Patent classifications
C07D475/00
USE OF PTERIDINONE DERIVATIVE SERVING AS EGFR INHIBITOR
The present invention relates to a pteridinone derivative serving as an EGFR inhibitor and use thereof. Specifically, the present invention relates to a compound represented by the following formula I, pharmaceutical composition comprising the compound of the following formula I, and use of the compound in preparation of drugs for treating EGFR-mediated diseases or inhibiting EGFR.
##STR00001##
Dihydropteridinone derivatives and uses thereof
The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
Dihydropteridinone derivatives and uses thereof
The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
COMPOUNDS AS MODULATORS OF ROR GAMMA
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
COMPOUNDS AS MODULATORS OF ROR GAMMA
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the variables are defined herein which are suitable for the modulation of ROR and the treatment of diseases related to the modulation of ROR. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
NON-PEPTIDE TARGETED THERAPEUTICS AND USES THEREOF
Described herein are non-peptide drug conjugates (NPDCs) that target tumor cells expressing cell surface peptide and protein G protein-coupled receptors and their use in the treatment and/or diagnosis of cancer.
Heterocyclic derivatives as modulators of kinase activity
The invention provides novel imidazol-piperidinyl derivatives of the formula (I) ##STR00001##
in which R.sup.1, R.sup.2, W, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
The present invention relates to a compound of the formula I
##STR00001##
wherein R.sup.1 to R.sup.6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
NOVEL IMMUNE SYSTEM MODULATORS
The present invention relates to a compound of Formula I:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Pteridines useful as HCV inhibitors and methods for the preparation thereof
The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.