Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles.

The invention is directed to compositions containing physiologically active compounds of general formula (I) wherein R1 is aryl or heteroaryl: R2 represent hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8,-C(=O)-NY3Y4,-CO2R8,-NY3Y4,-N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4,-N(R6)-C(=O)-OR7,-N(R6)-SO2-R7,-N(R6)-SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyno, halo, heteroaryl, lower alkyl,-C(=O)-OR5 or -C(=O)-NY3Y; and X1 represents N.CH. C-halo, C-CN,C-R7,C-NY3Y4,C-OH, C-Z2R7, C-C(=O)-OR5, C-C(=O)-NY3Y4, C-N(R8)-C(=0)-R7,C-SO2-NY3Y4,C-N(R8)-SO2-R7,C-alkenyl or C-NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

Pyrrolopyrimidines as protein kinase inhibitors

This invention is directed to compounds of the formula (I) to N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and to methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.

Benzimidazoles

The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles

The invention is directed to compositions containing physiologically active compounds of general formula (I):- wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z 1 R 8 , -C(=O)-NY 3 Y 4 , -CO 2 R 8 , -NY 3 Y 4 , -N(R 6 )-C(=O)-R 7 , -N(R 6 )-C(=O)-NY 3 Y 4 , -N(R 6 )-C(=O)-OR 7 , -N(R 6 )-SO 2 -R 7 , -N(R 6 )-SO 2 -NY 3 Y 4 and one or more halogen atoms; R 3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR 5 or -C(=O)-NY 3 Y; and X 1 represents CH, C-halo, C-CN, C-R 7 , C-NY 3 Y 4 , C-OH, C-Z 2 R 7 , C-C(=O)-OR 5 , C-C(=O)-NY 3 Y 4 , C-N(R 8 )-C(=O)-R 7 , C-SO 2 -NY 3 Y 4 , C-N(R 8 )-SO 2 -R 7 , C-alkenyl, C-alkynyl or C-NO 2 ; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

Pyrrolopyrimidines

Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.

Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

BENCIMIDAZOLS

LA PRESENTE INVENCION SE REFIERE A BENCIMIDAZOLES DE FORMULA GENERAL (I) EN DONDE R1,A5,W,X,Y,Z, SON GRUPOS FUNCIONALES DESCRITOS EN EL EXPEDIENTE. ESTOS COMPUESTOS INHIBEN A LAS PROTEINAS QUINASAS QUE SON UNA FAMILIA DE ENZIMAS QUE PARTICIPAN EN LOS EVENTOS DE SEÑALIZACION QUE CONTROLAN LA ACTIVACION, EL CRECIMIENTO Y LA DIFERENCIACION DE LAS CELULAS EN RESPUESTA A MEDIADORES EXTRACELULARES Y A CAMBIOS EN EL MEDIO AMBIENTE, POR LO TANTO SON DE UTILIDAD EN CUADROS TUMORALES AL EJERCER UN EFECTO ANTIANGIOGENICO.

BENCIMIDAZOLS

La invención se refiere a compuestos fisiológicamente activos la fórmula general (IX) y composiciones que contienen dichos compuestos, y sus profáRmacos y las sales y los solvatos aceptables para uso farmacéutico de dichos compuestos y sus profármacos, como tambiÉn a nuevos compuestos dentro del alcance de la fórmula (IX), y a procesos para su preparación. Dichos compuestos y composiciones tienen valiosas propiedades farmacéuticas, en particular la capacidad de inhibir las puinasas.

Azaindoles for inhibiting aurora2 and other kinases

The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Benzimidazoles and analogues and their use as protein kinases inhibitors

The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles

THE INVENTION IS DIRECTED TO PHYSIOLOGICALLY ACTIVE COMPOUNDS OF GENERAL FORMULA (I):- AND COMPOSITIONS CONTAINING SUCH COMPOUNDS; AND THEIR PRODRUGS, AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES OF SUCH COMPOUNDS AND THEIR PRODRUGS, AS WELL AS TO NOVEL COMPOUNDS WITHIN THE SCOPE OF FORMULA (I). SUCH COMPOUNDS AND COMPOSITIONS HAVE VALUABLE PHARMACEUTICAL PROPERTIES, IN PARTICULAR THE ABILITY TO INHIBIT KINASES.

Chemical compounds

The present invention concerns compounds of general formula (I): in which: R 1 represents hydrogen, R 4 , —C(═Y)—NHR 4 , —SO 2 NHR 4 , —C(=Z 1 )—R 4 , —SO 2 —R 4 or —C(=Z 1 )—OR 4 ; R 2 represents hydrogen, cyano, halogen or —C≡C—R 5 ; R 3 represents hydrogen, acyl, alkoxycarbonyl, alkyl, aroyl, aryl, aryloxycarbonyl, carboxy, cycloalkenyl, cycloalkyl, heteroaroyl, heteroaryl, heterocycloalkyl or —C(═O)—NY 1 Y 2 ; R 4 represents optionally substituted alkyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl or heteroaryl R 5 represents hydrogen or alkyl; R 6 represents alkyl, acyl, alkoxycarbonyl, alkylsulfonyl, aryl, arylsulfonyl, aroyl, cycloalkyl, cycloalkenyl, heteroaryl, heteroarylsulfonyl, heteroaroyl and heterocycloalkyl; R 7 represents optionally substituted alkyl, cycloalkyl or cycloalkylalkyl, R 8 represents hydrogen, alkyl, alkenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; R 9 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R 10 represents hydrogen or lower alkyl; R 11 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or alkyl optionally substituted by —NY 1 Y 2 ; R 12 represents aryl or heteroaryl; or alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl each optionally substituted Y represents O, S or NCN; Y 1 and Y 2 (Y 3 and Y 4 ) are independently in particular hydrogen, alkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycloalkyl; or the group —NY 1 Y 2 may form 5-7 membered ring or the group —NY 3 Y 4 (—NY 5 Y 6 ) may form a cyclic amine; Z (Z 1 ) represents O or S; Z 2 represents O or S(O) p ; n is zero or an integer 1 or 2; m is 1 or 2; p is 1 or 2; and their corresponding N-oxides, their prodrugs; their pharmaceutically acceptable salts and solvates (e.g. hydrates), also together with one or more pharmaceutically acceptable carriers or ...

Azaindoles

Azainodoler

Azaindoles

Chemical compositions containing physiologically active compounds of general formula (I): wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z 1 R 8 , —C(═O)—NY 3 Y 4 , —CO 2 R 8 , —NY 3 Y 4 , —N(R 6 )—C(═O)—R 7 , —N(R 6 )—C(═O)—NY 3 Y 4 , —N(R 6 )—C(═O)—OR 7 , —N(R 6 )—SO 2 —R 7 , —N(R 6 )—SO 2 —NY 3 Y 4 and one or more halogen atoms; R 3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, —C(═O)—OR 5 or —C(═O)—NY 3 Y; and X 1 represents N, CH, C-halo, C—CN, C—R 7 , C—NY 3 Y 4 , C—OH, C-Z 2 R 7 , C—C(═O)—OR 5 , C—C(═O)—NY 3 Y 4 , C—N(R 8 )—C(═O)—R 7 , C—SO 2 —NY 3 Y 4 , C—N(R 8 )—SO 2 —R 7 , C-alkenyl, C-alkynyl or C—NO 2 ; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

Benzimidazoles

The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Pyrrolopyrimidines as protein kinase inhibitors

Azaindoles

The invention is directed to compositions containing physiologically active compounds of general formula (I) (see formula I) wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8,-C(=O)-NY3Y4,-CO2R8,-NY3Y4,-N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4,-N(R6)-C(=O)-OR7, -N(R6)-SO2-R7,-N(R6)-SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR5 or -C(=O)-NY3Y; and X1 represents N, CH, C-halo, C-CN, C-R7, C-NY3Y4, C-OH, C-Z2R7, C-C(=O)-OR5, C-C(=O)-NY3Y4, C-N(R8)-C(=O)-R7, C-SO2-NY3Y4, C-N(R8)-SO2-R7, C-alkenyl, C-alkynyl or C-NO2; and their produgs, and pharmaceutically acceptable salts and solvates of such compounds and their produgs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

Substituted azaindoles as inhibitors of protein kinases, and process for their preparation

Physiologically active substituted azaindole compounds of general formula (I); compositions containing such compounds; their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs are disclosed, wherein the variables shown in formula (I) are as defined in the specification. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases, whereby these compounds are suitable for use in the treatment of disease states capable of being modulated by the inhibition of the protein kinases.

Azaindoles

The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and the ir prodrugs, as well as to novel compounds within the scope of formula (I). Suc h compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Azaindoles

The invention is directed to compounds of general formula (I):- and pharmaceutically acceptable salts and solvates of such compounds. Such compounds have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

azaindoles

CAZAINDOLES L'invention concerne des compositions contenant des composés actif: physiologiquement de la formule générale (I):- dans laquelle R1 est aryle ou hétéroaryle; R2 représente l'hydrogène, l'acyle, le cyano, l'halo, l'alcényle faible ou l'alkyle faible substitués sur option par un substituant choisi parmi le cyano, l'hétéroaryle, l'hétérocycloalkyle, -Z1R8, -C(=O)-NY3Y4, -CO2R8, -NY3Y4, -N(R6)-C(=O)-R7, -N(R6)-C(=0)-NY3y4 , -N(R6)-C(=O)-OR7, -N(R6)-SO2-R7, -N(R6)-SO2-NY3Y4 et un ou plusieurs atomes d'halogène; R3 représente l'hydrogène, l'aryle, le cyano,l'halo,l'hétéroaryle,l'alkylefaible,-C(=O)-OR5ou -C(=O)-NY3Y; et X1 représente N, CH, C-halo, C-CN, C-R7, C-NY3Y4, C-OH, C-Z2R7, C-C(=O)-OR5, C-C(=0)-NY3Y4, C-N(R8)-C (=0)-R7, C-SO2-NY3Y4, C-N(R8)-SO2-R7, C-alcényle, C-alcynyle ou C-NO2; et leurs prodrogues, les sels pharmaceutiquement acceptables et les solvates de tels composés et leurs prodrogues, ainsi que de nouveaux composés dans la perspective de la formule (I). Ces composés et compositions ont des propriétés pharmaceutiques intéressantes, en particulier la faculté d'inhiber les protéines kinases. CAZAINDOLES The invention relates to compositions containing active compounds: physiologically of the general formula (I): - in which R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, weak alkenyl or weak alkyl optionally substituted by a substituent chosen from cyano, heteroaryl, heterocycloalkyl, -Z1R8, -C (= O) -NY3Y4, -CO2R8, -NY3Y4, -N (R6) -C (= O) -R7, -N (R6) -C (= 0) -NY3y4, -N (R6) -C (= O) -OR7, -N (R6) -SO2-R7, -N (R6) -SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, weak alkyl, -C (= O) -OR5or -C (= O) -NY3Y; and X1 represents N, CH, C-halo, C-CN, C-R7, C-NY3Y4, C-OH, C-Z2R7, CC (= O) -OR5, CC (= 0) -NY3Y4, CN (R8 ) -C (= O) -R7, C-SO2-NY3Y4, CN (R8) -SO2-R7, C-alkenyl, C-alkynyl or C-NO2; and their prodrugs, ...