Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
1,4-diazine as one of the cyclos (Class 514/249)
  • Azabenzimidazoles as respiratory syncytial virus antiviral agents
    Patent number: 8927720
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: January 6, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • QUINOLONE COMPOUND
    Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • NOVEL HETEROARYLAMIDE DERIVATIVES HAVING ANTIANDROGENIC PROPERTIES
    Publication number: 20150005308
    Abstract: The invention relates to novel heteroarylamide derivatives having formula (I) and N-oxides, stereoisomers and pharmaceutically acceptable salts thereof, where RA, RB, R1 1, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 1, 2015
    Inventors: Jari Ratilainen, Milla Koistinaho, Anu Muona
  • PYRIDAZINONE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
    Publication number: 20150005300
    Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:
    Type: Application
    Filed: March 13, 2014
    Publication date: January 1, 2015
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: BRIDGET M. COLE, RICHARD A. NUGENT, ANDREW KOLODZIEJ, KAREN HANDLEY, YEVGEN BARSUKOV
  • Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
    Patent number: 8921368
    Abstract: Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: December 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Gregory D. Brown, Lidia M. Doweyko, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
  • Use of AMG 900 for the treatment of cancer
    Patent number: 8921367
    Abstract: The present invention relates to methods of using AMG 900, a small molecule pan aurora kinase inhibitor, for the treatment of cancer, including solid tumors, hematologically derived tumors and the like. The invention further provides pharmaceutical compositions, dosage ranges and treatment regimens for administering AMG 900 to treat cancer.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: December 30, 2014
    Assignee: Amgen Inc.
    Inventors: Gregory Friberg, Marc Payton
  • Substituted triazolo-pyridazine derivatives
    Patent number: 8921366
    Abstract: This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABA-A receptor antagonist and/or a ?2, ?3 and ?5 GABA-A receptor agonist.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: December 30, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Scott L. Harbeson
  • PHTHALAZINONE DERIVATIVES
    Publication number: 20140378442
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Application
    Filed: September 11, 2014
    Publication date: December 25, 2014
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • TRICYCLIC SULFONAMIDE COMPOUNDS AND METHODS OF MAKING AND USING SAME
    Publication number: 20140378462
    Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 25, 2014
    Applicant: ZAFGEN, INC.
    Inventors: Thomas D. Pallin, Hazel J. Dyke, Susan M. Cramp, Robert Zahler
  • Amino-derivatives as novel inhibitors of histone deacetylase
    Patent number: 8916554
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Dithiinopyridazinone derivates
    Patent number: 8916703
    Abstract: The present invention relates to new dithiinopyridazinone derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinone derivatives.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: December 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Rinolfi
  • PYRIDAZINONE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
    Publication number: 20140371225
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • 4-(Benzoimidazol-2-yl)-thiazole Compounds and Related Aza Derivatives
    Publication number: 20140371204
    Abstract: The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4?, R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 18, 2014
    Inventors: Eva Caroff, Marcel Keller, Thierry Kimmerlin, Emmanuel Meyer
  • BICYCLIC HETEROCYCLIC DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF
    Publication number: 20140371199
    Abstract: 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), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
    Type: Application
    Filed: April 1, 2013
    Publication date: December 18, 2014
    Applicant: Agency for Science, Technology and Research
    Inventors: Kassoum Nacro, Athisayamani Jeyaraj Duraiswamy, Lohitha Rao
  • Substituted pyridazine derivatives
    Patent number: 8912183
    Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: December 16, 2014
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • Phthalazinone derivatives
    Patent number: 8912187
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: December 16, 2014
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • PYRROLO[2,3-d]PYRIMIDINE TROPOMYSIN-RELATED KINASE INHIBITORS
    Publication number: 20140364415
    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: August 26, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Biomarkers for Prediction of Response to PARP Inhibition in Breast Cancer
    Publication number: 20140364434
    Abstract: Methods and systems for identifying a cancer patient suitable for treatment with a PARP inhibitor. A 6-gene, 7-gene and 8-gene predictor panels of genes that are predictive of patient resistance or sensitivity to PARP inhibitors such as Olaparib.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Anneleen Daeman, Denise M. Wolf, Laura J. Van 't Veer, Paul T. Spellman, Joe W. Gray
  • Quinoline and cinnoline derivatives and their applications
    Publication number: 20140364431
    Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Protein Kinase Inhibitors
    Publication number: 20140364436
    Abstract: The present invention relates to compounds of Formula VIII with absolute configuration R or S: as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: ASTAR BIOTECH LLC
    Inventors: Chunrong YU, Haihong HUANG, Dongfeng ZHANG, Peng LI
  • SUBSTITUTED PYRAZOLO[3',4':4,5]THIENO[2,3-C]PYRIDAZIN-3-AMINE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4
    Publication number: 20140364409
    Abstract: In one aspect, the invention relates to substituted pyrazolo[3?,4?:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 11, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, James M. Salovich
  • AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
    Publication number: 20140364435
    Abstract: The present invention relates to amino-substituted imidazopyndazine compounds of general formula (I): in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: December 10, 2012
    Publication date: December 11, 2014
    Inventors: Knut Eis, Florian Puehler, Ludwig Zorn, Volker Schulze, Detlev Sülzle, Philip Lienau, Andrea Hagebarth, Kirstin Petersen, Ulf Bomer
  • Substituted triazoles useful as AXl inhibitors
    Patent number: 8906922
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: December 9, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingu Ding
  • COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE
    Publication number: 20140357638
    Abstract: The present invention provides compositions for reducing amyloid plaque burden associated with Alzheimer's disease and methods of using the same.
    Type: Application
    Filed: February 27, 2014
    Publication date: December 4, 2014
    Applicant: EIP Pharma, LLC
    Inventor: John Jahangir Alam
  • Pyrazolopyrrolidine Derivatives and their Use in the Treatment of Disease
    Publication number: 20140349990
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • ANTIMICROBIAL AGENTS
    Publication number: 20140350024
    Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
  • SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
    Publication number: 20140349993
    Abstract: Provided herein are novel substituted bicyclic aza-heterocycle 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 19, 2012
    Publication date: November 27, 2014
    Inventors: Rebecca L. Casaubon, Radha Narayan, Christopher Oalmann, Chi B. Vu
  • Compounds and method for treatment of cancer
    Patent number: 8895556
    Abstract: The invention relates to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Critical Outcome Technologies Inc.
    Inventors: Wayne R. Danter, Cheuk Kun Lau
  • Methods of treating intestinal diseases and inflammatory conditions related to HIV-AIDS
    Patent number: 8895555
    Abstract: Provided herein are methods of treating intestinal diseases or inflammatory conditions, including HIV-AIDS, in which oxidative stress is a triggering or exacerbating factor by administering GVT to a patient suffering from the condition such that the condition is treated.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: November 25, 2014
    Assignee: Bach Pharma, Inc.
    Inventors: Mark O. Henry, William S. Lynn
  • New Somatostatin receptor subtype 4 (SSTR4) agonists
    Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Modulators of Aldehyde Dehydrogenase and Methods of Use Thereof
    Publication number: 20140343045
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Inhibitors of bruton'S tyrosine kinase
    Patent number: 8889682
    Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: November 18, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
  • Aurora Kinase Modulators and Method of Use
    Publication number: 20140336182
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: May 13, 2013
    Publication date: November 13, 2014
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Zihao HUA, Matthew W. MARTIN, Isaac MARX, Hanh Nho NGUYEN, Philip R. OLIVIERI, Kathleen PANTER FABER, Karina ROMERO, Laurie SCHENKEL, Ryan WHITE
  • ARYLOXMETHYL CYCLOPROPANE DERIVATIVES AS PDE10 INHIBITORS
    Publication number: 20140336195
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 13, 2014
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS
    Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • DIHYDROXY AROMATIC HETEROCYCLIC COMPOUND
    Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Glucocorticoid receptor antagonists
    Patent number: 8883786
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
    Patent number: 8883784
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: November 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • HETEROCYCLIC PROTEIN KINASE INHIBITORS
    Publication number: 20140329807
    Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
    Type: Application
    Filed: July 20, 2012
    Publication date: November 6, 2014
    Applicant: TOLERO PHARMACEUTICALS, INC.
    Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
  • HYBRID NECROPTOSIS INHIBITORS
    Publication number: 20140323489
    Abstract: The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 30, 2014
    Applicants: President and Fellows of Harvard College, University of Houston, Tufts University, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciencess
    Inventors: Junying YUAN, Alexei DEGTEREV, Gregory D. CUNY
  • POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
    Publication number: 20140323490
    Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: April 24, 2014
    Publication date: October 30, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
  • Lisofylline analogs and methods for use
    Patent number: 8871764
    Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 28, 2014
    Assignee: University of Virginia Patent Foundation
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • INHIBITION OF THE RENIN-ANGIOTENSIN SYSTEM FOR THE TREATMENT OF RENAL, VASCULAR AND CARTILAGE PATHOLOGY
    Publication number: 20140315808
    Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Talia WEINSTEIN, Uzi GAFTER, Zvi NEVO, Dror ROBINSON, Zoharia EVRON
  • Inhibiting G Protein Coupled Receptor 6 Kinase Polypeptides
    Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Potassium channel modulators
    Patent number: 8859549
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: October 14, 2014
    Assignee: AbbVie, Inc.
    Inventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
  • Protein kinase inhibitors
    Patent number: 8859553
    Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: October 14, 2014
    Assignee: Astar Biotech LLC
    Inventors: Chunrong Yu, Haihong Huang, Dongfeng Zhang, Peng Li
  • Crystalline forms for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt, pharmaceutical preparations containing the same and method for the production of said forms
    Publication number: 20140303169
    Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.
    Type: Application
    Filed: April 8, 2014
    Publication date: October 9, 2014
    Applicant: METRIOPHARM AG
    Inventors: Josef BREU, Wolfgang BRYSCH, Astrid KAISER, Beate LUDESCHER, Gerrit MAASS, Thomas MARTIN, Wolfgang MILIUS, Michael NIEDERMAIER
  • 2-CARBOXAMIDE CLYCLOAMINO UREA DERIVATIVES FOR USE IN TREATING VEGF-DEPENDENT DISEASES
    Publication number: 20140302022
    Abstract: The invention relates to the use of compounds of formula (I) in the treatment of warm-blooded animal target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical compositions comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventor: Christian Rene Schnell
  • PHTHALAZINES AS POTASSIUM ION CHANNEL INHIBITORS
    Publication number: 20140303168
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES
    Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian