Abstract: Constrained paclitaxel derivatives include a bridge extending from the C-3? phenyl to either the C4 or -3 positions. Many of the constrained paclitaxel derivatives provide activity comparable or superior to the natural product paclitaxel.
Type:
Grant
Filed:
January 14, 2005
Date of Patent:
December 25, 2007
Assignees:
Virginia Tech Intellectual Properties, Inc., Binghamton University, Emory University
Inventors:
David George Ian Kingston, Thota Ganesh, James Patrick Synder, Ami S. Lakdawala, Susan Lynn Bane
Abstract: The present invention relates to bicyclic tetrahydropyridine compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: Substituted 1,5-naphthyridine azolinones inhibit Cdk1 and are selective against Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts have antiproliferative activity and are useful as anti-cancer agents.
Abstract: The present invention relates to methods for making racemic 2-(7-chloro -1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)-1-isoindolinone and (+)-2-(7 -chloro-1,8-naphthyridine-2-yl)-3-(5-methyl-2-oxo-hexyl)-1-isoindolinone.
Type:
Grant
Filed:
April 27, 2006
Date of Patent:
December 4, 2007
Assignee:
Indevus Pharmaceuticals, Inc.
Inventors:
Sandra Marie Jennings, Timothy Lee Stuk
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor
Type:
Grant
Filed:
August 19, 2004
Date of Patent:
November 20, 2007
Assignee:
Wyeth
Inventors:
Ronald Charles Bernotas, Derek Cecil Cole, William Joseph Lennox
Abstract: Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal)
Abstract: The invention provides aporphine and oxoaporphine compounds that may be used to manufacture a medicaments for preventing or treating vascular dysfunctions that may result in ischemic and metabolic diseases or preventing complications associated with these diseases in human and mammal. The ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral thrombosis, ischemic cerebral embolism, hypoxic ischemic encephlopathy, ischemic cardiac disease or ischemic enteropathy etc. The metabolic disease may include diabetes-induced vascular diseases, such as hypertension, atherosclerosis, peripheral artery or venous thrombosis, retinopathy and nephropathy. Methods for treating ischemic and metabolic diseases or preventing complications are also disclosed.
Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
Type:
Grant
Filed:
March 8, 2005
Date of Patent:
October 30, 2007
Assignee:
Eli Lilly and Company
Inventors:
Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
Abstract: The present invention relates to the synthesis of intermediates for the preparation of compounds of formula (A): wherein n is 2 or 3 and various salt forms of these compounds.
Inventors:
Brian Christopher Bishop, Karel Marie Joseph Brands, Ian Frank Cottrell, Cameron John Cowden, Antony John Davies, Stephen Philip Keen, David Ross Lieberman, Gavin William Stewart
Abstract: Compounds represented by the general formula: [wherein R1 represents methoxy, ethyl, methylthio, etc., R2, R3 and R4 each represent hydrogen, a halogen, etc., R5 and R6 each represent —X5—X6—X7 (wherein X5 represents a single bond or —CO—, X6 represents a single bond, —NR3a, etc. and X7 and R3a each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.], salts thereof and hydrates of the foregoing.
Abstract: The invention relates to a process for obtaining and purifying pure ?-mangostin from the rind of the fruit (mangosteen) of Garcinia mangostana.
Type:
Grant
Filed:
July 14, 2005
Date of Patent:
October 23, 2007
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: Disclosed are compounds of formula A: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, R3, R21, A1, A2, X, and Z are as defined herein. Compounds of formula A are useful in the treatment of diseases and/or conditions related to cell differentiation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
Type:
Grant
Filed:
August 3, 2005
Date of Patent:
October 16, 2007
Assignee:
Serenex, Inc.
Inventors:
Gunnar J. Hanson, Roy W. Ware, Jr., Thomas E. Barta, He Huang
Abstract: The compounds of Formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors.
Abstract: A class of 8-fluoro-3-phenylimidazo[1,2-?]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
October 9, 2007
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Sarah Margaret Kelly, Kevin John Merchant, Kevin William Moore, Michael Reader
Abstract: Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
March 22, 2004
Date of Patent:
October 2, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Ravi P. Nargund, Zhixiong Ye, Liangqin Guo
Abstract: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine.
Type:
Grant
Filed:
December 13, 2004
Date of Patent:
October 2, 2007
Assignee:
Eli Lilly and Company
Inventors:
Jennifer Rebecca Allen, Albert Kudzovi Amegadzie, Kevin Matthew Gardinier, George Stuart Gregory, Steven Andrew Hitchcock, Paul J. Hoogestraat, Winton Dennis Jones, Jr., Daryl Lynn Smith
Abstract: The present invention is a thiobenzimidazole derivative represented by the following formula (1) or a medically acceptable salt thereof wherein said thiobenzimidazole derivative and a medically acceptable salt thereof have a potent activity of inhibiting human chymase. Thus, they are potential preventive and/or therapeutic agents clinically applicable to various diseases in which human chymase is involved.
Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.