Abstract: The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
March 30, 2010
Assignee:
Wyeth LLC
Inventors:
Casey Cameron McComas, Puwen Zhang, Eugene Anthony Terefenko, An Thien Vu, Stephen Todd Cohn
Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds has the structure of formula (IV) wherein: R1, R2, R3, R4, R5, R6, R7, R8, R5A, R6A, R7A, R8A, R22 and R23 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
Abstract: The present invention relates to 2-(1H-indolylsulfanyl)-benzyl amine derivatives of general formula (I): which are useful as SSRIs, and pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
March 7, 2008
Date of Patent:
January 26, 2010
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Karsten Juhl, Morten Bang Norgaard, Jimmy Sejberg
Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.
Type:
Grant
Filed:
January 12, 2007
Date of Patent:
January 12, 2010
Assignee:
Wyeth LLC
Inventors:
Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
Abstract: [2-(6-fluoro-1H-indol-3-ylsulfanyl)benzyl]methyl amine and pharmaceutically acceptable salts thereof, provided it is not the free base in a non-crystalline form are provided for the treatment of affective disorders.
Type:
Application
Filed:
September 27, 2007
Publication date:
December 31, 2009
Applicant:
H. LUNDBECK A/S
Inventors:
Jan Kehler, Karsten Juhl, Neil Anderson
Abstract: The present invention relates to indolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Abstract: The present invention discloses and claims compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) are also disclosed and claimed.
Type:
Grant
Filed:
February 13, 2007
Date of Patent:
December 8, 2009
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William Arthur Metz, Jr., Fa-Xiang Ding
Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
Type:
Application
Filed:
February 10, 2009
Publication date:
December 3, 2009
Applicant:
President and Fellows of Harvard College
Inventors:
Jose A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
Abstract: This invention relates to the functionalized cyanine dyes and more particularly, to the synthesis of chiral 3-substituted 2,3?-dymethyl-3H-indole and its derivatives as intermediates for preparation of cyanine dyes, to methods of preparing these dyes and the dyes so prepared.
Type:
Grant
Filed:
May 9, 2003
Date of Patent:
November 10, 2009
Assignees:
Carnegie Mellon University, GE Healthcare UK Limited
Inventors:
Ratnaker B. Mujumdar, Richard Martin West
Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
March 28, 2007
Date of Patent:
November 3, 2009
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
Type:
Application
Filed:
September 26, 2006
Publication date:
September 3, 2009
Applicant:
The Regents of the University of California
Inventors:
Jack Taunton, Michael Cohen, Kevin Shokat, Chao Zhang
Abstract: The present invention relates to 2-(1H-indolylsulfanyl)-benzyl amine derivatives of general formula (I): and pharmaceutical compositions comprising the compounds useful as SSRIs.
Type:
Grant
Filed:
December 21, 2005
Date of Patent:
July 21, 2009
Inventors:
Jan Kehler, Karsten Juhl, Jimmy Sejberg, Morten Bang Nørgaard
Abstract: This invention relates to selenophene compounds of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to treat cancer.
Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.
Abstract: Certain 1H-indole-2-carboxylates and -2-carboxamides are HIV reverse transcriptase inhibitors. These indole compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
Type:
Application
Filed:
December 28, 2007
Publication date:
March 19, 2009
Applicant:
Xcovery, Inc.
Inventors:
Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
Type:
Application
Filed:
October 27, 2007
Publication date:
January 15, 2009
Applicant:
AMIRA PHARMACEUTICALS, INC.
Inventors:
John Howard HUTCHINSON, Nicholas Simon STOCK, Jeffrey Roger ROPPE
Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
Type:
Grant
Filed:
June 9, 2005
Date of Patent:
December 30, 2008
Assignee:
Kalypsys, Inc.
Inventors:
James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
Type:
Application
Filed:
August 8, 2007
Publication date:
December 25, 2008
Applicant:
INSTITUTE OF MEDICINAL MOLECULAR DESIGN. INC.
Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.
Type:
Grant
Filed:
September 6, 2006
Date of Patent:
December 16, 2008
Assignee:
H. Lundbeck A/S
Inventors:
Thomas P. Blackburn, Michael J. Konkel, Lakmal W. Boteju, Ian Jamie Talisman, John M. Wetzel, Mathivanan Packiarajan, Heidi Chen, Hermo Jimenez
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Abstract: Disclosed herein is a method comprising reacting a phenolphthalein material and a primary hydrocarbyl amine in the presence of an acid catalyst to form a reaction mixture comprising 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine, wherein the phenolphthalein material comprises greater than or equal to 95 weight percent phenolphthalein, based on the total weight of phenolphthalein material; quenching the reaction mixture and treating the quenched reaction mixture to obtain a first solid. The first solid is then triturated with a trituration solvent and washed to obtain a second solid, wherein the second solid comprises greater than or equal to 97 weight percent 2-hydrocarbyl-3,3-bis(4-hydroxyaryl)phthalimidine, based on the total weight of the second solid. The second solid may be polymerized to form a polycarbonate.
Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (III) wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, R20, and R21 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Type:
Grant
Filed:
November 15, 2005
Date of Patent:
August 19, 2008
Assignee:
Allergan, Inc.
Inventors:
Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
March 2, 2006
Date of Patent:
August 12, 2008
Assignee:
Roche Palo Alto LLC
Inventors:
Chris Allen Broka, Jeffrey Allen Campbell
Abstract: The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
Type:
Grant
Filed:
March 28, 2003
Date of Patent:
July 15, 2008
Assignee:
AstraZeneca AB
Inventors:
Stefan Berg, Sven Hellberg, Martin Nylöf, Yafeng Xue
Abstract: The present invention relates to a novel bisimide compound useful as an acid generator for a chemically amplified resist composition used in manufacturing of semiconductor element and the like or a raw material for synthesizing heat resistant polymers, an acid generator and a resist composition using said compound and a method for pattern formation using said composition, and further relates to a synthetic n intermediate for a bisimide compound and a bis(N-hydroxy)phthalimide compound useful as an intermediate for a functional compound such as a heat resistant polymer or photosensitive material, and provides a bisimide compound shown by the general formula [1]: (wherein R and A1 are as defined in claim 1).
Type:
Grant
Filed:
November 28, 2002
Date of Patent:
May 20, 2008
Assignees:
Wako Pure Chemical Industries Ltd., Matsushita Electric Industrial Co., Ltd.
Abstract: Compounds and methods for preparing 2-aryl-3-(aminoaryl)-3-(hydroxyaryl)phthalimidines having a formula of: wherein R1 is independently selected from a group consisting of a hydrocarbyl radical, a nitro radical, and a halogen atom; “a” is an integer from 0–4; and Ar1 and Ar2 are each independently an aromatic radical, are disclosed. The 2-aryl-3-(aminoaryl)-3-(hydroxyaryl)phthalimidine compounds are useful for preparing other useful monomers and polymers.
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
March 6, 2007
Date of Patent:
March 18, 2008
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Sheryl D. Debenham, Kun Liu, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minication of side effects of cyclid menstrual bleeding. Additional uses of the invention include stimulation of food intake.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
March 18, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Weiqin Jiang, James J. Fiordeliso, Zhihua Sui
Abstract: A 5-fluorooxindole-3-carboxylic acid ester represented by a formula (2): wherein R1 is a group selected from the group consisting of an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms, an unsubstituted or substituted cycloalkyl group having 3 to 7 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 14 carbon atoms.
Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
Type:
Grant
Filed:
June 9, 2005
Date of Patent:
March 4, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Karen Elizabeth Lackey, Edgar Raymond Wood, III
Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.
Type:
Application
Filed:
January 12, 2007
Publication date:
August 30, 2007
Applicant:
Wyeth
Inventors:
Robert E. McDevitt, Yanfang Li, Albert J. Robichaud, Gavin D. Heffernan, Richard D. Coghlan, Ronald C. Bernotas
Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 11, 2003
Date of Patent:
July 31, 2007
Assignee:
Eli Lilly and Company
Inventors:
Matthew Lee Brown, Timothy Alan Grese, Prabhakar Kondaji Jadhav, David Andrew Neel, Mitchell Irvin Steinberg, Peter Ambrose Lander
Abstract: Cannabimimetic indole derivatives are presented which have preferentially high affinities for one of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals.
Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.
Type:
Grant
Filed:
June 17, 2003
Date of Patent:
May 15, 2007
Assignee:
Schering Corporation
Inventors:
Joseph A. Kozlowski, Bandarpalle B. Shankar, Neng-Yang Shih, Ling Tong
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
August 27, 2003
Date of Patent:
March 6, 2007
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Sheryl D. Debenham, Kun Liu, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
Type:
Grant
Filed:
October 12, 2002
Date of Patent:
February 13, 2007
Assignees:
The Scripps Research Institute, IRM LLC
Inventors:
Sheng Ding, Qiang Ding, Nathanael S. Gray
Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) production
Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.
Type:
Grant
Filed:
August 8, 2003
Date of Patent:
October 3, 2006
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Jo E. Handelsman, Robert M. Goodman, Doreen E. Gillespie, Alan D. Bettermann, Jon C. Clardy, Sean F. Brady
Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
Type:
Grant
Filed:
January 7, 2003
Date of Patent:
September 19, 2006
Assignee:
Sequoia Pharmaceuticals, Inc.
Inventors:
John W. Erickson, Michael Eissenstat, Abelardo Silva, Sergei Gulnik