Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Publication number: 20120157431Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: December 23, 2011Publication date: June 21, 2012Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20120157464Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.Type: ApplicationFiled: July 21, 2010Publication date: June 21, 2012Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
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Publication number: 20120157486Abstract: A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, penthiopyrad, fluopyram, boscalid, mancozeb, pyrimethanil, and bixafen provides synergistic control of selected fungi.Type: ApplicationFiled: November 30, 2011Publication date: June 21, 2012Applicant: DOW AGROSCIENCES LLCInventors: Beth Lorsbach, W. John Owen, Chenglin Yao
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Publication number: 20120157425Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 21, 2011Publication date: June 21, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120157383Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
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Publication number: 20120156225Abstract: Numerous diseases have been linked to the production of regulator cells. The present invention relates to the observation that the immune system is cycling in these diseases. Based on these observations, the present invention provides methods for treating diseases such as cancer and a HIV infection. The present invention also relates to methods of determining when a therapy to treat a disease characterized by the production of regulator cells should be administered to a patient.Type: ApplicationFiled: February 14, 2012Publication date: June 21, 2012Applicant: IMMUNAID PTY LTDInventor: Martin Leonard ASHDOWN
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Publication number: 20120157400Abstract: Methods for treating Kaposi's sarcoma involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Marla L. Weetall
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Publication number: 20120157485Abstract: A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, pentiopyrad, fluopyram, boscalid, mancozeb, and pyrimethanil provides synergistic control of selected fungi.Type: ApplicationFiled: November 30, 2011Publication date: June 21, 2012Applicant: DOW AGROSCIENCES LLCInventors: Beth Lorsbach, W. John Owen, Chenglin Yao
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Publication number: 20120157487Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20120157401Abstract: Methods for treating neurofibromatosis involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Harry H. Miao, Langdon Miller, Marla Weetall
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Publication number: 20120156212Abstract: The present invention relates to compounds as novel thymidylate synthase inhibitors, novel strategies to treat or prevent neoplasia in a subject, methods and compositions thereof.Type: ApplicationFiled: May 29, 2010Publication date: June 21, 2012Inventors: David A. Ostrov, Carmen J. Allegra
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Publication number: 20120148595Abstract: The present invention relates to GABA-linked anthracycline-lipid conjugates and to methods of using the conjugates to treat cancer. Methods for making the GABA-linked anthracycline lipid conjugates are also provided.Type: ApplicationFiled: March 11, 2010Publication date: June 14, 2012Applicant: Luitpold Pharmaceuticals, Inc.Inventors: Charles S. Swindell, Glenn G. Fegley, Hema M. Sundar, Richard Lawrence
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Publication number: 20120149677Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: August 16, 2010Publication date: June 14, 2012Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Publication number: 20120149723Abstract: This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals.Type: ApplicationFiled: August 16, 2010Publication date: June 14, 2012Inventor: Romano Di Fabio
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Publication number: 20120148690Abstract: A novel skin barrier function recovery acceleration method and accelerator are provided. The present invention provides a skin barrier function recovery accelerator that comprises a TRPA1 agonist capable of activating TRPA1 in epidermal cells.Type: ApplicationFiled: December 10, 2010Publication date: June 14, 2012Inventors: Mitsuhiro Denda, Moe Tsutsumi, Sumiko Denda
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Patent number: 8198273Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.Type: GrantFiled: May 4, 2010Date of Patent: June 12, 2012Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Publication number: 20120142716Abstract: The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound.Type: ApplicationFiled: August 15, 2008Publication date: June 7, 2012Inventors: Martin Bolli, Christoph Boss, Alexander Treiber
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Publication number: 20120142711Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.Type: ApplicationFiled: June 21, 2010Publication date: June 7, 2012Applicant: KTB TUMORFORSCHUNGSGESELLSCHAFT MBHInventors: André Warnecke, Ivonne Müller
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Publication number: 20120142717Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: June 7, 2012Inventors: Yun JIN, Zehong WAN, Qing ZHANG
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Publication number: 20120144510Abstract: The disclosure relates to an endothelin receptor antagonist for use in the prevention or treatment of brain metastases in combination with a cytotoxic chemotherapy agent, radiotherapy or both. The endothelin receptor antagonist may for example be bosentan, macitentan or a mixture of bosentan and macitentan.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: Board of Regents, The University of Texas SystemInventors: Isaiah J. Fidler, Sun-Jin Kim
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Patent number: 8193183Abstract: The present invention is directed to a compound of Formula (I) wherein Cy1, Cy2, L1, L2, and R1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemType: GrantFiled: April 16, 2007Date of Patent: June 5, 2012Assignee: Aventis Pharmaceuticals Inc.Inventors: Sungtaek Lim, Keith John Harris, David Stefany, Charles J. Gardner, Bin Cao, Ray Boffey, Timothy A. Gillespy, Joacy C. Aguiar, Hazel J. Dyke, Elsa A. Dechaux
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Publication number: 20120135950Abstract: Compositions and methods to treat lymphoma and cancer are disclosed. In particular, the method teaches treatment of lymphoma and cancer using anti-HERV-K(HML-2) therapies. Further taught are compositions and methods for characterizing patient samples to, for example, select or identify therapeutic options or assess the impact of therapies.Type: ApplicationFiled: May 21, 2010Publication date: May 31, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Mark H. Kaplan, Rafael Contreras-Galindo, David Markovitz
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Publication number: 20120135977Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Inventors: Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
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Publication number: 20120134987Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: December 15, 2011Publication date: May 31, 2012Inventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
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Publication number: 20120136017Abstract: Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fluoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.Type: ApplicationFiled: March 12, 2008Publication date: May 31, 2012Applicant: Southern Research Institute Office of Commercialization and Intellectual PropertyInventors: John A. Secrist, III, Kamal N. Tiwari, Joseph A. Maddry
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Publication number: 20120135089Abstract: The present invention provides, e.g., compounds having the structure of formula (I): The present invention also provides pharmaceutical compositions that include such compounds, and methods for modulating murine double minute 2 protein (Mdm2) E3 ligase activity, particularly the Mdm2-MdmX hetero-complex E3 ligase activity, using such compounds.Type: ApplicationFiled: March 17, 2010Publication date: May 31, 2012Inventors: Brent R. Stockwell, Ariel Herman
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Patent number: 8188275Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: GrantFiled: October 30, 2007Date of Patent: May 29, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 8188104Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: GrantFiled: September 17, 2008Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: Charles A. Flengte, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
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Patent number: 8188105Abstract: A therapeutic agent for inflammatory bowel disease contains, as an active ingredient, a uracil derivative or a pharmaceutically acceptable salt thereof, represented by formula (1) where the R1 and R2 groups are defined in the specification.Type: GrantFiled: October 10, 2008Date of Patent: May 29, 2012Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Kazuki Sakamoto, Fumio Nakagawa
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Publication number: 20120129847Abstract: Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like.Type: ApplicationFiled: October 5, 2011Publication date: May 24, 2012Inventors: Kevin Gene Peters, Robert Shalwitz
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Publication number: 20120128667Abstract: The present invention relates to the treatment of cancer, e.g., ovarian cancer, breast cancer, pancreatic cancer or colon cancer, with pentamidine and (a) oxaliplatin, (b) gemcitabine, (c) taxol, (d) 5-fluorouracil or (e) CPT 11.Type: ApplicationFiled: May 3, 2010Publication date: May 24, 2012Applicant: ONCOZYME PHARMA INC.Inventors: Terry Chow, Chiaoli Yeh, David Griller
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Publication number: 20120129878Abstract: Provided is a tablet having a high content of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active component. A tablet containing compound (A) or a salt thereof, and a fluidizer, which has a compound (A) content of 35-50 weight %.Type: ApplicationFiled: July 27, 2010Publication date: May 24, 2012Inventors: Yusuke Murakawa, Takayuki Okabe
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Publication number: 20120122891Abstract: 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: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: 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
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Publication number: 20120122844Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20120121698Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.Type: ApplicationFiled: April 29, 2010Publication date: May 17, 2012Applicant: AMARIN PHARMA, INC.Inventors: Mehar Manku, Jonathan Rowe
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Publication number: 20120122857Abstract: The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Guido BOLD, Andrea VAUPEL, Carole Pissot SOLDERMANN, Paul W. MANLEY
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Publication number: 20120122810Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20120122907Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 14, 2010Publication date: May 17, 2012Inventor: Christelle Boléa
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Publication number: 20120121502Abstract: The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.Type: ApplicationFiled: November 15, 2011Publication date: May 17, 2012Applicant: ACETYLON PHARMACEUTICALSInventors: John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
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Publication number: 20120122860Abstract: Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.Type: ApplicationFiled: May 4, 2010Publication date: May 17, 2012Inventors: Gary Conard Visor, Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Patent number: 8178131Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 13, 2009Date of Patent: May 15, 2012Assignee: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Patent number: 8178548Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: GrantFiled: September 17, 2008Date of Patent: May 15, 2012Assignee: Abbott LaboratoriesInventors: Pamela L. Donner, John T. Randolph, Allan C. Krueger, David A. Betebenner, Douglas K. Hutchinson, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, John E. Hengeveld, Rodger F. Henry, Xiaochun Lou, Geoff G. Z. Zhang
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Patent number: 8178549Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.Type: GrantFiled: October 1, 2008Date of Patent: May 15, 2012Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Francesca Cardullo, Paolo Dambruoso, Paola Marzorati, Fabrizio Micheli, Alessandra Pasquarello, Catia Seri, Giovanna Tedesco
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Publication number: 20120115894Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: February 22, 2010Publication date: May 10, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
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Patent number: 8173665Abstract: The invention relates to 4-cyanophenyl, 2-sulfanyl, 1-phenyl pyrimidine derivatives, processes for their preparation, and pharmaceutical compositions of the same. Compounds and compositions of the invention are useful in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.Type: GrantFiled: July 27, 2009Date of Patent: May 8, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenieh, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 8173663Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: GrantFiled: October 30, 2007Date of Patent: May 8, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 8173664Abstract: The present invention provides a class of modified pyrimidine compounds, compositions and methods of using the compounds as glucocorticoid receptor modulators.Type: GrantFiled: July 8, 2009Date of Patent: May 8, 2012Assignee: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicolas C. Ray, Karen Williams, Peter H. Crackett, Gwen Hickin, David A. Clark
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Publication number: 20120108529Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
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Publication number: 20120107307Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: March 23, 2010Publication date: May 3, 2012Applicant: ARDEA BIOSCIENCES INC.Inventors: Jean-Michel Vernier, Hong Woo Kim, Marion Hitchcock, Shunqi Yan
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande