1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Publication number: 20150051202Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: February 14, 2013Publication date: February 19, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
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Publication number: 20150050356Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.Type: ApplicationFiled: October 28, 2014Publication date: February 19, 2015Inventors: Neil P. DESAI, Patrick SOON-SHIONG, Vuong TRIEU
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Publication number: 20150051201Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Applicant: Genentech, Inc.Inventors: Charles Baker-Glenn, Bryan K. Chan, Jennafer Dotson, Anthony Estrada, Timothy Heffron, Joseph Lyssikatos, Zachary Sweeney
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Publication number: 20150051213Abstract: The present invention provides sitagliptin 4-methylsalicylate, sitagliptin myristate, sitagliptin isophthalate, sitagliptin isonicotinide, sitagliptin adipate, their polymorphic form, processes for their preparation and pharmaceutical compositions thereof.Type: ApplicationFiled: June 26, 2012Publication date: February 19, 2015Inventors: Suresh Babu Jayachandra, Jigar Bhaskarbhai Shah, Sailu Chiguru
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Publication number: 20150050210Abstract: The present invention is related to the field of pharmaceutical compositions for the treatment of various disease states, particularly neoplastic diseases and autoimmune diseases. It especially relates to the oral application of bendamustine and its derivatives. The invention further relates to a process for preparing a pharmaceutical composition which comprises bendamustine and its derivatives prepared by hot melt extrusion using pharmaceutically acceptable excipients. The invention also relates to such pharmaceutical compositions and hot melt extrudates.Type: ApplicationFiled: March 25, 2013Publication date: February 19, 2015Inventors: Akif Emre Tuereli, Bernd Baumstuemmler, Richard Ammer
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Patent number: 8957064Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: GrantFiled: February 2, 2010Date of Patent: February 17, 2015Assignee: Bayer Intellectual Property GmbHInventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Swen Hölder, Gerrit Beneke, Florian Dehmel, Armin Zülch, Andreas Strub, Stuart Ince, Hartmut Rehwinkel, Ningshu Liu, Ulf Bömer, Barbara Beckers
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Patent number: 8957068Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: GrantFiled: September 26, 2012Date of Patent: February 17, 2015Assignee: Novartis AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Publication number: 20150044148Abstract: The invention relates to a method of treating capillary hemangiomas in a human in need thereof by topically administering an effective amount of one or more alpha-2 adrenergic receptors agonist to the site of the capillary hemangiomas on the skin of the human.Type: ApplicationFiled: October 15, 2012Publication date: February 12, 2015Inventor: Warren J. Scherer
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Publication number: 20150045326Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
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Publication number: 20150045361Abstract: 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 LymphoType: ApplicationFiled: October 22, 2014Publication date: February 12, 2015Inventors: Yi CHEN, Timothy D. CUSHING, Jason A. DUQUETTE, Felix GONZALEZ LOPEZ DE TURISO, Xiaolin HAO, Xiao HE, Brian S. LUCAS, Lawrence R. MCGEE, Andreas REICHELT, Robert M. RZASA, Jennifer L. SEGANISH, Youngsook SHIN, Dawei ZHANG
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Patent number: 8952011Abstract: The invention provides compositions and methods for treating nasal congestion. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.Type: GrantFiled: August 26, 2013Date of Patent: February 10, 2015Assignee: Eye Therapies LLCInventor: Gerald Horn
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Patent number: 8952009Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: GrantFiled: August 2, 2013Date of Patent: February 10, 2015Assignee: Amgen Inc.Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, Wenge Zhong
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Patent number: 8952010Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: ?and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:Type: GrantFiled: February 6, 2012Date of Patent: February 10, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Hiroaki Inagaki, Tetsunori Fujisawa, Masao Itoh, Aki Yokomizo, Toshifumi Tsuda, Saito Higuchi, Biswajit Das, Rita Katoch, Dilip J. Upadhyay
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038513Abstract: Association between N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-yl-carbonylamino]ethoxy}benzamide of formula (I): an addition salt thereof with a pharmaceutically acceptable acid or base, and FOLFOX. Medicaments.Type: ApplicationFiled: July 3, 2012Publication date: February 5, 2015Inventors: Stéphane Depil, Anne Jacquet-Bescond, Ioana Kloos, Anne-Laure Sarry, Sriram Balasubramanian, Joseph Buggy
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Publication number: 20150037414Abstract: A controlled Release Pharmaceutical composition comprising an effective amount of Pravastatin and Fenofibrate, characterised in that the difference, in absolute value, between the times of maximal concentration (Tmax) of Pravastatin and Fenofibric acid is not less than 1.5 hours upon administration with food to humans.Type: ApplicationFiled: July 7, 2010Publication date: February 5, 2015Applicant: GALEPHAR M/FInventors: Arthur M. Deboeck, Philippe Baudier, Francis Vanderbist, Antonio Sereno
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Publication number: 20150038452Abstract: The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C mutations.Type: ApplicationFiled: August 14, 2014Publication date: February 5, 2015Inventor: Brian W. Buell
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Publication number: 20150037372Abstract: The present invention relates to a high-density lipoprotein (HDL)-like particle composite which is a drug-encapsulating apoA-I comprising apoA-I and a drug encapsulated in the apoA-I capable of releasing the drug encapsulated in the apoA-I under acidic pH conditions, and a preparation method thereof. Since the HDL-like particle composite of the present invention can release the encapsulated drug under acidic conditions, while remaining stable under non-acidic conditions over a wide temperature range, it can be widely used for the development of target-specific drugs.Type: ApplicationFiled: July 18, 2014Publication date: February 5, 2015Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITYInventors: Dae Hyuk KWEON, Jae Yoon SHIN
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Publication number: 20150038506Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.Type: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Applicants: Agency for Science, Technology and Research, University of BaselInventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Publication number: 20150038480Abstract: The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same.Type: ApplicationFiled: May 29, 2012Publication date: February 5, 2015Applicants: UNIVERSITY OF FLORIDA RESERCH FOUNDATION INCORPORTED, THE REGENTS OF THE UNIVERSITY OF COLORADO, a body corporateInventors: Aaron Michels, Maki Nakayama, David Ostrov
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Publication number: 20150037406Abstract: A novel crystalline form of sitagliptin sulfate is provided. In addition, a method for obtaining the crystalline form, pharmaceutical compositions comprising the novel crystalline form and the crystalline form for use as a medicament are provided.Type: ApplicationFiled: March 1, 2013Publication date: February 5, 2015Inventors: María del Carmen Bernabeu Martínez, Alicia Dobarro Rodríguez, Cristobal Galán Rodríguez
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Patent number: 8946203Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 5, 2013Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
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Patent number: 8946223Abstract: This invention provides compounds of formula (I): wherein X1, X2, R1a, R1b, R1c, R1d, n, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: April 11, 2011Date of Patent: February 3, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Janice Chin, Kenneth M. Gigstad, He Xu
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Patent number: 8946224Abstract: The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state.Type: GrantFiled: November 11, 2011Date of Patent: February 3, 2015Assignee: Redx Pharma LimitedInventors: Mark Craighead, Ronald Palin, Neil Murray, Derek Lindsay
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Publication number: 20150030676Abstract: This invention relates to an oral stabilized modified release pharmaceutical dosage form containing L-methylfolate calcium, which is primarily absorbed from proximal small intestine via a saturable human proton-coupled folate transporter (h-PCFT) mediated transport intended as monotherapy for the treatment of patients with MDDs and/or diagnosed with dysthymia, schizophrenia, or degenerative dementia of the Alzheimer type.Type: ApplicationFiled: July 29, 2014Publication date: January 29, 2015Inventors: Gopi M. VENKATESH, Micael GUILLOT, Jin-Wang LAI, Michael GOSSELIN, Nicole A. BEINBORN
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Publication number: 20150031679Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: September 29, 2014Publication date: January 29, 2015Inventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
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Publication number: 20150031685Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: March 5, 2013Publication date: January 29, 2015Applicant: Dr. Reeddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
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Publication number: 20150031652Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20150031669Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: January 29, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
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Publication number: 20150031668Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: July 15, 2014Publication date: January 29, 2015Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
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Publication number: 20150031700Abstract: The present invention relates to a method of treating, reducing, inhibiting, preventing and/or reversing cutaneous facial flushing caused by abnormal, endogenously-induced vasomotor instability associated with, but not limited to acne rosacea, menopause-associated hot flashes, hot flashes resulting from orchiectomy or ingestion of substances capable of inducing a cutaneous facial flushing reaction (e.g.: alcohol, chocolate, spices) by topical dermatological application of an effective dose of a composition comprising at least one ?2 adrenergic receptor agonist (such as a (2-imidazolin-2-ylamino) quinoxaline derivative such as brimonidine tartrate)and a suitable carrier.Type: ApplicationFiled: October 14, 2014Publication date: January 29, 2015Applicant: GALDERMA LABORATORIES INC.Inventor: Warren J. Scherer
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Publication number: 20150031699Abstract: The present invention relates to the use of Volasertib or a pharmaceutically acceptable salt thereof or the hydrate thereof for treating myelodysplastic syndrome (MDS).Type: ApplicationFiled: July 24, 2014Publication date: January 29, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Dorothea RUDOLPH, Tillmann TAUBE
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Patent number: 8940735Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 20, 2012Date of Patent: January 27, 2015Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Publication number: 20150025081Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: September 17, 2014Publication date: January 22, 2015Inventors: Andreas Ritzen, Morten Langgard, Jan Kehler, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Publication number: 20150023941Abstract: The present invention provides compositions comprising sugar, cysteine, and/or sugar-cysteine products, methods of preparing the same, and/or using the same.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Inventors: David Bagley, Scott Momii, Scott Nagasawa, Herbert T. Nagasawa
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Publication number: 20150025080Abstract: The present invention provides processes for the preparation of amorphous form of sitagliptin dihydrogen phosphate. It also provides a solid dispersion of sitagliptin dihydrogen phosphate, including in the amorphous form, and processes for its preparation.Type: ApplicationFiled: June 29, 2012Publication date: January 22, 2015Applicant: RANBAXY LABORATORIES LIMITEDInventors: Poonam Kaushik, Ram Thaimattam, Mohan Prasad, Sudershan Kumar Arora
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Publication number: 20150025041Abstract: Disclosed are methods of treating viral infections comprising, in one aspect, administering compounds that are phospholipase D inhibitors. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to antiviral therapies. For example, compounds having Phospholipase D activity (e.g., isoform selective Phospholipase D inhibitors) can be useful in antiviral therapies (e.g., influenza treatments).Type: ApplicationFiled: September 30, 2012Publication date: January 22, 2015Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, H. Alex Brown
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Publication number: 20150025058Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: January 22, 2013Publication date: January 22, 2015Applicant: MERCK PATENT GMBHInventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
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Patent number: 8937068Abstract: Pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: GrantFiled: November 10, 2006Date of Patent: January 20, 2015Assignee: Zentaris GmbHInventors: Irene Seipelt, Eckhard Claus, Eckhard Guenther, Tilmann Schuster, Michael Czech, Emmanuel Polymeropoulos
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Patent number: 8937069Abstract: The present invention provides compounds of formula (Ia) and (Ib) which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said compounds and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: GrantFiled: January 11, 2013Date of Patent: January 20, 2015Assignee: Novartis AGInventors: Claire Adcock, Catherine Leblanc
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Publication number: 20150018351Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: ApplicationFiled: July 10, 2014Publication date: January 15, 2015Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20150018358Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.Type: ApplicationFiled: October 2, 2014Publication date: January 15, 2015Inventors: Stuart D. SHANLER, Andrew ONDO
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Publication number: 20150018357Abstract: Disclosed are a crystal form of (6S)-5-methyltetrahydrofolate salt and a method for preparing the same. The crystal form is: Form C of the crystal form of (6S)-5-methyltetrahydrofolate calcium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.3±0.2 and 19.2±0.2; or the crystal form of (6S)-5-methyltetrahydrofolate strontium salt, where the X-ray diffraction pattern has diffraction peaks at the 2? angles of 6.5±0.2 and 22.0±0.2. The crystal form of (6S)-5-methyltetrahydrofolate salt of the present invention has the advantages of excellent physicochemical properties, good stability, high purity, good reproducibility, and being more suitable for production on an industrial scale.Type: ApplicationFiled: December 17, 2012Publication date: January 15, 2015Inventors: Zheqing Wang, Yongzhi Cheng, Heng Huang, Huizhen Li
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Publication number: 20150018345Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accepType: ApplicationFiled: February 20, 2013Publication date: January 15, 2015Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
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Publication number: 20150018334Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
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Patent number: 8933228Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).Type: GrantFiled: June 17, 2011Date of Patent: January 13, 2015Assignee: Respivert, Ltd.Inventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
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Patent number: 8933078Abstract: A method for treating cancer is described using combination therapies comprising the use of hyperbaric oxygen with histone deacetylase inhibitors, with and without glycolytic therapies. The patient is subjected to a hyperbaric environment of substantially pure oxygen. A predetermined dose of one or more HDACI substances is administered to the patient. In addition, glycolitic inhibitors may also be administered. Dosages, pressures, and durations are selected as described herein to have a therapeutic effect on the patient.Type: GrantFiled: November 26, 2011Date of Patent: January 13, 2015Assignee: Research Cancer Institute of AmericaInventor: Mohammed Amin Nezami
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Publication number: 20150010521Abstract: The present invention generally relates to compositions and methods for treatment of subjects having or at risk of arteriosclerosis, hypertension, sickle-cell anemia, or other conditions. In some cases, the composition may include nitric oxide. The nitric oxide may be present within a first phase comprising a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present in liposomes, micelles, or other vesicles containing nitric oxide. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid “stick,” etc., that can be rubbed or sprayed onto the skin, e.g., onto a location with acne, or on another suitable portion of the skin. Other aspects of the present invention are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.Type: ApplicationFiled: September 22, 2014Publication date: January 8, 2015Applicant: Transdermal Biotechnology, Inc.Inventor: Nicholas V. Perricone