Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/339)
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Patent number: 8202871Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.Type: GrantFiled: January 24, 2011Date of Patent: June 19, 2012Assignee: Sanofi-AventisInventors: Marco Baroni, Letizia Puleo
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Publication number: 20120142691Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: August 4, 2010Publication date: June 7, 2012Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
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Publication number: 20120142705Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventor: Robert Francis Kester
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Patent number: 8193352Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: September 2, 2009Date of Patent: June 5, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Publication number: 20120136009Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: wherein R1 is imidazolyl, pyridinyl or pyrimidinyl, any of which is optionally substituted by one group independently selected from C1-3alkyl and C1-3alkoxy.Type: ApplicationFiled: April 14, 2010Publication date: May 31, 2012Inventor: Kevin Dinnell
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Publication number: 20120136026Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 31, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20120129829Abstract: The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 10, 2011Publication date: May 24, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael M. Garst, Wha Bin Im
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Publication number: 20120129890Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: July 26, 2010Publication date: May 24, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
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Publication number: 20120122842Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: Abbott LaboratoriesInventors: Michael L. Curtin, Bryan K. Sorensen, Howard R. Heyman, Richard F. Clark, Kevin R. Woller, Omar J. Shah, Michael Michaelides, Chris Tse, Anil Vasudevan, Helmut Mack, Todd M. Hansen, Ramzi Sweis, Marina A. Pliushchev
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Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Publication number: 20120122854Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
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Publication number: 20120122931Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: July 26, 2010Publication date: May 17, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
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Patent number: 8178553Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 20, 2010Date of Patent: May 15, 2012Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
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Publication number: 20120115811Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.Type: ApplicationFiled: February 12, 2010Publication date: May 10, 2012Applicant: Amgen Inc.Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, Xian Yun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
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Publication number: 20120115903Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.Type: ApplicationFiled: November 9, 2011Publication date: May 10, 2012Applicant: Gruenenthal GmbHInventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Patent number: 8173689Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: GrantFiled: May 8, 2009Date of Patent: May 8, 2012Assignee: Novartis AGInventors: James C. Sutton, Marion Wiesmann
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Publication number: 20120108565Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), 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, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, 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: July 30, 2009Publication date: May 3, 2012Inventors: Lalima Sharma, Jitendra A. Sattigeri, Narest Kumar, Ajay Yadav, Rijwan Momim, Shahadat Ahmed, Ian A. Cliffe, Pradip Kumar Bhatnagar, Sanjay Ghosh, V. Samuel Raj, Dilip J. Upadhyay
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Publication number: 20120108611Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: December 29, 2011Publication date: May 3, 2012Inventors: Jean-Michel Altenburger, Valérie Fossey, Gilbert Lassalie, Frédéric Petit, Jean Claude Vernieres, Philip Janiak
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Publication number: 20120101105Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.Type: ApplicationFiled: May 31, 2010Publication date: April 26, 2012Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
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Publication number: 20120101132Abstract: The present invention relates to a new compound of formula (I) 6-(5-cyano-2-hydroxy-1H-indol-3-yl)pyridine-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, pharmaceutical formulations containing said compounds, to the use of said active compounds in therapy, and methods of prevention and/or treatment of conditions associated with glycogen synthase kinase-3 related disorders, comprising administering to a mammal, including human in need of such prevention and/or treatment, a therapeutically effective amount of said compound, as well as a process for preparing said compound.Type: ApplicationFiled: October 28, 2011Publication date: April 26, 2012Inventors: Martina Claesson, Suzanne Iverson Hemberg, Fredrik Lake
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Patent number: 8163927Abstract: The present invention relates to certain azabicyclic compounds of formula (I)?: wherein the several groups are defined herein and are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.Type: GrantFiled: March 30, 2007Date of Patent: April 24, 2012Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Fabrizio Micheli, Alessandra Pasquarello, Silvia Terreni
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Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Publication number: 20120094995Abstract: This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.Type: ApplicationFiled: January 27, 2010Publication date: April 19, 2012Applicant: ASTRAZENECA ABInventors: Jeffrey Scott Albert, Donald Andisik, Cristobal Alhambra, Todd Andrew Brugel, Glen E Ernst, William Frietze, Lindsay Hinkley, Jeffrey Gilbert Varnes, Xia Wang, Hui Xiong
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Patent number: 8158656Abstract: The present invention relates to 2-indolinone derivatives which are capable of inhibiting protein kinases and histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal protein kinase activities or abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.Type: GrantFiled: May 8, 2009Date of Patent: April 17, 2012Assignee: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping Lu, Zhi-Bin Li, Zhi-Qiang Ning
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Patent number: 8153664Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: October 2, 2007Date of Patent: April 10, 2012Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8153638Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: GrantFiled: August 23, 2010Date of Patent: April 10, 2012Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20120083495Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, 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 by mutation or frameshift.Type: ApplicationFiled: December 5, 2011Publication date: April 5, 2012Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20120083475Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.Type: ApplicationFiled: June 11, 2010Publication date: April 5, 2012Inventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
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Publication number: 20120083494Abstract: The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors.Type: ApplicationFiled: September 16, 2011Publication date: April 5, 2012Applicants: AETERNA ZENTARIS GmbH, University of Montpellier Il, University of Montpellier I, Centre National De La Recherche Scient.Inventors: Babette Aicher, Gilbert Mueller, Klaus Paulini, Lars Blumenstein, Peter Schmidt, Matthias Gerlach, Michael Teifel, Jean Martinez, Jean-Alain Fehrentz, Anne-Laure Blayo
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Patent number: 8143291Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: January 3, 2011Date of Patent: March 27, 2012Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20120071512Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 12, 2010Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Sylvie Chamoin, Christopher M. Adams, Chun Zhang
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Publication number: 20120070412Abstract: The present invention is directed to a combination product for treating or ameliorating hepatitis C virus (HCV) infection or disorders or symptoms associated therewith in a subject in need thereof comprising, a HCV inhibitor and one or more therapeutic agents selected from either or both a HCV protease inhibitor and one or more different therapeutic agents administered in combination in an effective amount to the subject.Type: ApplicationFiled: April 5, 2010Publication date: March 22, 2012Applicant: PTC THERAPEUTICS, INC.Inventors: Frederick C. Lahser, Zhengxian Gu
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Publication number: 20120071508Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Alain Philippe Poncelet, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert, Luc Van Hijfte
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Patent number: 8129372Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: April 20, 2009Date of Patent: March 6, 2012Assignee: Shionogi & Co., Ltd.Inventor: Masahiro Sakagami
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Patent number: 8129417Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: November 25, 2009Date of Patent: March 6, 2012Assignee: Abbott LaboratoriesInventors: Andrew O. Stewart, Xenia B. Searle, Daria Darczak, Ming Clinton Yeung, Stanley DiDomenico
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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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Patent number: 8119624Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: October 27, 2010Date of Patent: February 21, 2012Assignee: Pfizer Inc.Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20120040990Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20120040958Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20120040950Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.Type: ApplicationFiled: December 21, 2010Publication date: February 16, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
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Patent number: 8110681Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, 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 by mutation or frameshift.Type: GrantFiled: March 13, 2007Date of Patent: February 7, 2012Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Albany Molecular Research, Inc., Science Applications International Inc. (SAIC)Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20120029027Abstract: The invention relates to a compound of the general formula (I), where: R is a hydrogen atom or a group selected from the (C1-C6)alkyl or (C3-C7)-cycloalkyl groups, optionally substituted by one or more groups independently selected from a halogen atom anti the (C3-C7)-cycloalkyl, (C1-C6)alkyl, (C1-C6)alkoxy, and hydroxy groups; R1 is a phenyl group optionally substituted by one or more substituents independently selected from halogen atoms and the (C1-C6)alkyl, (C1-C6)alkoxy, halo-(C1C6)alkyl, hydroxy, halo-(C1-C6)alkoxy, (C1-C6)alkyl-thio, (C1-C6)alkyl-SO, and (C1-C6)alkyl-SO2 groups; R2 is one or more substituents selected from a hydrogen atom, halogen atoms, and the halo-(C1-C6)alkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)-cycloalkyl-(C1C3)alkyl, phenyl, benzyl, (C1-C6)alkoxy, (C1-C6)alkyl-thio, (C1-C6))alkyl-SO, and (C1-C6)alkyl-SO2 groups; and Het is a heteroaryl group; wherein said compound is in the form of a base or an acid addition salt.Type: ApplicationFiled: March 15, 2010Publication date: February 2, 2012Applicant: SANOFIInventors: Geneviève Estenne-Bouhtou, Florence Medaisko
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Publication number: 20120029016Abstract: There is provided compounds of formula I, wherein ring R1a to R1c, R2a to R2e, and X have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: December 30, 2009Publication date: February 2, 2012Applicant: BIOLIPOX ABInventor: Peter Nilsson
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Publication number: 20120028990Abstract: A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.Type: ApplicationFiled: April 14, 2010Publication date: February 2, 2012Inventors: Takashi Fujimura, Hiroyuki Kishino, Takashi Mizutani, Shunji Sakuraba, Takahide Sasaki, Nagaaki Sato
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Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Publication number: 20120022058Abstract: Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Graciela Barbieri Arhancet, Agustin Casimiro-Garcia, Xiangyang Chen, David Hepworth, Marvin Jay Meyers, David Walter Piotrowski, Raj Kumar Raheja
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Patent number: 8101608Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the 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, SGK, TrkA, TrkB and TrkC kinases.Type: GrantFiled: November 7, 2005Date of Patent: January 24, 2012Assignee: IRM LLC, a Delware Limited CorporationInventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh
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Patent number: 8101775Abstract: The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the S1P1 receptor.Type: GrantFiled: December 19, 2007Date of Patent: January 24, 2012Assignee: Glaxo Group LimitedInventors: Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
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Publication number: 20120015052Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: March 15, 2010Publication date: January 19, 2012Inventors: Christopher S. Burgey, Brendan M. Crowley, Zhengwu J. Deng, Daniel V. Paone, Craig M. Potteiger