Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
  • 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    Publication number: 20120283239
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 8, 2012
    Applicant: MSD OSS B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • Analogs of Indole-3-Carbinol and Their Use as Agents Against Infection
    Publication number: 20120283240
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: June 26, 2012
    Publication date: November 8, 2012
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • IRAK INHIBITORS AND USES THEREOF
    Publication number: 20120283238
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: January 10, 2012
    Publication date: November 8, 2012
    Applicant: NIMBUS IRIS, INC.
    Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse
  • IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
    Publication number: 20120283241
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 19, 2012
    Publication date: November 8, 2012
    Inventors: Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
  • SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
    Publication number: 20120277210
    Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
    Type: Application
    Filed: October 27, 2011
    Publication date: November 1, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Nathaniel Catron, David Lindley, Jonathan M. Miller, Eric A. Schmitt, Ping Tong
  • PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
    Publication number: 20120277209
    Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: June 22, 2012
    Publication date: November 1, 2012
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
  • DERIVATIVES OF N-[(1H-PYRAZOL-1-YL)ARYL]-1H-INDOLE OR 1H-INDAZOLE-3-CARBOXAMIDE, PREPARATION THEREOF AND APPLICATIONS THEREOF IN THERAPEUTICS
    Publication number: 20120277205
    Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.
    Type: Application
    Filed: September 13, 2011
    Publication date: November 1, 2012
    Applicant: SANOFI
    Inventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
  • 8-substituted isoquinoline derivative and the use thereof
    Patent number: 8299055
    Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: October 30, 2012
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 8299057
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; 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: Grant
    Filed: July 8, 2008
    Date of Patent: October 30, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Aminotriazolopyridines, compositions thereof, and methods of treatment therewith
    Patent number: 8299056
    Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 30, 2012
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Calabrese, Thomas Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
  • HETEROARYLOXY QUINAZOLINE DERIVATIVES
    Publication number: 20120270856
    Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
    Type: Application
    Filed: July 2, 2012
    Publication date: October 25, 2012
    Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
  • Antiviral Compounds
    Publication number: 20120270854
    Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.
    Type: Application
    Filed: April 20, 2012
    Publication date: October 25, 2012
    Applicant: PROSETTA ANTIVIRAL INC.
    Inventors: Clarence Hurt, Vishwanath Lingappa, Beverly Freeman, Anatolly Kitaygorodskyy, Andy Atuegbu
  • THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20120270855
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Application
    Filed: April 25, 2012
    Publication date: October 25, 2012
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Heterocyclic Modulators of Lipid Synthesis
    Publication number: 20120264737
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Application
    Filed: March 8, 2012
    Publication date: October 18, 2012
    Applicant: 3-V BIOSCIENCES, INC.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
    Publication number: 20120264739
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Application
    Filed: December 30, 2010
    Publication date: October 18, 2012
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • DISPIROPYRROLIDINE DERIVATIVES
    Publication number: 20120264738
    Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
    Type: Application
    Filed: March 9, 2012
    Publication date: October 18, 2012
    Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
  • SUBSTITUTED AMINOQUINOXALINES AS TYROSINE THREONINE KINASE INHIBITORS
    Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors
    Publication number: 20120258952
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 11, 2012
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Mark Laurence Boys, Michael F. Bradley, Robert Kirk DeLisle, D. David Hennings, April L. Kennedy, Fredrik P. Marmsater, Matthew David Medina, Mark C. Munson, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
  • NOVEL ANTIPLATELET AGENT
    Publication number: 20120258951
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 11, 2012
    Applicant: Mitsubishi Tanage Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • PYRROLO[2,3-d]PYRIMIDINE TROPOMYSIN-RELATED KINASE INHIBITORS
    Publication number: 20120258950
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
    Type: Application
    Filed: April 4, 2012
    Publication date: October 11, 2012
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Azetidine analogues of nucleosidase and phosphorylase inhibitors
    Patent number: 8283345
    Abstract: Disclosed are azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors, the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 9, 2012
    Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva University
    Inventors: Gary Brian Evans, Richard Hubert Furneaux, Ben William Greatrex, Vern L. Schramm, Peter Charles Tyler
  • Benzodiazepine Bromodomain Inhibitor
    Publication number: 20120252781
    Abstract: Benzodiazepine compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: November 3, 2010
    Publication date: October 4, 2012
    Inventors: James Bailey, Romain Luc Marie Gosmini, Olivier Mirguet, Jason Witherington
  • THIAZOLOPYRIMIDINE COMPOUNDS
    Publication number: 20120252777
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Application
    Filed: March 26, 2012
    Publication date: October 4, 2012
    Inventors: Johannes Cornelius Hermann, Lee Edwin Lowrie, JR., Matthew C. Lucas, Kin-Chun Thomas Luk, Fernando Padilla, Jutta Wanner, Wenwei Xie, Xiaohu Zhang
  • Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions
    Publication number: 20120252782
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
    Publication number: 20120252783
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20120252780
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 29, 2010
    Publication date: October 4, 2012
    Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
  • PYRAZOLO PYRIMIDINE DERIVATIVES
    Publication number: 20120252778
    Abstract: The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases.
    Type: Application
    Filed: March 26, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Wolfgang MILTZ, Berndt OBERHAUSER, Andrea VAUPEL, Juraj VELCICKY, Klaus WEIGAND, Rajender Reddy LELETI, Yugang LIU, Zhengming DU
  • HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
    Publication number: 20120252779
    Abstract: The invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: October 19, 2010
    Publication date: October 4, 2012
    Inventors: Nigel Ramsden, Richard John Harrison, Sally Oxenford, Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe
  • Analogs of indole-3-carbinol and their use as agents against infection
    Patent number: 8278341
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: October 2, 2012
    Assignee: SRI International
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • Amino-heterocyclic compounds
    Patent number: 8278295
    Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: October 2, 2012
    Assignee: Pfizer Inc.
    Inventors: Michelle M. Claffey, Christopher J. Helal, Patrick R. Verhoest
  • Substituted isoquinoline and isoquinolinone derivatives as inhibitors of Rho-kinase
    Patent number: 8278294
    Abstract: The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: October 2, 2012
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Joachim Brendel, Matthias Lohn
  • BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
    Publication number: 20120244149
    Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 27, 2012
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
  • 3-OXO-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES AS PARP INHIBITORS
    Publication number: 20120245142
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 27, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
  • 3-0X0-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES WITH SELECTIVE PARP-1 INHIBITION
    Publication number: 20120245143
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 27, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Elena Casale, Alexander Khvat, Mikhail Yurievitch Krasavin, Paolo Orsini, Helena Posteri, Alessandra Scolaro
  • MODULATORS OF TOLL-LIKE RECEPTOR 7
    Publication number: 20120244121
    Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE
    Publication number: 20120245144
    Abstract: Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: March 20, 2012
    Publication date: September 27, 2012
    Applicant: Genentech, Inc.
    Inventors: Timothy Heffron, Brian Safina, Steven Staben, Daniel P. Sutherlin, BinQing Wei, Richard Elliott, Robert Heald, Eileen M. Seward, Emanuela Gancia, Bohdan Waskowycz
  • Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics
    Patent number: 8273733
    Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: September 25, 2012
    Assignee: Sanofi
    Inventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
  • TRICYCLIC PYRAZOL AMINE DERIVATIVES
    Publication number: 20120238545
    Abstract: This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 20, 2012
    Applicant: MERCK SERONO SA
    Inventors: Pascale Gaillard, Isabelle Jeanclaude-Etter, Vincent Pomel, Eric Sebille, Seenisamy Jeyaprakashnarayanan, Mathilde Muzerelle
  • THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20120238544
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Application
    Filed: April 25, 2012
    Publication date: September 20, 2012
    Inventors: James P. Edwards, Daneile K. Neff, Deborah M. Smith, Jennifer D. Venable
  • FUSED AMINO PYRIDINE AS HSP90 INHIBITORS
    Publication number: 20120237508
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Application
    Filed: March 20, 2012
    Publication date: September 20, 2012
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • AMINOPYRAZOLOQUINAZOLINES
    Publication number: 20120238542
    Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
    Type: Application
    Filed: July 20, 2011
    Publication date: September 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Matthias Treu
  • Antiviral Compounds
    Publication number: 20120238543
    Abstract: Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Applicant: Prosetta Antiviral, Inc.
    Inventors: Clarence Hurt, Beverly Freeman, Vishwanath Lingappa, Andy Atuegbu, Anatoliy Kitaygorodskyy
  • HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
    Publication number: 20120232055
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: October 12, 2011
    Publication date: September 13, 2012
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: Ian S. MITCHELL, James F. BLAKE, Rui XU, Nicholas C. KALLAN, Dengming XIAO, Keith Lee SPENCER, Josef R. BENCSIK, Eli M. WALLACE, Stephen T. SCHLACHTER, Anna L. BANKA, Jun LIANG, Brian SAFINA, Birong ZHANG, Christine CHABOT, Steven DO
  • PYRROLOTRIAZINE COMPOUNDS
    Publication number: 20120232054
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.
    Type: Application
    Filed: April 28, 2010
    Publication date: September 13, 2012
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Kevin J. Moriarty, Dora Do-York Wong, Zenon Konteatis, Kristofer Moffett, Younghee Lee, Wenchun Chao
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20120232056
    Abstract: 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: Application
    Filed: March 2, 2012
    Publication date: September 13, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • FUSED RING AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS
    Publication number: 20120225856
    Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 6, 2012
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
  • PYRIDYL-AMINE FUSED AZADECALIN MODULATORS
    Publication number: 20120220565
    Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 30, 2012
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
  • Antimicrobial Compounds and Methods of Making and Using the Same
    Publication number: 20120220566
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 15, 2010
    Publication date: August 30, 2012
    Applicant: Rib-X Pharmaceuticals, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
  • THIENO- ADN FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20120214792
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 23, 2012
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders
    Publication number: 20120214791
    Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
    Type: Application
    Filed: February 20, 2012
    Publication date: August 23, 2012
    Inventors: Christopher John HELAL, Thomas Allen CHAPPIE, John Michael HUMPHREY, Patrick Robert VERHOEST, Eddie YANG