Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
Type:
Application
Filed:
January 29, 2003
Publication date:
December 11, 2003
Applicant:
Tularik Inc.
Inventors:
Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.
Type:
Application
Filed:
April 23, 2003
Publication date:
November 6, 2003
Inventors:
Iain Mair McDonald, Caroline Minli Rachel Low, Katherine Isobel Mary Steel, John Spencer
Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.
Type:
Application
Filed:
December 19, 2002
Publication date:
November 6, 2003
Inventors:
Xue-Min Cheng, Noe Erasga, Gary Frederick Filzen, Andrew Geyer, Chitase Lee, Bharat Kalidas Trivedi
Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses methods for making the disclosed compounds.
Type:
Application
Filed:
December 20, 2002
Publication date:
November 6, 2003
Inventors:
Xue-Min Cheng, Noe Erasga, Gary Frederick Filzen, Andrew Geyer, Chitase Lee, Bharat Kalidas Trivedi
Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).
Type:
Application
Filed:
December 3, 2002
Publication date:
October 9, 2003
Applicant:
The Procter & Gamble Company
Inventors:
Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
Abstract: To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.
Abstract: This invention describes C1-C6-epothilone fragments and an efficient process for the production of C1-C6-fragments of epothilones and derivatives thereof.
Type:
Application
Filed:
December 23, 2002
Publication date:
September 18, 2003
Applicant:
Schering AG
Inventors:
Ulrich Klar, Markus Berger, Bernd Buchmann, Wolfgang Schwede, Werner Skuballa
Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.
Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
Type:
Application
Filed:
August 5, 2002
Publication date:
August 21, 2003
Applicant:
Schering Aktiengesellschaft
Inventors:
Jurgen Westermann, Johannes Platzek, Orlin Petrov
Abstract: This invention provides a compound of the formula:
or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or
Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
Type:
Application
Filed:
November 20, 2002
Publication date:
August 14, 2003
Inventors:
Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
Abstract: The present invention relates to epothilone derivatives, having the following formula
in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
Type:
Grant
Filed:
May 26, 1998
Date of Patent:
August 12, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
Abstract: Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
Type:
Grant
Filed:
December 11, 2001
Date of Patent:
August 5, 2003
Assignee:
University of Kansas
Inventors:
Gunda I. Georg, Sajiv K. Nair, Emily Reiff, Ashok Rao Tunoori
Abstract: Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure
or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is I and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
July 1, 2003
Assignees:
Johns Hopkins University, Hauser, Inc.
Inventors:
Gary H. Posner, Hardwin O'Dowd, Suji Xie, Theresa A. Shapiro, Christopher Murray
Abstract: The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula:
[wherein R1 is a phenyl group which may have a lower alkoxy group(s) as a substituent(s) on the phenyl ring, and R2 is a group represented by the following general formula:
(wherein R3's, which may be the same or different, are each a carboxyl group, a lower alkoxy group or the like) or the like] and salts thereof.
Abstract: Compounds of the invention include 14-mehtyl epothilone derivatives. More generally, preferred compounds of the invention are those that can be produced by altering the epothilone PKS genes as described herein and optionally by action of epothilone modification enzymes and/or by chemically modifying the resulting epothilones produces when those genes are expressed.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
June 24, 2003
Assignee:
Kosam Biosciences, Inc.
Inventors:
Bryan Julien, Leonard Katz, Chaitan Khosla, Li Tang, Rainer Ziermann
Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.
Type:
Application
Filed:
August 30, 2002
Publication date:
June 19, 2003
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: The present invention relates to a novel 4′-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor.
Type:
Application
Filed:
October 3, 2002
Publication date:
June 5, 2003
Applicant:
CHEIL JEDANG Corporation
Inventors:
Il Hwan Cho, Jee Woong Lim, Ji Young Noh, Jong Hoon Kim, Sang Wook Park, Hyung Chul Ryu, Je Hak Kim, Hyung Ok Chun, So Young Wang, Eun Young Lee
Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
Type:
Application
Filed:
February 1, 2002
Publication date:
June 5, 2003
Inventors:
Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dongfang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
Abstract: The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof:
that includes preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof:
Abstract: The invention relates to a process for the preparation of a compound of the formula 1
Type:
Application
Filed:
January 15, 2002
Publication date:
April 3, 2003
Inventors:
Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony Cornelius O'Sullivan, Gottfried Seifert
Abstract: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: 1
Type:
Application
Filed:
April 11, 2002
Publication date:
March 6, 2003
Applicant:
Eli Lilly & Company Lily Corporate Center
Inventors:
Dawn A. Brooks, Christopher J. Rito, Anthony J. Shuker, Samuel J. Dominianni, Alan M. Warshawsky, Lynn S. Gossett, Donald P. Matthews, David A. Hay, Robert J. Ardecky, Pierre-Yves Michellys, John S. Tyhonas
Abstract: Novel benzotriazoles of the formula
in which
R, X1, X2, X3, X4 and Y have the meanings given in the description,
and their acid addition salts and metal salt complexes,
a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.
Type:
Grant
Filed:
September 26, 2001
Date of Patent:
February 18, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Lutz Assmann, Ralf Tiemann, Martin Kugler, Heinrich Schrage, Klaus Stenzel
Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
Type:
Application
Filed:
August 21, 2002
Publication date:
January 16, 2003
Inventors:
Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza
Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
Type:
Application
Filed:
June 12, 2002
Publication date:
January 2, 2003
Inventors:
Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
Abstract: A process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, hydroxymethyl, tifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; R3 is CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl or —CO2C1-6alkyl; and Y is N or CH comprising the step of preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4
Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Application
Filed:
March 27, 2002
Publication date:
November 28, 2002
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
Abstract: &agr;-Sulfenimino acid derivatives of formula I
including the optical isomers thereof and mixtures of such isomers, wherein
A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted,
B is a direct bond or optionally substituted alkylene,
E is hydrogen or optionally substituted aryl,
R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and
T is NH or oxygen,
have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.
The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.
Type:
Grant
Filed:
July 16, 2001
Date of Patent:
November 12, 2002
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
André Jeanguenat, Martin Zeller, Hugo Ziegler
Abstract: Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
Type:
Application
Filed:
December 11, 2001
Publication date:
October 24, 2002
Applicant:
THE UNIVERSITY OF KANSAS
Inventors:
Gunda I. Georg, Sajiv K. Nair, Emily Reiff, Ashok Rao Tunoori
Abstract: Compounds of formula (I)
are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
September 17, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
Abstract: Benzoylcyclohexanediones and benzoylpyrazoles, their preparation and their use as herbicides and plant growth regulators.
There are described benzoyl compounds of the formula (I), their preparation and their use as herbicides and plant growth regulators.
In this formula (I), R1, R2, R3 and R4 are various radicals, X is an alkylene chain which may contain a hetero atom and Het is a heterocycle or heteroaromatic ring.
Type:
Grant
Filed:
November 2, 2000
Date of Patent:
September 10, 2002
Assignee:
Aventis CropScience GmbH
Inventors:
Thomas Seitz, Lothar Willms, Thomas Auler, Hermann Bieringer, Felix Thürwächter
Abstract: A process is described which permits the preparation of Ritonavir with only five intermediate stages using the same starting materials as those used in the process described in WO 94/14436; the process described here is also particularly satisfactory from the point of view of environmental impact because nearly all of the carbon atoms used are subsequently incorporated in the final molecule. Finally, the improvement afforded by this novel process is linked with the fact that an inexpensive reagent, such as bis-trichloromethyl carbonate (BTC), is used in two of the five stages.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
June 18, 2002
Assignee:
Clariant Life Science Molecules (Italy) S.p.A.
Inventors:
Pietro Bellani, Marco Frigerio, Patrizia Castoldi
Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: 1
Type:
Application
Filed:
February 5, 2002
Publication date:
June 13, 2002
Inventors:
Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Joseph E. Sundeen, Rulin Zhao
Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.
Type:
Grant
Filed:
July 19, 2001
Date of Patent:
May 21, 2002
Assignee:
The University of Pittsburgh
Inventors:
Peter Wipf, Jonathan T. Reeves, Billy W. Day, Raghavan Balachandran
Abstract: Thiazole derivatives of formula II, in which R1 means C1-C4 alkyl, R2 means any protective group that can be chelated, R3 means hydrogen or C1-C4 alkyl, Y means CO2R4, CHO, CH—CH2 or CH2R5, whereby R4 stands for C1-C4 alkyl and an optionally substituted benzyl group, R5 stands for halogen, hydroxy, p-toluenesulfonate and —OSO2B and B stands for C1-C4 alkyl or C1-C4 perfluoroalkyl, can be produced free of diastereomers and are suitable for the production of epothilone A and epothilone B and derivatives thereof.
Type:
Grant
Filed:
June 14, 2000
Date of Patent:
May 7, 2002
Assignee:
Schering Aktiengesellschaft
Inventors:
Johann Mulzer, Anreas Mantoulidis, Elisabeth Oehler
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
April 30, 2002
Assignee:
Eli Lilly and Company
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) 1
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
March 19, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: The invention relates to a method of synthesis for a compound of formula (I),
wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.