Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20150126527Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: October 9, 2014Publication date: May 7, 2015Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20150126490Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.Type: ApplicationFiled: October 29, 2014Publication date: May 7, 2015Applicant: Novartis AGInventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
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Publication number: 20150110871Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.Type: ApplicationFiled: January 3, 2015Publication date: April 23, 2015Inventor: David Wong
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Patent number: 9005581Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.Type: GrantFiled: March 4, 2014Date of Patent: April 14, 2015Assignee: MediBeacon, LLCInventors: Amruta Poreddy, William L. Neumann
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Publication number: 20150099764Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: December 9, 2014Publication date: April 9, 2015Applicant: PARION SCIENCES, INC.Inventors: Michael Ross JOHNSON, William Robert Thelin, Richard C. Boucher
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Patent number: 8999996Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: GrantFiled: March 19, 2014Date of Patent: April 7, 2015Assignee: Karyopharm Therapeutics Inc.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Publication number: 20150087656Abstract: Prolongation compositions for prolonging the presence of drugs in blood.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Aida Salatinjants, Robert Salatinjants
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Patent number: 8980898Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: May 29, 2013Date of Patent: March 17, 2015Assignee: Parion Sciences, Inc.Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
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Publication number: 20150065431Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
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Patent number: 8969356Abstract: The present invention relates to pyrazine and pyridine 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 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: GrantFiled: May 12, 2011Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Joanne Pinder, Stephen Young, Philip Michael Reaper
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Publication number: 20150057279Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Publication number: 20150056305Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.Type: ApplicationFiled: August 13, 2014Publication date: February 26, 2015Applicant: PARION SCIENCES, INC.Inventors: Michael R. Johnson, William R. Thelin, Ronald A. Aungst, JR.
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Publication number: 20150057289Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: November 4, 2014Publication date: February 26, 2015Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Patent number: 8962623Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.Type: GrantFiled: February 29, 2012Date of Patent: February 24, 2015Assignee: Locus Pharmaceuticals, Inc.Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristofer K. Moffett, Younghee Lee, Dora Do-York Wong
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Patent number: 8962631Abstract: The present invention relates to pyrazine 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 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 II: wherein the variables are as defined herein.Type: GrantFiled: May 12, 2011Date of Patent: February 24, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
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Publication number: 20150051199Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.Type: ApplicationFiled: October 31, 2012Publication date: February 19, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
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Publication number: 20150051187Abstract: The present invention relates to pyrazine 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: ApplicationFiled: August 25, 2014Publication date: February 19, 2015Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
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Publication number: 20150045326Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
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Publication number: 20150045312Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.Type: ApplicationFiled: August 11, 2014Publication date: February 12, 2015Inventors: Michael Neary, Chad Beyer
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Publication number: 20150031661Abstract: The present invention relates to pyrazine 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: ApplicationFiled: March 24, 2014Publication date: January 29, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
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Publication number: 20150031682Abstract: The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.Type: ApplicationFiled: February 15, 2013Publication date: January 29, 2015Inventors: Yassir Younis, Kelly Chibale, Michael John Witty, David Waterson
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Patent number: 8937072Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.Type: GrantFiled: June 15, 2012Date of Patent: January 20, 2015Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
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Publication number: 20150018374Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1 is F, Cl or Br; R2 is H or F; and R3 is Cl or Br; and (b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.Type: ApplicationFiled: January 30, 2013Publication date: January 15, 2015Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, James Francis Bereznak
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Publication number: 20150011535Abstract: 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, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Armin HECKEL, Joerg KLEY
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Publication number: 20150011470Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: September 19, 2014Publication date: January 8, 2015Applicant: PFIZER INC.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Publication number: 20150005232Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.Type: ApplicationFiled: February 28, 2013Publication date: January 1, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
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Publication number: 20150005294Abstract: The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.Type: ApplicationFiled: January 10, 2013Publication date: January 1, 2015Applicants: CANCER RESEARCH TECHNOLOGY LIMITED, MERCK PATENT GMBHInventors: Kai Schiemann, Frank Stieber, Christina Esdar
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Patent number: 8921370Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: December 22, 2011Date of Patent: December 30, 2014Assignee: H. Lundbeck A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Publication number: 20140378461Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.Type: ApplicationFiled: February 14, 2013Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
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Publication number: 20140371196Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicants: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Itsuro SHIMADA, Kazuo KUROSAWA, Takahiro MATSUYA, Kazuhiko IIKUBO, Yutaka KONDOH, Akio KAMIKAWA, Hiroshi TOMIYAMA, Yoshinori IWAI
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Publication number: 20140356456Abstract: This invention relates to methods and compositions for treating pancreatic cancer. More specifically, this invention relates to treating pancreatic cancer with certain ATR inhibitors in combination with gemcitabine and/or radiation therapy. This invention also relates to methods and compositions for treating non-small cell lung cancer. More specifically, this invention relates to treating non-small cell lung cancer with an ATR inhibitor in combination with cisplatin or carboplatin, etoposide, and ionizing radiation.Type: ApplicationFiled: February 28, 2014Publication date: December 4, 2014Inventors: John Robert Pollard, Philip Michael Reaper
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Publication number: 20140350030Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.Type: ApplicationFiled: September 17, 2012Publication date: November 27, 2014Inventors: Dario Doller, Guiying Li
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Patent number: 8895564Abstract: Provided is a novel compound which simultaneously inhibits both NMDA receptors and ASIC1a, which are associated with neurodegenerative disease and so on, and thus is useful for the prevention and treatment of various nervous system diseases. A biguanide derivative represented by the following general formula (1), a salt thereof, or a hydrate of the derivative or the salt: wherein, X1 represents a halogen atom, R1 represents an alkyl group, an optionally substituted aryl group, or an optionally substituted aralkyl group.Type: GrantFiled: December 1, 2011Date of Patent: November 25, 2014Assignee: Nihon UniversityInventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
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Patent number: 8889693Abstract: The main object of the present invention is to provide a fibrosis inhibitor. The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient: In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.Type: GrantFiled: April 10, 2014Date of Patent: November 18, 2014Assignee: Nippon Shinyaku Co., Ltd.Inventors: Koji Murakami, Takuya Toramoto
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Patent number: 8889692Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: September 14, 2012Date of Patent: November 18, 2014Assignee: AstraZeneca ABInventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Patent number: 8883852Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.Type: GrantFiled: October 21, 2009Date of Patent: November 11, 2014Assignee: University of Pittburgh—Of the Commonwealth System of Higher EducationInventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
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Patent number: 8883842Abstract: The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I) wherein the radicals and symbols have the meanings as defined in the specification, for the preparation of a medicament for the treatment of myeloma, in particular, multiple myeloma, especially myeloma which is resistant to conventional chemotherapy; to a combination comprising an HDAC inhibitor and a compound effecting apoptosis of myeloma cells, preferably bortezomib, for simultaneous, separate or sequential use; to methods of treating myeloma; and to a pharmaceutical composition comprising said combination.Type: GrantFiled: March 4, 2010Date of Patent: November 11, 2014Assignee: Novartis AGInventor: Peter W Atadja
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Patent number: 8877759Abstract: 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: GrantFiled: September 4, 2012Date of Patent: November 4, 2014Assignee: Vertex Pharnaceuticals IncorporatedInventors: Jean-Damien Charrier, David Kay, 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
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Patent number: 8877760Abstract: Provided are substituted pyrazine-2-carboxamide compounds of Formula I: useful 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: GrantFiled: November 23, 2012Date of Patent: November 4, 2014Assignee: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Anjali Pandey
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Publication number: 20140323484Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 or 1; Q1 is selected from a bond; C(?O); S(O); SO2; and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom.Type: ApplicationFiled: November 16, 2012Publication date: October 30, 2014Inventors: Robert George Boyle, Richard Justin Boyce
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Publication number: 20140323423Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.Type: ApplicationFiled: May 2, 2014Publication date: October 30, 2014Applicant: Chrono Therapeutics, Inc.Inventors: Guy DiPierro, Steven A. Giannos
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Publication number: 20140323463Abstract: [Problem] A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided. [Means for Solution] The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention.Type: ApplicationFiled: January 15, 2013Publication date: October 30, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
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Publication number: 20140309209Abstract: 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: ApplicationFiled: November 23, 2012Publication date: October 16, 2014Inventors: Yonghong Song, Qing Xu, Zhaozhong J. Jia, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Patent number: 8859560Abstract: The present invention relates to a method of treating attention deficit hyperactivity disorder in a subject. This method includes selecting a subject with attention deficit hyperactivity disorder and administering to the selected subject a sodium/hydrogen exchanger inhibitor under conditions effective to treat the subject for attention deficit hyperactivity disorder. Methods of identifying compounds suitable to treat attention deficit hyperactivity disorder are also disclosed.Type: GrantFiled: February 15, 2013Date of Patent: October 14, 2014Assignee: The Research Foundation of State University of New YorkInventor: Stephen V. Faraone
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Patent number: 8859559Abstract: 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: GrantFiled: December 18, 2012Date of Patent: October 14, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Andreas Blum, Dieter Hamprecht, Joerg Kley
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Patent number: 8859558Abstract: This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.Type: GrantFiled: May 31, 2011Date of Patent: October 14, 2014Assignee: Dow AgroSciences, LLC.Inventors: Kristy Bryan, George E. Davis, Paul R. Graupner, Beth Lorsbach, W. John Owen, Francis E. Tisdell
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Patent number: 8853440Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.Type: GrantFiled: August 13, 2009Date of Patent: October 7, 2014Assignee: Mitsui Chemicals Agro, Inc.Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
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Patent number: 8846687Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.Type: GrantFiled: April 30, 2012Date of Patent: September 30, 2014Assignee: Novartis AGInventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
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Patent number: 8846688Abstract: This invention relates to sodium channel blocking phenyl guanidine compounds of Formula (I): pharmaceutical compositions comprising them, and methods of using them for blocking sodium channels, promoting hydration of mucosal surfaces, and for methods of treating diseases including cystic fibrosis, COPD, asthma, emphysema, chronic bronchitis, and pneumonia.Type: GrantFiled: June 8, 2012Date of Patent: September 30, 2014Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang