The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System (e.g., Benzofuranyl-benzimidazole, Etc.) Patents (Class 548/305.1)
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Publication number: 20100317100Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.Type: ApplicationFiled: June 11, 2010Publication date: December 16, 2010Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
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Patent number: 7851625Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.Type: GrantFiled: June 19, 2009Date of Patent: December 14, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Ahmad Khodabocus, Zhi-Hui Lu, Chris Hugh Senanayake, Hanxun Wei, Yongda Zhang
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Publication number: 20100305070Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: December 2, 2010Applicant: The University Court of the University of DundeeInventors: Steven Albert Everett, Saraj Ulhaq
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Patent number: 7833632Abstract: Provided is a material for an organic EL device realizing an organic EL device capable of having a high current efficiency even at a low voltage. Provided is a derivative of heterocyclic compound having a nitrogen atom represented by the following general formula (A-1) or (A-2). In the formulae, R1a to R5a each represent a substituent, Ar1a to Ar3a each represent a single bond or a divalent connecting group, and HAr represents a group represented by a general formula (A-3) or (A-4). R6a to R10a each represent a substituent.Type: GrantFiled: April 4, 2005Date of Patent: November 16, 2010Assignee: Idemitsu Kosan Co., Ltd.Inventors: Masahiro Kawamura, Hiroshi Yamamoto, Chishio Hosokawa
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Publication number: 20100286393Abstract: The present invention relates to compounds with an increased in vivo biological activity, and especially an increased pharmaceutical activity, such as an anti-nematodal or antifungal activity, an immunosuppresive activity, a metabolism influencing activity and/or an anti-cancer activity. Specifically, the present invention relates to compound comprising an artemisinin derivative according to the general formula (I) covalently linked at the 1 or the 2 position to a compound with a biological activity thereby increasing the biological activity of said compound or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 10, 2008Publication date: November 11, 2010Applicant: DAFRA PHARMA N.V.Inventors: Frans Herwing Jansen, Shahid Ahmed Soomro
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Publication number: 20100267712Abstract: Disclosed is a compound of Formula (I) in which W and R1-R6 are defined herein. Also disclosed is a method of treating spinal muscular atrophy, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced directly or indirectly by mutation or frameshift.Type: ApplicationFiled: September 26, 2008Publication date: October 21, 2010Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
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Patent number: 7812042Abstract: Therapeutic applications, such as prevention, treatment and supplementation, for the use of novel and other thiolatocobalamins to protect human cells against the effects of oxidative stress. In particular, this invention relates to the use of a novel synthetic thiolatocobalamin, N-acetyl-L-cysteinylcobalamin (NACCbl) to protect animal cells against oxidative stress damage. This invention also relates to the use of thiolatocobalamins, such as NACCbl, in lieu of current, commercially available forms of vitamin B12 for the treatment and prevention of conditions associated with oxidative stress damage and for dietary supplementation.Type: GrantFiled: September 20, 2007Date of Patent: October 12, 2010Assignees: Kent State University, University of ChesterInventors: Nicola E. Brasch, Catherine Stephanie Birch, John Henry Howatson Williams
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Publication number: 20100239496Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Publication number: 20100240702Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.Type: ApplicationFiled: May 15, 2008Publication date: September 23, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Brian Nicholas Cook, Stephane De Lombaert, Michel Jose Emmanuel, Xin Guo, Ming-Hong Hao, Jin Mi Kim, Ho Yin Lo, Chuk Chui Man, Tina Marie Morwick, Peter Allen Nemoto, Kevin Chungeng Qian, Hidenori Takahashi, Steven John Taylor
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Patent number: 7795250Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: June 8, 2005Date of Patent: September 14, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Publication number: 20100190830Abstract: The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: ApplicationFiled: August 2, 2007Publication date: July 29, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Heinz Fretz, Julien Pothier, Philippe Risch
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Publication number: 20100184747Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: July 22, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Jens Juergen Quant, Stephan Karl Zahn
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Publication number: 20100179147Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
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Patent number: 7732617Abstract: Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-?-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.Type: GrantFiled: May 25, 2007Date of Patent: June 8, 2010Assignees: Brock University, Cornell UniversityInventors: Jeffrey Atkinson, Robert S. Parker, Stephan Ohnmacht, Phillip John Nava, Ryan West
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Publication number: 20100119475Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.Type: ApplicationFiled: September 4, 2009Publication date: May 13, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Almstetter, Michael Thormann, Andreas Treml, Hans-Ulrich Demuth, Torsten Hoffman
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Publication number: 20100099643Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: December 22, 2009Publication date: April 22, 2010Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20100099128Abstract: The present invention relates to an enzyme substrate for detecting peptidase activity in microorganisms, of formula (I) below: in which X is S; NX1; O; or NX1-CO; R1 is nothing or one of the following substituents: Cl, Br, F, I, OH, or an alkyl, aryl or carboxyl group; R2 is nothing or one of the following substituents: Cl; O—CH2—O; O—CH3; F, diethylenediamine-CH3, NR3R4, Br, I, OH, an alkyl, aryl or carboxyl group, NO2, or X1 is selected from: H, C2H4Ph, OH, an alkyl group and an aryl group; R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms and P is a peptide.Type: ApplicationFiled: May 29, 2008Publication date: April 22, 2010Inventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
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Publication number: 20100087464Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC?, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.Type: ApplicationFiled: August 27, 2007Publication date: April 8, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela A. Albaugh
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Publication number: 20100081643Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: September 21, 2009Publication date: April 1, 2010Inventors: BRETT C. BOOKSER, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Publication number: 20100066243Abstract: An organic electroluminescent device is provided and includes: a pair of electrodes; and at least one organic layer between the pair of electrodes, the at least one organic layer including a light-emitting layer containing a light-emitting material. The at least one organic layer includes at least one layer containing an indole derivative represented by formula (1). R102, R103, R104, R105 and R106 each independently represents a hydrogen atom or a substituent; R101 represents a substituent linking via a carbon atom; R101 and R106 may be bonded to each other to form a ring; R107 represents a substituent; n101 represents 1 or 2; and n102 represents an integer of from 0 to 5, provided that n101+n102?6.Type: ApplicationFiled: November 27, 2007Publication date: March 18, 2010Applicant: FUJIFILM CORPORATIONInventors: Tatsuya Igarashi, Kazunari Yagi
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Publication number: 20100056514Abstract: Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).Type: ApplicationFiled: March 26, 2009Publication date: March 4, 2010Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: John Gerard JURCAK, Matthieu BARRAGUE, Timothy Alan GILLESPY, Michael Louis EDWARDS, Kwon Yon MUSICK, Philip Marvin WEINTRAUB, Yan DU, Ramalinga M. DHARANIPRAGADA, Ashfaq Ahmad PARKAR
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Publication number: 20100029615Abstract: The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, A, X, n, and are as defined herein. Such novel benzamidazole derivatives are useful in trv treatment of abnormal cell growth, such as cancer, in mammals. This invention ate relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing sue compounds.Type: ApplicationFiled: December 5, 2007Publication date: February 4, 2010Inventors: Michael John Munchhof, Lawrence Alan Reiter, Andrei Shavnya, Christopher Scott Jones, Qifang Li, Robert Gerald Linde ll
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Patent number: 7649008Abstract: Various crystal forms of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid from a solvent, and a process for production thereof are provided.Type: GrantFiled: May 14, 2004Date of Patent: January 19, 2010Assignee: Teijin Pharma LimitedInventors: Mitsuru Teramoto, Naoki Tsuchiya, Hiroshi Saitoh
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Patent number: 7615555Abstract: 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).Type: GrantFiled: April 20, 2005Date of Patent: November 10, 2009Assignee: AstraZeneca ABInventors: Alan Faull, Howard Tucker
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Publication number: 20090264655Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.Type: ApplicationFiled: June 19, 2009Publication date: October 22, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Ahmad KHODABOCUS, Zhi-Hui Lu, Chris Hugh Senanayake, Hanxun Wei, Yongda Zhang
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Patent number: 7582770Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: February 18, 2005Date of Patent: September 1, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20090203743Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-Type: ApplicationFiled: April 27, 2009Publication date: August 13, 2009Inventors: Dominique Louis Surleraux, Piet Tom Wigernick, Markieke Christiane Voets, Sandrine Marie Vendeville, Herman Augustinus De Kock, Bernhard Joanna Vergouwen
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Publication number: 20090197882Abstract: Novel indazole derivatives of the formula (I), in which R1-R3 have the meanings indicated in Claim (1), are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: June 18, 2007Publication date: August 6, 2009Inventors: Hans Peter Buchstaller, Hans-Michael Eggenweiler, Michael Wolf, Christian Sirrenberg
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Patent number: 7569700Abstract: The present invention relates to carboxamide derivative compounds of formula I in which R1-R6 and R12 are hereinafter defined and together comprise carboximide derivatives for the therapeutic treatment of diabetes, hyperglycemia, lipid and carbohydrate metabolism disorders, arteriosclerotic manifestations and disorders and other blood sugar related disorders through a metabolic blood sugar-lowering action.Type: GrantFiled: September 14, 2007Date of Patent: August 4, 2009Assignee: sanofi - aventisInventors: Elisabeth Defossa, Karl Schoenafinger, Gerhard Jaehne, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7566732Abstract: This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.Type: GrantFiled: October 28, 2004Date of Patent: July 28, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Usha Ramesh, Sarkiz D. Issakani, Gary Charles Look
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Patent number: 7563902Abstract: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays.Type: GrantFiled: January 25, 2006Date of Patent: July 21, 2009Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Rupert Herrmann, Wolfgang Jenni
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Publication number: 20090170859Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: ApplicationFiled: February 17, 2009Publication date: July 2, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Youla S. TSANTRIZOS, Catherine CHABOT, Pierre BEAULIEU, Christian BROCHU, Martin POIRIER, Timothy A. STAMMERS, Bounkham THAVONEKHAM, Jean RANCOURT
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Publication number: 20090163472Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 9, 2008Publication date: June 25, 2009Inventors: Konstantinos GAVARDINAS, Prabhakar Kondaji Jadhav
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Patent number: 7544698Abstract: Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: March 30, 2007Date of Patent: June 9, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: James P. Edwards, Brad M. Savall, Chandravadan R. Shah
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Publication number: 20090118259Abstract: The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: November 1, 2006Publication date: May 7, 2009Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Patent number: 7514569Abstract: A benzimidazolone compound represented by a general formula (1), (in the formula, each of R1, R2, R3 and R4 represents independently a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, or an alkoxy group having 1 to 5 carbon atoms).Type: GrantFiled: December 7, 2004Date of Patent: April 7, 2009Assignee: Dainippon Ink and Chemicals, Inc.Inventor: Masaki Hosaka
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Publication number: 20090069300Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Applicant: WyethInventors: Dahui Zhou, Jonathan Laird Gross, Albert Jean Robichaud
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Publication number: 20090062268Abstract: A compound having the structure set forth in Formula (I): wherein the variables Y, R1, R2, R3, R4 and R5 are as defined herein. Compounds described herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of such compounds and pharmaceutical compositions to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: July 25, 2008Publication date: March 5, 2009Applicant: LEAD THERAPEUTICS, INC.Inventor: Daniel CHU
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Publication number: 20090054397Abstract: The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 designates —(CO)h—(NRa)j—(CRb?CRc)k—Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like; Cy designates a 5- or 6-membered heteroaryl; and V each independently designate the formula -L-X—Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).Type: ApplicationFiled: April 29, 2008Publication date: February 26, 2009Inventors: Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Takashi Doko, Taro Terauchi, Yoshimitsu Naoe, Takafumi Motoki
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Publication number: 20080293792Abstract: Tocopherol derivatives having the general formula: wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-?-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.Type: ApplicationFiled: May 25, 2007Publication date: November 27, 2008Inventors: Jeffrey Atkinson, Robert S. Parker, Stephan Ohnmacht, Phillip John Nava, Ryan West
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Publication number: 20080286231Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.Type: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Applicant: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj, Robert Sommer
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Publication number: 20080234327Abstract: This invention is directed to compounds of formula (I): wherein m, R1, R2, R3 and R4 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.Type: ApplicationFiled: March 21, 2008Publication date: September 25, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Jean-Jacques Cadieux, Jianmin Fu, Rajender Kamboj, Zaihui Zhang
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Publication number: 20080214519Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5 and R6, R7, R8 and R9 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.Type: ApplicationFiled: June 2, 2006Publication date: September 4, 2008Inventors: Hiroki Koike, Sachiko Sakakibara
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Patent number: 7411072Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.Type: GrantFiled: June 13, 2003Date of Patent: August 12, 2008Assignee: Eli Lilly and CompanyInventors: Michael Joseph Coghlan, Jonathan Edward Green, Timothy Alan Grese, Prabhakar Kondaji Jadhav, Donald Paul Matthews, Mitchell Irvin Steinberg, Kevin Robert Fales, Michael Gregory Bell
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Publication number: 20080153873Abstract: The present invention is directed to dihydrobenzofuranyl derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: WyethInventors: Puwen Zhang, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell