Ring Or Polycyclo Ring System In Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/185)
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Patent number: 6670400Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.Type: GrantFiled: April 8, 2002Date of Patent: December 30, 2003Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6506937Abstract: Benzenesulfonylureas and -thioureas of the formula I where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is —[CR(3)2]n—, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO3 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used an antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: November 29, 2001Date of Patent: January 14, 2003Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gögelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 6495576Abstract: Compounds of formula (I) may be useful in treating diseases prevented by or ameliorated with potassium channel openers.Type: GrantFiled: January 14, 2002Date of Patent: December 17, 2002Assignee: Abbott LaboratoriesInventors: Michael E. Kort, Robert J. Gregg, William A. Carroll, Arturo Perez Medrano, Jürgen Dinges, Fatima Z. Basha
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Patent number: 6436925Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6410749Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 thType: GrantFiled: July 17, 2001Date of Patent: June 25, 2002Assignee: Nippon Soda Co., Ltd.Inventors: Eiji Katayama, Daisuke Sato, Hirohito Ooka, Tsutomu Inoue
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Patent number: 6384080Abstract: Compounds of formula (I) where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R4 is a group CR6R7R8 wherein R6 and R7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R8 is hydrogen; its prodrug and a salt thereof.Type: GrantFiled: April 23, 2001Date of Patent: May 7, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Kozo Sawada, Akio Kuroda, Takayuki Inoue, Natsuko Kayakiri, Yuki Sawada, Tsuyoshi Mizutani
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Patent number: 6339157Abstract: Aldehydes are catalytically combined with amines to form carboxamides in one step using an oxidant and a metal-ligand complex or metal/ligand composition.Type: GrantFiled: July 28, 2000Date of Patent: January 15, 2002Assignee: Symyx Technologies, Inc.Inventors: Xiaohong Bei, Anil Guram
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Patent number: 6323229Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: April 14, 1999Date of Patent: November 27, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Patent number: 6194458Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.Type: GrantFiled: October 21, 1999Date of Patent: February 27, 2001Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Patent number: 6194612Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.Type: GrantFiled: April 7, 1998Date of Patent: February 27, 2001Assignees: The Scripps Research Institute, CombiChem, Inc.Inventors: Dale L. Boger, Soan Cheng, Peter L. Myers
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Patent number: 6133315Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 16, 1999Date of Patent: October 17, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6107511Abstract: The present invention has for its object to provide a commercially useful, expedient and efficient method for purification and isolation of an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1) or its enantiomer, which is capable of removing the various contaminants, particularly said byproducts, whereby the problem of instability of the compound (1) or its enantiomer can be overcome and a high product yield can be insured.The present invention relates to a method of purifying and isolating an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1): ##STR1## (wherein X represents a halogen atom; one of P.sup.1 and P.sup.2 represents a hydrogen atom and the other represents an amino-protecting group, or P.sup.1 and P.sup.Type: GrantFiled: May 14, 1999Date of Patent: August 22, 2000Assignee: Kaneka CorporationInventors: Yasuyoshi Ueda, Katsuji Maehara, Tadashi Sugawa, Hiroshi Murao, Akira Nishiyama, Hajime Manabe
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Patent number: 6090981Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3).sub.2 ].sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z in Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: May 19, 1998Date of Patent: July 18, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David W. Laufer
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Patent number: 6018069Abstract: A purified acid addition salt of a (2S, 3S, 5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane, e.g., (2S, 3S, 5S)-2-tert-butoxycarbonylamino-3-hydroxy-5-amino-1,6-diphenylhexane, is obtained from its mixture, in an arbitrary ratio, with its (2S, 3S, 5R) stereoisomer in the presence of an inorganic or organic acid. The desired (2S, 3S, 5S) acid addition salt may be recovered from the mixture by, for example, recrystallization. These purified acid addition salts are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.Type: GrantFiled: May 26, 1999Date of Patent: January 25, 2000Assignee: Daicel Chemical Industries, Ltd.Inventors: Yoshiyuki Murai, Masahiro Nishikawa, Yoichiro Ueda, Ichiro Takase
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Patent number: 5998667Abstract: The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R.sup.1 represents C.sub.1 -C.sub.6 -halogenoalkylthio andR.sup.2 represents hydrogen, orR.sup.1 and R.sup.2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring,X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: June 4, 1998Date of Patent: December 7, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Albrecht Marhold, Christoph Erdelen
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Patent number: 5985881Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: August 2, 1997Date of Patent: November 16, 1999Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5972939Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: October 26, 1998Date of Patent: October 26, 1999Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
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Patent number: 5939554Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.Type: GrantFiled: April 17, 1997Date of Patent: August 17, 1999Assignee: NDSU Research FoundationInventors: Mukund P. Sibi, Prasad K. Despande, Anthony J. LaLoggia
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5852007Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: February 6, 1997Date of Patent: December 22, 1998Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5696123Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
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Patent number: 5663437Abstract: A new benzidine monomer composition containing an asymmetrically situated benzamide (iminobenzoyl) group: ##STR1## was prepared from the benzolyation reaction of 4,4'-dinitro-2-biphenylamine and benzoyl chloride, followed by catalytic hydrogenation. The compound can be used as a comonomer in the preparation of soluble thermoplastic polyamides, polyimides and other high performance polymers whose preparations require a diamine monomer.Type: GrantFiled: February 2, 1996Date of Patent: September 2, 1997Assignee: The United States of America as represented by the Secretary of the Air ForceInventor: Loon-Seng Tan
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Patent number: 5646329Abstract: 2-fluoro-cyclopropylamine is prepared in an advantageous manner by reacting an N-vinyl compound with a carbene of type FXC: (where X=chlorine or bromine) to give the corresponding cyclopropylamine derivative, replacing the radical X in this derivative by hydrogen, by reduction, and finally eliminating the other substituents on the hydrogen atom.Type: GrantFiled: November 2, 1995Date of Patent: July 8, 1997Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Albrecht Marhold, Stefan Bohm
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Patent number: 5637753Abstract: A process for the preparation of N-carbonylarylimine of the general formula I: ##STR1## in which Ar represent an aryl radical and R represent a phenyl or t-butoxy radical, by desulphonating the compound of the general formula II. ##STR2## The compounds of formula II are novel when R is t-butoxy.Type: GrantFiled: January 16, 1996Date of Patent: June 10, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Didier Bernard, Patrick Leon
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Patent number: 5637121Abstract: Poly(oxyalkylene) aromatic amides having the formula: ##STR1## or a fuel-soluble salt thereof; wherein a is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.3 is hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.4 is hydrogen or an acyl group of the formula: ##STR2## wherein A.sub.1 is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms and each R.sub.5 and R.sub.6 is independently selected in each --O--CHR.sub.5 --CHR.sub.6 -- unit; R.sub.Type: GrantFiled: December 30, 1994Date of Patent: June 10, 1997Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5629346Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.Type: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: Rohm and Haas CompanyInventors: H. Edwin Carley, Ashok K. Sharma, Colin Swithenbank
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Patent number: 5587513Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.Type: GrantFiled: January 20, 1995Date of Patent: December 24, 1996Inventors: Klaus Pohmer, Rainer Weber, Cornelia D orzbach-Lange, Reinhard Haida, Hans-Heinrich Moretto
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Patent number: 5538986Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.Type: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
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Patent number: 5318994Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.Type: GrantFiled: November 3, 1992Date of Patent: June 7, 1994Assignee: Adir et CompagnieInventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
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Patent number: 5298647Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.Type: GrantFiled: December 14, 1987Date of Patent: March 29, 1994Inventors: Dominique Robert, Louis Jung
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Patent number: 5284966Abstract: Intermediates for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers are described. The final compounds are useful intermediates for the synthesis of antibiotics like Chloramphenicol, Thiamphenicol and Florfenicol.Type: GrantFiled: December 18, 1992Date of Patent: February 8, 1994Assignee: Zambon Group S.p.A.Inventors: Marco Villa, Claudio Giordano, Silvia Cavicchioli, Silvio Levi
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Patent number: 5270343Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 .dbd.CR.sup.2 .dbd.CR.sup.3 CR.sup.4 .dbd.CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or is (CH.sub.2).sub.7 ;a=0 or 1; b= 0 or 1;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl;X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from:a) C.sub.1-4 alkyl, C.Type: GrantFiled: June 15, 1992Date of Patent: December 14, 1993Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5234946Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.Type: GrantFiled: August 30, 1991Date of Patent: August 10, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
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Patent number: 5225442Abstract: Compounds of general formula: ##STR1## in which A and R are defined in the description. Medicaments containing the same and useful for the treatment of melatoninergic disorders.Type: GrantFiled: January 3, 1992Date of Patent: July 6, 1993Assignee: Adir et CompagnieInventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
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Patent number: 5212312Abstract: Dyes of the formula ##STR1## in which F is the radical of an indigoid dye, of a benzothioxanthene or of an aromatic dye which contains at least 4 alicyclic and/or heterocyclic, fused six-membered rings and at least two ring keto groups and is not water-soluble, R.sub.1 is a substituted or unsubstituted C.sub.1-4 -alkyl radical, a substituted or unsubstituted cycloalkyl radical, a substituted or unsubstituted aryl radical or a radical of the formula--A--Qwhere A is a substituted or unsubstituted C.sub.1-4 -alkylene radical and Q is a basic radical, which may be quaternised, and R.sub.2 is hydrogen or a substituted or unsubstituted C.sub.1-4 -alkyl radical, or in which R.sub.1 and R.sub.2 together with the ##STR2## group are a phthalimide radical, and R.sub.3 is hydrogen, a substituted or unsubstituted C.sub.1-4 -alkyl radical, a substituted or unsubstituted aryl radical, a C.sub.1-4 -alkoxycarbonyl radical or a N,N-di-C.sub.1-4 -alkylcarboxamide radical and n is 1, 2, 3 or 4.Type: GrantFiled: September 22, 1986Date of Patent: May 18, 1993Assignee: Ciba-Geigy AGInventors: Jean-Marie Adam, Athanassios Tzikas
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Patent number: 5185465Abstract: Novel 4-phenyl-1,3-benzodiazepines and 2-amino-.alpha.-phenylphenethylamines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants. The 2-amino-.alpha.-phenylphenethylamines are useful as anticonvulsant and neuroprotective agents.Type: GrantFiled: October 16, 1990Date of Patent: February 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
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Patent number: 5169986Abstract: The present invention provides an organic nonlinear optical material including a benzylidene-aniline derivative having an electron-donating substituent introduced at the 4-position and an electron-accepting substituent introduced at the 4'-position, by selecting as the conjugated .pi. electronic system a benzylidene-aniline derivative having a large molelcular hyperpolarizability and yet a dipole moment as small as those of benzene derivatives, and introducing a molecular alignment-regulating substituent. The centrosymmetry in the bulk state of the material, for example, in the crystal state, is destroyed and the molecular alignment is regulated to such a bulk structure so that the optical nonlinearity possessed by the molecule is effectively utilized. The material exhibit a large optical nonlinearity never attained by conventional techniques.the intermolecular cohesive force due to the .pi. electron interaction between the molecules in the present invention is larger than that between a benzene derivative.Type: GrantFiled: October 19, 1990Date of Patent: December 8, 1992Assignee: Toray Industries, Inc.Inventors: Tetsuya Tsunekawa, Tetsuya Gotoh, Keiichi Egawa
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Patent number: 5169987Abstract: A squarylium compound represented by formula (III) ##STR1## wherein R.sub.4 represents a hydrogen atom, a methyl group, or a fluorine atom.Type: GrantFiled: December 7, 1990Date of Patent: December 8, 1992Assignee: Fuji Xerox Co., Ltd.Inventors: Yutaka Akasaki, Akihiko Tokida, Kaoru Torikoshi, Tooru Ishii, Hidemi Suto, Akira Imai
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Patent number: 5149709Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.Type: GrantFiled: July 3, 1990Date of Patent: September 22, 1992Assignee: Schering CorporationInventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
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Patent number: 5136085Abstract: Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X.sup.1 and X.sup.2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic acid amide, with a halobenzene in the presence of an alkyllithium reagent.Type: GrantFiled: July 3, 1991Date of Patent: August 4, 1992Assignee: Glaxo Inc.Inventors: Marty C. Johnson, Stephen V. Frye
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Patent number: 5136094Abstract: Secondary formamides having the structural formula:R.sup.1 CHR.sup.2 CH(OR.sup.3)NHCHOwhereinR.sup.1 is H, C.sub.1 -C.sub.6 alkyl or aryl;R.sup.2 is H, or C.sub.1 -C.sub.6 alkyl; andR.sup.3 is benzyl, C.sub.1 -C.sub.8 alkyl or hydroxyalkyl;are synthesized by reacting an acetal having the structural formula: R.sup.1 CHR.sup.2 CH(OR.sup.3).sub.2 wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, with formamide in the presence of a strong acid catalyst at a temperature in the range of 0.degree.-200.degree. C.Type: GrantFiled: March 10, 1988Date of Patent: August 4, 1992Assignee: Air Products and Chemicals, Inc.Inventors: Mark L. Listemann, Ronald Pierantozzi, Robert K. Pinschmidt, Jr.
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Patent number: 5118697Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
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Patent number: 5106407Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.Type: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
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Patent number: 5098996Abstract: Radioactive fluorine can be easily introduced into biologically active molecules containing amino groups. A p-bromomethyl benzoyl group is coupled to the amino group of the biologically active molecule, and bromine is displaced by fluorine. Alternatively, the bromine on the bromomethylbenzoyl group is first displaced by fluorine, and the fluoromethyl benzoyl group is then coupled to the amino group of the biologically active molecule. The compounds so produced are useful in diagnostic nuclear medicine.Type: GrantFiled: March 15, 1988Date of Patent: March 24, 1992Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Kenneth L. Kirk, David C. Furlano, Yechiel Shai
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Patent number: 5084593Abstract: Leuco dyes of the formula (I) are disclosed, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent an alkyl group having 1 to 10 carbon atoms; X represents hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms or a halogen; and Y represents R.sub.5 --Z--SO.sub.2 NH--, R.sub.6 --Z--CONH--, or ##STR2## in which Z represents ##STR3## R.sub.5 and R.sub.6 each represent hydrogen, an alkyl group having 1 to 10 carbon atoms, or a halogen; and R.sub.7 and R.sub.8 each represent hydrogen, a cyano group, or --COR.sub.9, in which R.sub.9 represents a lower alkyl group, a lower alkoxyl group, a phenyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, or a halogen; a naphthyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms or a halogen with the proviso that R.sub.7 and R.sub.8 are not both hydrogen.Type: GrantFiled: December 14, 1990Date of Patent: January 28, 1992Assignee: Ricoh Company, Ltd.Inventors: Hiroshi Gotoh, Shigeru Kusakata, Isao Shiojima
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Patent number: 5057623Abstract: An organic fluorine compound represented by the general formulaR.sub.f -(X).sub.h -R-Mwherein R.sub.f is a group selected from the following (a) and (b); ##STR1## X denotes a linking group selected from --O--, --S--, and --COO--, h denotes 0 or 1, R is a hydrocarbon chain comprising a phenylene group having an alkylene group with a total carbon number of 10 or more, or the derivative thereof, or an aliphatic alkylene group of a carbon number of 10 or more, and M is a group selected from --OH, --COOH, --SH, and --CONH.sub.2.The organic fluorine compound of the present invention greatly improves the dispersibility of magnetic powders in magnetic coating materials, has also an excellent rust prevention effect on metallic magnetic powders, and exhibits a marked dispersing effect even on fluorocarbon resin fine powders, which can be difficultly dispersed with conventional dispersing agents.Type: GrantFiled: October 13, 1989Date of Patent: October 15, 1991Assignee: Matsushita Electric Industrial Co., Ltd.Inventors: Yoshiaki Kai, Takashi Suzuki