Entries |
Document | Title | Date |
20080221137 | Quinazolines useful as modulators of voltage gated ion channels - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-11-2008 |
20080293749 | Pyrrolidine(thi)ones Substituted by Heterocyclic Substituents in The 3-Position - Pyrrolidine(thi)one compounds substituted by heterocyclic substituents in the 3-position, their preparation and use in pharmaceutical compositions, in particular as immunomodulators for treatment and/or inhibition of inflammatory and autoimmune diseases and haematological-oncological diseases. | 11-27-2008 |
20080318984 | Compounds Having Activity in Correcting Mutant-Cftr Processing and Uses Thereof - The invention provides compositions, pharmaceutical preparations and methods for correcting cellular processing (e.g., folding, trafficking, or post-translational modification) of a mutant-cystic fibrosis transmembrane conductance regulator protein (e.g., ΔF508 CFTR) that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more aminobenzothiazole-containing compounds, aminoarylthiazole-containing compounds, quinazolinylaminopyrimidinone-containing compounds, bisaminomethylbithiazole-containing compounds, or phenylaminoquino-line-containing compounds of the invention, or an analog or derivative thereof. | 12-25-2008 |
20090023758 | Macrocyclic Inhibitors of Hepatitis C Virus - Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR | 01-22-2009 |
20090118312 | Macrocylic Inhibitors of Hepatitis C Virus - Compounds of the formula I: | 05-07-2009 |
20090124641 | Mitotic Kinesin Inhibitors - The present invention relates to fluorinated 2-aminomethylquinazolinone derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 05-14-2009 |
20090131461 | Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity - Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y | 05-21-2009 |
20090143414 | Quinazoline Derivatives Having Tyrosine Kinase Inhibitory Activity - A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided. | 06-04-2009 |
20090312350 | Compositions comprising balaglitazone and further antidiabetic compounds - Methods for treating conditions benefiting from a decrease in insulin resistance, a reduction of plasma glucose levels, a reduction of plasma fatty acid levels, a reduction of plasma triglyceride levels or reduction of VLDL levels comprising the administration of a composition consisting essentially of balaglitazone in combination with one or more dipeptidyl peptidase-IV inhibitors to a patient in need thereof. | 12-17-2009 |
20100022565 | PHARMACEUTICAL COMPOSITIONS - Provided is a pharmaceutical composition comprising a calcilytic agent which, when administered orally to a subject induces a rapid and short-lasting absorption of the calcilytic agent and/or a rapid and short-lasting release of the parathyroid hormone. | 01-28-2010 |
20100029694 | Heterocyclic compounds and their use as aldosterone synthase inhibitors - Heterocyclic compounds of the general formula (I) | 02-04-2010 |
20100075997 | USE OF PKC INHIBITORS IN TRANSPLANTATION - The present invention pertains to the use of a PKC inhibitor in the treatment of insulin-producing cell and tissue rejection, such as islet transplantation rejection or rejection of transdifferentiated insulin-producing hepatocytes. | 03-25-2010 |
20100113488 | MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention relates generally to novel macrocycles of Formula (I): | 05-06-2010 |
20100113489 | MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS - The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin- 4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: | 05-06-2010 |
20100130519 | COMBINATION THERAPY COMPRISING AZD2171 AND AZD6244 OR MEK-INHIBITOR II - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with AZD6244 or MEK Inhibitor II; to a pharmaceutical composition comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to a combination product comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to the use of AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 05-27-2010 |
20100173917 | UREA DERIVATIVES AS ABL MODULATORS - The invention provides methods and compositions for treating conditions mediated by Bcr-Abl. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects. | 07-08-2010 |
20100179175 | USE OF PKC INHIBITORS IN OCULAR DISEASES - The present invention pertains to the use of a PKC inhibitor in the treatment of an ocular disorder. | 07-15-2010 |
20100210670 | METHODS AND COMPOSTIONS UTILIZIING QUINAZOLINONES - Quinazolinones of formulae (a, b, c and d) are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity. | 08-19-2010 |
20100298357 | MALEATE SALTS OF A QUINAZOLINE DERIVATIVE USEFUL AS AN ANTIANGIOGENIC AGENT - The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability. | 11-25-2010 |
20110207756 | ANTITUMOR AGENT FOR THYROID CANCER - The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. | 08-25-2011 |
20110230505 | QUINAZOLINE INHIBITORS OF BACE 1 AND METHODS OF USING - Dihydroquinazoline compounds, compositions containing them, the use of the compounds and compositions for the treatment of Alzheimer's disease are described. | 09-22-2011 |
20110269783 | NOVEL 2,3-DIAMINO-QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE - The present invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the derivatives for the manufacture of a medicament, to pharmaceutical compositions comprising the derivatives, and to methods of treating a disorder, disease or a condition responsive to activation of Kv7 channels. | 11-03-2011 |
20120165351 | QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I | 06-28-2012 |
20130102622 | Novel Quinazoline-2,4-Dione Derivative, and Medical Compositions for the Prophylaxis and Treatment of Cranial Nerve Disease Containing the Same - The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease. | 04-25-2013 |
20130217711 | Use of a Receptor-Type Kinase Modulator for Treating Polycystic Kidney Disease - The invention comprises use of a therapeutically effective amount of the compound of the formula below for preparation of a medicament for treating polycystic kidney diseases (PKD) in a mammal, such as human or feline (e.g., Persian cat).Formula (I). Also provided are the above compound and compositions comprising it for treating PKD. | 08-22-2013 |
20130225611 | Compositions and Methods for Reducing Cancer Cell Proliferation and Modulating Importin-Beta Function - The present disclosure provides methods of reducing proliferation of cancer cells. The methods include contacting the cancer cells with a 2,4-diaminoquinazoline compound. Also provided are methods of modulating importin-beta function (e.g., importin-beta-mediated nuclear import) in eukaryotic cells. The methods include contacting the eukaryotic cells with a 2,4-diaminoquinazoline compound. Pharmaceutical formulations that include a 2,4-diaminoquinazoline compound are also provided. | 08-29-2013 |
20130225612 | QUINAZOLINE DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO - The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase. | 08-29-2013 |
20130267542 | HISTONE DEACETYLASES (HDACS) INHIBITORS - Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed. | 10-10-2013 |
20130296348 | Bis-Quinazoline Derivatives as Inhibitors for Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase - Novel bis-quinazoline derivatives as tyrosine kinase inhibitors, synthesis of these compounds, and novel methods for treating tyrosine kinase mediated diseases or disorders using these compounds are disclosed. In particular, the present invention provides tethered quinazoline derivative dimers as inhibitors to the epidermal growth factor receptor (EGFR) tyrosine kinase, pharmaceutical compositions thereof, and their therapeutic uses for treating EGFR kinase-mediated diseases or disorders, such as various cancers, as well as synthetic methods for preparing these novel compounds. | 11-07-2013 |
20140045868 | RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. | 02-13-2014 |
20140155418 | Receptor-Type Kinase Modulators and Methods of Use - The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR. | 06-05-2014 |
20140221402 | QUINAZOLINE DERIVATIVE AND APPLICATION THEREOF - This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, | 08-07-2014 |
20150025091 | Maleate Salts of a Quinazoline Derivative Useful as an Antiangiogenic Agent - The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability. | 01-22-2015 |
20150376171 | SOLID STATE FORMS OF A QUINAZOLINE DERIVATIVE AND ITS USE AS A BRAF INHIBITOR - This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions. | 12-31-2015 |
20160016915 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), | 01-21-2016 |
20160199375 | RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF | 07-14-2016 |