Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
-
Patent number: 8969336Abstract: 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: GrantFiled: May 6, 2010Date of Patent: March 3, 2015Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
-
Publication number: 20150057218Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: November 3, 2014Publication date: February 26, 2015Inventors: Min ZHONG, Leping LI
-
Publication number: 20150057280Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Applicant: BASF SEInventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
-
Publication number: 20150057260Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: February 26, 2015Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
-
Patent number: 8962609Abstract: C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKK? and/or TBK-1: in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.Type: GrantFiled: July 18, 2011Date of Patent: February 24, 2015Assignee: Domainex LimitedInventors: Trevor Robert Perrior, Gary Karl Newton, Mark Richard Stewart, Rehan Aqil
-
Patent number: 8962622Abstract: Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R1, R2, R3, and m are defined herein.Type: GrantFiled: September 7, 2007Date of Patent: February 24, 2015Assignee: Roche Palo Alto LLCInventors: David Michael Goldstein, Levi Gong, Christophe Michoud, Wylie Solang Palmer, Achyutharao Sidduri
-
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
-
Publication number: 20150051195Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: ApplicationFiled: October 30, 2014Publication date: February 19, 2015Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
-
Publication number: 20150050274Abstract: The present invention relates to methods and biomarkers for detection and characterization of mature T-cell neoplasias/leukemias (e.g., T-cell prolymphocytic leukemia, Sezary syndrome) in biological samples (e.g., tissue samples, blood samples, plasma samples, cell samples, serum samples).Type: ApplicationFiled: August 14, 2014Publication date: February 19, 2015Inventors: Kojo Elenitoba-Johnson, Mark J. Kiel, Thirunavukkarasu Velusamy, Anagh Sahasrabuddhe, Delphine Rolland, Megan Lim
-
Patent number: 8957073Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): 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, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 11, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
-
Patent number: 8957068Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: GrantFiled: September 26, 2012Date of Patent: February 17, 2015Assignee: Novartis AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
-
Publication number: 20150045339Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).Type: ApplicationFiled: October 16, 2014Publication date: February 12, 2015Applicant: FUJIFILM CORPORATIONInventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
-
Publication number: 20150045353Abstract: In accordance with the present invention, there are provided formulations of gamma secretase modulators (GSMs) which are suitable for oral delivery and have improved transport properties relative to prior art formulations thereof. Also provided are methods for the preparation of such improved formulations and uses thereof for the delivery of GSMs to subjects in need thereof.Type: ApplicationFiled: August 9, 2013Publication date: February 12, 2015Applicant: Neurogenetic Pharmaceuticals, Inc.Inventors: William T. COMER, Maria Z. KOUNNAS, Bryan M. KNOX, Nathan S. BARKSDALE
-
Publication number: 20150045344Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, Sonja ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG, Jens SCHAMBERGER
-
Publication number: 20150045364Abstract: 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: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: NOVARTIS AGInventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
-
Publication number: 20150038481Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.Type: ApplicationFiled: May 21, 2013Publication date: February 5, 2015Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver
-
Patent number: 8946218Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: GrantFiled: May 10, 2011Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
-
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
-
Publication number: 20150031687Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: September 10, 2013Publication date: January 29, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Xianfeng Lin, Haixia Liu, Alexander V Mayweg, Zongxing Qiu, Hong Shen, Guozhi Tang, Lisha Wang, Guolong Wu, Shixiang Yan, Weixing Zhang, Mingwei Zhou, Wei Zhu
-
Patent number: 8940738Abstract: A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: August 11, 2010Date of Patent: January 27, 2015Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Daiki Sakai, Kazuki Nakayama, Kazutoshi Watanabe
-
Publication number: 20150025075Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: January 18, 2013Publication date: January 22, 2015Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm
-
Publication number: 20150023930Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.Type: ApplicationFiled: February 28, 2013Publication date: January 22, 2015Applicant: The McLean Hospital CorporationInventors: Diwan S. Rawat, Sunny Manohar, Ummadisetty Chinna Rajesh, Deepak Kumar, Anuj Thakur, Mohit Tripathi, Panyala Linga Reddy, Shamseer Kulangara Kandi, Satyapavan Vardhineni, Kwang-Soo Kim, Chun-Hyung Kim
-
Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
-
Publication number: 20150018331Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: March 24, 2014Publication date: January 15, 2015Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
-
Publication number: 20150018349Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 27, 2014Publication date: January 15, 2015Applicant: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
-
Publication number: 20150018335Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 7, 2013Publication date: January 15, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
-
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
-
Patent number: 8927547Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.Type: GrantFiled: May 20, 2011Date of Patent: January 6, 2015Assignee: Noviga Research ABInventors: Marita Högberg, Tommy Johansson, Emma Dahlstedt, Olof Smitt
-
Patent number: 8927009Abstract: A pharmaceutical capsule comprises a shell having encapsulated therewithin a liquid solution of ABT-263 or a pharmaceutically acceptable salt thereof in a substantially non-ethanolic carrier that comprises as pharmaceutically acceptable excipients (a) at least one phospholipid, (b) at least one solubilizing agent for the at least one phospholipid, selected from the group consisting of glycols, glycerides and mixtures thereof, (c) at least one non-phospholipid surfactant and (d) at least one sulfur-containing antioxidant. The capsule is useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: GrantFiled: December 21, 2010Date of Patent: January 6, 2015Assignee: AbbVie Inc.Inventors: Ping Tong, Deliang Zhou, Geoff G. Z. Zhang, Katherine R. Heemstra, Cristina M. Fischer, Nathaniel D. Catron, Eric A. Schmitt, Yeshwant D. Sanzgiri
-
Patent number: 8927525Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: GrantFiled: October 24, 2012Date of Patent: January 6, 2015Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
-
Patent number: 8927546Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: GrantFiled: September 22, 2010Date of Patent: January 6, 2015Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
-
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
-
Publication number: 20150005295Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.Type: ApplicationFiled: January 4, 2013Publication date: January 1, 2015Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
-
Publication number: 20150005297Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
-
Publication number: 20150005257Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.Type: ApplicationFiled: February 1, 2013Publication date: January 1, 2015Applicant: NIHON NOHYAKU CO. OLTD.Inventors: Eikou Satoh, Tetsuya Murata, Hiroto Harayama, Motofumi Nakano, Kosuke Fukatsu, Kayo Inukai, Ryota Kasahara, Yutaka Abe, Nobuyuki Hayashi, Naoya Fujita
-
Patent number: 8921336Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: GrantFiled: November 28, 2008Date of Patent: December 30, 2014Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
-
Publication number: 20140378450Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Novartis AGInventors: Giorgio CARAVATTI, Robin Alec FAIRHURST, Pascal FURET, Clive MCCARTHY, Heinrich RUEEGER, Frank Hans SEILER, Frédéric STAUFFER
-
Publication number: 20140378457Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: September 9, 2014Publication date: December 25, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
-
Publication number: 20140378443Abstract: The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.Type: ApplicationFiled: June 20, 2014Publication date: December 25, 2014Inventors: William L. Jorgensen, Karen S. Anderson
-
Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
-
Patent number: 8916553Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: July 25, 2011Date of Patent: December 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
-
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
-
Publication number: 20140371205Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Heinz STADTMUELLER, Ioannis SAPOUNTZIS
-
Patent number: 8912182Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: August 15, 2013Date of Patent: December 16, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
-
Publication number: 20140364429Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: AB PHARMA LTD.Inventor: Zheng-Yun James ZHAN
-
Publication number: 20140364398Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: PFIZER INC.Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
-
Patent number: 8906906Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: GrantFiled: August 5, 2010Date of Patent: December 9, 2014Assignee: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
-
Patent number: 8906917Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: GrantFiled: February 13, 2014Date of Patent: December 9, 2014Assignee: Corcept Therapeutics, Inc.Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
-
Patent number: 8906914Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.Type: GrantFiled: August 17, 2010Date of Patent: December 9, 2014Assignee: Janssen Pharmaceutica NVInventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad
-
Patent number: 8906916Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: July 19, 2011Date of Patent: December 9, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Christina Esdar, Hartmut Greiner