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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Patent number: 8664392Abstract: Provided are compounds and compositions of general Formula IX: E1-L-Ar—X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.Type: GrantFiled: January 6, 2012Date of Patent: March 4, 2014Assignee: MediBeacon, LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow
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Patent number: 8664228Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: May 11, 2009Date of Patent: March 4, 2014Assignee: Novartis AGInventors: Stephen Paul Collingwood, Catherine Howsham, Thomas Anthony Hunt
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Publication number: 20140057905Abstract: The present invention is directed to methods of inhibiting both proliferation and survival of cancer cells and for treating a subject having cancer. The present invention is further directed to methods of diagnosing cancer in a subject and identifying cancer therapeutics.Type: ApplicationFiled: April 2, 2012Publication date: February 27, 2014Applicant: NEW YORK UNIVERSITYInventors: Dafna Bar-Sagi, Cosimo Commisso, Rengin G. Soydaner-Azeloglu
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Publication number: 20140057873Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.Type: ApplicationFiled: November 1, 2013Publication date: February 27, 2014Inventor: Michael Farber
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Patent number: 8653086Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: GrantFiled: October 21, 2009Date of Patent: February 18, 2014Assignee: Oregon Health & Science UniversityInventors: Xiangshu Xiao, Bingbing Li
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Publication number: 20140044802Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. 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: April 5, 2013Publication date: February 13, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20140045791Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: July 15, 2013Publication date: February 13, 2014Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Ann-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran
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Publication number: 20140031372Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome.Type: ApplicationFiled: October 2, 2013Publication date: January 30, 2014Inventors: Benson M. Fong, Glenn V. Cornett
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Publication number: 20140031371Abstract: Polyaromatic 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: October 1, 2013Publication date: January 30, 2014Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross JOHNSON
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Publication number: 20140031370Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Publication number: 20140031348Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: July 9, 2013Publication date: January 30, 2014Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20140023615Abstract: The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.Type: ApplicationFiled: March 29, 2012Publication date: January 23, 2014Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Stephen I-Hong Hsu
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Patent number: 8628751Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: GrantFiled: April 15, 2010Date of Patent: January 14, 2014Assignee: Medi Beacon Development, LLCInventors: William L. Neumann, John N. Freskos
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Publication number: 20140011817Abstract: This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 21, 2013Publication date: January 9, 2014Applicant: Morehouse School of MedicineInventors: Zhigang Xiong, Roger P. Simon
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Patent number: 8614213Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: GrantFiled: August 5, 2009Date of Patent: December 24, 2013Assignee: Novartis AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Publication number: 20130338059Abstract: This disclosure relates to methods for differentiating between mammals having active and latent Tuberculosis disease, by determining the percentage of polyfunctional CD4+ T-cells expressing TNF-alpha, IFN-gamma, and IL-2, or by determining expression of IL-17.Type: ApplicationFiled: December 22, 2011Publication date: December 19, 2013Applicant: Centre Hospitalier Universitaire VaudoisInventors: Giuseppe Pantaleo, Alexandre Harari, Matthieu Perreau
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Publication number: 20130331396Abstract: Certain piperazinyl and piperidinyl urea compounds 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. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: August 13, 2013Publication date: December 12, 2013Applicant: Janssen Pharmaceutica NVInventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, mark Seierstad, Wei Xiao
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Publication number: 20130324559Abstract: 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: May 29, 2013Publication date: December 5, 2013Applicant: PARION SCIENCES, INC.Inventors: Michael Ross JOHNSON, William Robert THELIN, Richard C. BOUCHER
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Publication number: 20130303446Abstract: The invention relates to a pharmaceutical combination comprising the compound of formula I or pharmaceutically acceptable salts thereof in combination with at least one second therapeutic agent 2. The pharmaceutical combination of the invention is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.Type: ApplicationFiled: May 7, 2013Publication date: November 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bradford S. HAMILTON, Thomas RAUCH, Manami TSUTSUMI
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Publication number: 20130303548Abstract: Niacin prevents and/or reverses the development of experimental hepatic steatosis, deposition of triglycerides in liver and serum of individuals, deposition of total cholesterol in liver and serum in individuals, and inhibit liver lipid peroxidation and oxidative stress in individuals at risk of developing fatty liver disease or NAFLD. In cultured human hepatocytes, niacin inhibits alcohol-induced fat accumulation.Type: ApplicationFiled: November 22, 2011Publication date: November 14, 2013Applicant: The Regents of the University of CaliforniaInventors: Moti L. Kashyap, Shobha V. Kamanna, Vaijinath S. Kamanna
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Publication number: 20130303547Abstract: This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Brian E. Green, David D. Anderson, Todd D. Bosse, Curt S. Cooper, Larry L. Klein, Allan C. Krueger, Daniel P. Larson, Dachun Liu, Keith F. McDaniel, Christopher E. Motter, John K. Pratt, Todd W. Rockway, Teresa A. Rosenberg, Ming C. Yeung, Hui-Ju Chen, Jason P. Shanley
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Patent number: 8575175Abstract: The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.Type: GrantFiled: July 23, 2009Date of Patent: November 5, 2013Assignee: Toray Industries, Inc.Inventors: Fuko Matsuda, Katsuhiko Iseki, Hajimu Kurumatani, Mitsuko Miyamoto
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Patent number: 8575176Abstract: Polyaromatic 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: January 18, 2012Date of Patent: November 5, 2013Assignee: Parion Sciences, Inc.Inventor: Michael Ross Johnson
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Publication number: 20130288977Abstract: The present invention includes a treating step of treating neuronal growth cone with a regulatory factor to regulate macropinocytosis caused by a repulsive axon guidance molecule. The present invention can provide a new neuronal axon elongation regulating method etc.Type: ApplicationFiled: April 24, 2013Publication date: October 31, 2013Applicant: RIKENInventors: Katsuhiko MIKOSHIBA, Hiroyuki KABAYAMA
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Publication number: 20130281464Abstract: 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: ApplicationFiled: December 1, 2011Publication date: October 24, 2013Applicant: NIHON UNIVERSITYInventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
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Publication number: 20130274261Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.Type: ApplicationFiled: March 18, 2013Publication date: October 17, 2013Inventor: Arthur T. SANDS
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Publication number: 20130261133Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: The University of MontanaInventors: John Howard Hoody, David Brian Bolstad
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Publication number: 20130261122Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Applicant: N30 Pharmaceuticls, Inc.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20130252974Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: ApplicationFiled: May 15, 2013Publication date: September 26, 2013Applicant: SANOFIInventors: Jean-Michel Altenburger, Valerie Fossey, Daniel Galtier, Frederic Petit
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Publication number: 20130231351Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: January 23, 2013Publication date: September 5, 2013Applicant: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Publication number: 20130225587Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.Type: ApplicationFiled: November 9, 2011Publication date: August 29, 2013Applicants: Zhejiang Beta Pharma Incorporation, Fujian Haixi Pharmaceuticals, Inc.Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
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Publication number: 20130225487Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).Type: ApplicationFiled: March 12, 2013Publication date: August 29, 2013Applicant: Pfizer Inc.Inventor: Pfizer Inc.
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Publication number: 20130225531Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.Type: ApplicationFiled: December 19, 2012Publication date: August 29, 2013Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: The Board Of Trustees Of The University of Illinois
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Patent number: 8518950Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: January 25, 2006Date of Patent: August 27, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
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Patent number: 8518450Abstract: The invention provides a process for the production of nanoparticle carriers for drug delivery, said nanoparticles being produced by preparing a double emulsion of water-oil-water including one or more polymer which forms the basis of the nanoparticle carrier, blending the drug to be delivered into one of the emulsion phases, doping either the oil-phase or the outer-water phase with a carbohydrate, and spray drying the emulsion to form nanoparticles of a narrow particle size distribution of 100 nm to 1000 nm, which nanoparticles are substantially spherical.Type: GrantFiled: August 17, 2010Date of Patent: August 27, 2013Assignee: CSIRInventor: Lonji Kalombo
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Publication number: 20130217708Abstract: A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.Type: ApplicationFiled: September 29, 2011Publication date: August 22, 2013Applicant: Toyama Chemical Co., Ltd.Inventors: Keiko Takakura, Namika Nakamatsu, Sakiko Takeshima, Takayoshi Nakashima
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Publication number: 20130216625Abstract: The present invention relates to the use of a substance with the core structure of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the manufacture of a composition for the treatment of insulin resistance or diseases associated with insulin resistance, preferably in human subject in a daily dosage in a range of from about 5 mg to about 1500 mg. The invention furthermore relates to a method of treating insulin resistance or diseases associated with insulin resistance in a mammal, said method comprises administering to said mamma, preferably a human subject, a substance with the core structure of formula (I), preferably in a daily dosage in a range from about 5 mg to about 1500 mg. The substance is preferably isosteviol or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. Examples of diseases associated with insulin resistance and e.g.Type: ApplicationFiled: September 14, 2012Publication date: August 22, 2013Applicant: STEVIA APSInventors: Kjeld Hermansen, Per Bendix Jeppesen
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Publication number: 20130217707Abstract: 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: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: The Research Foundation of State University of New YorkInventor: The Research Foundation of State University of New York
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20130217706Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Yoúng-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20130213398Abstract: The present invention is directed toward respirable dry particles for delivery of divalent metal cation salts and/or monovalent cation salts to the respiratory tract and methods for treating a subject having a respiratory disease and/or infection.Type: ApplicationFiled: August 26, 2011Publication date: August 22, 2013Inventors: Michael M. Lipp, Jean C. Sung, Robert W. Clarke, David L. Hava
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Patent number: 8513261Abstract: Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.Type: GrantFiled: March 12, 2010Date of Patent: August 20, 2013Assignee: Toyama Chemical Co., Ltd.Inventors: Sahoe Kakuda, Setsuko Nishimura, Takafumi Hirota
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Patent number: 8507497Abstract: Provided is a method of treating cystic fibrosis in which an effective amount of a compound represented by formula (I) is administered to a subject in need thereof: where the structural variables are as defined herein.Type: GrantFiled: May 9, 2012Date of Patent: August 13, 2013Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
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Publication number: 20130203774Abstract: The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: AKINION PHARMACEUTICALS ABInventor: AKINION PHARMACEUTICALS AB
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130184293Abstract: The present invention relates to compositions and methods for treating diabetes mellitus, neuropsychological and neurological disorders in a particular group of patient. More specifically, the invention relates to methods of treating diabetes mellitus, neuropsychological and neurological disorders in patients having defective potassium channels. The invention may be used in human subjects, particularly adults or children, and is appropriate to treat various neurological disorders.Type: ApplicationFiled: December 12, 2012Publication date: July 18, 2013Applicants: UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE HOPITAUX DE PARISInventors: ASSISTANCE PUBLIQUE HOPITAUX DE PARIS, UNIVERSITE PARIS DESCARTES
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Publication number: 20130178482Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.Type: ApplicationFiled: June 26, 2012Publication date: July 11, 2013Applicant: Parion Sciences, Inc.Inventor: MICHAEL R. JOHNSON
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Publication number: 20130172367Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: November 27, 2012Publication date: July 4, 2013Applicant: BAYER CROPSCIENCE AGInventor: Bayer CropScience AG
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Patent number: 8476269Abstract: 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: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Patent number: 8461161Abstract: Compunds of the general formula wherein each of Z1-Z4 is N or CR1 wherein only two of said Z1-Z4 may be N are useful as kinase inhibitors.Type: GrantFiled: November 15, 2007Date of Patent: June 11, 2013Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Michael Francis Harte, James T. Palmer