Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 548/953)
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20150111875
    Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
  • Publication number: 20150111867
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Patent number: 9000110
    Abstract: A compound represented by the following formula (a): CH2?CR1—CONJ-CGR2—(CH2)n—COO-Q1-Rf1??(a) is provided. This compound is capable of forming a polymer having an oil repellency equivalent to polymers containing a polyfluoroalkyl group containing at least 8 carbon atoms, although the polyfluoroalkyl group contains up to 6 carbon atoms. In the formula, R1 is hydrogen atom or methyl group, R2 is hydrogen atom or a group represented by —(CH2)m—COO-Q2-Rf2 (r), n and m are independently an integer of 0 to 4, Rf1 and Rf2 are independently a polyfluoroalkyl group or a polyfluoroether group containing 1 to 6 carbon atoms, Q1 and Q2 are independently single bond or a divalent linkage group, J is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, and G is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: April 7, 2015
    Assignee: AGC Seimi Chemical Co., Ltd.
    Inventors: Fusae Ishiwata, Ryo Hirabayashi, Hirotaka Shimizu
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150057261
    Abstract: The present invention relates to azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20150051186
    Abstract: The present invention relates to aryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 14, 2014
    Publication date: February 19, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Patent number: 8957061
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: February 17, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20150045341
    Abstract: The present invention relates to disubstituted aryl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 6, 2014
    Publication date: February 12, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20150038440
    Abstract: This invention recites dihydrofuran substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in mammals and birds. The substituents A, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.
    Type: Application
    Filed: January 29, 2013
    Publication date: February 5, 2015
    Inventors: Nathan Anthony Logan Chubb, Valerie A. Vaillancourt
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Patent number: 8927527
    Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: January 6, 2015
    Assignees: EpicentRx, Inc., Alliant Techsystems Inc.
    Inventors: Mark D. Bednarski, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
  • Publication number: 20140371198
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Application
    Filed: June 23, 2014
    Publication date: December 18, 2014
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédict Pourbaix-L'ebraly
  • Publication number: 20140371464
    Abstract: The invention recites a chiral process for the synthesis of isoxazoline azetidine phenyl substituted derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, processes for making, and their use as a parasiticide in an animal.
    Type: Application
    Filed: January 29, 2013
    Publication date: December 18, 2014
    Inventors: Denis Billen, Sean David William Greenwood, Timothy Lee Stuk
  • Patent number: 8906899
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: December 9, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang
  • Publication number: 20140349988
    Abstract: The invention provides organonitro thioether compounds, compositions containing such compounds, isolated organonitro thioether compounds and methods for using such compounds and compositions to treat cancer in a patient. Exemplary organonitro thioether compounds described herein include 2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl thioethers and variants thereof. Another aspect of the invention provides a pharmaceutical composition, comprising a pharmaceutically acceptable carrier and an organonitro thioether compound described herein, such as a compound of Formula I or II. Another aspect of the invention provides a method of treating cancer in a patient. The method comprises administering to a patient in need thereof a therapeutically effective amount of an organonitro thioether compound described herein, such as a compound of Formula I or II, to treat the cancer.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 27, 2014
    Applicant: RadioRx, Inc.
    Inventors: Jan Scicinski, Bryan T. Oronsky
  • Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Publication number: 20140336376
    Abstract: Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. In the formula, Ar is an aromatic carbocyclic ring or a heterocyclic ring; and Ar2 is represented by any one of the following rings and the like.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 13, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tadakiyo NAKAGAWA, Kayo Matsumoto, Sen Takeshita, Tomomi Yoshida, Munetaka Tokumasu, Hiroki Inoue, Kaori Kobayashi
  • Publication number: 20140323462
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Patent number: 8871755
    Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: October 28, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140309418
    Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 16, 2014
    Inventors: Wantao Chen, Xu Wang, Zhiyuan Zhang, Chenping Zhang, Li Mao, Ping Zhang, Qin Xu, Ming Yan, Jianjun Zhang, Jinsong Pan, Yan Lv, Rongxin Deng, Weiliu Qiu
  • Patent number: 8859550
    Abstract: The present invention relates to salts, hydrates, and polymorphs of bicyclic heteroaryl compounds, and pharmaceutical compositions thereof, which may be useful as inhibitors of H4R for the treatment or prevention of diseases including allergic rhinitis.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: October 14, 2014
    Assignee: Kalypsys, Inc.
    Inventors: Pingyun Chen, Stephen A. R. Carino, Ricky Wayne Couch, Daniel S. Kinder, Beth A. Norton
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140303384
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Inventors: Brian A. Duclos, Richard Andrew Ewin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Derek James Sheehan, Susan Mary Kult Sheehan, Donald James Skalitzky, Rajendran Vairagoundar
  • Patent number: 8853392
    Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Publication number: 20140288034
    Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shinji NAKADE, Hirotaka Mizuno, Takeji ONO, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140275527
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: June 27, 2013
    Publication date: September 18, 2014
    Applicant: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20140275010
    Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Patent number: 8828985
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: September 9, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8809552
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: August 19, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Publication number: 20140228344
    Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140228341
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Patent number: 8802659
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: Biogen Idec MA Inc.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8791100
    Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 29, 2014
    Assignee: Novartis AG
    Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard, Nikolaus Johannes Stiefl
  • Publication number: 20140187533
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Patent number: 8759333
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Patent number: 8759533
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Patent number: 8759334
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 24, 2014
    Assignee: Galapagos NV
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédicte Pourbaix-L′ebraly
  • Publication number: 20140171390
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: VenatoRx Pharmaceuticals, Inc.
    Inventors: Christopher J. BURNS, Denis DAIGLE, Bin LIU, Daniel McGARRY, Daniel C. PEVEAR, Robert E. Lee TROUT
  • Publication number: 20140171402
    Abstract: The present invention relates to an azetidine derivative or a pharmaceutically acceptable salt thereof, and an antidepressant agent or a composition for the prevention or treatment of psychiatric disorders including the same. The azetidine derivative is useful as a triple reuptake inhibitor capable of inhibiting reuptake of the neurotransmitters, dopamine, serotonin, and norepinephrine at the same time.
    Type: Application
    Filed: September 4, 2012
    Publication date: June 19, 2014
    Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Min-soo Han, Young-Hue Han, Chi-Man Song, Dong-Yun Shin
  • Publication number: 20140135310
    Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 15, 2014
    Applicant: Adamed Sp. z o.o.
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
  • Publication number: 20140134193
    Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 15, 2014
    Applicant: PFIZER INC.
    Inventors: Chakrapani SUBRAMANYAM, Frank Erich KOEHN, Kenneth John DIRICO, Alessandra S. EUSTAQUIO, Michael Eric GREEN, Haiyin HE, Min HE, Christopher John O'DONNELL, Sujiet PUTHENVEETIL, Anokha RATNAYAKE, Jesse Alexander TESKE, Hui Yu YANG
  • Patent number: 8697682
    Abstract: This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: April 15, 2014
    Assignee: Novartis AG
    Inventors: Marilyn De La Cruz, Piotr H. Karpinski, Yugang Liu
  • Patent number: 8685958
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: April 1, 2014
    Assignee: AstraZeneca AB
    Inventor: Lars Anders Mikael Johansson
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140080802
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: October 28, 2013
    Publication date: March 20, 2014
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang