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8178544 |
2, 3-diamino-quinazolinone derivatives and their medical use
This invention provides 2,3-diamino-quinazolinone compounds of Formula (I) stereoisomers thereof, pharmaceutically-acceptable addition salts thereof, and N-oxides thereof, wherein the variables are...
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8178546 |
Diaryltriazoles 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 t...
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8168646 |
3,4-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...
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8142782 |
EGFR inhibitors promote axon regeneration
Compositions and methods for promoting neural regeneration in a patient determined to have a lesion in a mature CNS neuron are disclosed. The method comprises the step of contacting the neuron with...
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8093258 |
Use 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...
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8088782 |
Crystalline 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-methylcarbam
oylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in...
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8088766 |
Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors
Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases...
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8063055 |
Substituted 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,...
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8053434 |
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
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8048888 |
Anti-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...
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8044063 |
Quinazoline 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,...
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8003658 |
Quinazoline derivatives for inhibiting cancer cell growth and method for the preparation thereof
The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells, a method for the preparation thereof and a...
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7998949 |
Bicyclic heterocycles, drugs containing said compounds, use thereof, and method for production thereof
The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in...
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7989463 |
Biccyclic 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...
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7989462 |
4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of...
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7985755 |
2,4-diaminoquinazolines for spinal muscular atrophy
2,4-Diaminoquinazolines of formula (I) are provided herein and are useful for treating spinal muscular atrophy (SMA).
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7977347 |
Quinazoline 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...
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7959901 |
EGFR inhibitors promote axon regeneration
Compositions and methods for promoting neural regeneration in a patient determined to have a lesion in a mature CNS neuron are disclosed. The method comprises the step of contacting the neuron with...
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7947696 |
2-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...
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7939540 |
4-(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...
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7932262 |
Quinazolines 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...
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7932261 |
Macrocycle 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...
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7906522 |
2-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, substituted or...
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7888366 |
2,4-diaminoquinazolines for spinal muscular atrophy
2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).
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7863283 |
Sulphoximine-substituted quinazoline derivatives as immuno-modulators, their preparation and use as medicaments
The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various...
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7863333 |
N-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,...
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RE41998 |
Compositions and methods of treatment of sympathetically maintained pain
Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other d...
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7846938 |
Tartrate 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...
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7829566 |
4-amino-quinazolines
Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
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7820683 |
4-(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...
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7790732 |
5-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 thereof. Compounds...
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7790733 |
8-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 thereof. The compounds of...
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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 pharmaceutically acceptable acid addition salts and...
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7772232 |
Quinazolinyl compounds as inhibitors of potassium channel function
A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the...
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7754729 |
Quinazoline 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...
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7718663 |
Quinazoline derivatives and medicaments
An object of the present invention is to provide an antipruritic agent having a novel action mechanism. The present invention provides an antipruritic agent comprising a compound represented by the...
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7709479 |
Quinazoline derivatives and their use as pharmaceuticals
The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group...
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7700608 |
Quinazoline 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...
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7691866 |
2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines and methods of their use as inhibitors of Raf kinase
New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new...
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7625911 |
Amorphous 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-pheny
l) (erlotinib hydrochloride), to solid amorphous dispersion of erlotinib...
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7618975 |
4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of...
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7601713 |
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
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7576074 |
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...
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7572798 |
Combi-molecules having signal transduction inhibitory properties and DNA damaging properties
The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as...
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7547702 |
4-amino-quinazolines
Quinazolines of the formula (I) in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein 1bIX antagonists.
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7544691 |
Guanidine 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...
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7521456 |
N-(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-quinazolinami
ne mesylate. The invention also relates to pharmaceutical...
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7504409 |
Mucin 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...
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7498335 |
Method of producing an antiangiogenic or vascular permeability reducing effect
The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or...
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7465738 |
Compounds useful as promoters of SMN2
The present invention relates to compounds useful as promoters of the SMN2 gene. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using...
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