The Hetero Ring Contains Chalcogen Patents (Class 540/544)
Plural nitrogens in the heterocyclic ring (Class 540/545)
Polycyclo ring system which contains the hetero ring as one of the cyclos (Class 540/546)
  • Substituted hydroxamic acid compounds
    Patent number: 10647664
    Abstract: Disclosed are compounds of formulae: (I), and (II) and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R21, R22, R23, R34, R37, R33, R39, D, Q, Y, X, X1, X3, and X4 are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: May 12, 2020
    Assignees: Duke University, University of North Carolina
    Inventors: Pei Zhou, Eric J. Toone, Robert A. Nicholas
  • Salts and solid forms of (S)-3-(4-((4-(morpholinomethyl)benzyl) oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and compositions comprising and methods of using the same
    Patent number: 10596180
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: March 24, 2020
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Ether compounds and uses thereof
    Patent number: 10513515
    Abstract: The present invention provides compounds that modulate protein function, to restore protein homeostasis and/or cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions of these compounds are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions are also provided.
    Type: Grant
    Filed: August 6, 2018
    Date of Patent: December 24, 2019
    Assignee: BioTheryx, Inc.
    Inventors: Kyle W. H. Chan, Frank Mercurio, Aparajita Hoskote Chourasia, Leah Fung, Robert Sullivan
  • Formulations of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
    Patent number: 10080801
    Abstract: Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and/or an immune-related disorder.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: September 25, 2018
    Assignee: Celgene Corporation
    Inventors: Darshan Parikh, Anil Menon
  • Azepanyl-derivatives and pharmaceutical compositions comprising the same with antiparasitic activity
    Patent number: 9994577
    Abstract: The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i), for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: June 12, 2018
    Assignee: MERCK PATENT GMBH
    Inventor: Thomas Spangenberg
  • Triazine derivative
    Patent number: 9656995
    Abstract: The purpose of the present invention is to provide a novel triazine derivative of the formula (I): wherein R1 represents a substituted or unsubstituted lower alkyl group, R2 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group, A represents a nitrogen atom or C—R3, R3 represents a hydrogen atom, a cyano group, a substituted or unsubstituted acyl group, a substituted or unsubstituted sulfonyl group, or a substituted or unsubstituted carbamoyl group, and R4 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 15, 2014
    Date of Patent: May 23, 2017
    Assignee: CARNA BIOSCIENCES, INC.
    Inventors: Wataru Kawahata, Tokiko Asami, Masaaki Sawa, Yuko Asamitsu, Takayuki Irie, Takahiro Miyake, Takao Kiyoi
  • Processes for the preparation of (S)-3-(4- (4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and pharmaceutically acceptable forms thereof
    Patent number: 9309220
    Abstract: Provided are processes for the preparation of enantiomerically enriched or enantiomerically pure 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable form thereof.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: April 12, 2016
    Assignee: Celgene Corporation
    Inventors: John F. Traverse, Chengmin Zhang, Gregg B. Feigelson, Benjamin M. Cohen, William W. Leong
  • Salts and solid forms of (S)-3-(4- (4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and compositions comprising and methods of using the same
    Patent number: 9221788
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: December 29, 2015
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • HETEROCYCLIC COMPOUND
    Publication number: 20150141406
    Abstract: The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 31, 2013
    Publication date: May 21, 2015
    Inventors: Hiroshi Nara, Masaki Daini, Akira Kaieda, Taku Kamei, Toshihiro Imaeda, Fumiaki Kikuchi
  • SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS
    Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • PYRIMIDINE PYRAZOLYL DERIVATIVES
    Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Aminodihydrothiazine derivatives
    Patent number: 9029358
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a, and R4b, is each independently a hydrogen atom, halogen, or hydroxyl etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: May 12, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE DERIVATIVES
    Publication number: 20150111873
    Abstract: Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 23, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
  • SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS
    Publication number: 20150105370
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
  • IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
    Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • SUBSTITUTED BENZOTHIENYL - PYRROLOTRIAZINES AND USES THEREOF IN THE TREATMENT CANCER
    Publication number: 20150080371
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 11, 2012
    Publication date: March 19, 2015
    Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Heterocyclic compounds and uses thereof
    Patent number: 8975249
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: March 10, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20150051189
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 19, 2015
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • CXCR3 receptor antagonists
    Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Benzodioxane inhibitors of leukotriene production
    Patent number: 8946203
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20150031672
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINES, THEIR PREPARATION AND USE AS MEDICAMENTS
    Publication number: 20150031678
    Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 29, 2015
    Applicant: LABORATORIES DEL DR. ESTEVE S.A.
    Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
  • PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE DERIVATIVES
    Publication number: 20150018329
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 15, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS
    Publication number: 20150018338
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 7, 2014
    Publication date: January 15, 2015
    Applicant: NOVARTIS AG
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LEUOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Henrich RUEEGER, Michael SCHAEFER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
  • TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS
    Publication number: 20150011752
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: September 4, 2014
    Publication date: January 8, 2015
    Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
  • NOVEL TRIAZINE DERIVATIVE
    Publication number: 20150011751
    Abstract: To provide a novel triazine derivative represented by the following formula (I): A triazine derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, a substituted or unsubstituted heterocyclic fused ring, or a substituted or unsubstituted alkynyl group, R2 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group, R3 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, or a substituted or unsubstituted heterocyclic fused ring, R4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, or a halogen atom, and R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, or R1 and R5 may be combined to form a saturated or unsaturate
    Type: Application
    Filed: March 7, 2013
    Publication date: January 8, 2015
    Inventors: Wataru Kawahata, Tokiko Asami, Masaaki Sawa, Yuko Asamitsu, Takayuki Irie, Takahiro Miyake, Takao Kiyoi
  • MORPHOLINO SUBSTITUTED UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS
    Publication number: 20140378438
    Abstract: The invention relates to compounds of formula (I) wherein m, n, R1, T0 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds as well as methods of treating mTOR related diseases.
    Type: Application
    Filed: September 21, 2012
    Publication date: December 25, 2014
    Applicant: CELLZOME LIMITED
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
  • 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
  • KINASE INHIBITORS
    Publication number: 20140364411
    Abstract: Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: June 5, 2014
    Publication date: December 11, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Chi-Kit WOO, Lilian ALCARAZ, Carmelida CAPALDI
  • KINASE INHIBITORS
    Publication number: 20140364412
    Abstract: Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract
    Type: Application
    Filed: June 5, 2014
    Publication date: December 11, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Lilian Alcaraz, Christopher Hurley, Andrew Peter Cridland, Andrew Stephen Robert Jennings
  • HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
    Publication number: 20140349997
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF CCR2 ANTAGONISTS
    Publication number: 20140336374
    Abstract: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN
  • Bicyclic compounds and their use as antibacterial agents and ?-lactamase inhibitors
    Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
    Patent number: 8877744
    Abstract: The present invention relates to 1,4 Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Narquizian, Thomas Woltering, Wolfgang Wostl
  • 1,4 OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
    Publication number: 20140323469
    Abstract: This invention relates to compounds of the formula wherein and R1 to R3 are as described herein, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as pharmaceuticals for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Inventors: Hans Hilpert, Robert Narquizian
  • KINASE INHIBITORS
    Publication number: 20140323470
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
  • Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
    Patent number: 8853199
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: October 7, 2014
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • Salt and photoresist composition comprising the same
    Patent number: 8852846
    Abstract: The present invention provides a salt represented by the formula (I): wherein Q1 and Q2 independently each represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a C1-C20 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, W represents a group represented by the formula (W1), (W2), (W3), (W4) or (W5): and Z+ represents an organic counter ion.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yukako Anryu, Koji Ichikawa
  • KINASE INHIBITORS
    Publication number: 20140296208
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
  • Oxazine derivatives and their use in the treatment of neurological disorders
    Patent number: 8846658
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: September 30, 2014
    Assignee: Novartis AG
    Inventor: Siem Jacob Veenstra
  • BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS
    Publication number: 20140288051
    Abstract: New bicyclic compounds, their preparation, and their use as antibacterial agents, either alone or in combination with an antibiotic for the treatment of infections caused by ?-lactamase-producing pathogenic bacteria, are described.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Inventors: Samarendra N. MAlTI, Dai NGUYEN, Jehangir KHAN, Rong LING
  • NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES
    Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Aryl- or Heteroaryl-Substituted Benzene Compounds
    Publication number: 20140288041
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: May 12, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
  • Quinolin-4 (1H)-one derivatives as inhibitors of phosphatidylinositol 3-kinases
    Patent number: 8841288
    Abstract: Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: September 23, 2014
    Assignees: Universtà Degli Studi di Torino, Università Degli Studi del Piemonte Orientale “Amedeo Avogadro”
    Inventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
  • AZOLE DERIVATIVE
    Publication number: 20140275006
    Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
  • BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20140275003
    Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
  • CARBAZOLE COMPOUNDS USEFUL AS BROMODOMAIN INHIBITORS
    Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
    Patent number: 8828990
    Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: September 9, 2014
    Assignee: Genentech, Inc.
    Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Wendy Lee, Kirk D. Robarge
  • PIM KINASE INHIBITORS AND METHODS OF THEIR USE
    Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Formulations of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
    Patent number: RE49647
    Abstract: Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and/or an immune-related disorder.
    Type: Grant
    Filed: September 23, 2020
    Date of Patent: September 12, 2023
    Assignee: Celgene Corporation
    Inventors: Darshan Parikh, Anil Menon