C07D487/20

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.

TETRAHYDRO-SPIROINDOLINE-PYRROLOPYRROLE-TRIONES INHIBITORS OF THE NRF2-BETA-TRCP INTERACTION FOR USE IN THE TREATMENT OF FATTY LIVER DISEASE

The present invention relates to NRF2-βTrCP interaction inhibitors with general formula I and its derivate salts for use in the treatment of NRF2-related diseases caused by chronic inflammation and oxidative stress. More specifically the present invention relates to NRF2-βTrCP interaction inhibitors with specific formula I and its derivate salts for treating diseases of the liver related with chronic inflammation and oxidative stress, such as fatty liver disease.

TETRAHYDRO-SPIROINDOLINE-PYRROLOPYRROLE-TRIONES INHIBITORS OF THE NRF2-BETA-TRCP INTERACTION FOR USE IN THE TREATMENT OF FATTY LIVER DISEASE

The present invention relates to NRF2-βTrCP interaction inhibitors with general formula I and its derivate salts for use in the treatment of NRF2-related diseases caused by chronic inflammation and oxidative stress. More specifically the present invention relates to NRF2-βTrCP interaction inhibitors with specific formula I and its derivate salts for treating diseases of the liver related with chronic inflammation and oxidative stress, such as fatty liver disease.

SOLID STATE FORMS OF TRILACICLIB AND OF TRILACICLIB SALTS

The present disclosure encompasses solid state forms of Trilaciclib and of Trilaciclib salts, in embodiments crystalline polymorphs of Trilaciclib and of Trilaciclib salts, processes for preparation thereof, and pharmaceutical compositions thereof.

SOLID STATE FORMS OF TRILACICLIB AND OF TRILACICLIB SALTS

The present disclosure encompasses solid state forms of Trilaciclib and of Trilaciclib salts, in embodiments crystalline polymorphs of Trilaciclib and of Trilaciclib salts, processes for preparation thereof, and pharmaceutical compositions thereof.

SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF

The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

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DISPIROPYRROLIDINE DERIVATIVES

A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R.sup.1, R.sup.2, R.sup.3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.

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DISPIROPYRROLIDINE DERIVATIVES

A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R.sup.1, R.sup.2, R.sup.3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.

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SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
20220098211 · 2022-03-31 ·

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
20220098211 · 2022-03-31 ·

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.