Polycyclo Ring System Having The Plural Nitrogen Containing Additional Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/254.06)
  • Patent number: 10246440
    Abstract: Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: April 2, 2019
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Gilles Ouvry, Etienne Thoreau, Claire Bouix-Peter
  • Patent number: 10166230
    Abstract: The invention relates to a method for the treatment of vasomotor symptoms comprising the administration of a therapeutically effective amount of flibanserin.
    Type: Grant
    Filed: December 26, 2014
    Date of Patent: January 1, 2019
    Inventors: Vladimir Hanes, Anna Elizabeth Verbeek
  • Patent number: 10085979
    Abstract: Disclosed are methods of treating neuroblastoma in a cancer patient by administration of a Trk inhibitor in combination with one more chemotherapeutic agents. Also disclosed are pharmaceutical compositions comprising a Trk inhibitor and one or more chemotherapeutic agents.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: October 2, 2018
    Assignee: IGNYTA, INC.
    Inventors: Zachary Dolph Hornby, Gang Li, David Wesley Anderson, Garrett M. Brodeur, Radhika Iyer
  • Patent number: 9592208
    Abstract: A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor modulator; (b) a filler, and (c) a cyclodextrin.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: March 14, 2017
    Assignee: Novartis AG
    Inventor: Supriya Rane
  • Patent number: 9388179
    Abstract: Disclosed are compounds of Formula AA and Formula AB: wherein “Heteroaryl-1”, RA1, RA2, RB1, and RC are defined herein, which novel compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae AA and AB or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: July 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph E. Pero, Hannah D. G. F. Lehman, Mark E. Layton, Michael A. Rossi, Michael J. Kelly, III
  • Patent number: 9180191
    Abstract: The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: November 10, 2015
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: David Vincent Sheehan, Roland Douglas Shytle
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150126524
    Abstract: The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.
    Type: Application
    Filed: September 12, 2014
    Publication date: May 7, 2015
    Applicant: SPROUT PHARMACEUTICALS, INC.
    Inventors: Jaroslaw Mazurek, Mihaela Pop
  • Publication number: 20150111898
    Abstract: The invention relates to a method for the treatment of premenstrual and other female sexual disorders comprising the administration of a therpeutically effective amount of flibanserin.
    Type: Application
    Filed: September 3, 2014
    Publication date: April 23, 2015
    Applicant: Sprout Pharmaceuticals, Inc.
    Inventor: Robert Pyke
  • Patent number: 9012487
    Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: April 21, 2015
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
  • Patent number: 9012459
    Abstract: The disclosure is directed to a monohydrate crystalline form of 3-(5-(4-(3-fluoropropyl)piperazin-1-yl)benzimidazol-2-yl)-1-azaazulen-2-one, possessing diffraction peaks of about 12.9°, 15.9°, 17.9°, 21.2°, 22.9°, 23.5° and 24.5°. Its preparation method and pharmaceutical composition thereof are also provided.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: April 21, 2015
    Assignee: Industrial Technology Research Institute
    Inventors: Yen-Fang Wen, Yuan-Jang Tsai, Wan-Ru Chen, Tsan-Lin Hu, Chia-Mu Tu, Chih-Peng Liu
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Publication number: 20150104439
    Abstract: The invention provides a method for alleviating discogenic pain by administering a therapeutic agent that disrupts neuronal and/or vascular elements in the disc, which is typically a degenerated disc. Disruption of neuronal elements in the disk includes destroying nerve endings without substantially affecting the central body of the nerve, suppressing activation of the nerve endings, and inhibiting the growth of nerve endings into the disk. Disruption of vascular elements includes causing the vascular extensions to retract from the disk, or suppressing the formation of such extensions. The therapeutic agent may be administered locally via an interbody pump, a bolus or a depot, or may be administered systemically.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Josee Roy, Susan J. Drapeau, Jeffrey C. Marx
  • Patent number: 9006278
    Abstract: Controlled release systems release at least one pluribioactive antifungal drug exhibiting at least one additional bioactivity from the group consisting of spermiostatic, antineoplastic, antibacterial, antirestenotic and antiviral activities. The drug release system is designed for use as a spermiostatic contraceptive, intravaginal ringed-mesh which may also exhibit antiviral activity, an in situ-forming implant for treating different forms of cancer and topical film for treating or preventing bacterial and fungal infections.
    Type: Grant
    Filed: January 29, 2011
    Date of Patent: April 14, 2015
    Assignee: Poly-Med, Inc.
    Inventors: Shalaby W. Shalaby, Georgios T. Hilas, Sheila Nagatomi
  • Patent number: 8999981
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 7, 2015
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • Patent number: 8999968
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 7, 2015
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Patent number: 8999993
    Abstract: The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection).
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: April 7, 2015
    Assignee: Peter MacCallum Cancer Institute
    Inventors: Roger Francis Martin, Jonathan White, Pavel Lobachevsky, David Winkler, Colin Skene, Sebastian Marcuccio
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8987275
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: March 24, 2015
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
  • Publication number: 20150080410
    Abstract: Developed here is a mitotic network comprising a signature of up to 54 genes, and including also sub-sets of genes within the signature, which can identify members by requiring higher correlation values for a signature gene. The present mitotic network provides for methods for prognosis and diagnosis of various cancers. The mitotic network is conserved across cancers exhibiting aberrant mitotic activity and several genes in the network act as therapeutic targets. Development of other inhibitors of mitosis can apply expression values of the genes in the mitotic network from patient tissue to select patients during clinical validation of the new drugs.
    Type: Application
    Filed: May 19, 2014
    Publication date: March 19, 2015
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Zhi Hu, Jian-hua Mao, Wen-Lin Kuo, Ge Huang, Joe W. Gray
  • Publication number: 20150072994
    Abstract: The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 12, 2015
    Applicant: SPROUT PHARMACEUTICALS, INC.
    Inventors: Angelo Ceci, Marcus Schindler
  • Publication number: 20150065520
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150065495
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Patent number: 8969341
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20150057291
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: February 26, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150057292
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: November 6, 2014
    Publication date: February 26, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150057290
    Abstract: The present invention relates to the use of 1-[2-(4-(3-trifluoromethyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one, optionally in the form of its pharmaceutically acceptable acid addition salts and optionally in the form of its hydrates or solvates, for preparing a pharmaceutical composition with a neuroprotective activity.
    Type: Application
    Filed: June 30, 2014
    Publication date: February 26, 2015
    Inventor: Franco Borsini
  • Publication number: 20150051203
    Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150051222
    Abstract: The present invention relates to a process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide. Novel solid forms of this compound, their utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing them are also object of the present invention.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Natale Alvaro BARBUGIAN, Romualdo FORINO, Tiziano FUMAGALLI, Paolo ORSINI
  • Publication number: 20150051221
    Abstract: The invention relates to the use of flibanserin for the preparation of a medicament for the treatment of post-menopausal Sexual Desire Disorders.
    Type: Application
    Filed: June 24, 2014
    Publication date: February 19, 2015
    Inventors: Stephane Pollentier, Robert E. Pyke
  • Publication number: 20150011563
    Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 8, 2015
    Inventors: Franco Borsini, Kenneth Robert Evans
  • Publication number: 20150011548
    Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
    Type: Application
    Filed: October 9, 2012
    Publication date: January 8, 2015
    Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
  • Publication number: 20150011564
    Abstract: The present invention pertains to a compound of formula (I) wherein R1, R2, R3, and R4 are each hydrogen or sulfate monoester with the proviso that R1, R2, R3, and R4 cannot simultaneously be hydrogen, processess for their preparation and their use as pharmaceuticals in the treatment of CNS disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: January 8, 2015
    Applicant: Sprout Pharmaceuticals, Inc.
    Inventors: Astrid Volz, Ralf Lotz, Fabio Paleari
  • Publication number: 20150005288
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 1, 2015
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
  • Publication number: 20150005316
    Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 1, 2015
    Applicant: SPROUT PHARMACEUTICALS, INC.
    Inventors: Carlo Bombarda, Enrica Dubini, Antoine Ezhaya
  • Publication number: 20150004228
    Abstract: The invention relates to oral pharmaceutical compositions containing flibanserin, methods for the preparation thereof and use thereof as a medicament.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 1, 2015
    Inventors: Thomas Friedl, Guido Bernhard Edmund Radtke
  • Publication number: 20140378917
    Abstract: The present invention provides transdermal therapeutic systems for dispensing a pharmaceutical product, in particular a pharmaceutical product with a low tendency to spontaneously crystallize. The matrix layer or at least one of the matrix layers in said systems contains a silicone hot-melt adhesive, a pharmaceutical product, and particles made of crosslinked polyvinylpyrrolidone. The invention also relates to a method for producing said transdermal therapeutic systems.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 25, 2014
    Inventors: Horst Dzekan, Hans-Rainer Hoffmann, Michael Horstmann, Walter Mueller, Sandra Wiedersberg
  • Publication number: 20140371202
    Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I?) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: University Health Network
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter Brent Sampson, Miklos Feher, Donald E. Awrey
  • Publication number: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Publication number: 20140350012
    Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Publication number: 20140350010
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140343075
    Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 20, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
  • Patent number: 8889673
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: November 18, 2014
    Assignee: Genentech, Inc.
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
  • Publication number: 20140336200
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Publication number: 20140336170
    Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Fengbin Song, Zhihua Sui
  • Publication number: 20140315856
    Abstract: A method for treating cancer that includes administering a pharmaceutically effective amount of a composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.
    Type: Application
    Filed: June 6, 2014
    Publication date: October 23, 2014
    Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
  • Publication number: 20140315792
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: February 14, 2014
    Publication date: October 23, 2014
    Inventors: Rolf Wagner, John K. Pratt, Dachun Liu, Michael D. Tufano, David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Dooner, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, Yi Gao, Allan C. Krueger
  • Publication number: 20140315892
    Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
    Type: Application
    Filed: January 31, 2014
    Publication date: October 23, 2014
    Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster
  • Patent number: 8865713
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: October 21, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao