The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
  • Publication number: 20140018533
    Abstract: To provide a novel furanone derivative, and a medicine including the same.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 16, 2014
    Applicants: CARNA BIOSCIENCES, INC., SBI BIOTECH CO., LTD.
    Inventors: Takayuki Irie, Ayako Sawa, Masaaki Sawa, Tokiko Asami, Yoko Funakoshi, Chika Tanaka
  • Patent number: 8629276
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: January 14, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Margaret E. Sorenson, B. Narasimhulu Naidu, Kevin Peese, Barry L. Johnson, Manoj Patel
  • Publication number: 20140011677
    Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein A1, A2, A3, A4, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyridopyridines, pyridodiazines and pyridotriazines.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 9, 2014
    Applicant: Syngenta Limited
    Inventors: Matthew Robert Cordingley, Michael Drysdale Turnbull, Nigel James Willetts, Patrick Jelf Crowley
  • Publication number: 20140005165
    Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20130343992
    Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: December 26, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130345254
    Abstract: Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salts thereof, wherein A, B, R, and R6 are as defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: December 26, 2013
    Inventors: Anilkumar G. Nair, Joseph A. Kozlowski
  • Publication number: 20130345120
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: Glaxosmithkline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Patent number: 8614226
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: December 24, 2013
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20130338184
    Abstract: The invention in one embodiment is directed to a compound of Formula A: as defined herein, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 22, 2013
    Publication date: December 19, 2013
    Inventor: I. Robert Silverman
  • Patent number: 8604049
    Abstract: The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dennis Fiegen, Sandra Handschuh, Silke Hobbie, Matthias Hoffmann, Takeshi Kono, Yayoi Sato, Andreas Schnapp, Annette Schuler-Metz
  • Publication number: 20130317057
    Abstract: The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.
    Type: Application
    Filed: July 20, 2011
    Publication date: November 28, 2013
    Inventors: Scott B. Hoyt, Min K. Park, Clare London, Yusheng Xiong, D. Jonathan Bennett, Jaiqiang Cai, Paul Ratcliffe, Andrew Cooke, Emma Carswell, John MacLean, Rohit Saxena, Bheemashankar A. Kulkarni, Archana Gupta
  • Publication number: 20130317213
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • Patent number: 8592594
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: November 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Yongfu Liu, Hongying Yun, Mingwei Zhou
  • Publication number: 20130310365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: Janssen Pharmaceutical NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • Publication number: 20130310391
    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 tumours.
    Type: Application
    Filed: January 9, 2012
    Publication date: November 21, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Christian Sirrenberg, Thomas J.J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
  • Publication number: 20130310417
    Abstract: The present invention provides small molecules for endothelial cell activation and compositions thereof and methods of making and using the same.
    Type: Application
    Filed: February 23, 2012
    Publication date: November 21, 2013
    Applicant: The Regents of the University fo California
    Inventors: Daniel Cruz, Ohyun Kwon
  • Patent number: 8586601
    Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: November 19, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Anantha Sudhakar, Jeff Jacobs, Ahmad Hashash, Sean Ritchie, Hengqin Cheng
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Patent number: 8580814
    Abstract: Methods of treating, preventing or managing cancer, including certain leukemias are disclosed. The methods encompass the administration of enantiomerically pure (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.
    Type: Grant
    Filed: September 5, 2006
    Date of Patent: November 12, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Daniel C. Adelman, Jeffrey A. Silverman
  • Publication number: 20130296300
    Abstract: The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 7, 2013
    Inventors: Christopher W. Boyce, Salem Fevrier, Kevin D. McCormick, Anandan Palani, Robert G. Aslanian, Phieng Siliphaivanh, Joey L. Methot, William Colby Brown, Henry Vaccaro
  • Publication number: 20130296333
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Application
    Filed: July 9, 2013
    Publication date: November 7, 2013
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Publication number: 20130281433
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Publication number: 20130245062
    Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
    Type: Application
    Filed: November 27, 2012
    Publication date: September 19, 2013
    Applicant: CELLCEUTIX CORPORATION
    Inventor: KRISHNA MENON
  • Publication number: 20130244996
    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: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: 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
  • Publication number: 20130237538
    Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 12, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Clarence E. Hull, III, Thomas C. Malone
  • Patent number: 8518972
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
  • Publication number: 20130217705
    Abstract: The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.
    Type: Application
    Filed: October 27, 2011
    Publication date: August 22, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Yasunori Mitsuoka, Yuuji Kooriyama
  • Patent number: 8513420
    Abstract: The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections.
    Type: Grant
    Filed: March 18, 2008
    Date of Patent: August 20, 2013
    Inventor: Monika Mazik
  • Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Publication number: 20130210857
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: February 13, 2013
    Publication date: August 15, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8507682
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: August 13, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Patent number: 8507443
    Abstract: The present invention is an antineoplastic agent characterized by including at least one of taxol and taxol derivatives and a protein which is a mutant of diphtheria toxin, having an activity to inhibit a binding between HB-EGF and EGFR and substantially not having a toxicity of diphtheria toxin as active ingredients.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: August 13, 2013
    Assignee: The Research Foundation for Microbial Diseases of Osaka University
    Inventors: Eisuke Mekada, Shingo Miyamoto
  • Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
  • Publication number: 20130184253
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 19, 2012
    Publication date: July 18, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
  • Publication number: 20130178458
    Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 3, 2012
    Publication date: July 11, 2013
    Applicant: Vanderbilt University
    Inventor: Vanderbilt University
  • Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8481534
    Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8481738
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: July 9, 2013
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Patent number: 8476433
    Abstract: The present invention relates to the field of chemical-pharmaceutical industry and medicine. An agent, exhibiting the properties of a cognitive function promoter, was selected from 1,3-dimethyl-5-[(4-pyridylamino)methylene]barbituric acid and 4-amino-1-(3-nitro-2-oxo-1-pheny-1,2-dihydro-1,6-naphthyridin-5-yl)pyridinium chloride. The compounds, that are proposed as agents, exhibit potent biological activity.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: July 2, 2013
    Assignee: Unikorm
    Inventors: Valery Aleksandrovich Parshin, Tatyana Vasilyevna Golovko, Nelya Zarifovna Tugusheva, Marina Igorevna Medvedeva, Vladimir Vladimirovich Granik
  • Publication number: 20130165473
    Abstract: The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 27, 2013
    Applicant: ASTRAZENECA AB
    Inventor: AstraZeneca AB
  • Patent number: 8471026
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 25, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20130150339
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Amgen Inc.
    Inventor: Amgen Inc.
  • Patent number: 8461179
    Abstract: The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: June 11, 2013
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman, Peter A. Petillo
  • Patent number: 8461178
    Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumors and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: June 11, 2013
    Assignee: Aeterna Zentaris GmbH
    Inventors: Tilmann Schuster, Matthias Gerlach, Irene Seipelt, Emmanuel Polymeropoulos, Gilbert Mueller, Eckhard Guenther, Pascal Marchand, Julien Defaux
  • Patent number: 8461329
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: June 11, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
  • Patent number: 8461083
    Abstract: The present invention relates to novel herbicidal [1,8]-naphthyridines of Formula (Ia) or (Ib), or an agronomically acceptable salt of said compound wherein R2, R3, R4, R5, R6, R7, R8, n, m, X and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the [1,8]-naphthyridines, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: June 11, 2013
    Assignee: Syngenta Limited
    Inventors: Glynn Mitchell, David Phillip Bacon, Ian Henry Aspinall, Emma Briggs, Alaric James Avery, James Alan Morris, Claire Janet Russell, Roger Salmon
  • Publication number: 20130143899
    Abstract: The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Application
    Filed: February 4, 2011
    Publication date: June 6, 2013
    Inventors: Shifeng Pan, John E. Tellew, Yongqin Wan, Yongping Xie, Xing Wang, Xia Wang, Shenlin Huang, Zuosheng Liu, Qiong Zhang