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Class 514/266.4 - Nitrogen bonded directly to ring carbon of the 1,3-diazine ring of the quinazoline ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a ring carbon of the 1,3-diazine
No. of patents: 235
Last issue date: 05/15/2012


1            
NumberTitleIssue Date
8178546Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase Type 1 enzyme (11β-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atheroscle...
05/15/2012
81686463,4-dihydroquinazoline derivatives
Disclosed are 3,4-dihydroquinazoline derivatives of formula (I), a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and an...
05/01/2012
8093258Use of urokinase inhibitors for the treatment and/or prevention of neuropathological diseases
The present invention relates to methods and compositions for the treatment and/or prevention of neuropathological and/or neurodegenerative diseases. In particular, the invention delivers novel uses of inhibitors of Urokinase-type Plasminogen activator in the treatm...
01/10/2012
8088782Crystalline 4-(3-chloro-2-fluoroanilino)-7 methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate form A
4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and proc...
01/03/2012
8063055Substituted pyridone compounds and methods of use
The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The...
11/22/2011
8048888Anti-proliferative combination therapy using certain platinum-based chemotherapeutic agents and EGFR inhibitors or pyrimidine analogues
The present invention describes a method or uses of prevention and/or treatment of a cancer or a tumor, and in particular to a combination therapy, methods, compositions and pharmaceutical packages comprising an inhibitor of receptors of the EGFR family or a chemoth...
11/01/2011
8044063Quinazoline derivatives useful as anti-tumor medicament
The present invention relates to quinazoline derivatives of the formula (I) useful as anti-tumor medicaments, or a pharmaceutically acceptable salt thereof, the definition of the substituents R1, R1′, R2, R2′ are as de...
10/25/2011
7989463Biccyclic compounds as GATA modulators
Novel bicyclic compounds of the formula (I), stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of...
08/02/2011
79857552,4-diaminoquinazolines for spinal muscular atrophy
2,4-Diaminoquinazolines of formula (I) are provided herein and are useful for treating spinal muscular atrophy (SMA). ...
07/26/2011
7977347Quinazoline based EGFR inhibitors
The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR...
07/12/2011
79476962-amino-4-phenylquinazoline derivatives and the use thereof as HSP90 modulators
Novel phenylquinazoline derivatives of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for ...
05/24/2011
79395404-(3-benzoylaminophenyl)-6,7-dimethoxy-2-methylaminoquinazoline derivatives
A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like: wherein R represents hydroxyl, C1-6 alkoxy optionally subs...
05/10/2011
7932262Quinazolines for PDK1 inhibition
The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions. ...
04/26/2011
7932261Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β...
04/26/2011
79065222-aminoquinazoline derivatives
The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R1 and R2 may be the same or different and each represents a hydrogen atom, su...
03/15/2011
78883662,4-diaminoquinazolines for spinal muscular atrophy
2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA). ...
02/15/2011
7846938Tartrate salts of quinazoline based EGFR inhibitors containing a zinc binding moiety
The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives of Formula II, below. These compounds are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK...
12/07/2010
78206834-(1H-indazol-5-yl-amino)-quinazoline compounds as erbB receptor tyrosine kinase inhibitors for the treatment of cancer
A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by ...
10/26/2010
77907325-Chloro-4-alkyl-3,4-dihydro-quinazolin-2-ylamine derivatives
The present invention relates to compounds of formula I wherein R1, R2, R3 are as described in the specification and pharmaceutically acceptable acid addition salts and tautomers t...
09/07/2010
77907338-alkoxy or cycloalkoxy-4-methyl-3,4-dihydro-quinazolin-2-ylamines
The present invention relates to compounds of formula wherein R1, R2, R3, and n are as described in the specification and pharmaceutically acceptable acid addition salts ...
09/07/2010
7781441(3,4-dihydro-quinazolin-2-yl)-(2-aryloxy-ethyl)-amine
The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharma...
08/24/2010
7754729Quinazoline and quinoline derivatives as irreversible protein tyrosine kinase inhibitors
A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase a...
07/13/2010
7700608Quinazoline derivatives and their use in the treatment of thrombocythemia
A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof. ...
04/20/2010
7625911Amorphous form of erlotinib hydrochloride and its solid amorphous dispersion
The present invention relates to novel amorphous form of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl) (erlotinib hydrochloride), to solid amorphous dispersion of erlotinib hydrochloride and a carrier such as PVP or solid PEG, to processes for their...
12/01/2009
7544691Guanidine derivatives
The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic dru...
06/09/2009
7521456N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate
The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazoli...
04/21/2009
7504409Mucin synthesis inhibitors
The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronc...
03/17/2009
7456189Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation
Compounds of the formula having an inhibitory action on the signal transduction mediated by tyrosine kinases, and being useful for the treatment of oncoses and of benign prostate hyperplasia (BPH), of diseases of the lung a...
11/25/2008
7432275Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
Acid-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor act...
10/07/2008
7429597Substituted nitrogen-containing heterobicycles, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1,...
09/30/2008
7410975Small molecule toll-like receptor (TLR) antagonists
The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are...
08/12/2008
7388014Quinazoline derivatives and therapeutic use thereof
Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperprolifer...
06/17/2008
7368454(3,4-dihydro-quinazolin-2-yl)-aryl-amines
The present invention relates to methods for treating 5-HT5A receptor related diseases which comprises administering compounds of formula I wherein R1, R2,...
05/06/2008
7365096Methods for selectively inhibiting Janus tyrosine kinase 3 (Jak3)
Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a der...
04/29/2008
7358222Preventing airway mucus production by administration of EGF-R antagonists
Hypersecretion of mucus in the lungs is inhibited by the administration of an epidermal growth factor receptor (EGF-R) antagonist. The EGF-R antagonist may be in the form of a small organic molecule, an antibody, or portion of an antibody that binds to and blocks th...
04/15/2008
7348333Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds a...
03/25/2008
7348332(3,4-dihydro-quinazolin-2-yl)-indan-1-yl-amines
The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof.
03/25/2008
73234722,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof. ...
01/29/2008
7317019N-alkylated diaminopropane derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid a...
01/08/2008
7314880Cardioprotective delta opioid receptor agonists and methods of using same
The present invention relates to compositions and methods of treatment for cardioprotection through the use of non-peptidic delta opioid receptor agonist compound(s) that mediate cardioprotective effects of ischemic preconditioning. The compounds are used to reduce ...
01/01/2008
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