Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Type:
Application
Filed:
March 10, 2004
Publication date:
October 7, 2004
Inventors:
Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
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 invention relates to a process for preparing enantiomer-enriched 3-heteroaryl-3-hydroxypropanoic acid derivatives and 3-heteroaryl-1-aminopropan-3-ols, and to their use.
Type:
Application
Filed:
September 24, 2003
Publication date:
September 16, 2004
Inventors:
Frank Berendes, Markus Eckert, Nils Brinkmann, Claus Dreisbach, Ruth Meissner, Rainhard Koch
Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
Type:
Application
Filed:
February 25, 2004
Publication date:
September 2, 2004
Applicant:
Bristol-Myers Squibb Pharma Company
Inventors:
Jiacheng Zhou, Lynette May Oh, Philip Ma
Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
Type:
Application
Filed:
October 8, 2003
Publication date:
August 26, 2004
Inventors:
Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds are useful in the treatment of benign prostatic hyperplasia.
Type:
Application
Filed:
February 9, 2004
Publication date:
August 12, 2004
Applicant:
Pfizer Inc
Inventors:
Jens Bertil Ahman, Paul Blaise Hodgson, Sarah Jane Lewandowski, Robert Walton
Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
Type:
Application
Filed:
September 23, 2003
Publication date:
August 12, 2004
Inventors:
Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
Abstract: The present invention relates to a process for making a compound of structure 4
which comprises reacting a compound of structure 1 with vinyl sulfone in the presence of a Lewis-acid at a temperature in a range of from 40° C. to 170° C., wherein each R1 is independently H, fluoro, chloro or bromo.
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:
Grant
Filed:
February 10, 2003
Date of Patent:
August 10, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: There is provided a series of novel &agr;-(N-sulfonamido)acetamide compounds of the Formula (I) 1
Type:
Application
Filed:
December 20, 2002
Publication date:
July 1, 2004
Inventors:
Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
Abstract: The present invention relates to a class of compounds represented by the Formula I 1
Type:
Application
Filed:
November 20, 2003
Publication date:
July 1, 2004
Applicant:
G. D. Searle & Co.
Inventors:
Nizal Samuel Chandrakumar, Bipinchandra Nanubhai Desai, Balekudru Devadas, Alan Frank Gasiecki, Renee Huff, Ish K. Khanna, James W. Malecha, Julie M. Miyashiro, Shashidhar N. Rao, Joseph Gerace Rico, Thomas Edward Rogers, Peter Gerrard Ruminski, Mark Andrew Russell, Yi Yu
Abstract: Nitrone derivatives are efficiently prepared by increasing reagent concentrations in reaction solutions. Aldehydes and amines may be condensed to prepare an imine intermediate. Elimination of the solution media generally renders the imine formation more efficient. The imine is then reacted with a peroxysulfate oxidizing agent in a solution having at least about 0.1M concentration of the imine. The oxaziridine is rearranged to produce the nitrone derivative in high yield and good purity.
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
Type:
Application
Filed:
October 21, 2003
Publication date:
June 24, 2004
Applicant:
Vertex Pharmaceuticals Incorporated.
Inventors:
Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
Abstract: The present invention relates to vulcanization accelerators constituted by compounds, derived from secondary amines, belonging to the class of enamines and to a process for their preparation.
Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aminoalkyl-substituted aryl compounds of Formula I: 1
Abstract: The present invention relates to a process for effectively preparing prostaglandin derivatives and to a stereospecific alkyl halide containing 15S-alcohol group as a starting material.
Type:
Application
Filed:
October 24, 2003
Publication date:
June 17, 2004
Inventors:
Won-Hun Ham, Chang-Young Oh, Kee-Young Lee, Yong-Hyun Kim, Yiu-Suk Lee
Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
Type:
Application
Filed:
May 7, 2003
Publication date:
June 17, 2004
Inventors:
Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
June 15, 2004
Assignee:
Shin-Etsu Chemical Co., Ltd.
Inventors:
Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
Abstract: The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.
Type:
Application
Filed:
September 18, 2003
Publication date:
June 10, 2004
Inventors:
Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Craig William Lindsley, Karen Lynn Lobb, James Arthur Nixon, Richard Todd Pickard, John Mehnert Schaus, Takako Takakuwa, Brian Morgan Watson
Abstract: Compounds having an Rho kinase inhibitory activity. These compounds include the compound of general formula (I): Het-X-Z, pharmaceutically acceptable salts thereof and solvates of the same, wherein Het represents a monocyclic or dicyclic heterocycle group containing at least one nitrogen atom (for example, pyridyl, phthalimido); X represents (i) an —NH—C(═O)—NH-Q1- group, (ii) an —NH—C(═O)-Q2- group, etc. (wherein Q1 and Q2 represent each a bond, alkylene or alkenylene); and Z represents hydrogen, halogeno, a monocyclic, dicyclic ortricyclic carbon cycle or heterocycle, etc. (for example, optionally substituted phenyl).
Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII):
useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
May 18, 2004
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.
Type:
Application
Filed:
September 5, 2003
Publication date:
May 13, 2004
Inventors:
Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B, Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
Type:
Application
Filed:
October 14, 2003
Publication date:
May 6, 2004
Inventors:
Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
Type:
Application
Filed:
November 3, 2003
Publication date:
April 8, 2004
Inventors:
Penglie Zhang, Robert M. Scarborough, Bing-Yan Zhu
Abstract: Compounds of the formula:
are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Type:
Grant
Filed:
February 27, 2003
Date of Patent:
April 6, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R1 is (C1-3)alkyloxy, (C1-3)alkyloxy(C1-3)alkyl, (C1-3)alkylthio, (C1-3)alkylthio(C1-3)alkyl, (C1-3)alkylsulfinyl, (C1-3)alkylsulfinyl(C1-3)alkyl, (C1-3)alkylsulfonyl, (C1-3)alkylsulfonyl(C1-3)alkyl, (C1-3)alkyloxycarbonyl, (CH2)n—CO—NR8R9? or (CH2)n—NR8R9?; n is 0, 1 or 2; R2 is hydrogen or (C1-3?)alkyl; R3 is (C1-3)alkyl or (C1-3)alkyloxy(C1-3?)alkyl; R4 is (C1-3)alkyloxy(C1-3)alkyl; or R3 and R4 form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C1-3)alkyl or (C1-3)alkyloxy; R5 and R6 are independently (C1-3)alkyl; R7 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R8 and R9 are independently (C1-3)alkyl; or R8 and R9 form together with
Type:
Application
Filed:
July 18, 2003
Publication date:
March 25, 2004
Inventors:
Niall Morton Hamilton, David Jonathan Bennett
Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases.
Type:
Application
Filed:
September 29, 2003
Publication date:
March 25, 2004
Inventors:
Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Hebler, Gerhard Muller, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystaline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
Type:
Application
Filed:
June 19, 2003
Publication date:
March 18, 2004
Inventors:
Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
Abstract: The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.
Type:
Application
Filed:
September 4, 2003
Publication date:
March 11, 2004
Applicant:
Pfizer Inc
Inventors:
Harry R. Howard, Christopher J. Schmidt, Thomas F. Seeger, Mark L. Elliott
Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Application
Filed:
December 11, 2002
Publication date:
February 12, 2004
Inventors:
Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
Abstract: A method of synthesizing pure enantiomers of acylanalides such as Casodex® (bicalutamide) and its derivatives includes contacting a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: 1
Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
Type:
Application
Filed:
July 29, 2003
Publication date:
February 12, 2004
Inventors:
Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Pinelro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
Abstract: An NF-&kgr;B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R4 is H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.
Abstract: A compound of formula (I):
wherein:
R1 represents hydrogen, halogen, alkyl or alkoxy,
X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl,
A represents any one of the groups described in the description,
their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
February 3, 2004
Assignee:
Les Laboratoires Servier
Inventors:
Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
Abstract: The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization.
Type:
Application
Filed:
July 23, 2002
Publication date:
January 29, 2004
Inventors:
Dimitri Coucouvanis, Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Melissa L.P. Price, Sean M. O'Hare
Abstract: The present invention provides a compound of formula I
which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Type:
Grant
Filed:
November 5, 2002
Date of Patent:
January 27, 2004
Assignee:
Pharmacia and Upjohn Comapny
Inventors:
Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach