C07D473/16

STABILIZATION OF MHC COMPLEXES
20230111132 · 2023-04-13 ·

Provided, inter alia, are methods and compositions for treating cancer.

PROCESS FOR THE PREPARATION OF PURINE DERIVATIVES EXHIBITING CDK INHIBITORY ACTIVITY
20230104823 · 2023-04-06 ·

The present invention relates to a process for preparing a compound of formula [I], or a pharmaceutically acceptable salt thereof, said process comprising the steps of: (i) forming a reaction mixture comprising a compound of formula [II] and a compound of formula [III]; (ii) heating said reaction mixture to a temperature of at least about 130° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I] from the mixture and optionally recovering unreacted compound of formula [III]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R.sup.1 and R.sup.2 are each independently H, alkyl or haloalkyl; R.sup.3 and R.sup.4 are each independently H, alkyl, haloalkyl or aryl; R.sup.5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R.sup.6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR.sup.9; R.sup.7, R.sup.8 and each R.sup.9 are independently H, alkyl or haloalkyl, wherein at least one of R.sup.7, R.sup.8 and R.sup.9 is other than H. Further aspects of the invention relate to a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I].

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9-(2-oxacycloalkyl)-9H-purine-2,6-diamine derivatives and their use for the treatment of skin disorders

The invention relates to N.sup.2,N.sup.6-disubstituted-9-(2-oxacycloalkyl)-9H-purine-2, 6-diamine derivatives and their use as drugs and cosmetics. The compounds of the present invention exhibit a number of biological activities associated with oxidative stress inhibition, especially anti-aging, anti-inflammatory and anti-neurodegenerative biological activities. The invention also relates to cosmetic and pharmaceutical compositions containing such derivatives as active agents.

9-(2-oxacycloalkyl)-9H-purine-2,6-diamine derivatives and their use for the treatment of skin disorders

The invention relates to N.sup.2,N.sup.6-disubstituted-9-(2-oxacycloalkyl)-9H-purine-2, 6-diamine derivatives and their use as drugs and cosmetics. The compounds of the present invention exhibit a number of biological activities associated with oxidative stress inhibition, especially anti-aging, anti-inflammatory and anti-neurodegenerative biological activities. The invention also relates to cosmetic and pharmaceutical compositions containing such derivatives as active agents.

CYANO-PYRIMIDINE INHIBITORS OF EGFR/HER2
20230137932 · 2023-05-04 ·

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with EGFR and/or HER2 activity.

COMPOUNDS FOR TREATING CYSTIC FIBROSIS

The present invention relates to compounds of Formula (I) or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof. The invention further relates to the use of the compounds of Formula (I) for the treatment of cystic fibrosis. The invention also relates to a process for manufacturing compounds of Formula (I).

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COMPOUNDS FOR TREATING CYSTIC FIBROSIS

The present invention relates to compounds of Formula (I) or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof. The invention further relates to the use of the compounds of Formula (I) for the treatment of cystic fibrosis. The invention also relates to a process for manufacturing compounds of Formula (I).

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Substituted quinazolin-4-one derivatives

Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases. ##STR00001##

Substituted quinazolin-4-one derivatives

Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases. ##STR00001##

INHIBITORS OF CYCLIN-DEPENDENT KINASES

The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

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