1605 results about "Quinazoline" patented technology

The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

The present invention relates to quinazoline containing zinc-binding moiety based derivatives 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-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

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.

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have one of the following structures (I), (II) or (III):

or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R¹, R^2a, R^2b, R^2c, R^3a, R^3b, R^4a, R^4b, R^5a, R^5b, R⁶, A, B, G¹, G², L¹, L², m¹, m², n, x, y, X and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

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 relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R₂ is hydrogen, NR′R″, C_1-7 alkyl, arylC_1-7 alkyl or C_3-10 cycloalkyl; R₄ is amino, C_1-7 alkyl, C_2-7 alkenyl, C_3-10 cycloalkyl, C_3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C_1-7 alkyl or C_3-10 cycloalkyl-C_1-7 alkyl; R₅ is hydrogen or C_1-7 alkyl, or R₅ and R₄ together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C_1-7alkylene, C_2-7 alkenylene or C_2-7 alkynylene; R₆ is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C_1-7 alkyl-carbonyl or C_1-7 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.

Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.

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 C_1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)_n, C_1-7 alkylene, C_2-7 alkenylene and C_2-7 alkynylene; R₄ is selected from the group consisting of C_1-7 alkyl, C_2-7 alkenyl, C_3-10cycloalkyl, C_3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C_1-7 alkylene, C_2-7 alkenylene, and C_2-7 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.

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 clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Compounds of Formula I including all geometric and stereoisomers, N-oxides, and agriculturally suitable salts thereof, are disclosed which are useful as invertebrate pest control agents, (I) wherein A, B, J, K, L and R³ are as defined in the disclosure. Also disclosed are compositions for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I an N-oxide thereof or a suitable salt thereof and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, its N-oxide or a suitable salt of the compound (e.g., as a composition described herein).

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R_a, R_b, R_c and R_d 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 discloses a red organic electroluminescent phosphorescent material containing aryl united quinazoline metal iridium complexes and an organic electroluminescent device thereof. The organic electroluminescent device is in a layered doped structure, wherein Zn(BTZ)2 is selected as a substrate material of a luminescent layer, and serial complexes Ir(III) are selected as dopants. The invention provides a basic skeleton structure, i.e. a red organic electroluminescent phosphorescent material containing the aryl united quinazoline metal iridium complexes, modifies the structure with various different groups, is combined with the structural optimization of the organic electroluminescent device using the groups as dopants and realizes red phosphorescence emission with better purity and higher efficiency as comparison with a traditional red light material. The invention has simple manufacture process and provides excellent material for full color display and illumination application.