At Least Three Hetero Rings Containing Patents (Class 544/364)
-
Patent number: 7998963Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.Type: GrantFiled: February 12, 2009Date of Patent: August 16, 2011Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
-
Publication number: 20110195955Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: August 18, 2008Publication date: August 11, 2011Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
-
Publication number: 20110196150Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: February 10, 2011Publication date: August 11, 2011Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
-
Patent number: 7994174Abstract: The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 17, 2008Date of Patent: August 9, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Tara Hampton
-
Patent number: 7994202Abstract: A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the compound has a strong antagonistic action against EP1 receptors, and is useful, for example, as an active ingredient of a medicine for the prevention and/or treatment of overactive bladder. The compound is also useful as an active ingredient of a medicine for the prevention and/or treatment of symptoms such as frequency urinary, urinary urgency, or urinary incontinence.Type: GrantFiled: July 14, 2009Date of Patent: August 9, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto
-
Publication number: 20110190316Abstract: The invention relates to substituted pyridines and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of haematological disorders, preferably of leukopenia and neutropenia.Type: ApplicationFiled: July 21, 2009Publication date: August 4, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephan Siegel, Andreas Wilmen, Niels Svenstrup, Mark Jean Gnoth, Adrian Tersteegen, Ulrich Rester
-
Publication number: 20110190314Abstract: The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an ?4?2 positive allosteric modulator, a method of using the same, and a related article of manufacture.Type: ApplicationFiled: April 5, 2011Publication date: August 4, 2011Applicant: Abbott LaboratoriesInventors: Murali Gopalakrishnan, Marie P. Honore, Chih-Hung Lee, John Malysz, Jianguo Ji, Tao Li, Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson
-
Publication number: 20110183966Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: February 4, 2011Publication date: July 28, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
-
Publication number: 20110184173Abstract: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.Type: ApplicationFiled: December 17, 2008Publication date: July 28, 2011Applicant: THE KITASATO INSTITUTEInventors: Hiroshi Tomoda, Tohru Nagamitsu, Satoshi Omura
-
Publication number: 20110178091Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: ApplicationFiled: September 23, 2009Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
-
Publication number: 20110178062Abstract: Certain substituted indole and benzothiophene compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: February 28, 2008Publication date: July 21, 2011Inventors: Brett D. Allison, Cheryl A. Grice, Kelly J. McClure, Alejandro Santillan, JR.
-
Publication number: 20110172238Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: July 16, 2010Publication date: July 14, 2011Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, JR., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingcan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
-
Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
-
Patent number: 7977348Abstract: Solvates and crystalline forms of imatinib mesylate are described. Further, methods for preparing such solvates and crystalline forms of imatinib mesylate are described. The structure diagram below shows the chemical structure of imatinib mesylate.Type: GrantFiled: April 17, 2008Date of Patent: July 12, 2011Assignee: Sicor Inc.Inventors: Alexandr Jegorov, Miloslav Chudík, Judith Aronhime, Ale{hacek over (s)} Gavenda, Ji{hacek over (r)}í Faustmann
-
Publication number: 20110166139Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: ApplicationFiled: June 15, 2009Publication date: July 7, 2011Applicant: ASTRAZENECA ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
-
Publication number: 20110166116Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: July 7, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
-
Publication number: 20110166088Abstract: The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Corynebacterium, Bacillus spp., Enterobactericeae,’ (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Jitendra A. Sattigeri, Naresh Kumar, Ajay Yadav, Lalima Sharma, Ian A. Cliffe, Shibu B. Varughese, Shaikh Rizwan Shabbir, V. Samuel Raj, Dilip J. Upadhyay, Pradip K. Bhatnager
-
Publication number: 20110166132Abstract: The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: December 12, 2008Publication date: July 7, 2011Applicant: Amgen Inc.Inventors: Stephen A. Hitchcock, Jian J. Chen, Mqhele Vellah Ncube, Thomas Nixey, Albert Amegadzie, Roxanne Kunz, Wenyan Qian, Ning Chen, Christopher M. Tegley, Frenel F. De Morin, Chester Chenguang Yuan, Qingyian Liu, Jiawang Zhu, Tanya A.N. Peterkin, Jeffrey A. Adams, Essa Hu, Frank Chavez, JR.
-
Publication number: 20110160196Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: December 22, 2010Publication date: June 30, 2011Inventors: Zhaozhong J. Jia, Yonghong Song, Robert M. Scarborough, Carroll Scarborough, Anjali Pandey
-
Publication number: 20110150833Abstract: Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: June 23, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Yen Ting Chen, Yan Yin, Hampton Sessions, Michael P. Smolinski, Lei Yao, Bo Wang, Bozena Frackowiak-Wojtasek
-
Publication number: 20110152285Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.Type: ApplicationFiled: April 23, 2009Publication date: June 23, 2011Inventors: Graham Edward Morris Sibley, Robert Downham, Lloyd James Payne, Derek Law, Jason David Oliver, Mike Birch, Gareth Morse Davies, Patricia Suling Davies
-
Patent number: 7964602Abstract: The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.Type: GrantFiled: December 1, 2006Date of Patent: June 21, 2011Assignee: Glaxo Group LimitedInventors: Gregor James MacDonald, Darren Jason Mitchell, Mervyn Thompson, Susan Marie Westaway
-
Patent number: 7964597Abstract: Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: November 26, 2008Date of Patent: June 21, 2011Assignee: Glaxo Group LimitedInventors: Darren Jason Mitchell, Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
-
Publication number: 20110144122Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.Type: ApplicationFiled: December 13, 2010Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Francoise BONO, Sandrine DELBARY-GOSSART
-
Patent number: 7956066Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: June 7, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
-
Publication number: 20110129440Abstract: The present invention relates to novel Heterocyclic Urea and Thiourea Derivatives of formula (I), compositions comprising the Heterocyclic Urea and Thiourea Derivatives, and methods for using the Heterocyclic Urea and Thiourea Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: June 2, 2011Inventors: Praveen K. Tadikonda, David F. Cauble, Timothy J. Guzi, M. Arshad Siddiqui
-
Publication number: 20110130379Abstract: The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.Type: ApplicationFiled: July 15, 2009Publication date: June 2, 2011Applicant: CONVERGENCE PHARMACEUTICALS LIMITEDInventors: Paul John Beswick, Alister Campbell, Andrew Peter Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
-
Publication number: 20110130286Abstract: Piperazine compounds of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the piperazine compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one piperazine compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: July 23, 2009Publication date: June 2, 2011Applicant: BASF SEInventors: Liliana Parra Rapado, Eike Hupe, Matthias Witschel, Thomas Seitz, Anja Simon, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Trevor William Newton, Frank Stelzer, Tao Qu, William Karl Moberg, Dschun Song, Michael Rack, Timo Frassetto, Klaus Kreuz, Julia Major
-
Patent number: 7951807Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substituents A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: July 13, 2005Date of Patent: May 31, 2011Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Herve Geneste
-
Publication number: 20110124658Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: ApplicationFiled: December 28, 2007Publication date: May 26, 2011Applicant: ABBOTT GMBH & CO. KGInventors: Astrid Netz, Thorsten Oost, Herve' Geneste, Wilfried Martin Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
-
Publication number: 20110124628Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 22, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
-
Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). 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 relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
-
Patent number: 7947699Abstract: Described is a highly stable amorphous form of imatinib mesylate having a water content of less than 0.5 percent by weight, based on the total weight of the amorphous imatinib mesylate, (anhydrous amorphous imatinib mesylate), a process for preparation thereof, and pharmaceutical compositions.Type: GrantFiled: January 9, 2009Date of Patent: May 24, 2011Assignee: Actavis Group PTC EHFInventors: Mayur Devjibhai Khunt, Nilesh Sudhir Patil, Haushabhau Shivaji Pagire, Nitin Sharadchandra Pradhan, Jon Valgeirsson
-
Publication number: 20110118263Abstract: The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.Type: ApplicationFiled: June 30, 2009Publication date: May 19, 2011Applicant: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd.Inventors: Jianqi Li, Kai Gao, Na Lv
-
Publication number: 20110117591Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.Type: ApplicationFiled: October 20, 2010Publication date: May 19, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
-
Publication number: 20110118280Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
-
Publication number: 20110118246Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 19, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
-
Publication number: 20110118233Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: May 6, 2009Publication date: May 19, 2011Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
-
Publication number: 20110118208Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: March 13, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl Mcconnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
-
Publication number: 20110118236Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.Type: ApplicationFiled: March 25, 2009Publication date: May 19, 2011Inventors: Michiyo Mochizuki, Shotaro Miura
-
Patent number: 7943768Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: GrantFiled: December 18, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
-
Patent number: 7943622Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.Type: GrantFiled: June 6, 2007Date of Patent: May 17, 2011Assignee: Cornerstone Therapeutics, Inc.Inventors: Roger B. Clark, Daniel Elbaum
-
Patent number: 7943605Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: GrantFiled: October 25, 2006Date of Patent: May 17, 2011Assignee: UCB Pharma S.A.Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
-
Publication number: 20110112110Abstract: Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases.Type: ApplicationFiled: March 30, 2009Publication date: May 12, 2011Applicants: UNIVERSITA' DEGLISTUDI DI MILANO- BICOCCA, UNIVERSITE ' DE GENEVE, UNIVERSITE ' CLAUDE BERNARD DE LYON 1Inventors: Carlo Gambacorti Passerini, Rosalind Helen Gunby, Alfonso Zambon, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Cerric Schneider
-
Publication number: 20110112070Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 12, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
-
Publication number: 20110112074Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jean-Michel ALTENBURGER, Gilbert LASSALLE, Jean-Pascal HERAULT
-
Publication number: 20110112075Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jerome MENEYROL, Jean-Michel ALTENBURGER, Frédéric PETIT, Gilbert LASSALLE, Jean-Pascal HERAULT
-
Patent number: 7939534Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: July 31, 2007Date of Patent: May 10, 2011Assignee: Cytokinetics, Inc.Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
-
Publication number: 20110105429Abstract: The use of thiazole-4-carboxylic esters and thioesters of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Y1, Y2, Y3, W, X and G have the meanings given in the description, and also of agrochemically active salts thereof, as fungicides.Type: ApplicationFiled: April 18, 2009Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Pierre Cristau, Stefan Harrmann, Nicola Rahn, Arnd Voerste, Ulrik Wachendorff-Neumann, Tomoki Tsuchiya
-
Publication number: 20110105505Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 28, 2009Publication date: May 5, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGInventors: Frank Stieber, Timo Heinrich, Dirk Wienke