Abstract: This invention relates to benzopyran derivatives of the formula (1) or the formula (2) wherein R1 and R2 represent independently of each other hydrogen atom or C1-6alkyl group, R3 represents hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents hydrogen atom or C1-6 alkyl group, R5 represents C1-6 alkyl group substituted with C6-14 aryl group or heteroaryl group, R6 represents C1-6 alkyl group, C1-6 alkoxy group, halogen atom, nitro group, C(O)NH2, C(O)NHR8 or C(O)NR8R9, or pharmaceutically acceptable salts thereof.
Abstract: A method of oxidizing a carbon-carbon double bond wherein the compound having the carbon-carbon double bond is suppressed, the unreacted compound is separated from the reaction product, and thereafter the thus obtained unreacted compound is again used for the oxidizing reaction; and a process for producing an oxidized compound utilizing such an oxidizing method. When this method is used, an intended oxidized compound can be obtained with high selectivity and high productivity.
Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
Type:
Grant
Filed:
August 5, 2002
Date of Patent:
April 25, 2006
Assignee:
Schering AG
Inventors:
Jurgen Westermann, Johannes Platzek, Orlin Petrov
Abstract: Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain
Type:
Grant
Filed:
April 18, 2002
Date of Patent:
April 18, 2006
Assignee:
AstraZeneca AB
Inventors:
Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
Abstract: A method of stabilizing R-?-lipoic acid includes combining R-?-lipoic acid with nicotinamide in a weight ratio between about 10:4 to about 10:8. A composition for treating oxidative stress includes R-?-lipoic acid and nicotinamide in a weight ratio of between about 10:4 and about 10:8.
Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.
Type:
Grant
Filed:
January 16, 2004
Date of Patent:
April 11, 2006
Assignee:
CV Therapeutics, Inc.
Inventors:
Robert Jiang, Tim Marquart, Jeff Zablocki, Elfatih Elzein, Venkata Palle, Prabha Ibrahim
Abstract: An organic compound having at least one C—C double bond is epoxidized by means of hydrogen peroxide in the presence of at least one catalytically active compound and at least one solvent, wherein a product mixture comprising ?-hydroperoxyalcohols is reduced using at least one reducing agent.
Type:
Grant
Filed:
February 6, 2002
Date of Patent:
April 11, 2006
Assignee:
BASF Aktiengesellschaft
Inventors:
Joaquim Henrique Teles, Alwin Rehfinger, Anne Berg, Peter Rudolf, Norbert Rieber, Peter Bassler
Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
February 21, 2006
Assignee:
CV Therapeutics, Inc.
Inventors:
Prabha Ibrahim, Kevin Shenk, Elfatih Elzein, Venkata Palle, Jeff Zablocki, Kenneth S. Rehder
Abstract: Preparation of citalopram comprises the steps of: (a) converting the compound of Formula (I) to a compound of Formula (II), wherein R in Formula (I) represents a C2 to C5 alkylene group which may be substituted or unsubstituted, and R1 in the compounds of Formula (II) represents a carboxylic acid group or a salt or an ester thereof; and (b) converting the compound of Formula (II) to form citalopram or a pharmaceutically acceptable salt thereof, or a direct conversion of the compound of Formula (I) to citalopram
Type:
Grant
Filed:
March 7, 2001
Date of Patent:
February 21, 2006
Assignee:
Resolution Chemicals Limited
Inventors:
Alan K. Greenwood, Derek McHattie, Josef A. Rechka, Paul C. M. Hedger, Mark P. Gamble
Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
Abstract: A novel monomer compound having a lactone moiety of the present invention can be converted into polymers usable as resist materials with excellent properties, etc., and an alcohol compound having a lactone moiety of the invention is useful as a material for the monomer compound. The compounds are represented by the following general formula [1]: wherein one of R1 and R2 represents a hydrogen atom, an acryloyl group, or a methacryloyl group, and the other represents an alkyl group; R3 and R4 independently represent a hydrogen atom or an alkyl group; R5 and R6 both represent a hydrogen atom or are combined to form a methylene chain that may have an alkyl group; and R7 and R8 independently represent a hydrogen atom or a methyl group.
Type:
Grant
Filed:
June 10, 2004
Date of Patent:
January 31, 2006
Assignee:
Takasago International Corporation
Inventors:
Junji Nakamura, Shigetaka Numasawa, Hiroyuki Kenmochi, Yoji Hori
Abstract: The present invention relates to 5-nitrobenzofurans, to a process for preparing 5-nitrobenzofurans, and to 5-nitro-2,3-dihydrobenzofuran-3-ols, to a process for the preparation thereof and to intermediates.
Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
Type:
Grant
Filed:
August 23, 2001
Date of Patent:
November 15, 2005
Assignee:
SmithKline Beecham Corporation
Inventors:
Philip Anthony Harris, Robert N Hunter, Robert Walton McNutt, Jr., Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Robert Peel, Edgar Raymond Wood, III
Abstract: There is disclosed a process for the preparation of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1,13?-dihydroxy-9-oxo-19-norcyclopropa[g] tax-11-ene from 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1,13?-dihydroxy-9-oxo-7?-(trifluoromethyl sulfonyloxy) tax-11-ene by reaction with a molecular sieve in sulfolane.
Abstract: 2H-1-Benzopyran derivatives, processes for their preparation and use thereof for the preparation of pharmaceutical compositions for the prevention and treatment of postmenopausal pathologies.
Abstract: Motilide compounds having the formula (I), wherein R1, R2, R3, and R4 are as defined herein, and methods for their preparation and use in the treatment of diseases or conditions characterized by impaired gastric motility.
Type:
Grant
Filed:
August 26, 2003
Date of Patent:
September 20, 2005
Assignee:
Kosan Biosciences, Inc.
Inventors:
Daniel V. Santi, Brian Metcalf, Christopher Carreras, Yaoquan Liu, Robert McDaniel, Eduardo J. Rodriguez
Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
Abstract: The present invention provides compounds having improved stability over that of natural benzolactones, and a process for synthesizing these compounds. These compounds exhibit anti-cancer activity and inhibit V-ATPase activity.
Type:
Grant
Filed:
March 1, 2004
Date of Patent:
August 30, 2005
Assignee:
Board of Regents, The University of Texas System
Abstract: The invention relates to the use of cannabinoid compounds (derivatives of tetrahydrocannabinol) for decreasing cell proliferation in a mammal.
Type:
Grant
Filed:
May 17, 2001
Date of Patent:
July 5, 2005
Assignee:
Indevus Pharmaceuticals, Inc.
Inventors:
Sumner Burstein, Lawrence Recht, Robert B. Zurier