Abstract: The present invention relates to an antimicrobial compound having high safety as well as potent antimicrobial activity on a broad range of microorganisms represented by the following formula:
Abstract: The invention relates to certain novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
Type:
Grant
Filed:
May 2, 2002
Date of Patent:
September 6, 2005
Assignee:
SmithKline Beecham, PLC
Inventors:
Harshad Kantilal Rami, Mervyn Thompson, Paul Adrian Wyman
Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
August 30, 2005
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
February 6, 2003
Date of Patent:
July 19, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
May 24, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Soo Ko, George DeLucca, John Duncia, Ui Tae Kim, Joseph B. Santella III, Dean A. Wacker
Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.
Type:
Grant
Filed:
May 5, 2004
Date of Patent:
May 10, 2005
Assignee:
Bristol-Myers Squibb Company
Inventors:
Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
October 24, 2002
Date of Patent:
April 5, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
December 28, 2004
Assignees:
Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.
Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
January 20, 2004
Publication date:
December 23, 2004
Applicant:
G. D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
Abstract: The present invention relates to carboxamide compounds of general formula I 1
Type:
Application
Filed:
August 22, 2003
Publication date:
December 2, 2004
Applicant:
Boehringer Ingelheim International GmbH
Inventors:
Dirk Stenkamp, Martin Lenter, Heike-Andrea Wieland, Klaus Rudolf, Stephan George Mueller, Ralf R.H. Lotz, Kirsten Arndt, Philipp Lustenberger, Thorsten Lehmann-Lintz
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
March 30, 2004
Publication date:
November 18, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: The present invention relates dipeptidyl peptidase IV inhibition and, more particularly, relates to glutaminyl derivatives, wherein the glutamin residue is bound in a peptide manner to a moiety which imitates the amino acid residue prolin, especially to a nitrogen containing moiety, pharmaceutical compositions containing said compounds, and the use of said compounds in inhibiting dipeptidyl peptidase IV and dipeptidyl peptidase IV-like enzyme activity.
Type:
Application
Filed:
May 5, 2004
Publication date:
November 18, 2004
Inventors:
Hans-Ulrich Demuth, Matthias Hoffmann, Torsten Hoffmann, Andre J. Niestroj, Stephan Schilling, Ulrich Heiser
Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis.
Type:
Application
Filed:
February 2, 2004
Publication date:
November 11, 2004
Inventors:
Xian-Ping Lu, Zhibin Li, Aihua Xie, Leming Shi, Boyu Li, Zhiqiang Ning, Song Shan, Tuo Deng, Weiming Hu
Abstract: This invention provides biphenyl derivatives containing (i) a (biphenyl-2-yl)oxycarbonylamino- or (biphenyl-2-yl)aminocarbonylamino-substituted (2-7C)azacycloalkyl or (5-10C)azabicycloalkyl group; (ii) a substituted 2-(4-hydroxyphenyl)-2-hydroxyethylamino group; and a divalent hydrocarbon group, where each group is further defined and optionally substituted as described in the specification. The biphenyl derivatives of the invention possess both &bgr;2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Type:
Application
Filed:
February 13, 2004
Publication date:
October 21, 2004
Inventors:
Mathai Mammen, Sarah Dunham, Adam Hughes
Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
Type:
Application
Filed:
February 26, 2004
Publication date:
September 30, 2004
Applicants:
Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.
Inventors:
Michael Graupe, James T. Palmer, David John Aldous, Sukanthini Thurairatnam
Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.
Type:
Application
Filed:
December 23, 2003
Publication date:
September 16, 2004
Applicant:
Genzyme Corporation
Inventors:
Mark M. Staveski, Robert J. Miller, Sharon R. Nahill
Abstract: The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts: 1
Abstract: Compounds of general formula I
are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Type:
Grant
Filed:
June 1, 2000
Date of Patent:
August 17, 2004
Assignee:
AstraZeneca Canada Inc.
Inventors:
Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
Abstract: The present invention relates generally to prodrugs of fused GABA analogs, pharmaceutical compositions of prodrugs of fused GABA analogs, methods of making prodrugs of fused GABA analogs and methods of using prodrugs of fused GABA analogs and pharmaceutical compositions of prodrugs of fused GABA analogs to treat or prevent various diseases.
Abstract: Novel antagonists of ∝4&bgr;1 integrin and/or ∝4&bgr;7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.
Type:
Application
Filed:
February 23, 2004
Publication date:
July 22, 2004
Inventors:
Juan Miguel Jimenez Mayorga, Jordi Bach Tana, Jesus Maria Ontoria Ontoria, Eloisa Navarro Romero
Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Application
Filed:
December 3, 2002
Publication date:
June 24, 2004
Applicant:
Schering Corporation
Inventors:
John W. Clader, Anandan Palani, Ruo Xu, Mark D. McBriar, Jing Su, Haiqun Tang
Abstract: The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
March 16, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus.
Type:
Application
Filed:
February 10, 2003
Publication date:
March 4, 2004
Applicant:
MitoKor
Inventors:
Yazhong Pei, Soumitra S. Ghosh, Ian William James
Abstract: A thioaryl sulfonamide hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
Type:
Application
Filed:
January 21, 2003
Publication date:
February 19, 2004
Inventors:
Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Madeleine Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. Mc.Donald, Gary A. DeCrescenzo
Abstract: &agr;-and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
January 27, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.
Type:
Grant
Filed:
January 29, 2002
Date of Patent:
December 2, 2003
Assignee:
Novartis AG
Inventors:
Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Küsters, Michael Mutz
Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
Type:
Application
Filed:
November 20, 2002
Publication date:
October 16, 2003
Inventors:
Torbjorn Lundstedt, Anna Skottner, Elisabeth Seifert, Igor Starchenkov, Peteris Trapencieris, Valerjans Kauss, Ivars Kalvins, Arne Boman
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
May 30, 2002
Publication date:
October 9, 2003
Applicant:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
Type:
Application
Filed:
January 21, 2003
Publication date:
September 25, 2003
Applicant:
Parker Hughes Institute located at Roseville, Minnesota
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
Type:
Application
Filed:
November 27, 2001
Publication date:
September 25, 2003
Applicant:
BAYER CORPORATION
Inventors:
Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.
Type:
Application
Filed:
October 29, 2002
Publication date:
September 11, 2003
Applicant:
Beacon Laboratories, Inc, a Delaware corporation
Inventors:
Hsuan-Yin Lan-Hargest, Norbert L. Wiech