The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen (e.g., 2 Benzamidomethyl - Pyrrolidines, Etc.) Patents (Class 548/567)
Hydrogen or acyclic carbon bonded directly to the -c(=x)- (e.g., 2 pyrrolidine acrylamide, etc.) (Class 548/568)
  • Cis-substituted aminocyclopropane derivative
    Patent number: 6949662
    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:
    Type: Grant
    Filed: March 28, 2002
    Date of Patent: September 27, 2005
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Makoto Takemura, Youichi Kimura, Hisashi Takahashi, Yohhei Ishida
  • Heterocyclic ureas, their preparation and their use as vanilloid receptor antagonists
    Patent number: 6939891
    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
  • Biaryl compounds as serine protease inhibitors
    Patent number: 6936719
    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
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6919368
    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
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6897234
    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
  • Acyl sulfonamides as inhibitors of HIV integrase
    Patent number: 6890942
    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
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6875776
    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
  • Cathepsin cysteine protease inhibitors
    Patent number: 6835727
    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.
    Inventors: Osamu Okamoto, Jean-Pierre Falgueyret, Renata Marcella Oballa, Petpiboon Prasit, Robert Rydzewski
  • Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Publication number: 20040260095
    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
  • New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
    Publication number: 20040242572
    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
  • Alpha- and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Publication number: 20040229922
    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
  • Glutaminyl based DP IV-inhibitors
    Publication number: 20040229848
    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
  • Hemiasterlin derivatives and uses thereof
    Publication number: 20040229819
    Abstract: The present invention provides compounds having formula (I): 1
    Type: Application
    Filed: September 22, 2003
    Publication date: November 18, 2004
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
    Publication number: 20040224992
    Abstract: Compounds of Formula (I) 1
    Type: Application
    Filed: February 24, 2004
    Publication date: November 11, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles Lawrence Cywin, Tina Marie Morwick, John Robert Proudfoot, David Thomson
  • Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity
    Publication number: 20040224991
    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
  • Biphenyl derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
    Publication number: 20040209860
    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
  • Substituted ureas and carbamates
    Publication number: 20040209925
    Abstract: The invention provides compounds of formula I: 1
    Type: Application
    Filed: November 26, 2003
    Publication date: October 21, 2004
    Applicants: ELAN PHARMACEUTICALS, INC., PHARMACIA & UPJOHN COMPANY
    Inventors: Shon R. Pulley, John A. Tucker
  • Calcilytic compounds
    Publication number: 20040192741
    Abstract: Novel calcilytic compounds and methods of using them are provided.
    Type: Application
    Filed: January 21, 2004
    Publication date: September 30, 2004
    Applicant: SmithKline Beecham Corporation & NPS Pharmaceuticals
    Inventors: Maria Amparo Lago, James Francis Callahan, Pradip Kumar Bhatnagar, Eric G. Del Mar, William M. Bryan, Joelle L. Burgess
  • Novel compounds and compositions as cathepsin inhibitors
    Publication number: 20040192742
    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
  • Anti-inflammatory compositions and methods
    Publication number: 20040180871
    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
  • Amides, useful in the inhibition of il-8-induced chemotaxis of neutrophils
    Publication number: 20040181073
    Abstract: N-(2-aryl-propionyl)-amides of formula (I) are described.
    Type: Application
    Filed: October 27, 2003
    Publication date: September 16, 2004
    Inventors: Marcelo Allegretti, Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Ginfranco Caselli, Maria Candida Cesta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, Giulio Agostino Gandolfi, Maria Carla Gandolfi, Arrigo Aldo Gandolfi, Francesco Colotta
  • Novel aliphatic compound, method of synthesis, and method of utilization
    Publication number: 20040162435
    Abstract: The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts: 1
    Type: Application
    Filed: December 17, 2003
    Publication date: August 19, 2004
    Inventors: Tadakazu Tamai, Kazuyoshi Yoshikai, Masazumi Nishikawa, Kunio Ogasawara, Itsuki Murota
  • Compounds
    Patent number: 6777561
    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
  • Arginine derivatives
    Publication number: 20040147567
    Abstract: An arginine derivative represented by the formula: 1
    Type: Application
    Filed: November 14, 2003
    Publication date: July 29, 2004
    Inventors: Atsuro Nakazato, Taketoshi Okubo, Hiroki Umemiya
  • Aspartyl protease inhibitors
    Publication number: 20040147454
    Abstract: The present invention provides compounds having the formula: 1
    Type: Application
    Filed: December 10, 2003
    Publication date: July 29, 2004
    Inventor: Wenjin Yang
  • Cell differentiation inducer
    Publication number: 20040147569
    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.
    Type: Application
    Filed: January 9, 2004
    Publication date: July 29, 2004
    Applicant: Schering Aktiengesellschaft
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi
  • Prodrugs of fused GABA analogs, pharmaceutical compositions and uses thereof
    Publication number: 20040147455
    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.
    Type: Application
    Filed: December 11, 2003
    Publication date: July 29, 2004
    Inventor: Mark A. Gallop
  • Urea derivatives as integrin alpha 4 antagonists
    Publication number: 20040142982
    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
  • MCH antagonists for the treatment of obesity
    Publication number: 20040122017
    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
  • Antiangiogenic drug to treat cancer, arthritis and retinopathy
    Publication number: 20040110959
    Abstract: Compounds having Formula I 1
    Type: Application
    Filed: July 10, 2003
    Publication date: June 10, 2004
    Inventors: Megumi Kawai, Jack Henkin, George S. Sheppard, Richard A. Craig
  • Bombesin receptor antagonists
    Publication number: 20040110768
    Abstract: Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: 1
    Type: Application
    Filed: December 4, 2003
    Publication date: June 10, 2004
    Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
  • N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040058961
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: July 10, 2003
    Publication date: March 25, 2004
    Inventors: Soo S. Ko, James R. Pruitt, Dean A, Wacker, Douglas G. Batt
  • Terminally-branched polymeric linkers and polymeric conjugates containing the same
    Publication number: 20040053976
    Abstract: The present invention is directed to polymeric-prodrug transport forms of the formula: 1
    Type: Application
    Filed: August 8, 2003
    Publication date: March 18, 2004
    Inventors: Anthony J. Martinez, Annapurna Pendri, Richard B. Greenwald, Yun H. Choe
  • 2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
    Patent number: 6706735
    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
  • Compounds for inhibiting insulin secretion and methods related thereto
    Publication number: 20040044049
    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
  • Hydroxypropyl amides for the treatment of Alzheimer's disease
    Publication number: 20040039034
    Abstract: The present invention relates to compounds of formula (I): 1
    Type: Application
    Filed: April 30, 2003
    Publication date: February 26, 2004
    Inventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
  • Thioaryl sulfonamide hydroxamic acid compounds
    Publication number: 20040034071
    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
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040034063
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: February 6, 2003
    Publication date: February 19, 2004
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
  • &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Patent number: 6683648
    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
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040002515
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: October 24, 2002
    Publication date: January 1, 2004
    Inventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
  • Antipathogenic benzamide compounds
    Publication number: 20030236198
    Abstract: Antipathogenic benzamide compounds having the formula 1
    Type: Application
    Filed: June 6, 2002
    Publication date: December 25, 2003
    Applicant: GeneSoft, Inc.
    Inventors: Roland W. Burli, Jacob A. Kaizerman, Peter Jones
  • Fermentative preparation process for and crystal forms of cytostatics
    Patent number: 6656711
    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
  • Beta-sulfone derivatives as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
    Publication number: 20030212056
    Abstract: The present application describes novel &bgr;-sulfone derivatives of formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: November 13, 2003
    Inventors: Jingwu Duan, Gregory R. Ott
  • Substituted cyclohexane derivatives
    Publication number: 20030199550
    Abstract: The present invention provides compounds of formula (I) 1
    Type: Application
    Filed: December 10, 2002
    Publication date: October 23, 2003
    Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Georges Hirth, Hans-Peter Maerki, Olivier Morand
  • Novel melanocortin receptor agonists and antagonists
    Publication number: 20030195212
    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
  • Alpha-and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Publication number: 20030191319
    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
  • Anthranilamides and methods of their use
    Publication number: 20030187033
    Abstract: The present invention is related to anthranilamides of formula I, 1
    Type: Application
    Filed: April 26, 2002
    Publication date: October 2, 2003
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • R-isomers of nonnucleoside inhibitors
    Publication number: 20030181717
    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
  • omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
    Publication number: 20030181442
    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
  • Novel delta dicarbonyl compounds and methods for using the same
    Publication number: 20030171409
    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