Patent classifications
C07D213/73
ARYLAMIDE DERIVATIVE HAVING ANTITUMOR ACTIVITY
The present disclosure provides, for example, a compound represented by general formula (6) below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt:
##STR00001##
wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently —CR.sub.2═ or —N═, R.sub.2 is, for example, a halogen atom, R.sub.1 is, for example, —S(═O).sub.2—NH—R.sub.8, R.sub.8 is, for example, a C1-6 alkyl group, R.sub.3 is, for example, a hydrogen atom, R.sub.5 is, for example, a halogen atom, R.sub.6 is, for example, a hydrogen atom, and R.sub.4 is, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.
ANTICANCER COMPOUNDS
Disclosed are compounds of formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof. The compounds of the invention are BDII-selective inhibitors of BET proteins, and have therapeutic potential for treating cancer, acute kidney disease, and viral infections, among other diseases.
Compounds and methods of use
This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.
Compounds and methods of use
This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.
ACLY inhibitors and uses thereof
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
INHIBITORS OF ALPHA 2 BETA 1 INTEGRIN AND METHODS OF USE THEREOF
Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.
INHIBITORS OF ALPHA 2 BETA 1 INTEGRIN AND METHODS OF USE THEREOF
Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.
1,2,4-OXADIAZOL-5-ONE DERIVATIVES FOR THE TREATMENT OF CANCER
The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A1 is —N═ or —C(R3)=; A2 is —N═ or —CH═; L is —NH—; B1 and B2 are independently —N═ or —C(R2b)=; B3 and B4 are independently —C(R2b)=; no more than one R2b on B1, B2, B3 and B4 is other than hydrogen; R1a is hydrogen, halogen, C1-C3alkyl (n-alkyl) optionally substituted with one R4, or R1a is —NH.sub.2, —NH(C1-C3alkyl (n-alkyl)), —NH(C(═O)—C1-C2alkyl), —N(C1-C3alkyl (n-alkyl)).sub.2, —OC1-C3alkyl (n-alkyl), C1-C3haloalkyl (n-alkyl) or —OC1-C3haloalkyl (n-alkyl); R1b is hydrogen, halogen, C1-C3alkyl (n-alkyl), —OC1-C3alkyl (n-alkyl), —NH.sub.2, —NH(C1-C3alkyl (n-alkyl)) or —N(C1-C3alkyl (n-alkyl)).sub.2; R1a and R1b may together form a —CH═CH—CH═CH— moiety in which one or two non-adjacent CH are optionally replaced by N; R2a is halogen, C1-C6alkyl, C1-C6haloalkyl, cyclopropyl, cyclobutyl, —OR6, —NHC(═O)—C3-C6cycloalkyl, Cycle Q, —SF.sub.5 or group Y (formula (Y)); wherein X is a 3- or 4-membered carbocyclic ring and R8 is halogen, cyano, C1-C6alkyl, C1-C6haloalkyl or —C1-C6alkyl-CN; and wherein R2b, R3, R4, R6 and R8 are as defined in the claims; as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.
##STR00001##
Benzocarbonyl compounds
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Benzocarbonyl compounds
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.