C07D267/18

Amino acid conjugates of quetiapine, process for making and using the same
09597403 · 2017-03-21 · ·

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.

SULFONAMIDES DERIVED FROM TRICYCLYL-2-AMINOCYCLOALKANOLS AS ANTICANCER AGENTS

A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus:

##STR00001##

The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

SULFONAMIDES DERIVED FROM TRICYCLYL-2-AMINOCYCLOALKANOLS AS ANTICANCER AGENTS

A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus:

##STR00001##

The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

c-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as c-Abl). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

c-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as c-Abl). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

Synthesis of vinylic protected alcohol intermediates
12435049 · 2025-10-07 · ·

Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound D, wherein OPG and R.sup.1 are described herein. Compound D can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof. ##STR00001##

Synthesis of vinylic protected alcohol intermediates
12435049 · 2025-10-07 · ·

Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound D, wherein OPG and R.sup.1 are described herein. Compound D can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof. ##STR00001##

C-ABL TYROSINE KINASE INHIBITORY COMPOUND EMBODIMENTS AND METHODS OF MAKING AND USING THE SAME

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as c-Abl). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

C-ABL TYROSINE KINASE INHIBITORY COMPOUND EMBODIMENTS AND METHODS OF MAKING AND USING THE SAME

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as c-Abl). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.