Abstract: The invention includes tetrahydroquinoline and related compounds of formula I and pharmaceutical compositions thereof, that exhibit useful antibacterial activity again a wide range of human and veterinary pathogens
Type:
Grant
Filed:
March 7, 2007
Date of Patent:
October 20, 2009
Assignee:
Pharmacia & Upjohn Company LLC
Inventors:
Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
Type:
Grant
Filed:
October 20, 2008
Date of Patent:
October 13, 2009
Assignee:
Eisai Corporation of North America
Inventors:
Vincent Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy D. Xing, Qun Liu
Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
Type:
Grant
Filed:
December 16, 2008
Date of Patent:
October 13, 2009
Assignee:
Wyeth
Inventors:
Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
Abstract: Fused-ring triazole compounds which inhibit proliferation of cells and exhibit a unique and intense fluorescence are provided. Also provided are methods for synthesizing these compounds and methods for using these compounds to inhibit cell proliferation and infection and to label and fluorescently detect selected molecules.
Type:
Grant
Filed:
July 28, 2006
Date of Patent:
October 6, 2009
Assignees:
University of Medicine and Dentistry of New Jersey, Rutgers, the State University, Lehigh University
Inventors:
Jeffrey D. Laskin, Ned Heindel, Diane Heck, Anna Marie Vetrano, Christophe Guillon, Peter DeMatteo
Abstract: A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.
Abstract: The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia.
Type:
Grant
Filed:
June 10, 2008
Date of Patent:
September 29, 2009
Assignee:
NicOx, S.A.
Inventors:
David S. Garvey, L. Gordon Letts, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson, Shiow-Jyi Wey
Abstract: Provided herein are novel substituted phenyl oxazolidinones and to processes for the synthesis thereof. Also provided are pharmaceutical compositions comprising one or more compounds described herein The compounds described can be useful antimicrobial agents, which can be effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci, as well as, anaerobic organisms, such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms, such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
Type:
Grant
Filed:
October 4, 2005
Date of Patent:
September 8, 2009
Assignee:
Choongwae Pharma Corporation
Inventors:
Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
Abstract: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).
Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Type:
Grant
Filed:
November 6, 2008
Date of Patent:
September 1, 2009
Assignee:
Anadys Pharmaceuticals, Inc.
Inventors:
Stephen E. Webber, Frank Ruebsam, Martin Tran, Peter Dragovich, Liansheng Li, Douglas Eric Murphy, David Kucera, Zhongxiang Sun, Chinh Viet Tran
Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating hepatitis C virus infections: wherein Z is X is N or CR9; Y is —(CR4R5)n—; n is 2, 3, 4, or 5; and R1 through R9 are defined herein.
Type:
Grant
Filed:
December 12, 2007
Date of Patent:
September 1, 2009
Assignee:
Anadys Pharmaceuticals, Inc.
Inventors:
Chinh V. Tran, Frank Ruebsam, Yuefen Zhou, Peter Dragovich, Alan X. Xiang
Abstract: This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections, and to pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
August 25, 2009
Assignee:
IRM LLC
Inventors:
Valentina Molteni, Xiaohui He, Yun He, Andreas Kreusch, Juliet Nabakka, Kunyong Yang
Abstract: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.
Type:
Grant
Filed:
March 3, 2006
Date of Patent:
August 25, 2009
Assignee:
The Scripps Research Institute
Inventors:
Julius Rebek, Jr., Shen Gu, Shannon Biros
Abstract: The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).
Type:
Grant
Filed:
July 15, 2004
Date of Patent:
August 25, 2009
Assignee:
AstraZeneca
Inventors:
Roger Bonnert, Stewart Gardiner, Fraser Hunt, Iain Walters
Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.
Type:
Grant
Filed:
September 6, 2006
Date of Patent:
August 25, 2009
Assignee:
Board of Trustees of Michigan State University
Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Type:
Grant
Filed:
February 24, 2006
Date of Patent:
August 18, 2009
Assignee:
Renovis, Inc.
Inventors:
Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, Jianhua He, legal representative, Zhi-Liang Wei, Carl Kaub, YunFeng Fang
Abstract: Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.