Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
Ring sulfur in the bicyclo ring system (Class 514/301)
Ring oxygen in the bicyclo ring system (Class 514/302)
Exactly three ring nitrogens in the bicyclo ring system (Class 514/303)
  • Azole Compounds as PIM Inhibitors
    Publication number: 20140187553
    Abstract: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 3, 2014
    Applicant: AMGEM INC.
    Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
  • SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE
    Publication number: 20140187576
    Abstract: 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.
    Type: Application
    Filed: October 25, 2013
    Publication date: July 3, 2014
    Inventors: Ae Ri Kim, Jin Hwa Lee, Ki Sook Park, Jong Ryoo Choi, Tae Hee Lee, Jay Hyok Chang, Do Hyun Nam, Hoon Choi
  • BICYCLIC ORGANIC COMPOUNDS SUITABLE FOR THE TREATMENT OF INFLAMMATORY OR ALLERGIC CONDITIONS
    Publication number: 20140187550
    Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Application
    Filed: December 16, 2013
    Publication date: July 3, 2014
    Applicant: Novartis AG
    Inventor: Roger John Taylor
  • 7-AZAINDOLE DERIVATIVES SUITABLE FOR TREATMENT OF CANCERS
    Publication number: 20140187551
    Abstract: Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.
    Type: Application
    Filed: May 29, 2012
    Publication date: July 3, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • Positive allosteric modulators of mGluR2
    Patent number: 8765767
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, Zhaoxing Meng
  • Indazolyl, benzimidazolyl, benzotriazolyl substituted indolinone derivatives as kinase inhibitors useful in the treatment of cancer
    Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Compounds
    Patent number: 8765743
    Abstract: The invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: July 1, 2014
    Assignee: Glaxosmithkline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Monocyclic CGRP receptor antagonists
    Patent number: 8765759
    Abstract: The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold G. Selnick, Ian M. Bell, Melody McWherter, Donnette D. Staas, Shawn J. Stachel, Thomas Steele, Craig Stump, Michael R. Wood, C. Blair Zartman
  • Indole derivatives as selective androgen receptor modulators (SARMS)
    Patent number: 8765782
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: July 1, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • 1,8-naphthyridine compounds for the treatment of cancer
    Patent number: 8765954
    Abstract: Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: July 1, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Daniel C. Adelman, Marc J. Evanchik, Anantha Sudhakar, Jeffrey William Jacobs, Jeffrey A. Silverman
  • ARYL AND HETEROARYL FUSED LACTAMS
    Publication number: 20140179667
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: PFIZER INC.
    Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
  • Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
    Publication number: 20140179672
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: November 1, 2013
    Publication date: June 26, 2014
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Alexey GROMOV, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
  • QUINOLONE COMPOUND
    Publication number: 20140179675
    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 1 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: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • DIAZOLE AMIDES
    Publication number: 20140179733
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Pyrrolopyridines as kinase inhibitors
    Patent number: 8758830
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: Grant
    Filed: August 23, 2013
    Date of Patent: June 24, 2014
    Assignee: Array BioPharma, Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives and uses thereof
    Patent number: 8759341
    Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: June 24, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
  • Substituted bicyclic amines for the treatment of diabetes
    Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • METHODS FOR TREATING DEPRESSION, NEURODEGENERATION, INHIBITING AMYLOID BETA DEPOSITION, DELAYING SENESCENCE, AND EXTENDING LIFE SPANS WITH HETEROCYCLIC COMPOUNDS
    Publication number: 20140171452
    Abstract: Disclosed is an antidepressant, neuroprotectant, amyloid ? deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I):
    Type: Application
    Filed: February 12, 2014
    Publication date: June 19, 2014
    Applicant: ZENYAKU KOGYO KABUSHIKI KAISHA
    Inventors: Yoshimasa YAMAGUCHI, Ryogo YUI, Toshiyuki MATSUNO, Kenichi SAITOH, Hitoshi MIYASHITA, Takeshi NAGATA
  • TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST
    Publication number: 20140171463
    Abstract: Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: MediciNova, Inc.
    Inventors: Michael E. KALAFER, Kenneth W. Locke, Kazuko Matsuda, Richard E. Gammans
  • BICYCLIC INHIBITORS OF ALK
    Publication number: 20140171429
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Application
    Filed: January 20, 2012
    Publication date: June 19, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
  • TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
    Publication number: 20140171406
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • HISTONE DEMETHYLASE INHIBITORS
    Publication number: 20140171432
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 19, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones
    Publication number: 20140171451
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Applicant: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
    Patent number: 8754100
    Abstract: A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by A?.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: June 17, 2014
    Assignee: EISAI R&D Management Co., Ltd.
    Inventors: Noritaka Kitazawa, Daisuke Shinmyo, Koichi Ito, Nobuaki Sato, Daiju Hasegawa, Toshiyuki Uemura, Toru Watanabe
  • N-cyclobutyl-imidazopyridine-methylamine as TRPV1 antagonists
    Patent number: 8754101
    Abstract: A compound of formula (I) wherein X represents a H atom, or a CH2OH group, Y represents a H atom, or a CH2OH group, but X and Y are not both CH2OH groups and Ar is selected from or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: June 17, 2014
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Gianpaolo Bravi, Aurelie Cecile Champigny, Diane Mary Coe, Deborah Needham, Daniel Terence Tape
  • Nitrogen containing compounds and their use
    Patent number: 8754102
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: June 17, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Compounds and compositions as c-kit kinase inhibitors
    Patent number: 8754071
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: June 17, 2014
    Inventors: Valentina Molenti, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
  • Antiviral drugs for treatment of infection
    Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8754103
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: June 17, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20140163009
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 12, 2014
    Applicant: CHDI Foundation
    Inventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
  • BROMODOMAIN INHIBITORS
    Publication number: 20140162971
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 14, 2013
    Publication date: June 12, 2014
    Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
  • DIBENZOOXEPIN DERIVATIVE
    Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • HETEROCYCLIC COMPOUND
    Publication number: 20140163001
    Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 12, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
  • Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones
    Publication number: 20140163038
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 12, 2014
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
  • Methods For Reducing Blood Pressure
    Publication number: 20140163061
    Abstract: The present invention provides methods and medicaments for reducing blood pressure. Methods and medicaments for treating or preventing hypertension are also provided.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicant: FibroGen, Inc.
    Inventors: Volkmar Guenzler-Pukall, Qingjian Wang, Ingrid Langsetmo Parobok, Guangjie Guo
  • Anti-constipation composition
    Patent number: 8748454
    Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.
    Type: Grant
    Filed: December 27, 2011
    Date of Patent: June 10, 2014
    Assignee: Sucampo AG
    Inventor: Ryuji Ueno
  • Modulators of cystic fibrosis transmembrane conductance regulator
    Patent number: 8748612
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: June 10, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Peter D. J. Grootenhuis, Sara S Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T. D. Fanning
  • Solid forms of a pharmaceutically active substance
    Patent number: 8748455
    Abstract: The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: June 10, 2014
    Assignees: Plexxikon Inc., Hoffman-La Roche Inc.
    Inventors: Prabha N. Ibrahim, Gary Conard Visor, Shan-Ming Kuang, Baoshu Zhao, Ralph Diodone, Karsten Fähnrich, Urs Schwitter
  • HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
    Publication number: 20140155398
    Abstract: The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A? B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
    Type: Application
    Filed: November 22, 2013
    Publication date: June 5, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Ashwani Kumar Verma, Kumaragurubaran Nagaswamy, Lalima Sharma, Soma Ghosh, Balkrishna Ramchandra Kale, Aniruddha Mondal, Punit Kumar Srivastava, Sunanda Ghosh Dastidar, Rijwan Jaffer Momin, Pradip Balu Wagh, Sonali Nanasaheb Pansare, Pramod Raosaheb Markad, Yogesh Balasaheb Khairnar, Rie Miyauchi, Takeshi Murata, Masayuki Ishizaki, Masatoshi Nagamochi, Shin Iimura
  • BRAF Mutations Conferring Resistance to BRAF Inhibitors
    Publication number: 20140155399
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 5, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Levi Garraway, Caroline Emery
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze
  • PYRUVATE KINASE ACTIVATORS FOR USE IN THERAPY
    Publication number: 20140155408
    Abstract: Described herein are methods for using compounds that activate pyruvate kinase.
    Type: Application
    Filed: May 3, 2012
    Publication date: June 5, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventor: Shin-San Michael Su
  • NOVEL COMPOUNDS
    Publication number: 20140155375
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 5, 2014
    Applicant: GlaxoSmithKline Interllectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • Anti-Inflammation Compounds
    Publication number: 20140155387
    Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 5, 2014
    Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREA
    Inventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
  • HETEROCYCLE AMINES AND USES THEREOF
    Publication number: 20140155379
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 5, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
    Publication number: 20140155367
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Application
    Filed: November 18, 2013
    Publication date: June 5, 2014
    Applicants: Novartis AG, IRM LLC
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
  • Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as Janus kinase inhibitors
    Patent number: 8741895
    Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: June 3, 2014
    Assignee: Incyte Corporation
    Inventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks
  • N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives as modulators of alpha 2 adrenergic receptors
    Patent number: 8741921
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: June 3, 2014
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8741920
    Abstract: The present invention relates to a composition comprising the compound of formula (1), and the compound of formula (B),
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
    Patent number: 8741897
    Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell