Class / Patent application number | Description | Number of patent applications / Date published |
514266240 | The additional hetero ring consists of carbon and chalcogen as the only ring members | 73 |
20080306097 | Cancer Treatment Method - Disclosed herein is a method of treating breast cancer that has metastasized to the brain in a mammal by administration of 4-quinazolinamines and pharmaceutical compositions containing the same. In particular, the method relates to methods of treating breast cancer brain metastases which overexpress erbB2 by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof. | 12-11-2008 |
20090042916 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 02-12-2009 |
20090076043 | DEUTERIUM-ENRICHED ALFUZOSIN - The present application describes deuterium-enriched alfuzosin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076044 | VEGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to VEGFR inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors. | 03-19-2009 |
20090124643 | Use of a Cannabinoid CB1 Receptor Antagonist for Preparation of Drugs Useful for the Prevention and Treatment of Benign Prostatic Hypertrophy - The present invention relates to the use of cannabinoid CB1 receptor antagonist for the preparation of drugs useful for the prevention and treatment of benign prostatic hypertrophy. | 05-14-2009 |
20090156620 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 06-18-2009 |
20090215802 | DEUTERIUM-ENRICHED LAPATINIB - The present application describes deuterium-enriched lapatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 08-27-2009 |
20090281130 | QUINAZOLINE DERIVATIVES - Quinazoline derivatives of the following formula: | 11-12-2009 |
20090281131 | DIEBENZOFURAN DERIVATIVES AS INHIBITORS OF PDE-4 AND PDE-10 - The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-α). | 11-12-2009 |
20090306105 | Bicyclic heterocycles, medicaments containing these compounds, their use and process for preparing them - The present invention relates to bicyclic heterocycles of the general formula (I), their tautomers, their stereoisomers, their mixtures and their salts, in particular physiologically tolerable salts with inorganic or organic acids, which have valuable pharmacological properties, in particular an inhibiting action on the signal transduction transmitted by tyrosinekinases, their use for the treatment of illnesses, in particular tumours and also benign prostatic hyperplasia (BPH), of disorders of the lungs and the bronchia and their preparation. | 12-10-2009 |
20090306106 | FORMS OF CRYSTALLINE LAPATINIB AND PROCESSES FOR PREPARATION THEREOF - The present invention provides new crystalline forms of lapatinib base, Form X and Form Y, and amorphous lapatinib base, pharmaceutical compositions comprising the new crystalline forms of lapatinib base, and/or the amorphous lapatinib base, and processes for their preparation. | 12-10-2009 |
20090312351 | Processes for the Preparation of Alfuzosin - The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline alfuzosin base. The invention also relates to pharmaceutical compositions that include the pure alfuzosin or a pharmaceutically acceptable salt thereof. | 12-17-2009 |
20090318479 | SUBSTITUTED RING FUSED AZINES AND THEIR USE IN CANCER THERAPY - The present invention relates to substituted ring fused azines and methods of using said compounds in treating cancers. More specifically, the present invention relates to the preparation of 4-alkyl-2-(heterocyclic)-azines and their use as cancer agents or drugs for cancer therapy. The compounds of the invention display favourable in vivo and in vitro activity against selected cancers. | 12-24-2009 |
20090318480 | METHOD FOR TREATING CANCER HARBORING EGFR MUTATIONS - The present invention relates to a method of treatment of patients suffering from cancer and harbouring mutations of EGFR in the tumour, for instance an activating mutation of the EGFR or a mutation responsible for resistance or the emergence of acquired resistance to treatment with reversible EGFR and/or HER2 inhibitors or irreversible inhibitors such as CI-1033, EKB-569, HKI-272 or HKI-357, comprising administering an effective amount of the irreversible EGFR inhibitor BIBW2992 (1) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline, to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent, in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery, and to the use of a BIBW 2992 (1) for preparing a pharmaceutical composition for the treatment of patients suffering from cancer and harbouring mutations of EGFR in the tumour. | 12-24-2009 |
20100010022 | CANCER TREATMENT METHOD - A method of treating cancer is described including administration of a pyrimidine derivative and a quinazoline derivative as well as a pharmaceutical composition including the same. | 01-14-2010 |
20100010023 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - A compound of general formula I | 01-14-2010 |
20100063074 | Cancer Treatment Method - The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and pharmaceutical compositions containing the same. In particular, the method relates to a methods of treating cancers which are mediated by the tyrosine kinases EGFR and/or erbB2 by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof. | 03-11-2010 |
20100087459 | FORMS OF LAPATINIB COMPOUNDS AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel crystalline and amorphous lapatinib compounds and processes for preparing them | 04-08-2010 |
20100120804 | Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors - A process for the preparation of a compound of formula (I) | 05-13-2010 |
20100173918 | METHODS AND COMPOSITIONS FOR DETERMINING THE EFFICACY OF BREAST CANCER THERAPEUTICS - The present disclosure relates to a method, kit and controls for detecting phosphorylated Tyr | 07-08-2010 |
20100249160 | Cancer Treatment Method - A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolineamines. | 09-30-2010 |
20110009435 | HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - The present invention relates to compounds of Formula I | 01-13-2011 |
20110009436 | NOVEL THERAPEUTIC USES OF ADRENERGIC ALPHA-1 RECEPTOR ANTAGONISTS - The disclosure relates to methods of using an adrenergic α-1 receptor antagonist or its pharmaceutically acceptable salts for treating and/or preventing interstitial cystitis, overactive bladder or detrusor overactivity. | 01-13-2011 |
20110028499 | PHARMACEUTICAL COMBINATION COMPRISING VITAMIN K - It is found that compounds having PPARδ agonistic activity induced abnormal blood coagulation or muscular disorder. A pharmaceutical combination comprising vitamin K and a compound having PPARδ agonistic activity can prevent the abnormal blood coagulation. A pharmaceutical composition comprising vitamin K can prevent muscular disorder. | 02-03-2011 |
20110046168 | METHODS OF TREATING DISEASES USING QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - A compound of general formula I | 02-24-2011 |
20110053964 | 4-AMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-aminoquinazolines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2. | 03-03-2011 |
20110071169 | Preparation of polymorphic form of lapatinib ditosylate - The present invention is directed to two novel polymorph form (Form A and Form B) of lapatinib ditosylate, wherein Form A is the hydrate ditosylate salt of lapatinib, and Form B is anhydrate ditosylate salt of lapatinib. The present invention is further directed to amorphous form of lapatinib ditosylate and its solid dispersion. The present invention further provides processes for the preparation of Form A, Form B, Amorphous form and solid dispersion of lapatinib ditosyalte, and a pharmaceutical composition comprising the said forms. Form A and Form B were characterized by X-RPD, DSC, TGA and FT-IR, and can be prepared from recrystallizing lapatinib ditosylate in a mixture of tetrahydrofuran (THF) and water. | 03-24-2011 |
20110092524 | Agent for Enhancing Corneal Epithelial Barrier Function - The invention relates to a pharmacological action of a compound which functions as a PPARγ agonist on the barrier function of the corneal epithelium. A PPARγ agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPARγ agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery. | 04-21-2011 |
20110190323 | CORTISTATIN ANALOGUES AND SYNTHESES THEREOF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R | 08-04-2011 |
20110201633 | ALFUZOSIN TABLETS AND SYNTHESIS - A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day. | 08-18-2011 |
20110263621 | NEW COMBINATION OF ACTIVE INGREDIENTS CONTAINING AN a1-ANTAGONIST AND A PDE 4 INHIBITOR - The subject of the present invention is a new combination of active ingredients consisting of alfuzosin and PDE 4 inhibitor, and pharmaceutical compositions containing them, for ameliorating and/or treating benign prostatic hyperplasia, urinary disorders, disorders related to bladder dysfunction, lower urinary tract symptoms associated or not associated with benign prostatic hyperplasia, urinary incontinence, bladder outlet obstruction associated or not associated with benign prostatic hyperplasia, interstitial cystitis and overactive bladder. | 10-27-2011 |
20110301185 | CANCER TREATMENT METHOD - The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound. | 12-08-2011 |
20110312982 | Cancer Treatment Method - A method of treating cancer is described including administration of a 4-quinazolinamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolinamines. | 12-22-2011 |
20120015965 | PHARMACEUTICAL COMPOSITION COMPRISING N-[3-CHLORO-4-[(3-FLUOROPHENYL)METHOXY] PHENYL]-6-[5[[[2-(METHYLSULFONYL) ETHYL]AMINO]METHYL]-2-FURYL]-4- QUINAZOLINAMINE - The present invention relates to a pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine as active pharmaceutical ingredient and a process of preparing such composition. | 01-19-2012 |
20120108615 | SMALL MOLECULE INHIBITORS OF BACTERIAL MOTILITY AND A HIGH THROUGHPUT SCREENING ASSAY FOR THEIR IDENTIFICATION - Certain compounds are provided that can selectively inhibit motile bacteria such as | 05-03-2012 |
20120129876 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 05-24-2012 |
20120208833 | 4-(Substituted Anilino)-Quinazoline Derivatives Useful as Tyrosine Kinase Inhibitors - The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors. | 08-16-2012 |
20120295928 | METHODS FOR DETECTING AND REDUCING IMPURITIES OF LAPATINIB AND SALTS THEREOF - Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: | 11-22-2012 |
20130018062 | Pain therapy with metabolism blocked antifolatesAANM Nair; Madhavan G.AACI MobileAAST ALAACO USAAGP Nair; Madhavan G. Mobile AL US - The perception of pain precedes the manifestation of measurable and quantifiable clinical symptoms of most diseases. Pain is an early warning signal at the beginning of a physical abnormality. The present invention discloses novel methods to ameliorate or reverse diseases at their warning stages by therapeutic intervention of pain before a definite clinical diagnosis of the abnormality can be made. Unprecedented methods to eliminate pain caused by inflammatory autoimmune response or inflammatory allergic response or malignant and benign neoplastic growth by administering metabolism blocked antifolate compounds are described. | 01-17-2013 |
20130035350 | Novel Quinazoline Derivatives - This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds. | 02-07-2013 |
20130072507 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 03-21-2013 |
20130096145 | Use of 1H-quinazoline-2,4-diones - The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of spasticity. | 04-18-2013 |
20130131089 | DOSAGE FORMS OF ELINOGREL AND METHODS OF INJECTABLE ADMINISTRATION THEREOF - The present invention is concerned with a liquid delivery form of Elinogrel for the treatment of thrombosis which is notable for its improved dosage properties and stability. The dosage form is a liquid or a lyophilized form which is reconstituted for an injectable formulation comprising: a) at least about 3 mg/ml or up to about 15 mg/ml Elinogrel or a pharmaceutically acceptable salt thereof (post reconstitution or in liquid form), and b) at least one pharmaceutically acceptable excipient. Further aspects of the present invention concern the preparation and use of such a formulation. | 05-23-2013 |
20130131090 | SALTS OF LAPATINIB - The present invention provides novel dioxalate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel monobesylate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of monohydrate form of lapatinib ditosylate. The present invention further provides a process for the preparation of anhydrous form of lapatinib ditosylate. | 05-23-2013 |
20130165459 | PHARMACEUTICAL COMPOSITION AND DOSAGE FORMS OF ELINOGREL AND METHODS OF USE THEREOF - The present invention is concerned with a solid delivery form of elinogrel for the treatment of thrombosis which is notable for its multi-pH dissolution, immediate release and improved pharmacokinetic properties and stability in storage. The delivery and dosage form is a solid, oral formulation comprising: a) at least about 15% by weight elinogrel or a pharmaceutically acceptable salt thereof relative to the total weight of the overall pharmaceutical composition, and b) at least one pharmaceutically acceptable carrier. A further aspect of the present invention concerns the preparation and use of such a formulation. | 06-27-2013 |
20130172374 | SOLID COMPOSITION FOR CONTROLLED RELEASE OF IONIZABLE ACTIVE AGENTS WITH POOR AQUEOUS SOLUBILITY AT LOW PH AND METHODS OF USE THEREOF - A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37° C.; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL™, POLYOX™ WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration. | 07-04-2013 |
20130178487 | QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF CANCER DISEASES - The present invention relates to the use of quinazolines of formula (I), | 07-11-2013 |
20130252979 | PHARMACEUTICAL COMPOSITIONS, DOSAGE FORMS AND NEW FORMS OF THE COMPOUND OF MULA (I), AND METHODS OF USE THEREOF - The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y | 09-26-2013 |
20130289056 | METHODS OF ADMINISTERING AN EGFR INHIBITOR - Disclosed are methods of treating a patient having cancer with an EGFR inhibitor requiring an active step of avoiding or modifying the co-administration of such drugs with P-gp modulators. This invention also relates to a medicament for treating a patient having cancer, comprising an EGFR inhibitor as the active product ingredient, customized for avoiding co-administration with P-gp inducers and/or inhibitors by an instruction added to the medicament or the package containing said medicament. | 10-31-2013 |
20130289057 | N-ARYLAMINOMETHYLENE BENZOTHIOPHENONES FOR TREATMENT OF CARDIOVASCULAR DISEASE - The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: | 10-31-2013 |
20130296350 | Method of Treatment or Prophylaxis - The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT | 11-07-2013 |
20130331405 | PIK3CA Mutation Status and SASH1 Expression Predicts Synergy Between Lapatinib and an AKT Inhibitor in HER2 Positive Breast Cancer - Methods for identifying a cancer patient, such as a breast cancer patient, suitable for treatment with a 4-anilinoquinazoline kinase inhibitor, such as lapatinib, and an AKT inhibitor, comprising detecting modulated expression of HER2 (ERBB2) and SASH1 or protein encoded thereof and detecting PIK3CA mutation status. High levels of expression in HER2 and high levels of SASH1 and/or positive PIK3CA mutation status indicate a patient that is suitable for treatment with a 4-anilinoquinazoline kinase inhibitor, such as lapatinib and an AKT inhibitor. | 12-12-2013 |
20140011822 | METHODS AND MATERIALS FOR REDUCING VENOUS STENOSIS FORMATION OF AN ARTERIOVENOUS FISTULA OR GRAFT - This document provides methods and materials for reducing venous stenosis formation of an arteriovenous fistula or graft. For example, methods and materials for using VEGF inhibitors to reduce venous stenosis formation of arteriovenous fistulas or grafts are provided. | 01-09-2014 |
20140051713 | NOVEL SALTS AND POLYMORPHIC FORMS OF AFATINIB - Afatinib salts and crystalline forms thereof are described in the present application and processes for their preparation. Crystalline forms of Afatinib are also described in the present application and processes for their preparation. The present invention also includes pharmaceutical compositions of such Afatinib salts and crystalline forms thereof or crystalline forms of Afatinib, methods of their preparation and the use thereof in the treatment of a patient in need thereof. | 02-20-2014 |
20140066466 | Necroptosis Inhibitors and Methods of Use Therefor - Described herein are compositions that inhibit the production of TNFα downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNFα production or CD40 activation. | 03-06-2014 |
20140128417 | ALKYNE SUBSTITUTED QUINAZOLINE COMPOUND AND METHODS OF USE - The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer). | 05-08-2014 |
20140221405 | PLATELET ADP RECEPTOR INHIBITORS - Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof. | 08-07-2014 |
20140221406 | QUINAZOLINE-7-ETHER COMPOUNDS AND METHODS OF USE - The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination. | 08-07-2014 |
20140256753 | QUINAZOLINONE ANALOGS AND USE OF QUINAZOLINONE ANALOGS FOR TREATING OR PREVENTING CERTAIN VIRAL INFECTIONS - Provided is a process for treating or preventing a viral infection in a subject, wherein the viral infection is from a flavivirus selected from the group consisting of Hepatitis C Virus (genotypes 1-7) and Japanese Encephalitis Virus. The process includes administering to the subject a therapeutically effective amount of at least one compound represented by the formula: (Formula (I)) | 09-11-2014 |
20150065527 | BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - A pharmaceutical formulation comprising the compound of formula | 03-05-2015 |
20150073002 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 03-12-2015 |
20150119411 | INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS - Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus. | 04-30-2015 |
20150126539 | SUBSTITUTED AMINOQUINAZOLINES USEFUL AS KINASES INHIBITORS - The present invention is directed to novel quinazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions. | 05-07-2015 |
20150291568 | NEW COMPOUNDS HAVING A PROTECTIVE ACTIVITY AGAINST TOXINS WITH INTRACELLULAR ACTIVITY - The present invention concerns a new family of 2,3-dihydroquinazolin-4(1H)-one compounds of general formula (I), and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as ricin or Shiga toxin, for example, using retrograde transport to intoxicate cells. | 10-15-2015 |
20150366868 | CANCER TREATMENT METHOD - A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolineamines. | 12-24-2015 |
20160031860 | ALKYNE SUBSTITUTED QUINAZOLINE COMPOUND AND METHODS OF USE - The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer). | 02-04-2016 |
20160038490 | COMPOSITIONS AND METHODS FOR TREATING DYSPROLIFERATIVE DISEASES - Methods are provided for treating cancer and other dysproliferative diseases by administering to a subject in need there of a therapeutically effective amount of a synergistic composition comprising an HER2 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; and a CYP26 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; wherein said therapeutically effective amount suppresses the growth of dysproliferative cells in vivo. Compositions comprising a combination of an HER2 inhibitor, or a pharmaceutically acceptable salt or prodrug thereof; and a CYP26 inhibitor a pharmaceutically acceptable salt or prodrug thereof are also described. | 02-11-2016 |
20160051551 | BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - A pharmaceutical formulation comprising the compound of formula | 02-25-2016 |
20160096826 | CO-CRYSTALS OF LAPATINIB MONOACID SALTS - The present invention refers to co-crystals of monoacid salts of the pharmaceutical active ingredient named Lapatinib and to processes for the preparation thereof and medical uses. | 04-07-2016 |
20160122329 | CRYSTALLINE FORMS OF AFATINIB DI-MALEATE - The present disclosure encompasses crystalline forms of Afatininb di-maleate and methods of their use. | 05-05-2016 |
20160175308 | THERAPEUTIC AGENTS FOR MODULATING THYMIC FUNCTION AND/OR GROWTH AND/OR TREATING VARIOUS DISORDERS | 06-23-2016 |
20180021340 | METHODS AND COMPOSITIONS FOR THE TREATMENT OR PREVENTION OF ABNORMAL BONE FORMATION IN A SOFT TISSUE | 01-25-2018 |
20190144434 | HALOGENATED QUINAZOLIN-THF-AMINES AS PDE1 INHIBITORS | 05-16-2019 |