Polycyclo Ring System Having The Additional Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.06)
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Publication number: 20140121206Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: GlaxoSmithKliine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Patent number: 8703760Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: December 17, 2010Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
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Publication number: 20140107057Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.Type: ApplicationFiled: May 30, 2012Publication date: April 17, 2014Applicant: Syngenta Participations AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Patent number: 8697869Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 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: GrantFiled: March 21, 2011Date of Patent: April 15, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
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Publication number: 20140088112Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 30, 2012Publication date: March 27, 2014Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 8680101Abstract: The invention relates to a pharmaceutical composition containing pimobendan as an active ingredient. The invention also relates to a crystalline form of pimobendan, as well as to a combination of said crystalline form with at least one other therapeutically active ingredient. Moreover, the invention relates to uses of said crystalline form, as well as to a pharmaceutical composition containing it. Finally, the invention relates to a process for preparing a crystalline form of pimobendan.Type: GrantFiled: December 16, 2010Date of Patent: March 25, 2014Assignee: Eurovet Animal Health B.V.Inventors: Marinus Maria Martinus Boeren, Rudolf Johannes Paridaans, Sanita Petkune, Viesturs Lusis, Dzintra Muceniece
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Patent number: 8673917Abstract: The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.Type: GrantFiled: September 2, 2009Date of Patent: March 18, 2014Assignee: SanofiInventors: Gerhard Zoller, Marc Dietrich Voss, Hans Matter, Andreas Herling
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Publication number: 20140051672Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; 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: August 7, 2013Publication date: February 20, 2014Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy Brian HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
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Patent number: 8653079Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: December 11, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Patent number: 8629144Abstract: The invention relates to novel polymorphic and hydrate forms and salts of 6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline, to methods for their preparation, to pharmaceutical compositions comprising at least one of said polymorphic or hydrate forms or salts, and to the therapeutic and/or prophylactic use of such compositions. The invention also provides new manners for preparing said compound.Type: GrantFiled: June 19, 2008Date of Patent: January 14, 2014Assignee: Janssen Pharmaceutica NVInventors: Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Carina Leys, Julius Walter Jozef Dickens, Sigrid Carl Maria Stokbroekx
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Patent number: 8623870Abstract: Compounds of the formula (I), in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 10, 2009Date of Patent: January 7, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8623862Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: GrantFiled: September 13, 2011Date of Patent: January 7, 2014Assignee: SanofiInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Publication number: 20130331382Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: December 12, 2013Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
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Publication number: 20130324545Abstract: AKR1B1 (EC 1.1.1.21) is an aldose reductase that has mainly been associated with the polyol pathway, and more recently with lipid deperoxidation. We have discovered that the primary activity of this enzyme is rather a PGFS activity, catalyzing the transformation of PGH2 into PGF2?. AKR1B1 as a therapeutic target, and method for modulating its expression and activity are provided. Methods for regulating the expression and activity of PGF2? are also provided.Type: ApplicationFiled: July 17, 2013Publication date: December 5, 2013Applicant: UNIVERSITE LAVALInventors: Michael Fortier, Pierre Chapdelaine, Eva Bresson, Éric Madore
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Publication number: 20130324529Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: JANSSEN PHARMACEUTICA NVInventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
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Patent number: 8580968Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: GrantFiled: March 1, 2012Date of Patent: November 12, 2013Assignee: AbbVie Inc.Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
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Patent number: 8575118Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 19, 2012Date of Patent: November 5, 2013Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Patent number: 8569312Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: April 4, 2013Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130261129Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 29, 2013Publication date: October 3, 2013Applicant: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
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Publication number: 20130261103Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 31, 2011Publication date: October 3, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
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Patent number: 8546393Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: GrantFiled: January 26, 2010Date of Patent: October 1, 2013Assignee: SanofiInventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20130225591Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.Type: ApplicationFiled: September 14, 2010Publication date: August 29, 2013Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
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Patent number: 8513235Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: GrantFiled: April 10, 2009Date of Patent: August 20, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Publication number: 20130210773Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 21, 2011Publication date: August 15, 2013Inventor: Craig W. Lindsley
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Publication number: 20130203690Abstract: Phosphodiesterase type III (PDE III) inhibitor or a “Ca2+-sensitizing agent” or a pharmaceutically acceptable derivative thereof is used in the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure, and as a medication for the reverse remodeling of the heart of a patient with asymptomatic (occult) heart failure and their delayed onset of clinical symptoms.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens, Rainer Kleeman, Christian Troetschel, Andrea Vollmar
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Publication number: 20130197008Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.Type: ApplicationFiled: September 14, 2012Publication date: August 1, 2013Applicant: Pfizer Inc.Inventors: Robert O. HUGHES, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
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Patent number: 8486946Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: February 12, 2010Date of Patent: July 16, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk
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Patent number: 8486979Abstract: The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.Type: GrantFiled: June 6, 2008Date of Patent: July 16, 2013Assignee: AbbVie Inc.Inventors: Jianguo Ji, Chih-Hung Lee, Kevin B. Sippy, Tao Li, Murali Gopalakrishnan
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Publication number: 20130177613Abstract: A packaging assembly or kit includes packaging material containing a solid formulation including pimobendan dispersed in a polyvalent acid. The kit may also include a package leaflet or user instruction including the information concerning use of the solid formulation, for example, via the oral route for the prevention and/or treatment of congestive heart failure in a mammal in need of such prevention or treatment, preferably in a dog, cat or rodent.Type: ApplicationFiled: March 14, 2013Publication date: July 11, 2013Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Martin A. Folger, Bernhard Hassel, Stefan Henke, Jens Lehmann (nee Schmalz)
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Publication number: 20130178478Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: January 10, 2013Publication date: July 11, 2013Applicant: Hoffman-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8481537Abstract: The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.Type: GrantFiled: July 27, 2007Date of Patent: July 9, 2013Assignee: LG Life Sciences Ltd.Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130172323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: May 6, 2011Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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Patent number: 8476274Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: October 18, 2012Date of Patent: July 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Patent number: 8466153Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: December 5, 2007Date of Patent: June 18, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Gregor James MacDonald, José Ignacio Andrés-Gil, Frans Alfons Maria Van Den Keybus, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Publication number: 20130150344Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.Type: ApplicationFiled: August 3, 2011Publication date: June 13, 2013Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
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Publication number: 20130150326Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Publication number: 20130137700Abstract: Provided is a compound having a PDE10A inhibitory action, and useful as a medicament for the prophylaxis or treatment of mental diseases such as schizophrenia and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.Type: ApplicationFiled: August 3, 2011Publication date: May 30, 2013Inventors: Tomoaki Hasui, Makoto Fushimi, Hironori Kokubo, Takenori Hitaka, Shotaro Miura, Jun Kunitomo, Takahiko Taniguchi
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Publication number: 20130131062Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: May 23, 2013Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Publication number: 20130123254Abstract: The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.Type: ApplicationFiled: September 14, 2012Publication date: May 16, 2013Inventors: Barbara Biemans, Georg Jaeschke, Lothar Lindemann, Wolfgang Muster, Heinz Stadler, Eric Vieira
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Publication number: 20130096128Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: September 28, 2012Publication date: April 18, 2013Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20130090342Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.Type: ApplicationFiled: June 16, 2011Publication date: April 11, 2013Applicant: NOVARTIS AGInventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
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Publication number: 20130084332Abstract: This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.Type: ApplicationFiled: August 13, 2012Publication date: April 4, 2013Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Martin FOLGER, Stefan LEHNER, Annette GRAVE, Norbert POELLINGER, Randolph Seidler
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Patent number: 8404683Abstract: 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, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Patent number: 8399468Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: GrantFiled: March 2, 2010Date of Patent: March 19, 2013Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G. Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Patent number: 8357689Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: July 25, 2008Date of Patent: January 22, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch