Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.
Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1=R2=H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.
Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.
Type:
Grant
Filed:
June 15, 2005
Date of Patent:
February 12, 2008
Assignee:
Lanxess Deutschland GmbH
Inventors:
Hans-Christian Militzer, Boris Bosch, Markus Eckert, Benjamin Meseguer
Abstract: The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.
Type:
Grant
Filed:
May 26, 2006
Date of Patent:
February 12, 2008
Assignee:
Novartis AG
Inventors:
Guido Bold, Janet D King, Joerg Frei, Richard Heng, Paul W Manley, Bernhard Wietfeld, Jeanette M Wood
Abstract: The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents.
Type:
Grant
Filed:
August 12, 2004
Date of Patent:
February 5, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bruce A. Ellsworth, Chongqing Sun, Annapurna Pendri
Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations.
Abstract: The present invention provides sodium channel blockers represented by formula (I): where the structural variables are defined herein. The compounds of the present invention may be used for treating a variety of conditions as described herein.
Abstract: An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the
Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteonaimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention. In particular, the invention relates to treatment of viral infections using terphenyl derivatives.
Type:
Grant
Filed:
January 25, 2005
Date of Patent:
December 25, 2007
Assignee:
Yale University
Inventors:
Andrew D. Hamilton, Justin Ernst, Brendan Orner
Abstract: The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
May 5, 2003
Date of Patent:
December 25, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jennifer X. Qiao, Donald J. Pinto, Michael J. Orwat, Sarah R. Friedrich, Wei Han
Abstract: A method for producing a hydroxy-amino ester, or derivative thereof, is provided. A substituted ?-ketodiester having a ketone group and two ester functional groups is contacted with a ketoreductase under conditions permitting the reduction of the ketone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. The carboxylic acid is converted to an amine or a derivative thereof to produce a hydroxy-amino ester or derivative thereof. A number of novel hydroxy-amino esters are prepared by the method.
Type:
Grant
Filed:
December 16, 2004
Date of Patent:
November 27, 2007
Assignee:
BioCatalytics, Inc.
Inventors:
J. David Rozzell, Jr., Spiros Kambourakis
Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Abstract: A compound of formula I wherein X, Y, X? & Y? are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz.
Abstract: The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.
Abstract: Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents.
Type:
Grant
Filed:
October 7, 2004
Date of Patent:
November 6, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles Lawrence Cywin, Roman Wolfgang Fleck, Eugene Richard Hickey, Weimin Liu, Tina Marie Morwick, John Robert Proudfoot, Denice M. Spero
Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
Type:
Grant
Filed:
December 12, 2003
Date of Patent:
November 6, 2007
Assignees:
Elan Pharmaceuticals, Inc., Wyeth
Inventors:
Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
Abstract: Certain methods are disclosed that are useful in the preparation of CCK2 active amidophenyl-sulfonylamino-quinoxaline compounds of the formula: wherein R1, R2, Ra and Rb are defined.
Type:
Grant
Filed:
August 4, 2004
Date of Patent:
October 30, 2007
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani, Chennagiri R. Pandit
Abstract: Provided is a method for preparing oltipraz. The method includes reacting methyl 2-methyl-3-(pyrazin-2-yl)-3oxopropionate with phosphorus pentasulfide in the presence of a mixed solvent of toluene and xylene, followed by recrystallization.
Type:
Grant
Filed:
November 25, 2003
Date of Patent:
October 30, 2007
Assignee:
CJ Corporation
Inventors:
Jin Wan Kim, Kwang Do Choi, Jee Woong Lim, Kwang Hyeg Lee, Sang Ho Lee