A61K31/527

SPIROCYCLIC ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER

The present invention encompasses compounds of formula (I)

##STR00001##

wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, Z, R.sup.3 to R.sup.5, ring A, ring B, p, q, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

SPIROCYCLIC ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER

The present invention encompasses compounds of formula (I)

##STR00001##

wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, Z, R.sup.3 to R.sup.5, ring A, ring B, p, q, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

SPIROHETEROCYCLE DERIVATIVE HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
20250026765 · 2025-01-23 · ·

Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.

A compound represented by Formula (I):

##STR00001##

wherein R.sup.1 is a hydrogen atom or the like; A.sup.1 is each independently CR.sup.2R.sup.2; A.sup.2 is each independently CR.sup.3R.sup.3, R.sup.2 is each independently a hydrogen atom or the like; R.sup.2 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:

##STR00002##

or the like
wherein R.sup.4 is a group represented by Formula:

##STR00003##

or the like
wherein A.sup.3 is each independently CR.sup.13R.sup.13; A.sup.4 is each independently CR.sup.14R.sup.14; R.sup.13 is each independently a hydrogen atom or the like; R.sup.13 is each independently a hydrogen atom or the like; R.sup.14 is each independently a hydrogen atom or the like; R.sup.14 is each independently a hydrogen atom or the like; q and r are each independently 1 or the like; R.sup.10 and R.sup.11 are each independently substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.8 is a hydrogen atom or the like, or a pharmaceutically acceptable salt thereof.

SPIROHETEROCYCLE DERIVATIVE HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
20250026765 · 2025-01-23 · ·

Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.

A compound represented by Formula (I):

##STR00001##

wherein R.sup.1 is a hydrogen atom or the like; A.sup.1 is each independently CR.sup.2R.sup.2; A.sup.2 is each independently CR.sup.3R.sup.3, R.sup.2 is each independently a hydrogen atom or the like; R.sup.2 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:

##STR00002##

or the like
wherein R.sup.4 is a group represented by Formula:

##STR00003##

or the like
wherein A.sup.3 is each independently CR.sup.13R.sup.13; A.sup.4 is each independently CR.sup.14R.sup.14; R.sup.13 is each independently a hydrogen atom or the like; R.sup.13 is each independently a hydrogen atom or the like; R.sup.14 is each independently a hydrogen atom or the like; R.sup.14 is each independently a hydrogen atom or the like; q and r are each independently 1 or the like; R.sup.10 and R.sup.11 are each independently substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.8 is a hydrogen atom or the like, or a pharmaceutically acceptable salt thereof.

SPIROCYCLIC COMPOUND AS KRAS-G12C INHIBITOR
20250034161 · 2025-01-30 ·

The present invention relates to a spirocyclic compound, represented by formula (I), as a KRAS-G12C inhibitor, which can be used in the preparation of a drug for treating KRAS G12C-mediated tumors.

##STR00001##

SPIROCYCLIC COMPOUND AS KRAS-G12C INHIBITOR
20250034161 · 2025-01-30 ·

The present invention relates to a spirocyclic compound, represented by formula (I), as a KRAS-G12C inhibitor, which can be used in the preparation of a drug for treating KRAS G12C-mediated tumors.

##STR00001##

TRICYCLIC LACTAMS FOR USE IN HSPC-SPARING TREATMENTS FOR RB-POSITIVE ABNORMAL CELLULAR PROLIFERATION

This invention is in the area of tricyclic lactam compounds for and methods of treating selected Rb-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.

TRICYCLIC LACTAMS FOR USE IN HSPC-SPARING TREATMENTS FOR RB-POSITIVE ABNORMAL CELLULAR PROLIFERATION

This invention is in the area of tricyclic lactam compounds for and methods of treating selected Rb-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.

Methods and compositions for treating bacterial infection

The present disclosure relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present disclosure provides compounds as therapeutic agents against bacterial infections (e.g., biofilms). The present disclosure also provides compounds as therapeutic agents in methods for treating pneumonia, methods for reducing bacterial virulence, methods for treating a bacterial wound infection, and methods for treating a urinary tract infection. The present disclosure also provides methods for treating a bacterial infection, wherein the bacterial infection has or is suspected of having an antibiotic-resistant bacteria. The present disclosure also provides surfaces coated with the chemical compounds disclosed herein.

Methods and compositions for treating bacterial infection

The present disclosure relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present disclosure provides compounds as therapeutic agents against bacterial infections (e.g., biofilms). The present disclosure also provides compounds as therapeutic agents in methods for treating pneumonia, methods for reducing bacterial virulence, methods for treating a bacterial wound infection, and methods for treating a urinary tract infection. The present disclosure also provides methods for treating a bacterial infection, wherein the bacterial infection has or is suspected of having an antibiotic-resistant bacteria. The present disclosure also provides surfaces coated with the chemical compounds disclosed herein.