Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

NOVEL COMPOUNDS THAT ARE ERK INHIBITORS

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).

Benzamide imidazopyrazine Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

NOVEL COMPOUNDS THAT ARE ERK INHIBITORS

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).

BTK Inhibitors

Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

BTK inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

Heterocyclic compounds as ERK inhibitors

The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

NOVEL HETEROCYCLIC COMPOUNDS AS ERK INHBITORS

The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. 2. The compound of claim 1 , wherein R is H.4. The compound of wherein Ris selected from the group consisting of: phenyl claim 1 , pyridyl claim 1 , methylpyridyl claim 1 , methylindazolyl claim 1 , methylbenzothiazolyl claim 1 , pyridazinyl claim 1 , dihydropyran claim 1 , dioxidodihydrothiopyran claim 1 , dioxidotetrahydrothiopyran claim 1 , imidazolyl claim 1 , teterahydropyran claim 1 , benzofuranyl claim 1 , indazolyl claim 1 , pyridazinyl claim 1 , indazolyl claim 1 , imidazopyridly claim 1 , benzooxazolyl claim 1 , benzothiadiazolyl claim 1 , benzooxadiazolyl claim 1 , benzothiazolyl claim 1 , pyridine-one claim 1 , triazolopyridinyl claim 1 , dihydrobenzoimidazolyl claim 1 , benzohydrofuranyl; and wherein said Ris optionally substituted with 1 or more substitutents independently selected from the group consisting of: ═O claim 1 , —OH claim 1 , alkyl claim 1 , cycloalkyl claim 1 , haloalkyl claim 1 , alkoxy claim 1 , halo claim 1 , —NH—C(═O)-alkyl claim 1 , —S(═O)—N(alkyl)—C(═O)-alkyl claim 1 , cyano claim 1 , —S(═O)-alkyl claim 1 , —NH claim 1 , and —OC(═O)alkyl.5. The compound of claim 1 , wherein said Ris alkyl claim 1 , which is unsubstituted or substituted with at least one aryl.7. The compound of claim 6 , wherein:(a) n is 1; or(b) n is 1 and m is 0, 1 or 2; or{'sup': 3', '3', '3, 'sub': 3', '3, '(c) n is 1, m is 1 or 2, and Ris selected from the group consisting of halo, haloalkyl, —OSi(alkyl), hydroxyl, alkyl, cycloalkyl, alkoxy, aryl, —C(═O)OH, —C(═O)—O-alkyl, —C(═O)N(alkyl), —C(═O)NH-alkyl; or wherein two Rgroups together with the carbon atom to which both Rgroups are attached form —C(═O ...

Novel compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

BTK INHIBITORS

Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders. 1. (canceled)2. (canceled)3. The compound of claim 38 , wherein ring K is defined as: Bis C(R) claim 38 , Bis C(R) claim 38 , Bis C(R) claim 38 , and Bis C(R); and R claim 38 , R claim 38 , Rand Reach are H or halogen.4. (canceled)5. The compound of claim 38 , wherein ring L is selected from the group consisting of pyridyl claim 38 , pyrimidyl claim 38 , and thiazolyl.6. The compound of claim 38 , wherein Ris selected from the group consisting of hydrogen claim 38 , fluorine claim 38 , chlorine claim 38 , CN claim 38 , cyclopropyl claim 38 , (1-3C)alkyl and (1-2C) alkoxy; the (1-3C)alkyl group of which is optionally substituted with one or more halogen.7. The compound of claim 6 , wherein Ris selected from the group consisting of hydrogen claim 6 , fluorine claim 6 , methyl claim 6 , ethyl claim 6 , propyl claim 6 , cyclopropyl claim 6 , methoxy and trifluoromethyl.8. The compound of claim 38 , wherein Ris selected from the group consisting of: RC(O) claim 38 , RNHC(O) claim 38 , RC(O)NH claim 38 , RSO claim 38 , (3-7C)cycloalkyl(1-4C)alkyl claim 38 , (6-10C)aryl(1-4C)alkyl claim 38 , (1-6C)alkyl claim 38 , (1-5C)heteroaryl(1-4C)alkyl claim 38 , halo(1-6C)alkyl claim 38 , hydroxyl(1-6Calkyl claim 38 , (1-4C)alkoxy(1-6C)alkyl claim 38 , (1-4C)alkoxy(1-6C)alkyl and (1-6C)alkoxyl.9. The compound of claim 8 , wherein Ris selected from the group consisting of: RC(O) claim 8 , RNHC(O) claim 8 , RC(O)NH claim 8 , (6-10C)aryl(1-4C)alkyl claim 8 , (1-5C)heteroaryl(1-4C)alkyl claim 8 , halo(1-6C)alkyl claim 8 , hydroxyl(1-6Calkyl claim 8 , (1-4C)alkoxy(1-6C)alkyl claim 8 , (1-4C)alkoxy(1-6C)alkyl and (1-6C)alkoxyl.10. The ...

BTK INHIBITORS

Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders. 2. The compound of claim 1 , wherein ring K is defined as:{'sub': 1', '2', '3', '4, 'sup': 7', '8', '9', '10, 'Bis C(R), Bis C(R), Bis C(R), and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 9', '10, 'Bis N, Bis N, Bis C(R), and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 8', '10, 'Bis N, Bis C(R), Bis N, and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 8', '9, 'Bis N, Bis C(R), Bis C(R), and Bis N; or'}{'sub': 1', '2', '3', '4, 'sup': 7', '8, 'Bis C(R), Bis C(R), Bis N, and Bis N; or'}{'sub': 1', '2', '3', '4, 'sup': 7', '9, 'Bis C(R), Bis N, Bis C(R), and Bis N.'}3. The compound of claim 2 , wherein ring K is defined as: Bis C(R) claim 2 , Bis C(R) claim 2 , Bis C(R) claim 2 , and Bis C(R); and R claim 2 , R claim 2 , Rand Reach are H or halogen.4. The compound of claim 1 , wherein ring L is selected from the group consisting of pyridyl claim 1 , pyrimidyl claim 1 , pyridazyl claim 1 , triazinyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , pyrazolyl claim 1 , thiadiazolyl claim 1 , and isothiazolyl.5. The compound of claim 4 , wherein ring L is selected from the group consisting of pyridyl claim 4 , pyrimidyl claim 4 , and thiazolyl.6. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , CN claim 1 , cyclopropyl claim 1 , (1-3C)alkyl and (1-2C) alkoxy; the (1-3C)alkyl group of which is optionally substituted with one or more halogen.7. The compound of claim 6 , wherein Ris selected from the group consisting of hydrogen claim 6 , fluorine claim 6 , methyl claim 6 , ethyl claim 6 , propyl claim 6 , ...

BTK INHIBITORS

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders. 4. The compound of selected from the group consisting of:4-(8-amino-3-(2-oxooctahydro-1H-cyclopropa[a]indolizin-5-yl)imidazo[1,5-a]pyrazin-1-yl)-3-ethoxy-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide;4-(8-amino-3-((6′S,8a′R)-1′,1′-difluoro-3′-oxohexahydro-1′H-spiro[cyclopropane-1,2′-indolizin]-6′-yl)imidazo[1,5-a]pyrazin-1-yl)-3-ethoxy-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide;4-(8-amino-3-((6′R,8a′S)-1′,1′-difluoro-3′-oxohexahydro-1′H-spiro[cyclopropane-1,2′-indolizin]-6′-yl)imidazo[1,5-a]pyrazin-1-yl)-3-ethoxy-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide;4-(8-amino-3-((6′R,8a′S)-3′-oxohexahydro-1′H-spiro[cyclopropane-1,2′-indolizin]-6′-yl)imidazo[1,5-a]pyrazin-1-yl)-3-ethoxy-5-fluoro-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide;4-{8-amino-3-[(6′R,8a′S)-1′,3′-dioxohexahydrospiro[cyclopropane-1,2′-indolizin]-6′-yl)imidazo[1,5-a]pyrazin-1-yl}-3-ethoxy-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide;4-{8-amino-3-[(6′R,8a′S)-1′,3′-dioxohexahydrospiro[cyclopropane-1,2′-indolizin]-6′-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide;4-{8-amino-3-[(6′R,8a′S)-1′,3′-dioxohexahydrospiro[cyclopropane-1,2′-indolizin]-6′-yl]imidazo[1,5-a]pyrazin-1-yl}-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide;4-{8-amino-3-[(6′R,8a′S)-1′,3′-dioxohexahydrospiro[cyclopropane-1,2′-indolizin]-6′-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(4-methylpyridin-2-yl)benzamide;4-{8-amino-3-[(6′R,8a′S)-1′,3′-dioxohexahydrospiro[cyclopropane-1,2′-indolizin]-6′-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(4-cyclopropylpyridin-2-yl)benzamide;4-{8-amino-3-[(1′S,6′R,8a′S)-1′-hydroxy-3′- ...

BENZAMIDE IMIDAZOPYRAZINE BTK INHIBITORS

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders. 5. The compound of selected from the group consisting of:(1R,3S)-3-[8-amino-1-(4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid;(1S,3R)-3-(8-amino-1-{4-[(4-cyclopropylpyridin-2-yl)carbamoyl]phenyl}imidazo[1,5-a]pyrazin-3-yl)cyclohexanecarboxylic acid;(1R,3S)-3-(8-amino-1-{4-[(4-cyclopropylpyridin-2-yl)carbamoyl]phenyl}imidazo[1,5-a]pyrazin-3-yl)cyclohexanecarboxylic acid;(1R,3S)-3-[8-amino-1-(2-methoxy-4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid;(1S,3R)-3-[8-amino-1-(4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid(1S,3R)-3-(8-amino-1-{4-[(4-ethylpyridin-2-yl)carbamoyl]phenyl}imidazo[1,5-a]pyrazin-3-yl)cyclohexanecarboxylic acid;(1S,3R)-3-(8-amino-1-{4-[(4-cyclopropylpyridin-2-yl)carbamoyl]phenyl}imidazo[1,5-a]pyrazin-3-yl)cyclohexanecarboxylic acid;(1S,3R)-3-(8-amino-1-{4-[(4-cyclopropylpyridin-2-yl)carbamoyl]-2-fluorophenyl}imidazo[1,5-a]pyrazin-3-yl)cyclohexanecarboxylic acid;(1S,3R)-3-[8-amino-1-(2-fluoro-4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid;(1S,3R)-3-[8-amino-1-(2-methoxy-4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid;(1S,3R)-3-[8-amino-1-(4-{[4-(cyclopropyloxy)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclohexanecarboxylic acid;(1S,3R)-3-[8-amino-1-(4-{[4-(trifluoromethyl)pyridin-2-yl]carbamoyl}phenyl)imidazo[1,5-a]pyrazin-3-yl]cyclopentanecarboxylic acid;(1R,3S)- ...

Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer

Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

Polycyclic indazole derivatives and their use as ERK inhibitors for the treatment of cancer

Novel heterocyclic compounds as erk inhibitors

The present invention provides a compound of the Formula I:(Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Novel heterocyclic compounds as erk inhibitors

Compounds that are erk inhibitors

COMPOUNDS THAT ARE ERK INHIBITORSDisclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0. No Figure.

Novel compounds that are erk inhibitors

Disclosed are the ERK inhibitors of formula (1):and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring)cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).

Compounds derived from substituted n- (1h-indazol-5-yl) pyrrolidin-3-carboxamide, erk inhibitors; pharmaceutical composition; and its use in the treatment of cancer.

UN COMPUESTO DE FORMULA 1.0: O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO, DONDE R1, R2 Y Q SON COMO SE DESCRIBEN EN LA MEMORIA DESCRIPTIVA; COMPOSICION FARMACEUTICA QUE COMPRENDE DICHO COMPUESTO; Y USO DE DICHO COMPUESTO PARA PREPARAR UN MEDICAMENTE UTIL EN EL TRATAMIENTO DE CANCER. A COMPOSITE OF FORMULA 1.0: OR A PHARMACEUTICALLY ACCEPTABLE SALT OF THE SAME, WHERE R1, R2 AND Q ARE AS DESCRIBED IN THE DESCRIPTIVE MEMORY; PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUND; AND USE OF SUCH COMPOUND TO PREPARE A MEDICALLY USEFUL IN CANCER TREATMENT.

Btk inhibitors

Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydopyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Compounds that are ERK inhibitors

Benzamide imidazopyrazine btk inhibitors

Benzamide imidazopyrazine btk inhibitors