thioalkoxyl group having 1 to 4 carbon atoms; an aryloxy group; a methylenedioxy group; an aralkyl group; or an unsubstituted or substituted aryl group; R.sup.Type: GrantFiled: June 18, 1993Date of Patent: March 29, 1994Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga
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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: 5298659Abstract: Azomethines can be prepared by the condensation of cycloalkanones and anilines in the presence of acid homogeneous catalysts while the water of reaction is removed azeotropically, the condensation being carried out in a continuous reaction in a column-like reactor to which a temperature profile is applied, the starting materials being fed in in the low-temperature region, and, of the reaction products, the water of reaction to be removed azeotropically being discharged also in the low-temperature region and the azomethine produced being discharged in the high-temperature region.Type: GrantFiled: January 14, 1993Date of Patent: March 29, 1994Assignee: Bayer AktiengesellschaftInventors: Reinhard Langer, Hans-Josef Buysch, Paul Wagner
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Patent number: 5298513Abstract: 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 ora 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: May 29, 1992Date of Patent: March 29, 1994Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5292896Abstract: Styrene derivatives of the formula ##STR1## and an electrophotographic photoconductor comprising an electroconductive support material and a photosensitive layer comprising at least one styrene derivatives of the same formula are disclosed, in which Ar represents an unsubstituted of substituted phenyl group or an unsubstituted or substituted styryl group, R represents hydrogen, a lower alkyl group or an unsubstituted or substituted phenyl group, and A is selected from the group consisting of ##STR2## wherein R.sup.1 represents a lower alkyl group or a lower alkoxy group, R.sup.2 and R.sup.3 each represent a lower alkyl group, an aralkyl group, or an unsubstituted or substituted phenyl group.Type: GrantFiled: September 4, 1991Date of Patent: March 8, 1994Assignee: Ricoh Company, Ltd.Inventors: Masayuki Shoshi, Masaomi Sasaki
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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: 5284847Abstract: Novel thieno[2,3-b]pyrazine-2,3(1H,3H)-diones or tautomeric forms thereof of the formula (I) ##STR1## The compounds are useful in the treatment of neurological and psychiatric diseases.Type: GrantFiled: October 16, 1992Date of Patent: February 8, 1994Assignee: Novo Nordisk A/SInventors: Anker S. Jorgensen, Peter Faarup, Erling Guddal, Lone Jeppesen
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Patent number: 5283363Abstract: The invention relates to a new process for the preparation of (hetero)arylalk(en/in)ylamines of the formula (I) ##STR1## in which A represents ethane-1,2-diyl (ethylene, dimethylene, --CH.sub.2 --CH.sub.2 --) or represents ethene-1,2-diyl (ethenylene, vinylene, --CH.dbd.CH--) or represents ethine-1,2-diyl (ethinylene, --C.ident.C--),characterized in that(a) in the event that, in formula (I), A represents ethine-1,2-diyl, halogeno(hetero)aryl compounds of the general formula (II)Ar--X (II)are reacted with aminoalkinyl compounds of the general formula (III) ##STR2## and, if appropriate, (b) in the event that, in formula (I), A represents ethane-1,2-diyl or ethene-1,2-diyl, the new (hetero)aralkinylamines which are obtained by the process step described under (a), of the general formula (Ia), ##STR3## are reacted with a hydrogenating agent, if appropriate in the presence of a catalyst and if appropriate in the presence of a diluent, the definitions applying to Ar, R.sup.1, R.sup.Type: GrantFiled: January 16, 1992Date of Patent: February 1, 1994Assignee: Bayer AktiengesellschaftInventors: Dietmar Kuhnt, Thomas Himmler, Heinz Ziemann
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Patent number: 5262539Abstract: Electrophilic aromatic compounds can be reacted with sulphenamides in the presence of bases to form the corresponding aromatic amines.Type: GrantFiled: April 9, 1991Date of Patent: November 16, 1993Assignee: Bayer AktiengesellschaftInventors: Mieczyslaw Makosza, Maciej Bialecki
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Patent number: 5206387Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond of (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: October 19, 1992Date of Patent: April 27, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5201934Abstract: Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur;R.sup.1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl;R.sup.2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl or naphthyl, or one of the groups stated for R.sup.1 ;R.sup.3 and R.sup.4 are nitro, cyano, halogen, substituted or unsubstituted amino, alkoxy, alkylthio, substituted or unsubstituted alkenyl, alkynyl, phenyl, phenoxy or phenylthio, or one of the groups stated for R.sup.1 ;R.sup.5 is formyl, 4,5-dihydrooxazol-2-yl or COYR.sup.6 (Y.dbd.O,S);R.sup.6 is hydrogen, cycloalkyl, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkenyl or phenyl,phthalimido, tetrahydrophthalimido, succinimido, maleimido, benzotriazolyl ora group --N.dbd.CR.sup.7 R.sup.8, whereR.sup.7 and R.sup.8 are hydrogen or alkyl, and R.sup.8 may also be cycloalkyl, phenyl, or R.sup.7 and R.sup.8 together form a 4- to 7-membered alkylene chain;and if R.sup.Type: GrantFiled: October 3, 1990Date of Patent: April 13, 1993Assignee: BASF AktiengesellschaftInventors: Peter Muenster, Gerd Steiner, Wolfgang Freund, Bruno Wuerzer, Karl-Otto Westphalen
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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: 5183818Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.Type: GrantFiled: August 27, 1991Date of Patent: February 2, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
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Patent number: 5183904Abstract: Novel compounds and methods for the formation of disulfide linkages are presented. The novel compounds employed are substituted 2-iminothiolane hydrohalide linking agents of the following formula (I): ##STR1## wherein, X is halogen;R.sub.1 is COOR.sub.5 ; halogen; nitro; unsubstituted or halogenated C.sub.1-8 alkyl; unsubstituted or halogenated C.sub.1-8 alkoxy; unsubstituted or halogenated C.sub.2-8 alkenyl; unsubstituted or halogenated C.sub.2-8 alkynyl; unsubstituted C.sub.3-8 cycloalkyl; unsubstituted aryl; aryl substituted with 1 to 3 substituents selected from halogen, amino, unsubstituted or halogenated C.sub.1-8 alkyl, or unsubstituted or halogenated C.sub.1-8 alkoxy; unsubstituted heterocycle; or heterocycle substituted with 1 to 3 substituents selected from amino, halogen, unsubstituted or halogenated C.sub.1-8 alkyl, or unsubstituted or halogenated C.sub.1-8 alkoxy;each of R.sub.2, R.sub.3 and R.sub.4 is independently hydrogen or selected from the values of R.sub.1 ; orR.sub.1 and R.sub.Type: GrantFiled: November 20, 1991Date of Patent: February 2, 1993Assignee: Xoma CorporationInventors: Stephen F. Carroll, Dane A. Goff
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Patent number: 5182348Abstract: Compounds of the formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 have the meanings given in the description, and the other radicals have the following meanings:X, Y and Z denote identical or different divalent radicals --O--, --S--, --N(R.sup.9)-- or --C(R.sup.10).dbd.C(R.sup.11)--, with the proviso that at least one of the radicals, X, Y and Z is not a radical of the formula --C(R.sup.10).dbd.C(R.sup.11)--, and whereinR.sup.9 is a hydrogen atom, a branched or unbranched C.sub.1 - to C.sub.8 -alkyl radical or an optionally substituted phenyl radical, andR.sup.10 and R.sup.11 are, in each case, identical or different radicals which have one of the meanings of R.sup.1,R.sup.7 and R.sup.8 denote identical or different radicals, that is to say hydrogen atoms or C.sub.1 - to C.sub.6 -alkyl or phenyl radicals, andn, m and o denote identical or different integers with a value of from 1 to 10.Type: GrantFiled: August 19, 1991Date of Patent: January 26, 1993Assignee: Wacker-Chemie GmbHInventors: Hermann Braeunling, Richard Becker, Georg Bloechl
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Patent number: 5166346Abstract: Process for the preparation of thiophene derivatives and also new dihydrothiophene 1-oxides.Thiophene derivatives having an--optionally substituted--amino group on the thiophene ring are prepared by dehydrogenating dihydrothiophenes, substituted in a manner identical to that of the desired thiophene derivatives, by means of H.sub.2 O.sub.2, the dihydrothiophenes being reacted with H.sub.2 O.sub.2 in a first reaction stage in a neutral medium to give the corresponding sulfoxides, which are then rearranged into the thiophene derivatives by means of acid in the second reaction stage.The dihydrothiophene 1-oxides formed as intermediates in this reaction are new compounds. Like the thiophene derivatives formed from them by rearrangement with acid, they are intermediates, mainly in the sector of plant protection agents and pharmaceuticals.Type: GrantFiled: December 20, 1990Date of Patent: November 24, 1992Assignee: Hoechst AktiengesellschaftInventors: Robert Rippel, Hans-Wolfram Flemming, Manfred Rukwied
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Patent number: 5164499Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: January 2, 1990Date of Patent: November 17, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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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: 5159087Abstract: Aromatic diolefinic compounds including 1,4-divinylbenzene derivatives, which are useful not only as organic photoconductive materials for electrophotography, but also as intermediates for producing diethyl aromatic compounds which are also useful as organic photoconductive materials for electrophotography, the aromatic diethyl compounds, an electrophotographic photoconductor containing any of the above aromatic diethyl compounds in a photosensitive layer thereof, and a charge transporting medium containing any of the aromatic diethyl compound are disclosed.Type: GrantFiled: January 17, 1991Date of Patent: October 27, 1992Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Mitsuru Hashimoto
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Patent number: 5155232Abstract: An organic material for non-linear optics comprising:an electron donor group constituted by a heteroaromatic cycle;an electron attractor group selected from NO.sub.2 and CN; andan electron effect transmitter group selected from an aromatic system of the phenyl ring type, or a chain having n atoms of carbon including a double or a triple bond (n<4).Type: GrantFiled: April 2, 1990Date of Patent: October 13, 1992Assignee: Alcatel N.V.Inventors: Jean-Francois Fauvarque, Victorien Ratovelomanana, Anny Jutand, Christian Amatore
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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: 5145975Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.Type: GrantFiled: July 6, 1990Date of Patent: September 8, 1992Assignee: The Rockefeller UniversityInventors: Graeme B. Henderson, Peter C. Ulrich, Anthony Cerami
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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: 5132411Abstract: Compounds of the formula ##STR1## wherein R is halo,R.sub.1 is cyano; (C.sub.1-6 alkoxy)carbonyl; (C.sub.3-6 alkenyl)oxycarbonyl; C.sub.1-4 alkylsulfonyl; phenylsulfonyl; (C.sub.1-4 alkyl)carbonyl; benzoyl; carbamoyl; (C.sub.1-4 alkyl)carbamoyl; N,N-di-(C.sub.1-4 alkyl)carbamoyl; phenylcarbamoyl; benzyloxycarbonyl; or (C.sub.1-6 alkoxy)carbonyl, (C.sub.3-6 alkenyl)oxycarbonyl, C.sub.1-4 alkylsulfonyl, phenylsulfonyl or (C.sub.1-4 alkyl)carbamoyl substituted by one or two substituents independently selected from chloro, bromo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano and acyl, andR.sub.2 is formyl, cyano, --CH.dbd.C(R.sub.4).sub.2 or --CH.dbd.N--OH,wherein (1) each R.sub.4 is independently cyano; (C.sub.1-6 alkoxy)carbonyl; (C.sub.3-6 alkenyl)oxycarbonyl; (C.sub.3-6 alkynyl)oxycarbonyl; or (C.sub.1-6 alkoxy)carbonyl, (C.sub.3-6 alkenyl)oxycarbonyl or (C.sub.3-6 alkynyl)oxycarbonyl substituted by one or two substituents independently selected from chloro, bromo, C.sub.1-4 alkyl, C.sub.Type: GrantFiled: March 19, 1990Date of Patent: July 21, 1992Assignee: Sandoz Ltd.Inventors: Robert Egli, Beat Henzi
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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: 5118704Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.Type: GrantFiled: September 11, 1991Date of Patent: June 2, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5096905Abstract: The invention relates to elaiophylin derivatives of the formulae (I), (I'), (III) and (III') ##STR1## in which the C.dbd.C double bonds in the 2,3 and 4,5 position may also be hydrogenated and in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings indicated. The invention furthermore relates to a process for the preparation of these elaiophylin derivatives, and the use thereof as pharmaceuticals, in particular as anthelmintic pharmaceuticals.Type: GrantFiled: September 14, 1989Date of Patent: March 17, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein