486 results about "Quinazoline derivatives" patented technology

The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula Iwherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q3 is CR2, X1 is N or CRc, Y is CRc, X2 and X3 are each C(R5)(R6), R7 is O. Compounds of Formula I are useful in the treatment of diseases and / or conditions related to cell proliferation, such as cancer The current invention is also directed toward pharmaceutical compositions comprising compounds of the invention.

An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; Q represents NR10, CR11R2, carbonyl, O, S(═O)m, wherein m is 0 to 2, or urea; R1 to R3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R4 represents H; R5 to R8 each independently represent H, halogen, alkyl, or alkoxy; and R9 represents an optionally substituted carbocyclic or heterocyclic group.

The present invention provides an amido quinazoline derivative which has recipient singal conductance for inhibition of epidermal growth factors with anti-tumor activity. The novel compounds with a structure identical to quinazoline has quite high activity for inhibition of tumor cells, in particular to the remarkable inhibition effects on the growth of tumor cells of EGFR high expression. And the effective inhibition concentration is 5 times higher than the medicine IRESSA on the market.

The present invention provides composition and methods of inhibiting quinone reductase 2 (QR2). The methods are useful in the treatment of malaria and autoimmune diseases. The compositions of the invention comprise quinoline and quinazoline derivatives. The invention also provides methods for inhibiting the activity of QR2 by contacting the enzyme with one or more compositions of the invention.

An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:wherein X represents CH or N; Z represents O or S; Q represents NR10, CR11R2, carbonyl, O, S(═O)m, wherein m is 0 to 2, or urea; R1 to R3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R4 represents H; R5 to R8 each independently represent H, halogen, alkyl, or alkoxy; and R9 represents an optionally substituted carbocyclic or heterocyclic group.

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR′R″ and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-Λ / -oxide, a solvate or a pro-drug thereof.

The present invention relates to methods and compositions for the inhibition of adaptor protein / protein tyrosine kinase protein interactions, especially wherein those interactions involving a protein tyrosine kinase capable of complexing with a member of the SH2-and / or SH3-containing family of adaptor proteins are associated with a cell proliferative disorder. Specifically, the present invention relates to particular compounds, especially quinazoline derivative compounds, and methods utilizing such compounds.

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

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, HERl 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.

The invention relates to a 4-aromatic aminoquinazoline compounds with general formula of (I) or a receivable salt pharmaceutically and the application in preparing the drugs for treating the tumour. Wherein, R1, R2 are hydrogen, halogen, nitryl, amino, alkyl of C1-6, alkylamino of C1-6 or alkoxy of C1-6, or the group replaced by the alkylamino on the terminal of the alkyl of C1-6, alkylamino and alkoxy; X is N,O or S; Ar is aromatic ring or heteroaromatic groups replaced by the ester of C5 to C8. The invention can inhibit the increase of the tumour cell obviously and has obvious inhibited effect on the tyrosine kinase of the cell, and has activity equal to that of the positive drugs Gefitinib and Erlotinib and even exceeds the positive control.

The invention relates to quinazoline derivatives having a general formula (I), and mixture of their optically active body or racemic body, and diastereoisomer, their pharmaceutically acceptable salts, hydrate or solvate, wherein R1, R2, A, X and Q1 are defined in the specification. The derivatives can be used for preparing protein tyrosine coyness inhibitor, and for preparing medicament for treating and / or preventing cancer and other hyperplasia diseases.

An image pickup device comprises an organic photoelectric conversion film sandwiched between at least two electrodes, wherein the organic photoelectric conversion file comprises a specific quinacridone derivative or a specific quinazoline derivative.

Methods for preparing compounds having the following structure (I):or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b and R4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

The invention belongs to the technical field of medicine and specifically relates to an aniline substituted quinazoline derivative with a general formula (I), pharmaceutically acceptable salt thereof or stereo isomer thereof. R1, R2, R3, R4, R5, R6, L and n are defined in the instruction. The invention also relates to a preparation method of the compounds, medicinal preparations containing the compounds and purpose of the compounds in preparation of medicaments for treating tumour.

Methods for preparing compounds having the following structure (I):or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b and R4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.

The present invention relates to a novel imidazoquinazoline derivative, a process for preparing the same, and an organic electronic device using the same. The imidazoquinazoline derivative according to the present invention serves as hole injecting, hole transporting, electron injecting, electron transporting, or a light emitting material in an organic electronic device including an organic light emitting device, and the device according to the present invention exhibits excellent characteristics in efficiency, operating voltage, and stability.

The invention discloses a pentadienone-containing 4-substituted quinazoline derivative. A structure of the pentadienone-containing 4-substituted quinazoline derivative is represented as the following general formula (I), wherein a group shown in the specification is at a position 2 or a position 3 or a position 4 of a benzene ring; R1 is hydrogen, monosubstituted halogen atom or polysubstituted halogen atom, monosubstituted methyl or polysubstituted methyl, or polysubstituted methoxy; R2 is ortho, meta, para monosubstituted or polysubstituted nitrophenyl, ortho, meta, para monosubstituted or polysubstituted halogen atom phenyl, ortho, meta, para monosubstituted or polysubstituted methoxyphenyl, 2-chlorine-5-nitrophenyl, 4-chlorine-3-nitrophenyl, ortho, meta, para monosubstituted trifluoromethylphenyl, five-membered heterocyclic aryl or substituted five-membered heterocyclic aryl, or ortho, meta, para monosubstituted or polysubstituted hydroxyphenyl. The invention further discloses a preparation method for the pentadienone-containing 4-substituted quinazoline derivative and a use of the pentadienone-containing 4-substituted quinazoline derivative in preparing anti-cancer drugs.

The invention discloses a 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative and a preparation method thereof. The structural formula of the product is shown in a formula (i), wherein Ar represents aryl, substituted aryl, heterocyclic aryl or substituted heterocyclic aryl. The preparation method of the 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative comprises the following steps of: reacting aromatic formaldehyde or heterocyclic aromatic formaldehyde with ortho-amino toluamide at high temperature to obtain a 2-aryl quinazoline-4(3H)-ketone derivative or a 2-heterocyclic aryl quinazoline-4(3H)-ketone derivative; subsequently reducing the 2-aryl quinazoline-4(3H)-ketone derivative or the 2-heterocyclic aryl quinazoline-4(3H)-ketone derivative into a 2-aryl-3,4-dihydro quinazoline derivative or a 2-heterocyclic aryl-3,4-dihydro quinazoline derivative by using an appropriate reducing agent; and finally synthesizing the 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative by using an oxidizing agent in an oxidation mode. Compared with the conventional synthesis method, the preparation method has the advantages of easy and available raw material, simple synthesis method, temperate reaction condition, high yield and the like, is easy to purify, and is a synthesis method applicable to industrial production.

The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline 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-site cleaving enzyme and BACE.

The invention discloses a quinazoline derivative and a pharmaceutically acceptable salt thereof showed in a formula I, or their enantiomer, diastereoisomer, tautomer, racemate, solvate, metabolic precursor or prodrug. The invention also discloses a preparation method, an intermediate, a composition and an application. The quinazoline derivative has good antineoplastic activity.

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 following general formula (1): wherein R1 represents a hydrogen atom or alkyl; the ring Q represents a cyclohexylene group or a phenylene group; A1 and A2 represent a single bond or an alkylene group; E represents —NHCO—; A3 represents a single bond or a divalent saturated or unsaturated aliphatic hydrocarbon group; R3 represents a non-cyclic aliphatic hydrocarbon group; and R4 and R5 are the same or different and each represents a hydrogen atom or alkyl, or a pharmaceutically acceptable salt thereof as an active ingredient.

This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and / or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells and a pharmaceutical composition comprising same as an active ingredient.

The present invention provides a quinazoline compound shown in formula (I), or pharmaceutically acceptable salt thereof. R1, R2 and R7 are independently and respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halogenate C1-6 alkyl, halogenate C1-6 alkoxy, hydroxyl C1-6 alkyl, hydroxyl C1-6 alkoxy, C1-6 alkoxy C1-6 alkoxy, C3-8 cycloalkyloxy, optional aryl or heteroaryl substituted by R6, nitryl, amino, C1-6 alkylamino, and di(C1-6 alkyl)amino; it comprises at least one C3-8 heterocycloalkyloxy selected from N, O, S heteroatoms; Z is -NR4-, C(R5)2, S or -O-, R4 being hydrogen or C1-3 alkyl, and R5 being selected from hydrogen or C1-3 alkyl; R3 is selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or halogenate C1-6 alkyl; R6 is selected from hydrogen, C1-3 alkyl, hydroxyl, halogen, C1-3 alkoxy; and n is 0 to 5. The present invention further provides a preparation method of the compound shown in formula (I) or the pharmaceutically acceptable salt and pharmaceutical usage thereof, which can be used as medicines or lead compounds for curing diseases such as tumour and cancer related to protein tyrosine kinase.

Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.

The present invention relates to quinazoline derivatives of formula I:wherein X, Y, Z, R1, R2, R3, and R4 are as defined herein. The invention also relates to a method of preparing these compounds, and use of these compounds for inhibiting tumor growth.

The invention discloses a phosphorescence iridium complex by taking a quinazoline derivative as a ligand and an organic electroluminescent device thereof. The structure of the phosphorescence iridium complex disclosed by the invention is represented by the formula (I) or the formula (II) described in the specification, wherein Ar represents aryl, substituted aryl, heterocyclic aryl and substituted heterocyclic aryl; R can be one of a halogen atom, alkyl, substituted alkyl, alkoxy, aryloxy, alkyl sulphanyl, aryl sulphanyl, aromatic amino, fatty amino and heterocyclic substituent; L^Y can be one of N^COOH, N^OH, beta-diketone, N^NH and the like; N^N can be bipyridyl, biquinolyl, phenanthroline and derivatives thereof and the like; and Z can be a hexafluorophosphoric acid radical, a perchloric acid radical and the like. A light-emitting layer of the electroluminescent device disclosed by the invention is prepared by adopting a spin coating and film-preparing method under a specified condition, has the advantages of being low in cost, simple for operation and steady in chemical property, and is beneficial to preparing large-screen electroluminescent devices.