1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
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Publication number: 20130074927Abstract: The invention provides highly fluorescent materials comprising a single (n=0) or a series (n=1, 2, etc.) of benzo heterocyclic systems. The photo-stable highly luminescent chromophores are useful in various applications, including in wavelength conversion films. Wavelength conversion films have the potential to significantly enhance the solar harvesting efficiency of photovoltaic or solar cell devices.Type: ApplicationFiled: September 25, 2012Publication date: March 28, 2013Applicant: NITTO DENKO CORPORATIONInventor: NITTO DENKO CORPORATION
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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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: 8404679Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.Type: GrantFiled: April 23, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20130072679Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: September 13, 2012Publication date: March 21, 2013Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Henner Knust, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Mingwei Zhou
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Publication number: 20130072485Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical ResearchInventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
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Publication number: 20130072470Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: September 20, 2012Publication date: March 21, 2013Applicant: ABBVIE INC.Inventors: Neil Wishart, Dominique F. Bonafoux, Kristine E. Frank, Adrian D. Hobson, Donald B. Konopacki, Gloria Y. Martinez, Lu Wang
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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: 8399666Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: October 30, 2006Date of Patent: March 19, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John H. Hutchinson, Petpiboon Peppi Prasit, Mark Moran, Jillian F. Evans, Brian Andrew Stearns, Jeffrey Roger Roppe, Yiwei Li, Jasmine Eleanor Zunic, Jeannie M. Arruda, Nicholas Simon Stock, Mustapha Haddach
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Patent number: 8399504Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: GrantFiled: April 21, 2009Date of Patent: March 19, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
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Publication number: 20130065907Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Stephan Roever, Uwe Grether
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Publication number: 20130065906Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: March 13, 2012Publication date: March 14, 2013Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bernd NOSSE, Andreas BLUM, Steffen BREITFELDER, Armin HECKEL, Frank HIMMELSBACH, Elke LANGKOPF, Bernd WELLENZOHN, Neil J. ASHWEEK, Nicole HARRIOTT
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Patent number: 8394834Abstract: The present invention relates to a compounds of formula I wherein R1, R2, Ar1, Ar2, R?, R?, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 16, 2010Date of Patent: March 12, 2013Assignee: Hoffman-La Roche Inc.Inventors: Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20130060027Abstract: Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.Type: ApplicationFiled: October 31, 2012Publication date: March 7, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130048505Abstract: Copper plating baths containing a leveling agent that is a reaction product of one or more of certain cyclodiaza-compounds with one or more epoxide-containing compounds that deposit copper on the surface of a conductive layer are provided. Such plating baths deposit a copper layer that is substantially planar on a substrate surface across a range of electrolyte concentrations. Methods of depositing copper layers using such copper plating baths are also disclosed.Type: ApplicationFiled: August 22, 2011Publication date: February 28, 2013Applicant: Rohm and Haas Electronic Materials LLCInventors: Zukhra I. NIAZIMBETOVA, Maria Anna Rzeznik
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Publication number: 20130053362Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: February 28, 2013Applicants: INTELLKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20130052281Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 22, 2012Publication date: February 28, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: William FARNABY, Charlotte FIELDHOUSE, Catrina KERR, Natasha KINSELLA, David LIVERMORE, Kevin MERCHANT, David MILLER, Katherine HAZEL
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Patent number: 8383625Abstract: Compounds of formula (I) in salt or zwitterionic form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: December 22, 2005Date of Patent: February 26, 2013Assignee: Novartis AGInventors: Neil J Press, Collingwood P Stephen
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Publication number: 20130045965Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
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Publication number: 20130040928Abstract: The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitrogen T-U represents C?C, V represents N, W represents C?O, R2 represents Cl or H, R3=H and R4=Me, A represents wherein n=m=1, X represents —CH2— and E represents —CH—, and D represents oxygen, along with the various isomers and mixtures thereof in any proportions, and the pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 15, 2011Publication date: February 14, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Samuel Mialhe, Didier Junquero, Karine Valeille
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Patent number: 8372838Abstract: Compounds of the formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.Type: GrantFiled: February 22, 2011Date of Patent: February 12, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-Metz, Rainer Walter, Dieter Wiedenmayer
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Patent number: 8372837Abstract: Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: July 15, 2009Date of Patent: February 12, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Dean A. Wacker, Karen A. Rossi, Ying Wang, Gang Wu
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Patent number: 8372836Abstract: Pharmaceutical compositions comprising a poorly water soluble ionizable drug, a cationic species and a dispersion polymer are disclosed, together with a process for forming the compositions. The neutral form of the drug has (i) a solubility of less than 1 mg/ml, in aqueous solution at a pH between 6 and 7, (ii) a solubility of less than 20 mg/mL in a volatile organic solvent, and (iii) an acidic pKa value of greater than 5. At least 90 wt % of the drug in the solid dispersion being in a non-crystalline form. The drug, the cationic species, and the dispersion polymer constitute at least 80 wt % of the solid dispersion.Type: GrantFiled: October 8, 2007Date of Patent: February 12, 2013Assignee: Bend Research, Inc.Inventors: Rodney James Ketner, Douglas Alan Lorenz, David Keith Lyon
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Publication number: 20130030001Abstract: The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.Type: ApplicationFiled: August 1, 2012Publication date: January 31, 2013Applicants: PULMAGEN THERAPEUTICS (SYNERGY) LIMITED, ASTRAZENECA ABInventors: Richard James BULL, Elizabeth Anne SKIDMORE, Rhonan Lee FORD, Andrew Nigel MATHER, Antonio METE
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130029978Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.Type: ApplicationFiled: December 24, 2010Publication date: January 31, 2013Inventors: Tomoyuki Kamino, Yoshitaka Maeda
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Publication number: 20130029999Abstract: Pyridazinyl compounds, compositions and related methods of use.Type: ApplicationFiled: October 1, 2012Publication date: January 31, 2013Applicant: NORTHWESTERN UNIVERSITYInventors: DANIEL MARTIN WATTERSON, LINDA J. VAN ELDIK, HEATHER BEHANNA, HANTAMALALA RALAY RANAIVO
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Publication number: 20130029984Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130030002Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.Type: ApplicationFiled: April 15, 2011Publication date: January 31, 2013Applicant: E I DuPont De Nemours and CompanyInventors: Mary Ann Hanagan, Andris Juris Liepa, Eric Allen Marshall, Robert James Pasteris
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Publication number: 20130023499Abstract: Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: January 4, 2012Publication date: January 24, 2013Applicant: Gilead Connecticut, Inc.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, David M. ARMISTEAD, Joseph RAKER
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Publication number: 20130023530Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventor: Euroscreen S.A.
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Publication number: 20130023526Abstract: The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.Type: ApplicationFiled: April 30, 2012Publication date: January 24, 2013Applicant: Abbott LaboratoriesInventors: David J. Calderwood, Eric C. Breinlinger, Steven L. Swann, Venkata Srikanth Chitty, Subramanyah Seetharama Shastry Hosahalli, Subhendu Mukherjee, Siva Sanjeeva Rao Thunuguntla
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Publication number: 20130023538Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Publication number: 20130023502Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.Type: ApplicationFiled: January 25, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
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Publication number: 20130023539Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.Type: ApplicationFiled: June 18, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
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Publication number: 20130023494Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 5, 2011Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue
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Patent number: 8357679Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.Type: GrantFiled: May 13, 2009Date of Patent: January 22, 2013Assignee: MSD Oss B.V.Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
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Publication number: 20130018055Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: January 17, 2012Publication date: January 17, 2013Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
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Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Publication number: 20130018053Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: April 18, 2011Publication date: January 17, 2013Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
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Publication number: 20130018054Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
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Patent number: 8354535Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.Type: GrantFiled: March 26, 2010Date of Patent: January 15, 2013Assignee: Nycomed GmbHInventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
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Patent number: 8354411Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: GrantFiled: February 4, 2010Date of Patent: January 15, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Jun Kunitomo
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Patent number: 8354410Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 9, 2011Date of Patent: January 15, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
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Publication number: 20130012380Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkylType: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20130012381Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents have the meanings as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: March 21, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20130012485Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.Type: ApplicationFiled: December 20, 2007Publication date: January 10, 2013Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
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Publication number: 20130012503Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: January 10, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson