Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.07)
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Patent number: 8685960Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: GrantFiled: May 5, 2009Date of Patent: April 1, 2014Assignee: Elexopharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20140057873Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.Type: ApplicationFiled: November 1, 2013Publication date: February 27, 2014Inventor: Michael Farber
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Publication number: 20140051682Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: September 24, 2013Publication date: February 20, 2014Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
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Publication number: 20140038944Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts, Nicholas Sean Flinn
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Patent number: 8642610Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.Type: GrantFiled: February 6, 2012Date of Patent: February 4, 2014Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Publication number: 20140031321Abstract: The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of idebenone, benazepril, rolipram, moxonidine, lamivudine, loxoprofen, terbinafine, synephrine, 6-aminoindazole, and a Vitamin D analog, or a pharmaceutically acceptable salt of any of thereof.Type: ApplicationFiled: January 14, 2013Publication date: January 30, 2014Applicant: CELTAXSYS, INC.Inventor: Erica Brook Goodhew
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Publication number: 20140011770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Patent number: 8617587Abstract: The present invention relates to the supply and production of an animal medicine consisting of a substrate in pellet or tablet form, which is attractive to livestock and domestic animals, in which fine-grained particles of a neutral-tasting, physiologically compatible, solid carrier material are embedded, which is characterized in that said fine-grained particles of carrier material have an average diameter of 0.09 to 0.8 mm and are coated with an active substance from veterinary medicine, and said active substance layer is covered with a protective layer of a physiologically compatible polymer matrix, and to the production of this animal medicine. It also relates to the usage of said double-coated, fine-grained particles of carrier material in the production of a preparation for veterinary medicine.Type: GrantFiled: December 3, 2009Date of Patent: December 31, 2013Assignee: Novartis AGInventors: Hubert Thoma, Uwe Thomas Schote, Ute Isele
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Patent number: 8609685Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.Type: GrantFiled: November 5, 2008Date of Patent: December 17, 2013Assignee: CISI SCRLInventors: Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario De Mayo De Mari Milani, Ilaria Motto, Carmelo Drago
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Publication number: 20130317008Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment or prevention of heart failure of any aetiology.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Brian GUTH, Randolph SEIDLER, Juergen DAEMMGEN
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Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
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Publication number: 20130303517Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Christopher W. Boyce, Sylvia Joanna Degrado, Xiao Chen, Jun Qin, Robert D. Mazzola, JR., Younong Yu, Kevin D. McCormick, Anandan Palani, Dong Xiao, Robert George Aslanian, Jie Wu, Ashwin Umesh Rao, Phieng Siliphaivanh, Joey L. Methot, Hongjun Zhang, Elizabeth Helen Kelley, William Colby Brown, Qin Jiang, Jolicia Polivina Gauuan, Andrew J. Leyhane, Purakkattle Johny Biju, Pawan K. Dhondi, Li Dong, Salem Fevrier, Xianhai Huang, Henry M. Vaccaro
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Patent number: 8580779Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: December 12, 2011Date of Patent: November 12, 2013Assignee: Allergan, Inc.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8575150Abstract: According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.Type: GrantFiled: December 7, 2009Date of Patent: November 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Christian Fischer, Joey Methot, Hua Zhou, Adam J. Schell, Benito Munoz, Alexey A. Rivkin, Sean P. Ahearn, Stephanie Chichetti, Rachel N. MacCoss, Sam Kattar, Matthew Christopher, Chaomin Li, Andrew Rosenau, William Colby Brown
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Publication number: 20130287688Abstract: Methods and compositions for improving the delivery and/or efficacy of a therapy (e.g., a cancer therapy) are disclosed. In one embodiment, methods and compositions for treating or preventing a cancer (e.g., a solid tumor such as a desmoplastic tumor) by administering to a subject an anti-hypertensive agent, as a single agent or in combination with a microenvironment modulator and/or a therapy, e.g., a cancer therapy (for example, a therapeutic agent or therapy, including immunotherapy (e.g., antibodies, vaccine, cell-based), nanotherapeutics, radiation therapy, photodynamic therapy, low molecular weight chemotherapeutics, molecularly targeted therapeutics and/or oxygen radical) are disclosed.Type: ApplicationFiled: March 15, 2013Publication date: October 31, 2013Applicants: XTUIT PHARMACEUTICALS, INC., THE GENERAL HOSPITAL CORPORATIONInventors: The General Hospital Corporation, Xtuit Pharmaceuticals, Inc.
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Publication number: 20130281438Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.Type: ApplicationFiled: January 7, 2012Publication date: October 24, 2013Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Liang Cheng, Xijie Liu, Yuandong Hu, Xinhe Xu, Zhihua Liu, Lipeng Zhang, Wei Wu, Shulong Wang, Yu Shen, Gen Li, Yin Wang, Sheng Zhao, Chonglong Li, Jia Tang, Honghao Yu
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Publication number: 20130261106Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.Type: ApplicationFiled: April 2, 2013Publication date: October 3, 2013Applicant: SANOFIInventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
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Publication number: 20130261081Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).Type: ApplicationFiled: September 12, 2011Publication date: October 3, 2013Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
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Patent number: 8541404Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: GrantFiled: November 3, 2010Date of Patent: September 24, 2013Assignee: ElexoPharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Patent number: 8541405Abstract: Methods for the preparation of Ivabradine sulfate and form I crystal thereof. In particular, the Ivabradine sulfate and the preparation methods thereof, and the stable form I crystal of Ivabradine sulfate and the preparation methods thereof.Type: GrantFiled: October 29, 2009Date of Patent: September 24, 2013Assignee: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Piaoyang Sun, Yongjiang Chen, Guangliang Yu
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Patent number: 8524701Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology.Type: GrantFiled: June 13, 2008Date of Patent: September 3, 2013Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Brian Guth, Randolph Seidler, Juergen Daemmgen
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Patent number: 8513233Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that interacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.Type: GrantFiled: October 11, 2007Date of Patent: August 20, 2013Assignee: Shanghai Institute of Materia Medica, CASInventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
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Publication number: 20130210805Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.Type: ApplicationFiled: October 6, 2011Publication date: August 15, 2013Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
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Publication number: 20130203690Abstract: Phosphodiesterase type III (PDE III) inhibitor or a “Ca2+-sensitizing agent” or a pharmaceutically acceptable derivative thereof is used in the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure, and as a medication for the reverse remodeling of the heart of a patient with asymptomatic (occult) heart failure and their delayed onset of clinical symptoms.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens, Rainer Kleeman, Christian Troetschel, Andrea Vollmar
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Publication number: 20130196977Abstract: The present invention provides methods for the prevention of, delay progression to overt to, or the treatment of diastolic dysfunction or diastolic heart failure which method comprises administering to a warm-blooded animal a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with (i) an ACE inhibitor or a pharmaceutically acceptable salt thereof; or (II) an angiotensin II receptor blocker or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 10, 2012Publication date: August 1, 2013Inventors: David Louis FELDMAN, Friedrich Cameron LUFT, Dominik Nicolas Mueller, Randy Lee Webb
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Patent number: 8492373Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 1, 2010Date of Patent: July 23, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
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Publication number: 20130184256Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
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Publication number: 20130178424Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: February 13, 2013Publication date: July 11, 2013Applicant: AbbVie Deutschland GmbH & Co. KGInventor: AbbVie Deutschland GmbH & Co. KG
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Publication number: 20130178464Abstract: Delta crystalline form of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in the treatment of cardiovascular diseases.Type: ApplicationFiled: January 3, 2013Publication date: July 11, 2013Applicant: LES LABORATOIRES SERVIERInventor: LES LABORATOIRES SERVIER
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Publication number: 20130158008Abstract: The present invention relates to a solid composition containing ivabradine or a pharmaceutically acceptable salt thereof. Further, the invention relates to a method for the preparation of such a composition as well as a pharmaceutical product comprising such a composition.Type: ApplicationFiled: June 14, 2011Publication date: June 20, 2013Applicant: ratiopharm GmbHInventors: Dominique Meergans, Daniela Stumm, Jens Geier
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Publication number: 20130150345Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: January 18, 2013Publication date: June 13, 2013Applicant: AMURA THERAPEUTICS LIMITEDInventor: AMURA THERAPEUTICS LIMITED
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Patent number: 8440652Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: GrantFiled: March 2, 2012Date of Patent: May 14, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Publication number: 20130116213Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: June 20, 2011Publication date: May 9, 2013Applicant: HANMI SCIENCE CO., LTD.Inventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
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Publication number: 20130116239Abstract: The present invention relates to pharmaceutical compositions with delayed release which contain ivabradine adipate as active substance. The present invention furthermore relates to processes for the preparation of this composition and certain salts of ivabradine.Type: ApplicationFiled: June 14, 2011Publication date: May 9, 2013Applicant: ratiopharm GnbHInventors: Ramesh Matioram Gidwani, Mayur Vilas Kolhatkar, Dominique Meergans, Ralph Stefan, Jens Geier
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Publication number: 20130109672Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).Type: ApplicationFiled: April 26, 2011Publication date: May 2, 2013Applicant: The United States of America,as represented by the Secretary, Department of Health and Human ServiceInventors: Matthew B. Boxer, Min Shen, Douglas S. Auld, Craig J. Thomas, Martin J. Walsh
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Publication number: 20130101514Abstract: Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.Type: ApplicationFiled: October 10, 2012Publication date: April 25, 2013Applicant: Complexa, Inc.Inventor: Complexa, Inc.
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Publication number: 20130084335Abstract: The present invention relates to a pharmaceutical composition containing ivabradine or a pharmaceutically acceptable salt thereof. The invention further relates to a method for the preparation of such a composition.Type: ApplicationFiled: June 14, 2011Publication date: April 4, 2013Applicant: ratiopharm GmbHInventors: Dominique Meergans, Katrin Rimkus, Jens Geier
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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: 20130078284Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Patent number: 8389279Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).Type: GrantFiled: July 28, 2011Date of Patent: March 5, 2013Assignee: Cambridge Enterprise LimitedInventors: David J. Grainger, David John Fox
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Patent number: 8377922Abstract: The present invention relates to a benzazepinone compound represented by the following formula (I): wherein R1 represents a C1-C6 alkyl group or halogeno C1-C6 alkyl group, R2 represents a carboxyl group which may be protected, and Y represents a group represented by the formula (II): wherein Z represents CH or a nitrogen atom, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 14, 2008Date of Patent: February 19, 2013Assignee: Ube Industries, Ltd.Inventors: Naoto Suzuki, Yasunori Tsuzaki, Kimihiko Yoshimura, Masahiko Hagihara, Yukinori Wada, Masao Maruyama, Nobuyoshi Fujii, Yasuhiro Aga
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Publication number: 20130040937Abstract: The present invention relates to an If blocker or a pharmaceutically acceptable salt thereof and methods of using the If blocker or a pharmaceutically acceptable salt thereof to treat and/or prevent heart failure (HF) in a feline patient. The invention also relates to improving the quality of life, improving the general health condition, as well as, prolonging the life expectancy in feline patients suffering from heart failure, specifically heart failure due to one or more of the following etiologies hypertrophic cardiomyopathy (HCM), restrictive cardiomyopathy (RCM), unclassified cardiomyopathy (UCM), dilated cardiomyopathy (DCM) and/or arrhythmogenic right ventricular cardiomyopathy (ARVC).Type: ApplicationFiled: August 13, 2012Publication date: February 14, 2013Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Balazs Albrecht, Martin FOLGER, Saskia Kley, Ingo Lang, Randolph Seidler
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Publication number: 20130018041Abstract: This invention is directed to compounds of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, as isolated stereoisomers or mixtures thereof, or pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Rigel Pharmaceutical, Inc.Inventors: Somasekhar Bhamidipati, Jeffrey Clough, Ankush Argade, Rajinder Singh, Vadim Markovtosov, Pingyu Ding, Jiaxin Yu, Andy Atuegbu, Hui Hong, Ihab Darwish, Sambaiah Thota
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Publication number: 20130018040Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.Type: ApplicationFiled: July 30, 2012Publication date: January 17, 2013Applicant: University of Washington through its Center for CommercializationInventors: Wesley C. VAN VOORHIS, Wilhelmus G.J. HOL, Eric T. LARSON, Dustin James MALY, Ethan MERRITT, Kayode K. OJO
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Publication number: 20130012444Abstract: The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.Type: ApplicationFiled: June 27, 2012Publication date: January 10, 2013Applicant: SANOFIInventors: Norbert NAGEL, Bruno BAUMGARTNER, Harald BERCHTOLD, Oliver PLETTENBURG, Dieter KADEREIT, Mandy MOHNICKE, Simon GESSLER, Joachim TILLNER
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Publication number: 20130012479Abstract: The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments.Type: ApplicationFiled: June 27, 2012Publication date: January 10, 2013Applicant: SANOFIInventors: Norbert NAGEL, Bruno BAUMGARTNER, Harald BERCHTOLD, Oliver PLETTENBURG, Dieter KADEREIT, Mandy MOHNICKE, Simon GESSLER, Joachim TILLNER
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Publication number: 20120329780Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.Type: ApplicationFiled: April 23, 2012Publication date: December 27, 2012Applicant: Origenis GmbHInventors: Michael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube