Oxy, Aldehyde Or Ketone Group In Acid Moiety Patents (Class 560/23)
  • Publication number: 20140221662
    Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.
    Type: Application
    Filed: December 17, 2010
    Publication date: August 7, 2014
    Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES, LIANHE CHEMICAL TECHNOLOGY CO., LTD.
    Inventors: Dawei Ma, Shaolin Zhu, Shouyun Yu, You Wang, Qianghui Zhou
  • Patent number: 8703991
    Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: April 22, 2014
    Assignee: Wellstat Therapeutics Corporation
    Inventors: David D. Wirth, Richard Hudspeth
  • Publication number: 20140058104
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Application
    Filed: October 29, 2013
    Publication date: February 27, 2014
    Applicant: ZERIA PHARMACEUTICAL CO., LTD.
    Inventors: Masaaki NAGASAWA, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20130053598
    Abstract: The invention relates to a method for producing a cross-coupling product of a benzenoid dizonium salt according to the general formula (I), wherein the groups R1, R2, R3, R4, and R5 represent hydrogen, halogen, an alkyl, alkenyl, aryl, alkoxy, aryloxy, nitro, cyano, hydroxy, acetyl, and/or diazo groups independently of each, and X represents BF4, Cl, F, SO3CH3, CO2CH3, PF6, ClO2CH3, or CIO4, comprising the following steps: (a) providing a benzenoid amide, which with the exception of the diazo function has the same substituents R1, R2, R3, R4, and R5 as the benzenoid diazonium salt of the general formula (I), and hydrolytically cleaving the amide to form an amine or providing a corresponding amine, (b) diazotizing the amine thus obtained or provided with a nitrite, and (c) subsequently reacting the benzenoid diazonium salt with a coupling partner in the presence of a catalyst to form a cross-coupling product, wherein the coupling parter is represented by the general formula (II), R6, R7, and R8 are the same or
    Type: Application
    Filed: April 22, 2010
    Publication date: February 28, 2013
    Applicant: ZYLUM BETEILIGUNGSGESELLSCHAFT MBH & CO. PATENTE II KG
    Inventors: Nicolas Boege, Andreas Kreipl, Bernd Schmidt, Frank Hoelter, René Berger
  • Publication number: 20120202994
    Abstract: The invention relates to a method for carrying out a chemical reaction for producing a target compound by heating in a reactor a reaction medium containing at least one first reactant, such that a chemical bond inside the first reactant or between the first and a second reactant is formed or modified. The reaction medium is brought into contact with a solid heating medium that can be warmed by electromagnetic induction and that is inside the reactor and is surrounded by the reaction medium. Said heating medium is heated by electromagnetic induction with the aid of an inductor and the target bond is formed from the first reactant or from the first and a second reactant and said target bond is separated from the heating medium.
    Type: Application
    Filed: April 16, 2012
    Publication date: August 9, 2012
    Inventors: Carsten Friese, Andreas Kirschning, Jürgen Wichelhaus, Sascha Volkan Ceylau
  • Patent number: 8236519
    Abstract: In general, the present invention provides a reliable assay for the quantitative determination of p-aminophenol in an aqueous sample. More particularly, the present invention provides a rapid enzyme-based assay for the quantitative determination of acetaminophen in a sample. The assay employs a xylenol chromophore and a catalyst that is preferably a weak oxidizer. The assay provides reliable results in the presence or absence of N-acetylcystiene (NAC) and can therefore be used to monitor acetaminophen levels during NAC treatment. Methods and kits for determining acetaminophen concentration in an aqueous sample are also provided.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: August 7, 2012
    Assignee: Sekisui Diagnostics, LLC
    Inventors: Michael Bulger, Jan Holinsky
  • Publication number: 20120158127
    Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the corresponding diamines or diisocyanates thereof, wherein each X independently represents —CH2COO—, —CH(CH3)COO—, —CH2CH2OCH2COO—, —CH2CH2CH2CH2CH2COO—, —(CH2)yCOO— where y is 2 to 4 or 6 to 24, or —(CH2CH2O)z?CH2COO— where z? is 2 to 24; each Y represents —COCH2O—, —COCH(CH3)O—, —COCH2OCH2CH2O—, —COCH2CH2CH2CH2CH2O—, —CO(CH2)mO— where m is 2 to 4 or 6 to 24, or —COCH2O(CH2CH2O)n— where n is 2 to 24; R? is hydrogen, benzyl or straight-chained or branched alkyl; p is 1 to 4; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO2, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.
    Type: Application
    Filed: February 22, 2012
    Publication date: June 21, 2012
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20100217028
    Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.
    Type: Application
    Filed: March 30, 2010
    Publication date: August 26, 2010
    Applicant: NICOX S.A.
    Inventors: Piero DEL SOLDATO, Giancarlo SANTUS, Francesca BENEDINI
  • Patent number: 7569518
    Abstract: A pyridazine compound represented by formula (1): has an excellent plant disease controlling effect.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: August 4, 2009
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Morishita, Akio Manabe
  • Patent number: 7465755
    Abstract: The present invention relates to hydrazide derivatives of Formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such hydrazide derivatives. Said hydrazide derivatives are useful in the treatment of preterm labor, dysmenorrhea, fertility disorders, asthma, hypertension, undesired blood clotting, preelampsia, eclampsia, an eosinophil disorder, undesired bone loss, renal dysfunction, an immune deficiency disorder, ichthyosis, elevated intraocular pressure, infertility, sexual dysfunction, gastric ulcers and inflammatory disorders.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Serono SA
    Inventors: Gian Luca Araldi, Yihua Liao, Nadia Brugger
  • Patent number: 7381831
    Abstract: Disclosed is a compound of the formula and dimers thereof, wherein R, R2, X and Z are as described herein. The compounds are useful as colorants, particularly in applications such as phase change inks.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: June 3, 2008
    Assignee: Xerox Corporation
    Inventors: Jeffrey H. Banning, Rina Carlini, James D. Mayo
  • Patent number: 7312244
    Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: December 25, 2007
    Assignee: Cellgate, Inc.
    Inventors: Linda Clifford, legal representative, Laurence J. Marton, Aldonia L. Valasinas, Venodhar K. Reddy, Benjamin Frydman, deceased
  • Patent number: 7129357
    Abstract: In one embodiment, the present application discloses a process for making the compound of the formula:
    Type: Grant
    Filed: September 13, 2004
    Date of Patent: October 31, 2006
    Assignee: Schering Corporation
    Inventors: David R. Andrews, Suhan Tang, Wenxue Wu, Sami Y. Kalliney, Anantha Sudhakar, Christopher Nielsen
  • Patent number: 6852874
    Abstract: A process for catalyzing asymmetric dihydroxylations of olefins employs an Os(VI) complex as a catalytic intermediate in the formation of chiral vicinal diol products. The process requires a chiral bidentate ligand that favors diol formation in the “second cycle” of asymmetric dihydroxylation.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: February 8, 2005
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Malin Andersson, Robert Epple, Valery Fokin
  • Patent number: 6846936
    Abstract: The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: January 25, 2005
    Assignee: Sanofi-Synthelabo
    Inventor: Michel Biard
  • Patent number: 6730700
    Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: May 4, 2004
    Assignee: Renovis, Inc.
    Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
  • Patent number: 6696592
    Abstract: The present invention provides methods of making 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives according to the following general reaction scheme: The invention also provides intermediates useful in making such 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives as well as methods for making such intermediates.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: February 24, 2004
    Assignee: NicOx-S.A.
    Inventor: Donald G. McIntyre
  • Patent number: 6639093
    Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: October 28, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Pieter Ooms, Bernd-Ulrich Schenke
  • Patent number: 6630600
    Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: October 7, 2003
    Assignee: AstraZeneca AB
    Inventors: Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
  • Patent number: 6630598
    Abstract: A process of reacting a nitroaniline compound of formula (2): with an acid anhydride or acid halide is carried out in the presence of an alkali metal compound or an alkaline earth metal compound to produce an acylnitroaniline derivative. The process further includes the step of reacting the resulting product with a compound of formula (5); R2—Y to produce an N-acylnitroaniline derivative of formula (1): The N-acylnitroaniline derivative of formula (1) is a useful intermediate for the production of pharmaceuticals.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: October 7, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Tomoyasu Yoshida
  • Patent number: 6600063
    Abstract: The present invention relates to novel antimycobacterial compounds and in particular to antimycobacterial compounds comprised of derivatives of phenyl 4-aminosalicylate. This invention further relates to methods for their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them. The novel methods of the invention yield derivatives of phenyl 4-aminosalicylate on a multi-gram scale and in high purity for subsequent biological evaluation in drug discovery.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: July 29, 2003
    Assignee: Board of Trustees of Wellesley College
    Inventor: Michael J. Hearn
  • Patent number: 6566547
    Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.
    Type: Grant
    Filed: October 11, 1985
    Date of Patent: May 20, 2003
    Assignee: Zeneca Limited
    Inventors: Michael J Bushell, Kevin Beautement, John M Clough, Vivienne M Anthony, Paul deFraine, Christopher R Godfrey
  • Publication number: 20030053964
    Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.
    Type: Application
    Filed: April 5, 2002
    Publication date: March 20, 2003
    Inventors: Pieter Ooms, Bernd-Ulrich Schenke
  • Patent number: 6531624
    Abstract: A process for producing a benzoylacrylic acid derivative (formula 1) in high yield through a small number of steps and a simple purification step. The process comprises reacting 2,4,5-trifluoro-3-methyl-6-nitrobenzoyl chloride with a compound (formula 2) to yield an aminoacrylic acid derivative (formula 1) and then reacting the aminoacrylic acid derivative (formula 1) with an amine derivative represented by R2—NH2, wherein R2 is a cycloalkyl group or the like.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: March 11, 2003
    Assignees: Asahi Glass Company Ltd., Katayama Seiyakusyo Co., Ltd.
    Inventors: Naoto Morita, Takashi Inagaki
  • Patent number: 6469181
    Abstract: The present invention provides a processes, having practical utility, for preparing 2-oxindoles, N-hydroxy-2-oxindoles, or mixtures thereof comprising: catalytically hydrogenating a 2-nitroarylmalonate diester to produce a 2-(N-hydroxyamino)arylmalonate diester, a 2-aminoarylmalonate diester, or mixtures thereof as a first reaction intermediate; cyclizing, by intramolecular aminolysis of one ester group, the first reaction intermediate to produce a N-hydroxy-2-oxindole-3-carboxylate ester, 2-oxindole-3-carboxylate ester, or mixtures thereof as a second reaction intermediate; and hydrolyzing and decarboxylating the remaining ester group of the second reaction intermediate to produce the N-hydroxy-2-oxindole, the 2-oxindole, or mixtures thereof, wherein the cyclization reaction and the hydrolysis and decarboxylation reaction are conducted in situ with the catalytic hydrogenation reaction without isolation of said reaction intermediates.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: October 22, 2002
    Assignee: Catalytica, Inc.
    Inventors: John M. Gruber, A. Ray Bulls, John H. Grate
  • Patent number: 6403638
    Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 11, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6379590
    Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: April 30, 2002
    Assignee: AlliedSignal Inc.
    Inventors: Chengjiu Wu, Jianhui Shan
  • Patent number: 6369194
    Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: April 9, 2002
    Assignee: Yale University
    Inventor: Harry H. Wasserman
  • Patent number: 6342523
    Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have the formula: where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: January 29, 2002
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
  • Publication number: 20020004608
    Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1
    Type: Application
    Filed: May 16, 2001
    Publication date: January 10, 2002
    Inventors: Leo Alig, Katrin G. Zbinden, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Hans Peter Wessl
  • Patent number: 6329547
    Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 11, 2001
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Eiichi Shirasawa, Koji Konomi, Masaki Ichikawa, Hiroshi Suhara
  • Patent number: 6310245
    Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 is
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: October 30, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Uwe Kardorff, Regina Luise Hill, Michael Rack, Wolfgang von Deyn, Stefan Engel, Martina Otten, Matthias Witschel, Ernst Baumann, Joachim Rheinheimer, Guido Mayer, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 6306840
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 23, 2001
    Assignee: Biogen, Inc.
    Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
  • Patent number: 6307088
    Abstract: The present invention concerns alkyl esters of &bgr;-amino acid derivatives which are useful in the synthesis of taxol and analogs.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: October 23, 2001
    Assignees: NaPro BioTherapeutics, Inc., Bryn Mawr College
    Inventors: Charles S. Swindell, Nancy Krauss
  • Patent number: 6147224
    Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: November 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6136999
    Abstract: A chemical compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 may be H or electron withdrawing group, R.sub.2 may be H or electron withdrawing group, R.sub.3 may be H or electron withdrawing group, R.sub.4 may be H or electron withdrawing group, R.sub.5 may be H or electron withdrawing group, R.sub.6 may be an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: October 24, 2000
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: Madhavi C. Chander, James D. McChesney, Jan Zygmunt
  • Patent number: 6130246
    Abstract: The compounds of formula I ##STR1## wherein: a) X is O, andY is OC.sub.1 -C.sub.4 alkyl; orb) X is O or S, andY is NHCH.sub.3have fungicidal properties and can be used in plant protection for controlling and preventing disease infestation.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: October 10, 2000
    Assignee: Novartis Crop. Protection Inc.
    Inventors: Hugo Ziegler, Rene Zurfluh
  • Patent number: 6111115
    Abstract: A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: August 29, 2000
    Assignees: Nippon Chemiphar Co., Ltd., Ube Industries, Ltd.
    Inventors: Masao Yamamoto, Kunio Kobayashi, Katsumasa Harada, Shigeyoshi Nishino, Hiroshi Sasaki
  • Patent number: 6072060
    Abstract: An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process incudes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, cephalomanninne and various analogs, including photoaffinity labeling candidates.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: June 6, 2000
    Assignee: Bryn Mawr College
    Inventors: Charles S. Swindell, Nancy Krauss
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6049006
    Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, tifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: April 11, 2000
    Assignee: American Home Products Corp.
    Inventors: Thomas Joseph Commons, Susan Christman
  • Patent number: 6034272
    Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: March 7, 2000
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Susan Christman
  • Patent number: 6028205
    Abstract: Taxane derivatives having alternative C2 substituents.
    Type: Grant
    Filed: December 8, 1997
    Date of Patent: February 22, 2000
    Assignee: Florida State University
    Inventors: Robert A. Holton, Chunlin Tao
  • Patent number: 6025507
    Abstract: Borneol derivatives of formula I ##STR1## in which R.sup.1 to R.sup.5 and X.sup.1 to X.sup.2 are defined in the specification, and the method of making the same.
    Type: Grant
    Filed: August 28, 1998
    Date of Patent: February 15, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Hernamm Graf, Gunter Neef, Siegfried Blechert
  • Patent number: 6025516
    Abstract: The present invention provides an efficient route to the C-13 side chain of the anti-cancer drug paclitaxel (TAXOL) and its analogs. The process includes the resolution of racemic erythro 2-hydroxy-3-amino-3-phenylpropionamide by diastereomeric crystallization and its conversion via various intermediates to the threo-ethylester and threo-methylester isomers.
    Type: Grant
    Filed: October 14, 1998
    Date of Patent: February 15, 2000
    Assignee: Chiragene, Inc.
    Inventors: Sowmianarayanan Ramaswamy, Venkat G. Reddy, Yalin Luo
  • Patent number: 5985919
    Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5886206
    Abstract: A process for production of l-alkylthiomethanediphosphonic acid compound or 1-arylthiomethanediphosphonic acid compound characterized by removing a thiolate byproduct as an insoluble salt, in the condensation represented by the following formula: ##STR1## wherein R'.sub.1 represents a linear or branched alkyl group having 1 to 6 carbon atoms, R.sub.2 represents an alkyl or aryl group, R.sub.1 represents a pharmaceutically allowable cation, hydrogen atom, or linear or branched alkyl group having 1 to 6 carbon atoms. The present invention significantly improves the yield compared with conventional methods, and simplifies the purification process at the same time, thus is extremely useful in an economical and industrial points of view.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: March 23, 1999
    Assignee: Toray Industries, Inc.
    Inventors: Norio Kawabe, Keijiro Takanishi, Hiromi Uchiro, Kouichi Tsuruta, Ryuichi Haruta
  • Patent number: 5856578
    Abstract: The present invention relates to a process for the preparation of aromatic amino compounds which are substituted by a least one group comprising at least one unsaturated carbon-carbon bond, by catalytic hydrogenation of corresponding aromatic nitro compounds in the presence of a modified noble metal catalyst, wherein the noble metal catalyst used is platinum modified with a metal selected from the group consisting of lead, mercury, bismuth, germanium, cadmium, arsenic, antimony, silver and gold, and to novel noble metal catalysts for use in this process.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: January 5, 1999
    Assignee: Norvartis Corporation
    Inventors: Urs Siegrist, Peter Baumeister
  • Patent number: RE36718
    Abstract: An object of the present invention is to provide a safe method of commercially producing optically active aminoalcohol derivatives, which serve as intermediates for the synthesis of medicinal chemicals such as the immunopotentiating anticancer agent bestatin, in a simple and easy manner in high yields and with high levels of selectivity.The present invention consists in a method of producing 3-amino-1-nitro-4-phenyl-2-butanol derivatives of the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a hydrogen atom or an amino group protecting group, and a method of producing 3-amino-2-hydroxy-4-phenylbutyric acid derivatives derivable therefrom.
    Type: Grant
    Filed: March 30, 1999
    Date of Patent: May 30, 2000
    Assignee: Kaneka Corporation
    Inventors: Masaru Mitsuda, Shigeo Hayashi, Junzo Hasegawa, Noboru Ueyama, Takehisa Ohashi, Masakatsu Shibasaki