The Additional Hetero Ring Is A 1,3-diazine Ring (including Hydrogenated) Patents (Class 514/263.21)
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Publication number: 20130116266Abstract: Compounds that inhibit P13K? activity, including compounds that selectively inhibit P13K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (P13K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which P13K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: December 27, 2012Publication date: May 9, 2013Applicant: ICOS CORPORATIONInventor: Icos Corporation
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Publication number: 20130116267Abstract: The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HTV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K P110 delta.Type: ApplicationFiled: July 13, 2011Publication date: May 9, 2013Inventors: Peter D. Katsikis, Alina C. Boesteanu, Martin Turner
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Publication number: 20130109703Abstract: The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.Type: ApplicationFiled: March 18, 2011Publication date: May 2, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Peter Eickelmann, Gerd Luippold, Michael Mark, Leo Thomas
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Publication number: 20130096104Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.Type: ApplicationFiled: March 15, 2011Publication date: April 18, 2013Applicant: GENENTECH, INC.Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang, Aihe Zhou
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Publication number: 20130089512Abstract: New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: June 14, 2011Publication date: April 11, 2013Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
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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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Publication number: 20130072459Abstract: The present invention provides a pharmaceutical composition for the prevention and treatment of a non-alcoholic fatty liver disease (NAFLD), containing an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof. Further, the present invention provides a method for the prevention or treatment of a non-alcoholic fatty liver disease, including administering an effective amount of an active ingredient selected from the group consisting of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof to a mammal including a human in need thereof. Further, the present invention provides use of Compound 1 represented by formula 1, sitagliptin, vildagliptin, linagliptin or a pharmaceutically acceptable salt thereof, for manufacturing a pharmaceutical composition for the prevention or treatment of a non-alcoholic fatty liver disease.Type: ApplicationFiled: March 23, 2011Publication date: March 21, 2013Inventors: Gook-Jun An, Eun-Kyoung Yang, Eun-Jung Cho, Yu-Na Chae, Song-Hyen Choi, Ha-Dong Kim, Chang-Yell Shin, Mi-Kyung Kim, Woo-Young Kwak, Heung-Jae Kim, Moon-Ho Son, Soon-Hoe Kim
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Publication number: 20130071323Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administering a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and administering at least one additional therapeutic agent.Type: ApplicationFiled: March 9, 2012Publication date: March 21, 2013Applicant: Gilead Calistoga LLCInventors: W. Michael Gallatin, Roger G. Ulrich, Neill A. Giese, Brian Lannutti, Langdon Miller, Thomas M. Jahn
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Publication number: 20130064887Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases.Type: ApplicationFiled: March 7, 2012Publication date: March 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Masanori ITO, Kenji EGUSA, Roman MESSERSCHMID, Peter SCHNEIDER
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Publication number: 20130065858Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: October 22, 2012Publication date: March 14, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., MILLENNIUM PHARMACEUTICALS, INC.Inventors: MILLENNIUM PHARMACEUTICALS, INC., SUNESIS PHARMACEUTICALS, INC.
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Publication number: 20130064812Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and one or more additional therapeutic agents optionally selected from the group consisting of bendamustine, rituximab, and ofatumumab.Type: ApplicationFiled: March 9, 2012Publication date: March 14, 2013Applicant: Gilead Calistoga LLCInventors: W. Michael GALLATIN, Roger G. Ulrich, Neill A. Giese, Brian Lannutti, Albert Yu, Langdon Miller, Thomas M. Jahn
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Patent number: 8377947Abstract: Use of a composition for treating Alzheimer's disease, osteoporosis, sleep apnea, erectile dysfunction, McArdle disease, or a carbohydrate metabolism disorder, or for reducing aging or fatigue. The composition includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5?-monophosphate-activated protein kinase activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.Type: GrantFiled: March 15, 2010Date of Patent: February 19, 2013Inventor: Chien-Hung Chen
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Publication number: 20120322728Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing diabetes mellitis, optionally in combination with a second treatment. Furthermore, the present invention also provides methods of inducing remission of the symptoms of diabetes mellitis in a patient comprising administering a thiazolidinedione analogue and a GLP-1 agonist.Type: ApplicationFiled: December 15, 2010Publication date: December 20, 2012Applicant: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
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Patent number: 8318750Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Patent number: 8309543Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 23, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
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Publication number: 20120282255Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.Type: ApplicationFiled: April 6, 2012Publication date: November 8, 2012Inventor: Greg Plucinski
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Publication number: 20120277150Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: April 11, 2012Publication date: November 1, 2012Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Munetaka OHKOUCHI
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Patent number: 8293752Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: October 23, 2012Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Weirong Chen, Jennifer Cossrow, Lloyd Franklin, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Benjamin Lane, Adam Littke, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Publication number: 20120263675Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.Type: ApplicationFiled: October 20, 2010Publication date: October 18, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun
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Publication number: 20120258950Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: PFIZER LIMITEDInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20120258170Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.Type: ApplicationFiled: March 19, 2012Publication date: October 11, 2012Applicant: Nutracryst Therapeutics Private LimitedInventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
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Patent number: 8258141Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: April 19, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120219622Abstract: The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.Type: ApplicationFiled: May 9, 2012Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Anja KOHLRAUSCH, Patrick ROMER, Gerd SEIFFERT
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Publication number: 20120219623Abstract: The present invention relates to therapeutic uses of pharmaceutical compositions or combinations of a DPP-4 inhibitor with metformin.Type: ApplicationFiled: October 1, 2010Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Thomas Meinicke
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Publication number: 20120207845Abstract: The invention relates to a method for treating disorders or diseases of a tight junction comprising delivering a pharmaceutical composition of nanoparticles to the tight junction, wherein the nanoparticles consist of positively charged chitosan, a negatively charged substrate, optionally a zero-charge compound, and at least one bioactive agent for treating said disorders or diseases of the tight junction of an animal subject.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Inventors: Hsing-Wen Sung, Kiran Sonaje, Ho-Ngoc Nguyen, Er-Yuan Chuang, Hosheng Tu
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Publication number: 20120208831Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: April 17, 2012Publication date: August 16, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Michael MARK, Roland MAIER, Ralf R. H. LOTZ, Mohammad TADAYYON
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Patent number: 8232281Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.Type: GrantFiled: May 4, 2007Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
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Publication number: 20120184519Abstract: The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HIV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta.Type: ApplicationFiled: March 12, 2012Publication date: July 19, 2012Inventors: Peter D. Katsikis, Alina C. Boesteanu, Martin Turner
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Publication number: 20120178767Abstract: The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.Type: ApplicationFiled: July 21, 2010Publication date: July 12, 2012Applicant: Gilead Calistoga LLCInventor: Roger G. Ulrich
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Patent number: 8207175Abstract: The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular the inhibition of those enzymes.Type: GrantFiled: June 21, 2006Date of Patent: June 26, 2012Assignee: University Court of the University of DundeeInventors: Daniel Marinus Ferdinand Van Aalten, Ian Michael Eggleston
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Publication number: 20120157430Abstract: The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: December 19, 2011Publication date: June 21, 2012Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Thomas P. Maduskuie, JR., Richard B. Sparks
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Publication number: 20120157459Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: December 24, 2010Publication date: June 21, 2012Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Patent number: 8202861Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 9, 2004Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120129874Abstract: The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production.Type: ApplicationFiled: December 22, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Sieger, Waldemar Pfrengle
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Publication number: 20120122776Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in paediatric patients.Type: ApplicationFiled: January 29, 2010Publication date: May 17, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eva Ulrike Graefe-Mody, Dietmar Neubacher, Thomas Rauch, Hans-Juergen Woerle
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Publication number: 20120121530Abstract: The present invention relates to certain DPP-4 inhibitors for treating and/or preventing oxidative stress, vascular stress and/or endothelial dysfunction as well as to the use of such DPP-4 inhibitors in treatment and/or prevention of diabetic or non-diabetic patients, including patient groups at risk of cardiovascular and/or renal disease.Type: ApplicationFiled: November 14, 2011Publication date: May 17, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Andreas DAIBER, Odd-Eric JOHANSEN, Michael MARK, Sanjaykumar PATEL, Hans-Juergen WOERLE
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Patent number: 8178541Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 20, 2008Date of Patent: May 15, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz, Mohammad Tadayyon
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Publication number: 20120107398Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and pioglitazone, processes for the preparation thereof, and their use to treat certain diseases.Type: ApplicationFiled: May 4, 2011Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter SCHNEIDER, Thorsten NEUHAUS
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Publication number: 20120108614Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: May 14, 2009Publication date: May 3, 2012Inventor: Jayhong A. Chong
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Patent number: 8163761Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: June 23, 2008Date of Patent: April 24, 2012Assignee: Hydra Biosciences, Inc.Inventors: Howard Ng, Manfred Weigele, Magdalene Moran, Jayhong Chong, Christopher Fanger, Glenn R. Larsen, Donato Del Camino, Neil Hayward, Steven P. Adams, Amy Ripka
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Publication number: 20120094894Abstract: The invention relates to antidiabetic medications which are suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia, inter alia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions. The medication is a mono treatment with a DPP-4 inhibitor <preferably linagliptin> or a combination treatment with a DPP-4 inhibitor and a second and/or third antidiabetic.Type: ApplicationFiled: February 12, 2010Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eva Ulrike Graefe-Mody, Hans-Juergen Woerle
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Patent number: 8153628Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the group consisting of oxazoyl, isoxazoyl, thiazolyl, and isothiazoyl; and Z1 is a 5-14 member substituted or unsubstituted heteroaryl ring; which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: July 22, 2009Date of Patent: April 10, 2012Assignee: Forest Laboratories Holdings LimitedInventors: Guoquan Wang, Jayson M Rieger, Robert D Thompson
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Publication number: 20120083473Abstract: Provided herein are methods for treating certain conditions, including fibrosis, inflammatory, and autoimmune conditions, with conjugated compounds having Toll-like receptor modulatory activity.Type: ApplicationFiled: September 20, 2011Publication date: April 5, 2012Inventors: Johanna Holldack, Alberto Mantovani, Antonio Sica, Nadia Passini, Roberto Maj, Alcide Barberis
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Publication number: 20120065154Abstract: This invention generally relates to pyrazolo pyrimidine derivatives useful as, inter alia, inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. More specifically, the invention relates to pyrazolo pyrimidine derivatives, including derivatives and analogs of SDR inhibitors, pharmaceutical compositions containing derivatives and analogs of SDR inhibitors, methods of making derivatives and analogs of SDR inhibitors and methods of use thereof.Type: ApplicationFiled: January 28, 2011Publication date: March 15, 2012Applicant: The Regents of the University of CaliforniaInventors: Masahiro Tanaka, Chao Zhang, Kevan M. Shokat, Alma L. Burlingame, Kirk Hansen, Raynard L. Bateman, Stephen G. DiMagno
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Patent number: 8119648Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 20, 2008Date of Patent: February 21, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz
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Publication number: 20120040982Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: October 25, 2011Publication date: February 16, 2012Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Patent number: 8114877Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: January 12, 2006Date of Patent: February 14, 2012Assignee: Novartis AGInventors: Robin A Fairhurst, Roger J Taylor
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Publication number: 20120035158Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: October 25, 2011Publication date: February 9, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20120015964Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: June 17, 2011Publication date: January 19, 2012Applicant: ICOS CorporationInventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg
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Patent number: 8093246Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: GrantFiled: December 12, 2007Date of Patent: January 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu