Plural 1,3-diazine Rings Patents (Class 544/296)
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Publication number: 20140275095Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Curt A. Dvorak, Brock T. Shireman
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Patent number: 8835430Abstract: 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: GrantFiled: September 26, 2013Date of Patent: September 16, 2014Assignee: 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
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Publication number: 20140252280Abstract: The present invention relates to compounds of formula (I), a process for their production and their use in electronic devices, especially electroluminescent devices. When used as electron transport and/or host material for phosphorescent emitters in electroluminescent devices, the compounds of formula I may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.Type: ApplicationFiled: November 7, 2012Publication date: September 11, 2014Applicant: BASF SEInventors: Thomas Schaefer, Ute Heinemeyer, Nicolle Langer, Annemarie Wolleb, Christian Lennartz, Soichi Watanabe, Teresa Marina Figueira Duarte, Gerhard Wagenblast, Didier Bauer, Ingo Muenster, Christian Schildknecht, Heinz Wolleb
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Publication number: 20140249024Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.Type: ApplicationFiled: July 13, 2012Publication date: September 4, 2014Applicant: BASF SEInventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
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Publication number: 20140248236Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.Type: ApplicationFiled: November 7, 2012Publication date: September 4, 2014Inventors: Michael G. Natchus, Richard Arrendale
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Publication number: 20140243290Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: April 17, 2014Publication date: August 28, 2014Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20140239273Abstract: An anthracene derivative is represented by a formula (1) below, in which at least one of Ar1, Ar2, Ar3, L1, L2 and L3 is a group derived from a skeleton represented by a formula (10) below,Type: ApplicationFiled: December 18, 2013Publication date: August 28, 2014Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Sayaka MIZUTANI, Takayasu Sado
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Patent number: 8815862Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.Type: GrantFiled: December 3, 2012Date of Patent: August 26, 2014Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
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Publication number: 20140235620Abstract: 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: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: 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
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Publication number: 20140235582Abstract: Compounds of Formula (I) wherein B is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; Y is a linker moiety selected from the group consisting of a direct bond. R, R1, R2, and R3 are each individually selected from the group consisting substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or heterocycle.Type: ApplicationFiled: August 27, 2012Publication date: August 21, 2014Applicants: Sanford-Burnham Medical Research Institute, Southern Research InstituteInventors: Marintha L. Heil, Nicholas D.P. Cosford, Nicholas Pagano, Peter Teriete
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Patent number: 8802657Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: October 22, 2012Date of Patent: August 12, 2014Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Patent number: 8795691Abstract: The present invention is directed to implants and the modification of the surface of implants using amino acid or polypeptide functionalized rosette nanotubes.Type: GrantFiled: March 16, 2011Date of Patent: August 5, 2014Assignees: Brown University, National Research Council of Canada, The Governors of the University of AlbertaInventors: Thomas J. Webster, Hicham Fenniri, Usha Devi Hemraz
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Publication number: 20140213595Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: September 4, 2013Publication date: July 31, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Allan C. KRUEGER, John T. RANDOLPH, Christopher E. MOTTER, Preethi KRISHNAN, Neeta C. MISTRY, Tami J. PILOT-MATIAS, Sachin V. PATEL, Xiaoyan LI, Todd N. SOLTWEDEL, Lissa T. NELSON
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Publication number: 20140206585Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.Type: ApplicationFiled: June 4, 2012Publication date: July 24, 2014Applicants: UNIVERSITA DI BOLOGNA, Queen's University at KingstonInventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
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Publication number: 20140203252Abstract: An organic electroluminescent element which has a substrate, a pair of electrodes disposed on this substrate and composed of an anode and a cathode, and at least one organic layer disposed between these electrodes and including a light-emitting layer, and in which a compound expressed by General Formula 1-1 is contained in at least one layer of the aforementioned light-emitting layer(s) exhibits high luminous efficiency, excellent blue color purity, and little change in chromaticity accompanying drive deterioration.Type: ApplicationFiled: June 5, 2012Publication date: July 24, 2014Applicant: UDC Ireland LimitedInventors: Tetsu Kitamura, Koji Takaku, Wataru Sotoyama, Yasunori Yonekuta, Toshihiro Ise, Saki Takada, Toru Watanabe
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Patent number: 8785467Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: September 26, 2011Date of Patent: July 22, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
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Patent number: 8785461Abstract: The present invention relates to a novel intermediate useful in the preparation of bosentan and to processes for the preparation of said intermediate and bosentan. The invention further relates to compositions comprising bosentan prepared according to the processes of the invention and their use in the treatment of endothelin-receptor mediated disorders.Type: GrantFiled: February 6, 2009Date of Patent: July 22, 2014Assignee: Generics [UK] LimitedInventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Vikas Padalkar, Hemant Mande
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Patent number: 8778954Abstract: Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPAR?-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound.Type: GrantFiled: September 29, 2010Date of Patent: July 15, 2014Assignee: Kowa Company, Ltd.Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Patent number: 8778955Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.Type: GrantFiled: June 6, 2007Date of Patent: July 15, 2014Assignee: Sanofi-Aventis Deutschland GmbHInventors: Olaf Ritzeler, Gerhard Jaehne
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Publication number: 20140187568Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rakesh SINGH, Anu MITTAL, Gopal Singh BISHT, Mahavir Singh KHANNA, Rajesh Kumar THAPER, Mohan PRASAD
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Publication number: 20140187569Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rakesh SINGH, Anu MITTAL, Gopal Singh BISHT, Mahavir Singh KHANNA, Rajesh Kumar THAPER, Mohan PRASAD
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Publication number: 20140179681Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: January 8, 2014Publication date: June 26, 2014Inventor: Joseph P. Errico
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Publication number: 20140170066Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.Type: ApplicationFiled: February 24, 2014Publication date: June 19, 2014Applicants: Merck & Co., Inc., Visen Medical, Inc.Inventors: Milind Rajopadhye, Guojie Ho, Bohumil Bednar, Le T. Duong, Paul J. Coleman
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Publication number: 20140171430Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: April 20, 2012Publication date: June 19, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
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Publication number: 20140155382Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
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Publication number: 20140155407Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.Type: ApplicationFiled: October 21, 2011Publication date: June 5, 2014Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
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Patent number: 8741450Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electroluminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.Type: GrantFiled: August 31, 2012Date of Patent: June 3, 2014Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
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Patent number: 8735416Abstract: The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subject, more in particular infections with viruses having glycosilated envelope proteins such as Retroviridae (i.e., Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B, or C.Type: GrantFiled: April 23, 2012Date of Patent: May 27, 2014Assignee: Technische Universitaet Carolo-Wilhelmina zu BraunschweigInventors: Jan Balzarini, Monika Mazik
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Publication number: 20140142117Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, 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 11, 2013Publication date: May 22, 2014Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
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Publication number: 20140142094Abstract: This disclosure relates to compounds, methods for their preparation, pharmaceutical compositions including these compounds and methods for the treatment of cellular proliferative disorders, including, but not limited to cancer. The method includes administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 30, 2012Publication date: May 22, 2014Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: M.V. Ramana Reddy, E. Premkumar Reddy
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Publication number: 20140142308Abstract: Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials.Type: ApplicationFiled: March 27, 2012Publication date: May 22, 2014Applicant: NANKAI UNIVERSITYInventors: Yongsheng Chen, Xiangjian Wan, Yongsheng Liu, Zhi Li, Jiaoyan Zhou, Fei Wang, Guangrui He, Guankui Long
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Publication number: 20140142081Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Publication number: 20140135219Abstract: The present invention relates to the use of the ALS inhibitor herbicides for controlling unwanted vegetation in ALS inhibitor herbicide tolerant Brassica plants, more especially, the present invention relates to the use of ALS inhibitor herbicides for control of unwanted vegetation in Brassica growing areas which Brassica plants comprise non-transgenic mutations of their endogenous acetolactate synthase (ALS) genes I and III.Type: ApplicationFiled: May 4, 2012Publication date: May 15, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ruediger Hain, MIchael Schindler, Katharina Wölfel, Ulrich Ebbinghaus-Kintscher, Arnd Voerste, Olga Malsam, Peter Lösel, Ulrich Görgens
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Publication number: 20140128482Abstract: The present invention relates to improved hydrogel materials using water gellants that are comprised of polymer backbones P to which hydrogen bonding 4H-units are covalently attached via a hydrophobic linker L. Optionally, the hydrogel contains additional ingredients or additives. These new reversible hydrogels can easily be fine-tuned in their mechanical performance and function and are especially suitable for biomedical applications.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicant: SupraPolix B.V.Inventors: Travis Wayne BAUGHMAN, Gaby Maria Leonarda Van Gemert, Henricus Marie Janssen, Egbert Willem Meijer, Anton Willem Bosman
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Publication number: 20140124756Abstract: A compound having an indolocarbazole ring structure is represented by the following general formula (1), and is used as a material for forming a highly efficient and highly durable organic electroluminescent device. The compound features excellent hole injection/transport capability, has electron blocking power and is highly stable in the form of a thin film. wherein, A is a divalent aromatic hydrocarbon group or aromatic heterocyclic group, Ar1 to Ar4 are monovalent aromatic hydrocarbon groups or aromatic heterocyclic groups, and R1 to R9 are hydrogen atoms, deuterium atoms, fluorine atoms, chlorine atoms, cyano groups, nitro groups, alkyl groups, cycloalkyl groups, alkenyl groups, alkyloxy groups, cycloalkyloxy groups, aromatic hydrocarbon groups, aromatic heterocyclic groups or aryloxy groups.Type: ApplicationFiled: February 14, 2012Publication date: May 8, 2014Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Norimasa Yokoyama, Makoto Nagaoka, Sawa Izumi, Hiroshi Ookuma, Shuichi Hayashi
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Publication number: 20140128368Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Patent number: 8716477Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.Type: GrantFiled: November 12, 2010Date of Patent: May 6, 2014Assignee: Ranbaxy Laboratories LimitedInventors: Rakesh Singh, Anu Mittal, Gopal Singh Bisht, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20140113922Abstract: 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 19, 2013Publication date: April 24, 2014Applicant: GLAXO GROUP LIMITEDInventors: Yun JIN, Zehong Wan, Qing Zhang
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Patent number: 8703768Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: April 22, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
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Patent number: 8697715Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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: March 1, 2013Date of Patent: April 15, 2014Assignees: Array BioPharma, Inc., Genentech, Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Patent number: 8697694Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: April 15, 2014Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Jeremy Clark, Hollis S. Kezar, III, Vinay M. Girijavallabhan, Yuhua Huang, Regina Huelgas, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, Anita T. Fowler, Feng Geng, John A. Secrist, III, Neng-Yang Shih, Vishal Verma, Francisco Velazquez, Srikanth Venkatraman
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Publication number: 20140100231Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
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Publication number: 20140100214Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Patent number: 8685976Abstract: The subject invention discloses an agent for promoting cell adhesion to a support, comprising a dispirotripiperazine derivative represented by Formula I below or a salt thereof; a method for promoting cell adhesion to a support comprising adding the dispirotripiperazine derivative represented by Formula I below or a salt thereof to a culture medium, or applying the same to a support; and an agonist of a heparin sulfate that comprises the dispirotripiperazine derivative represented by Formula I below or a salt thereof, and that promotes cell adhesion and/or cell growth.Type: GrantFiled: June 16, 2009Date of Patent: April 1, 2014Assignee: Kyoto UniversityInventors: Motonari Uesugi, Sayumi Yamazoe
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Patent number: 8685964Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: GrantFiled: October 12, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
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Patent number: 8673891Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom, and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)RB (RB is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.Type: GrantFiled: February 5, 2010Date of Patent: March 18, 2014Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
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Publication number: 20140073788Abstract: Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions.Type: ApplicationFiled: November 11, 2013Publication date: March 13, 2014Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Andrei W. Konradi, Jenifer L. Smith, Michael S. Dappen, Christopher M. Semko
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Publication number: 20140073620Abstract: This invention relates to a compound of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.Type: ApplicationFiled: August 16, 2013Publication date: March 13, 2014Applicant: CANCER THERAPEUTICS CRC PTY LIMITEDInventors: Richard Charles FOITZIK, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
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Patent number: 8664226Abstract: Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPAR? activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.Type: GrantFiled: April 16, 2010Date of Patent: March 4, 2014Assignee: Kowa Company, Ltd.Inventors: Toru Miura, Kazuhiro Onogi, Seiichi Sato, Junya Tagashira, Gen Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya