Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy. ##STR00001##

Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy. ##STR00001##

Methods of treating cancer by administering a compound of Formula I, ##STR00001##
or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R.sup.1 is halo; R.sup.2 is halo; and Q is CH or N.

The present application provides a quinolyl-substituted carboxylic acid compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as a method for preparing the compound, a use of the compound, and a formulation containing the quinolyl-substituted carboxylic acid compound or the pharmaceutically acceptable salt thereof. This type of compounds are inhibitors for AXL and/or VEGFR2 protein kinase, and can be used to treat diseases caused by abnormality of the two protein kinases, such as, tumor, etc. ##STR00001##

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

Provided is compound of formula (I):

##STR00001##

where: X and Y may be identical or different and represent O, NH, or S; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 may be identical or different and represent H, halogen, CN, NO.sub.2, (C.sub.1-4)alkyl, (C.sub.1-4)haloalkyl, (C.sub.2-4)alkenyl, OH, O(C.sub.1-4)alkyl, O(C.sub.1-4)haloalkyl, N(R.sup.A)R.sup.B, C(O)N(R.sup.A)R.sup.B, C(O)R.sup.A, CO.sub.2R.sup.A, CHO, C.sub.2-4alkenyl substituted with CN, C.sub.2-4alkenyl substituted with COOH, C.sub.2-4alkenyl substituted with CHO, or C.sub.2-4alkenyl substituted with OH; R.sup.A and R.sup.B may be identical or different and represent H, (C.sub.1-4)alkyl, (C.sub.1-4)haloalkyl, or (C.sub.2-4)alkenyl; A.sub.1, A.sub.2, A.sub.3, and A.sub.4 may be identical or different and represent CH or N with the proviso that A.sub.1 and A.sub.2 cannot be N and that R.sub.5 and R.sub.10 are absent when A.sub.3 and A.sub.4 are N; or a pharmaceutically acceptable salt thereof, stereoisomer thereof, or mixture comprising stereoisomers thereof.

Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X.sup.1, X.sup.2, R.sup.1-4 and R.sup.13-18 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed. ##STR00001##