Polycyclo Ring System Having The Additional Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.04)
  • Patent number: 10308639
    Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m?, A?, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: June 4, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Jerry Evarts, Joshua Kaplan, Leena Patel, Stephane Perreault, Barton W. Phillips, Gary Phillips, Jennifer A. Treiberg, Suet Chung Yeung
  • Patent number: 10301322
    Abstract: The present invention provides processes for the preparation of Edoxaban (1) and salts thereof, as well as intermediates thereof. In particular, intermediate compounds and/or salts of the Formulae (3), (4), (6-A), (7-A), (8-A), (9-A) and (10-AS) are provided.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: May 28, 2019
    Assignee: Apotex Inc.
    Inventors: Prabhudas Bodhuri, Avedis Karadeolian, Eduardo Gustavo Cammisa, Stuart P. Green, Melanie R. A. Green, Alfredo Paul Ceccarelli
  • Patent number: 10285946
    Abstract: The present invention is directed to lyophilized pharmaceutical preparations comprising melphalan flufenamide, or pharmaceutically acceptable salts thereof, and sucrose. Further independent claims are directed to methods for their preparation, compositions comprising the lyophilized pharmaceutical preparations and their use in the treatment of cancer.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: May 14, 2019
    Assignee: Oncopeptides AB
    Inventors: Jack Spira, Fredrik Lehmann
  • Patent number: 9868720
    Abstract: The present invention provides for pyrimidine compounds of Formula I-I and embodiments thereof In Formula I-I in which R1, R2, R3, R4, R5, R6, m, n and the “het” ring are as described herein. Also provided are pharmaceutical compositions comprising compounds of Formula I and methods of using such compounds and compositions.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: January 16, 2018
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Snahel Patel
  • Patent number: 9834549
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1).
    Type: Grant
    Filed: May 13, 2016
    Date of Patent: December 5, 2017
    Assignee: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 9567343
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: February 14, 2017
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie, Rochdi Bouhelal
  • Patent number: 9296743
    Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: March 29, 2016
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter Guzzo, Matthew David Surman, Alan John Henderson, May Xiaowu Jiang, Mark Hadden, James Grabowski, Alexander Usyatinsky
  • Patent number: 9296733
    Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: March 29, 2016
    Assignee: NOVARTIS AG
    Inventors: Robin Alec Fairhurst, Pascal Furet, Frank Stephan Kalthoff, Andreas Lerchner, Heinrich Rueeger
  • Patent number: 9242983
    Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: January 26, 2016
    Assignees: K.U. Leuven Research & Development
    Inventors: Steven S. Bondy, David A. Oare, Gerhard Puerstinger
  • Patent number: 9199963
    Abstract: Provided is a compound having a melanin-concentrating hormone receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of obesity and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: December 1, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Hideyuki Igawa, Masashi Takahashi, Keiko Kakegawa, Minoru Ikoma, Jumpei Aida
  • Publication number: 20150141353
    Abstract: This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
    Type: Application
    Filed: October 14, 2014
    Publication date: May 21, 2015
    Inventors: William E. Delaney, IV, John O. Link, Hongmei Mo, David W. Oldach, Adrian S. Ray, William J. Watkins, Cheng Yong Yang, Weidong Zhong
  • Publication number: 20150133448
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Application
    Filed: January 21, 2015
    Publication date: May 14, 2015
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro OKANO, Muneyoshi MAKABE
  • Publication number: 20150132327
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Application
    Filed: January 21, 2015
    Publication date: May 14, 2015
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro OKANO, Muneyoshi MAKABE, Kouki OGAWA
  • Publication number: 20150126517
    Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 7, 2015
    Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Patent number: 9018212
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: April 28, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Publication number: 20150105394
    Abstract: Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 16, 2015
    Inventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Lawrence G. Hamann
  • Publication number: 20150094306
    Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 2, 2015
    Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
  • Publication number: 20150087627
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.
    Type: Application
    Filed: April 15, 2014
    Publication date: March 26, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • Publication number: 20150087650
    Abstract: The present invention relates to 1-aza-bicy-cloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R?); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Application
    Filed: December 3, 2014
    Publication date: March 26, 2015
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien ROY, Thomas TROXLER, Konstanze HURTH, Mathias FREDERIKSEN
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Publication number: 20150080370
    Abstract: The present disclosure 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 R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: March 17, 2014
    Publication date: March 19, 2015
    Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
  • Patent number: 8980888
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: March 17, 2015
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Akihiro Okano, Muneyoshi Makabe, Kouki Ogawa
  • Patent number: 8981101
    Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: March 17, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Publication number: 20150057286
    Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Ulrich REISER
  • Publication number: 20150051206
    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: Application
    Filed: August 29, 2012
    Publication date: February 19, 2015
    Applicant: IRM LLC
    Inventors: Jon Loren, Xiaolin Li, Xiaodong Liu, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh, Paul Vincent Rucker
  • Publication number: 20150051215
    Abstract: The present invention is directed to compounds or pharmaceutically acceptable salts thereof for use in the treatment of fibrotic diseases such as idiopathic pulmonary fibrosis (IPF).
    Type: Application
    Filed: February 4, 2013
    Publication date: February 19, 2015
    Inventors: Richard Francis Wooster, Pauline Teresa Lukey, Patrick John Thompson Vallance
  • Publication number: 20150031702
    Abstract: The present invention is directed to compounds or pharmaceutically acceptable salts thereof for use in the treatment of cough, in particular idiopathic chronic cough, cough variant asthma, cough associated with thoracic tumour or lung cancer, viral and post-viral cough, upper airways cough syndrome (UACS) or post nasal drip cough, and cough associated with disorders such as gastro oesophageal reflux disease (both acid and non acid reflux), chronic bronchitis, chronic obstructive pulmonary disease (COPD), interstitial lung disease (such as idiopathic pulmonary fibrosis (IPF)), congestive heart disease, sarcoidosis and infection (such as whooping cough.
    Type: Application
    Filed: February 4, 2013
    Publication date: January 29, 2015
    Inventor: Emilio Merlo Pich
  • Publication number: 20150025065
    Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Holger WAGNER
  • Publication number: 20150018363
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 15, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Tsuneo Yasuma, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
  • Patent number: 8921555
    Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: December 30, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • Publication number: 20140378447
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Application
    Filed: September 4, 2014
    Publication date: December 25, 2014
    Inventors: Akihiro OKANO, Muneyoshi MAKABE, Kouki OGAWA
  • Publication number: 20140378448
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Application
    Filed: September 4, 2014
    Publication date: December 25, 2014
    Inventors: Akihiro OKANO, Muneyoshi MAKABE
  • Publication number: 20140371201
    Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
  • Patent number: 8912181
    Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
  • Publication number: 20140357633
    Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 4, 2014
    Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
  • Patent number: 8889676
    Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-ox
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: November 18, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
  • Publication number: 20140336176
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: PFIZER INC.
    Inventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
  • Patent number: 8883788
    Abstract: Provided is a compound having a PDE10A inhibitory action, and useful as a medicament for the prophylaxis or treatment of mental diseases such as schizophrenia and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: November 11, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomoaki Hasui, Makoto Fushimi, Hironori Kokubo, Takenori Hitaka, Shotaro Miura, Takahiko Taniguchi
  • Patent number: 8877742
    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: Grant
    Filed: June 8, 2012
    Date of Patent: November 4, 2014
    Assignee: GlaxoSmithKline Intellectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • Publication number: 20140323492
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: May 23, 2011
    Publication date: October 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Publication number: 20140303158
    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: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: 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
  • Publication number: 20140303142
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 9, 2014
    Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Acharya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
  • Publication number: 20140296203
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 25, 2012
    Publication date: October 2, 2014
    Inventors: Jongwon Lim, Elizabeth Helen Kelley, Joey L. Methot, Hua Zhou, Alessia Petrocchi, Faruk Mansoor, Christian Fischer, Brendan O'Boyle, David Joseph Guerin, Corey E. Bienstock, Christopher W. Boyce, Matthew H. Daniels, Danielle Falcone, Ronald D. Ferguson, Salem Fevrier, Xianhai Huang, Kathryn Ann Lipford, David L. Sloman, Kevin Wilson, Wei Zhou, David Witter, Milana M. Maletic, Phieng Siliphaivanh
  • Publication number: 20140275026
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined 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 12, 2014
    Publication date: September 18, 2014
    Inventors: Le Wang, John Pratt, Lisa A. Hasvold, Dachun Liu, Yujia Dai, Steven D. Fidanze, James H. Holms, Robert A. Mantei, Keith F. McDaniel, George S. Sheppard, William J. McClellan
  • Publication number: 20140275013
    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 parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION, IRM LLC
    Inventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh Nagle, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL, Michael Herman GELB, Frederick Simmons BUCKNER, Hari Babu TATIPAKA, Neil Richard NORCROSS, John Robert GILLESPIE
  • Publication number: 20140275101
    Abstract: The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.
    Type: Application
    Filed: March 18, 2013
    Publication date: September 18, 2014
    Inventors: Jun Qiu, Qui Gao, Shuang Liu, Min Hu, Yuh-Lin Allen Yang, Matthew Isherwood, Rasidul Amin
  • Publication number: 20140275040
    Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Proximagen Limited
    Inventors: Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
  • Publication number: 20140256736
    Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev