1,4-diazine Ring Patents (Class 544/120)
  • Patent number: 8673891
    Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom, and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)RB (RB is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 18, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
  • Patent number: 8669252
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Publication number: 20140031336
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 30, 2014
    Applicant: Glaxosmithkline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Patent number: 8637500
    Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; 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, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Ning Chen, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Essa Hu Harrington, Matthew R. Kaller, Roxanne K. Kunz, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Aaron C. Siegmund, Guomin Yao
  • Patent number: 8637508
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • Publication number: 20140024647
    Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 18, 2012
    Publication date: January 23, 2014
    Inventor: Akira Yukimasa
  • Publication number: 20130316981
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 28, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
  • Patent number: 8575336
    Abstract: The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: November 5, 2013
    Assignee: Pfizer Limited
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anjil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Publication number: 20130281449
    Abstract: The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: January 11, 2012
    Publication date: October 24, 2013
    Applicant: NOVARTIS AG
    Inventors: Konstanze Hurth, Rainer Martin Lueoend, Rainer Machauer, Ulf Neumann, Heinrich Rueeger, Michael Schaefer, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • Publication number: 20130281432
    Abstract: Pyridone and pyrazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: August 31, 2011
    Publication date: October 24, 2013
    Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
  • Patent number: 8557983
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: October 15, 2013
    Assignee: Abbvie Inc.
    Inventors: George A. Doherty, Laura A. Hexamer, Robert A. Mantei, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Todd M. Hansen
  • 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
  • Patent number: 8536166
    Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 17, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
  • Patent number: 8530468
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: September 10, 2013
    Assignee: Cancer Research Technology Limited
    Inventors: Ian Collins, John Charles Reader, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Michael Cherry
  • Patent number: 8524710
    Abstract: The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: September 3, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20130196984
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines 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: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.
    Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
  • Patent number: 8497265
    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: Grant
    Filed: May 12, 2011
    Date of Patent: July 30, 2013
    Assignee: 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: 20130184259
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.
    Type: Application
    Filed: November 16, 2012
    Publication date: July 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Publication number: 20130178470
    Abstract: The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
    Type: Application
    Filed: September 9, 2011
    Publication date: July 11, 2013
    Applicant: HANGZHOU BENSHENG PHARACEUTICALS CO., LTD.
    Inventors: Rongzhen Xu, Fuwen Xie, Hongxi Lai, Frank Rong
  • Publication number: 20130172349
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Novartis AG
    Inventor: Novartis AG
  • Patent number: 8476269
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
  • Publication number: 20130165412
    Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
    Type: Application
    Filed: September 14, 2012
    Publication date: June 27, 2013
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Publication number: 20130165432
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Application
    Filed: February 21, 2013
    Publication date: June 27, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130165443
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: August 23, 2012
    Publication date: June 27, 2013
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20130143860
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
    Type: Application
    Filed: January 31, 2013
    Publication date: June 6, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130137660
    Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: YM Biosciences Australia Pty Ltd
    Inventor: YM Biosciences Australia Pty Ltd
  • Publication number: 20130137635
    Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.
    Type: Application
    Filed: February 9, 2011
    Publication date: May 30, 2013
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventor: Arthur Thomas Sands
  • Publication number: 20130131040
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: May 23, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20130115310
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 9, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130102586
    Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 25, 2013
    Applicant: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
  • Publication number: 20130102605
    Abstract: The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: April 21, 2011
    Publication date: April 25, 2013
    Inventors: Peng Liang, Morihiro Mitsuya, Yoshio Ogino, Changhe Qi, Hidekazu Takahashi, Paul Tempest, Jiabing Wang, Yuguang Wang, Zhenzhen Wang, Shaohua Zhang, Nanyan Zhou, Jiuxiang Zhu
  • Publication number: 20130095193
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: September 4, 2012
    Publication date: April 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Publication number: 20130089624
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
  • Publication number: 20130065900
    Abstract: The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group —CH2CH2— which together with the said one carbon atom forms a cyclop
    Type: Application
    Filed: May 12, 2011
    Publication date: March 14, 2013
    Applicant: SENTINEL ONCOLOGY LIMITED
    Inventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce
  • Patent number: 8394806
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: March 12, 2013
    Assignee: YM Biosciences Australia Pty Ltd
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Patent number: 8383660
    Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: February 26, 2013
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
  • Publication number: 20130040933
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like.
    Type: Application
    Filed: April 21, 2011
    Publication date: February 14, 2013
    Inventors: Brandon Cash, Christian Fischer, Yudith Garcia, Joon Jung, Jason Katz, June Kim, Alexey Rivkin, Adam Schell, Tony Siu, David Witter, Hua Zhou
  • Publication number: 20130040931
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
    Type: Application
    Filed: January 14, 2011
    Publication date: February 14, 2013
    Applicant: Amgen Inc.
    Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Publication number: 20130040949
    Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: December 29, 2010
    Publication date: February 14, 2013
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
  • Publication number: 20130029968
    Abstract: The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
    Type: Application
    Filed: July 5, 2012
    Publication date: January 31, 2013
    Applicant: PFIZER LIMITED
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Patent number: 8357685
    Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: January 22, 2013
    Assignee: Glaxo Group Limited
    Inventor: John Liddle
  • Publication number: 20130018046
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
  • Publication number: 20130012500
    Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Inventors: Gurdip BHALAY, Emma BUDD, Graham Charles BLOOMFIELD, Stephen Paul COLLINGWOOD, Andrew DUNSTAN, Lee EDWARDS, Peter GEDECK, Catherine HOWSHAM, Peter HUNT, Thomas Anthony HUNT, Paul OAKLEY, Nichola SMITH
  • Patent number: 8338413
    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: March 7, 2012
    Date of Patent: December 25, 2012
    Assignee: Novartis AG
    Inventor: Heinrich Rueeger
  • Publication number: 20120321559
    Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
    Type: Application
    Filed: August 24, 2012
    Publication date: December 20, 2012
    Inventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Publication number: 20120316172
    Abstract: The invention relates to compounds of formula IA and IB wherein R1, R2, R3, R4 and Z are as defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formulas IA and IB have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 13, 2012
    Inventors: Guido Galley, Cédric Ghellamallah, Roger Norcross, Philippe Pflieger
  • Publication number: 20120316165
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 13, 2012
    Inventors: Guido Galley, Roger Norcross, Philippe Pflieger