Abstract: This invention concerns a compound of formula 1
Type:
Application
Filed:
August 20, 2003
Publication date:
May 27, 2004
Inventors:
Paul Adriaan Jan Janssen, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Jan Heeres, Frederik Frans Desire Daeyaert, Georges Joseph Cornelius Hoornaert, Frans Joseph Cornelius Compernolle, Amuri Kilonda
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C 1-4 alkyl, 4) C 3-7 cycloalkyl, 5) CF3, 6) OCF3, 7) C 1-4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3.
Type:
Application
Filed:
August 1, 2003
Publication date:
May 20, 2004
Inventors:
Mary Beth Young, Philippe G. Nantermet, Harold G. Selnick, Peter D. Williams
Inventors:
Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
Type:
Application
Filed:
July 3, 2003
Publication date:
March 11, 2004
Inventors:
Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
Type:
Application
Filed:
December 2, 2002
Publication date:
March 11, 2004
Inventors:
Michael J. Ricks, Richard B. Rogers, William H. Dent, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
Type:
Application
Filed:
December 2, 2002
Publication date:
February 19, 2004
Inventors:
Michael J. Ricks, William H. Dent, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesei, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
Abstract: Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.
Type:
Application
Filed:
June 23, 2003
Publication date:
February 12, 2004
Inventors:
Martin Krueger, Andreas Huth, Orlin Petrov, Dieter Seidelmann, Karl-Heinz Thierauch, Martin Haberey, Andreas Menrad, Alexander Ernst
Abstract: Disclosed are compounds of formula (I):
wherein:
Y represents a group (CH2)n, wherein n represents 0, 1 or 2;
R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted;
R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O
Type:
Grant
Filed:
December 16, 2002
Date of Patent:
January 13, 2004
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp, Kevin Thewlis
Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II
wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and
wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
Type:
Grant
Filed:
November 14, 2000
Date of Patent:
January 6, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Type:
Application
Filed:
February 24, 2003
Publication date:
December 25, 2003
Applicant:
Emisphere Technologies, Inc.
Inventors:
Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold, David Gschneidner, Koc-Kan Ho
Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.
Type:
Application
Filed:
February 27, 2003
Publication date:
December 4, 2003
Inventors:
Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
Abstract: Diarylanines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.
Type:
Application
Filed:
September 13, 2002
Publication date:
December 4, 2003
Inventors:
Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
Abstract: The invention relates to novel pesticidally active &agr;-sulfin and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the specification, and R8 is either hydrogen, (a), (b), (c), (d) or (e) wherein R11, R12, R13, R15 and R17 are each independently hydrogen or C1-C4 alkyl, R13 is C4-C12 alkyl, C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R16 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR18R19— or —NR2O—, wherein R18, R19 and R20 independently of each other are hydrogen or C1-C4 alkyl. The novel compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
Type:
Application
Filed:
May 6, 2003
Publication date:
December 4, 2003
Inventors:
Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
Type:
Application
Filed:
June 5, 2003
Publication date:
December 4, 2003
Inventors:
Eu-Gene Oh, Sung-Bo Ko, Won-Yeob Kim, Kyung-Hwa Kim, Dennis W. Choi, Laura L. Dugan, Tae-Cheon Kang, Jae-Young Koh, Kyung-Mi Kim, In-Jae Shin
Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using the sodium channel blockers.
Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula:
in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.
Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.
Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula;
and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.
Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
Type:
Application
Filed:
February 10, 2003
Publication date:
September 25, 2003
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The present invention provides compounds of Formula (I): 1
Type:
Application
Filed:
October 23, 2002
Publication date:
August 28, 2003
Inventors:
Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
Type:
Grant
Filed:
September 29, 2000
Date of Patent:
August 19, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
Abstract: The present invention relates to a process for the preparation of both the phenyl pyrazine derivative 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine and an intermediate in the synthesis of 2,6-diamino-3(2,3,5-trichlorophenyl)pyrazine, 2-{[Cyano-(2,3,5-trichlorophenyl)-methyl]-amino}-acetamidine or a salt thereof.
Abstract: Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
Type:
Application
Filed:
November 15, 2002
Publication date:
July 31, 2003
Inventors:
Patrick R. Verhoest, Robert Louis Hoffman, Jeffrey W. Corbett, Michael Dalton Ennis, Kristine E. Frank, Jian-Min Fu
Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
Type:
Application
Filed:
June 4, 2002
Publication date:
June 26, 2003
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof:
in which the group D is selected from a group of formula (A), (B) or (C) below:
in which
P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s);
A is a single bond, a C1-6alkylene or a C2-6alkenylene group;
R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
n is 0, 1, 2 or 3; and
R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or
in which Ra is an alkyl group containing 1 to 20 carbon atoms o
Type:
Grant
Filed:
July 19, 2000
Date of Patent:
April 15, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Steven Mark Bromidge, Stephen Frederick Moss
Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I):
wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
Abstract: The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical formulations containing the pyrazine derivatives and methods of use of these formulations as anti-tumor agents and to treat solid-tumor cancers, angiogenesis, diabetic retinopathy, rheumatoid arthritis, endometriosis and psoriasis.
Type:
Application
Filed:
September 19, 2001
Publication date:
March 27, 2003
Inventors:
Gee-Hong Kuo, Peter J. Connolly, Catherine Prouty, Alan DeAngelis, Aihua Wang, Linda Jolliffe, Steve Middleton, Stuart Emanuel
Abstract: This invention provides compounds of Formula I having the structure
wherein,
U, V, and W are as defined hereinbefore,
or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
Type:
Grant
Filed:
July 12, 2001
Date of Patent:
March 25, 2003
Assignee:
Wyeth
Inventors:
Mark Anthony Ashwell, William Ronald Solvibile
Abstract: The invention relates to a process for the preparation of carbonyl compounds by the oxidation of alcohols in the presence of osmium compounds as catalysts in water or a solvent mixture containing water.
Type:
Application
Filed:
July 23, 2002
Publication date:
March 20, 2003
Inventors:
Markus Eckert, Hans-Christian Militzer, Matthias Beller, Christian Dobler, Gerald Mehltretter, Uta Sundermeier
Abstract: There are described cycloalkyl derivatives of the formula (I)
Type:
Application
Filed:
May 10, 2002
Publication date:
March 13, 2003
Applicant:
Aventis Pharma S.A.
Inventors:
Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.
Type:
Application
Filed:
July 18, 2002
Publication date:
December 12, 2002
Inventors:
Andrew Michael Derrick, Nicholas Murray Thomson
Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Application
Filed:
March 14, 2002
Publication date:
December 5, 2002
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
Abstract: Compounds of the general formula P1-L-P2; wherein “P1” is a pyrazinoylguanidine sodium channel blocker, “L” is a linking group, and “P2” is either (i) a pyrazinoylguanidine sodium channel blocker or (ii) a P2Y2 receptor agonist, are disclosed. Pharmaceutical formulations containing the same and methods of use thereof to hydrate mucosal surfaces such as airway mucosal surfaces are also disclosed.
Abstract: The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are hydroxyethylamine tripeptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV. Consequently, the compounds of this invention may be advantageously used in the treatment of HIV infection, either alone or in combination with other inhibitors of HIV viral replication or with pharmacoenhancers such as cytochrome P450 inhibitors.
Type:
Grant
Filed:
November 20, 2001
Date of Patent:
October 29, 2002
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Joseph Armstrong Martin, Sally Redshaw, Steven Swallow, Gareth John Thomas
Abstract: Inclusion complexes of glipizide and a nonionic surfactant with cyclodextrin and cyclodextrin derivatives. A method of preparing the inclusion complexes of glipizide and a nonionic surfactant with cyclodextrin and cyclodextrin derivatives, by wetting cyclodextrin or a derivative thereof with a nonionic surfactant, and mixing the resulting mixture with glipizide. A pharmaceutical composition containing an inclusion complex of glipizide and a nonionic surfactant with cyclodextrin and cyclodextrin derivatives, in combination with pharmaceutically acceptable excipients.
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: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
July 23, 2002
Assignee:
UCB, S.A.
Inventors:
Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
Abstract: The present invention relates to novel heteroaryl-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.
Type:
Application
Filed:
September 7, 2001
Publication date:
May 30, 2002
Inventors:
Gerald McMahon, Peng Cho Tang, Laura Kay Shawver, Klaus Peter Hirth