C07D498/20

UREA, AMIDE, AND SUBSTITUTED HETEROARYL COMPOUNDS FOR CBL-B INHIBITION

Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

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UREA, AMIDE, AND SUBSTITUTED HETEROARYL COMPOUNDS FOR CBL-B INHIBITION

Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

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MACROCYCLIC COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.

BCL6 inhibitors

The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: ##STR00001##
wherein X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.30, R.sup.31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.

BCL6 inhibitors

The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: ##STR00001##
wherein X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.30, R.sup.31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.

COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS

The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I,

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and pharmaceutically acceptable slats thereof, pharmaceutical compositions comprising such compounds and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula Ito a subject in need thereof.

COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS

The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I,

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and pharmaceutically acceptable slats thereof, pharmaceutical compositions comprising such compounds and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula Ito a subject in need thereof.

Macrocyclic spiroethers as Mcl-1 inhibitors

Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R.sup.8, R.sup.9a, R.sup.9b, R.sup.9c, R.sup.9d, X, Y, Z, Z.sup.1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer. ##STR00001##

Macrocyclic indole derivatives

The present invention relates to macrocyclic indole derivatives of general formula (I) ##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

SPIROCYCLIC DEGRONIMERS FOR TARGET PROTEIN DEGRADATION

This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.