104 results about "Bromodomain" patented technology

The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I)wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof or a hydrate or solvate as an active ingredient.

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

The present invention features compounds useful for and methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.

The invention relates to compounds of Formulas I-VII (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating cellular signaling pathways and biological processes associated therewith including inhibition of kinase activity such as PI-3 kinase or inhibition of bromodomain proteins or both at the same time as well as to therapeutic methods for treating a disease associated with aberrant PI3K and / or bromodomain proteins.

The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I:and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various 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.

This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease.

Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

A cannabis-based flavonoid pharmaceutical composition including any one or more selected from among the group of Cannflavin A, Cannflavin B. Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside and their derivatives selected from among the group of Geraldol, Rhamnetin, Isorhamnetin, Rhamnazin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and histone acetylases. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include but are not limited to brain, breast, colon, renal liver, lung, pancreatic, pigmented villonodular synovitis, prostate, leukemia, melanomam, tenosynovial giant cell tumor, as well as any other cancers that overexpress the oncogenic factors inhibited, by the cannabis flavonoids or their derivatives herein identified.

A method of treating diffuse large B-cell lymphoma comprising administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound, said thienotriazolodiazepine compound being represented by Formula (I), wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; --NR5--(CH2)m--R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or --NR7--CO--(CH2)n-- R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is --(CH2)a--CO--NH--R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or --(CH2)b--COOR10 wherein b is an integer of 1-4, and R10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof, wherein the patient has activated B-cell diffuse large B-cell lymphoma.

The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

The present invention provides methods for treating cancer using combinations of bromodomain and extra-terminal (BET) protein inhibitors and certain chemotherapeutic drugs.

The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.

Disclosed are substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such4substituted5-(3,5-dimethylisoxazol- 4-yl)indoline-2-one compound processes for the preparation thereof,and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby,such as certain cancers.

Methods of inhibiting replication of human cytomegalovirus (HCMV) are disclosed. In various configurations, these methods comprise administering a therapeutically effective amount of a bromodomain inhibitor to a subject in need thereof. Bromodomain inhibitors including methyltriazolodiazepine-related compounds, 3,5-dimethylisoxazole-related compounds, 3-methyldihydroquinazolinone-related compounds, N-acetyl-2-methyltetrahydroquinoline-related compounds, quinazolone-related compounds, diazobenzene-related compounds, and triazolopyridazine-related compounds can be used to inhibit viral replication.

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.