The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
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Patent number: 8476285Abstract: The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.Type: GrantFiled: June 30, 2009Date of Patent: July 2, 2013Assignee: Myrexis, Inc.Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
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Publication number: 20130165426Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.Type: ApplicationFiled: July 5, 2011Publication date: June 27, 2013Applicant: UNIVERSITÉ DE MONTRÉALInventors: Réjean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
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Publication number: 20130165427Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: August 24, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: Jayhong A. Chong
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Publication number: 20130165428Abstract: 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: February 21, 2013Publication date: June 27, 2013Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130131038Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: May 23, 2013Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodríguez Escrich, Maria Cristina Sicre Gonzåles
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Publication number: 20130123280Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: ApplicationFiled: November 1, 2012Publication date: May 16, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130123229Abstract: Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects.Type: ApplicationFiled: October 11, 2012Publication date: May 16, 2013Applicant: MAKSCIENTIFIC, LLCInventor: MAKScientific, LLC
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Publication number: 20130109704Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: December 19, 2012Publication date: May 2, 2013Applicant: NEUROSEARCH A/SInventor: NeuroSearch A/S
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Patent number: 8431583Abstract: At least one compound of following formula I: in which: X is C or N, Y is CH3 or OH, and Z is H or CH3, or one of its pharmaceutically acceptable salts, hydrates, esters or isomers, for use in the manufacture of a medicament to treat pathologies in which an imbalance between cell division and apoptosis is involved.Type: GrantFiled: September 12, 2008Date of Patent: April 30, 2013Assignees: Centre National de la Recherche Scientifique, Universite de Rennes 1, Universite Paris Descartes, Universite de Bretagne Occidentale, Centre Hospitalier Universitaire de BrestInventors: Laurent Meijer, Karima Bettayeb, Hervé Galons, Nassima Oumata, Christian Berthou, Karine Lester
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Publication number: 20130102576Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.Type: ApplicationFiled: October 19, 2012Publication date: April 25, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130096134Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: June 30, 2011Publication date: April 18, 2013Applicant: Amgen Inc.Inventors: Jason A. Duquette, Brian Lucas
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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: 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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Publication number: 20130085151Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 30, 2011Publication date: April 4, 2013Applicant: Amgen IncInventor: Brian Lucas
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Publication number: 20130079303Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2012Publication date: March 28, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20130079327Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.Type: ApplicationFiled: May 30, 2011Publication date: March 28, 2013Inventors: Shingo Yamamoto, Toshio Yoshizawa
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Patent number: 8404674Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: March 4, 2008Date of Patent: March 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
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Publication number: 20130072504Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.Type: ApplicationFiled: January 24, 2011Publication date: March 21, 2013Applicant: CYCLACEL LIMITEDInventors: Benjamin Mark Skead, Christopher Peter Worrall, Jonathan Charles Christian Atherton, Julian Scott Northen, Philippe Fernades
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Publication number: 20130059869Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: ApplicationFiled: February 22, 2012Publication date: March 7, 2013Inventors: 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: 20130053406Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.Type: ApplicationFiled: August 23, 2010Publication date: February 28, 2013Applicant: Myrexis, Inc.Inventors: SE-HO KIM, Herbert L. Ley, III, Ashok Bajji
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Patent number: 8383634Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: May 23, 2011Date of Patent: February 26, 2013Assignee: Signal Pharmaceuticals, LLCInventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
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Patent number: 8372852Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: May 11, 2012Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Publication number: 20130035325Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.Type: ApplicationFiled: November 16, 2010Publication date: February 7, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
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Publication number: 20130029944Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: June 20, 2012Publication date: January 31, 2013Applicant: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
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Publication number: 20130029982Abstract: 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, 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: 20130012526Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 18, 2011Publication date: January 10, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
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Publication number: 20130012515Abstract: A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: November 11, 2010Publication date: January 10, 2013Applicant: UCB PHARMA S.A.Inventors: Gilles Raphy, Roland Bürli, Alan Findlay Haughan
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Publication number: 20130005748Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Patent number: 8343961Abstract: The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: January 1, 2013Assignee: ArQule, Inc.Inventors: Robert Nicewonger, Audra Dalton, Chris Brassard, Mark A. Ashwell, Rocio Palma
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NOVEL HYDRAZONE DERIVATIVES HAVING POTENT ANTITUMOR ACTIVITY TOWARD MULTI-DRUG RESISTANT TUMOR CELLS
Publication number: 20120329747Abstract: A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: Hiremagular N. JAYARAM, Praveen KUSUMANCHI, Mario GRIFANTINI, Palmarisa FRANCHETTI, Loredana CAPPELLACCI, Riccardo PETRELLI -
Publication number: 20120329776Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: November 4, 2011Publication date: December 27, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
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Publication number: 20120315291Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.Type: ApplicationFiled: February 8, 2011Publication date: December 13, 2012Applicant: GLAXOSMITHKLINE LLCInventors: Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
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Publication number: 20120309774Abstract: The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.Type: ApplicationFiled: August 16, 2012Publication date: December 6, 2012Inventors: Anthony BEAUGLEHOLE, Jayson M. RIEGER, Robert D. THOMPSON
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Publication number: 20120308609Abstract: The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: February 8, 2011Publication date: December 6, 2012Applicant: GlaxoSmithKline LLCInventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
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Patent number: 8324224Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: GrantFiled: June 27, 2011Date of Patent: December 4, 2012Assignee: Gilead Sciences, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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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: 8318718Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: November 16, 2009Date of Patent: November 27, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20120289503Abstract: A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.Type: ApplicationFiled: January 21, 2011Publication date: November 15, 2012Applicant: APREA ABInventors: Styrbjorn Bystrom, Charlotta Liljebris, Ninus Caram-Lelham
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Patent number: 8309555Abstract: The present invention provides 2,6-disubstituted purine compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional 2,6-disubstituted purine compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.Type: GrantFiled: September 21, 2009Date of Patent: November 13, 2012Assignee: The Scripps Research InstituteInventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
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Publication number: 20120277257Abstract: Disclosed herein are methods of treating diseases and disorders responsive to inhibition of Hsp90, pharmaceutical compositions, pharmaceutical dosage forms and medicaments useful for the treatment of diseases responsive to inhibition of Hsp90, and methods of making the pharmaceutical compositions, pharmaceutical dosage forms and medicaments.Type: ApplicationFiled: May 14, 2012Publication date: November 1, 2012Applicant: MYREXIS, INC.Inventors: Margaret YU, Daniel A. WETTSTEIN, Vijay R. BAICHWAL, Damon I. PAPAC, Gaylen M. ZENTNER, Mark S. WILLIAMS
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Publication number: 20120277206Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: May 11, 2012Publication date: November 1, 2012Applicant: Andrea Boesciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Patent number: 8288397Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: December 16, 2008Date of Patent: October 16, 2012Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
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Publication number: 20120258974Abstract: Provided are methods of improving the cardiac condition of post-myocardial infarction (MI) patients and reducing cardiovascular death and hospitalization due to heart failure or arrhythmias, by administering a therapeutically effective amount of an A2B adenosine receptor antagonist.Type: ApplicationFiled: April 5, 2012Publication date: October 11, 2012Inventors: Luiz Belardinelli, Hongyan Zhong, Dewan Zeng
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Publication number: 20120252783Abstract: 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: June 15, 2012Publication date: October 4, 2012Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20120252782Abstract: 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: June 15, 2012Publication date: October 4, 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: 20120245169Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: January 13, 2012Publication date: September 27, 2012Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20120244121Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
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Publication number: 20120245140Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: September 27, 2012Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodríguez Escrich, Maria Cristina Sicre Gonzåles