C07D295/108

Simple oxidative functionalized of alkyl aryl ketones
11203580 · 2021-12-21 · ·

The present invention refers to a process for reacting an alkyl aryl ketone obtaining thereby the corresponding aryl oxirane or α-functionalized alkyl aryl ketal, the aryl oxirane or α-functionalized alkyl aryl ketal obtained by the process as well as the α-functionalized ketone obtained by the process.

1-phenylpropanone compounds and use thereof

The present invention relates to a 1-phenylpropanone compound of formula (I), wherein X is CH.sub.2 or an atom selected from the group consisting of O, S and Se, n is an integer from 4 to 6, A is a substituent selected from the group consisting of 4-morpholyl, 1-piperidinyl, 4-methyl-1-piperazinyl, A being optionally substituted with a (C.sub.1-C.sub.3)alkyl or (C.sub.1-C.sub.3)acyl substituent, with the proviso that when X is CH.sub.2, n is equal to 5, for use as an antitumoral agent in the treatment of breast cancer, chronic lymphatic leukemia or neuroblastoma. The invention also concerns new 1-phenylpropanone compounds, and compounds as antitumoral agents. ##STR00001##

1-phenylpropanone compounds and use thereof

The present invention relates to a 1-phenylpropanone compound of formula (I), wherein X is CH.sub.2 or an atom selected from the group consisting of O, S and Se, n is an integer from 4 to 6, A is a substituent selected from the group consisting of 4-morpholyl, 1-piperidinyl, 4-methyl-1-piperazinyl, A being optionally substituted with a (C.sub.1-C.sub.3)alkyl or (C.sub.1-C.sub.3)acyl substituent, with the proviso that when X is CH.sub.2, n is equal to 5, for use as an antitumoral agent in the treatment of breast cancer, chronic lymphatic leukemia or neuroblastoma. The invention also concerns new 1-phenylpropanone compounds, and compounds as antitumoral agents. ##STR00001##

SUBSTITUTED 3-AMINO-4-METHYLBENZENESULFONAMIDES AS SMALL MOLECULE INHIBITORS OF UBIQUITIN-SPECIFIC PROTEASE 28
20230271918 · 2023-08-31 ·

The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof and pharmaceutical composition comprising the compound of formula (I). The present composition also relates to methods treating a disease or disorder associated with ubiquitin-specific protease 28 (USP28), methods of treating cancer, and methods of inhibiting USP28.

##STR00001##

METHOD FOR PREPARING GLUCOPYRANOSYL DERIVATIVES AND INTERMEDIATES THEREOF

A method for preparing glucopyranosyl derivatives as sodium dependent glucose cotransporter (SGLT) inhibitors, an intermediate thereof, and a method for preparing the intermediate.

METHOD FOR PREPARING GLUCOPYRANOSYL DERIVATIVES AND INTERMEDIATES THEREOF

A method for preparing glucopyranosyl derivatives as sodium dependent glucose cotransporter (SGLT) inhibitors, an intermediate thereof, and a method for preparing the intermediate.

Method for making propenamide compound

A compound of formula (I), ##STR00001##
wherein R.sup.1 is an optionally substituted aryl or an optionally substituted heteroaryl, R.sup.2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R.sup.3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.

Method for making propenamide compound

A compound of formula (I), ##STR00001##
wherein R.sup.1 is an optionally substituted aryl or an optionally substituted heteroaryl, R.sup.2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R.sup.3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.

Dual NAV1.2/5HT2a inhibitors for treating CNS disorders

Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.

Dual NAV1.2/5HT2a inhibitors for treating CNS disorders

Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.