Patent classifications
C07D213/75
ARYL AND HETEROARYL COMPOUNDS, AND THERAPEUTIC USES THEREOF IN CONDITIONS ASSOCIATED WITH THE ALTERATION OF THE ACTIVITY OF GALACTOCEREBROSIDASE
The application is directed to compounds of formulae (IA) and (IB): (IA) and (IB), and their salts and solvates, wherein R.sup.1a, R.sup.2a, .sup.A1, A.sup.2, A.sup.3, A.sup.4, R.sup.1b, R.sup.2b, B.sup.1, B.sup.2, B.sup.3, and G are as set forth in the specification, as well as to methods for their preparation, N pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., lysosomal storage diseases, such as Krabbe's disease, and α-synucleinopathies, such as Parkinson's disease.
##STR00001##
ARYL AND HETEROARYL COMPOUNDS, AND THERAPEUTIC USES THEREOF IN CONDITIONS ASSOCIATED WITH THE ALTERATION OF THE ACTIVITY OF GALACTOCEREBROSIDASE
The application is directed to compounds of formulae (IA) and (IB): (IA) and (IB), and their salts and solvates, wherein R.sup.1a, R.sup.2a, .sup.A1, A.sup.2, A.sup.3, A.sup.4, R.sup.1b, R.sup.2b, B.sup.1, B.sup.2, B.sup.3, and G are as set forth in the specification, as well as to methods for their preparation, N pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., lysosomal storage diseases, such as Krabbe's disease, and α-synucleinopathies, such as Parkinson's disease.
##STR00001##
ARYL-N-ARYL DERIVATIVES FOR TREATING A RNA VIRUS INFECTION
A compound of formula (Ic)
##STR00001## wherein X.sup.2 represents a —CO—NR.sub.k— group, wherein R.sub.k represents a hydrogen atom or a methyl group, a —NH—CO—NH— group, a —OCH.sub.2— group, a —CH(OH)— group, a —NH—CO— group, a —O— group, a —O—(CH.sub.2).sub.s—O—, a —CO— group, a —SO.sub.2— group, a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or 4 heteroatoms, —a NH—SO.sub.2— or a —SO.sub.2—NH— group; Y.sup.2 represents a hydrogen atom, a halogen atom, a hydroxyl group, a (C.sub.1-C.sub.4)alkoxy group, a
##STR00002##
a
##STR00003##
group, a
##STR00004##
group, a morpholinyl group, optionally substituted by a (C.sub.1-C.sub.4)alkyl group, a piperazinyl group, a piperidinyl group, or a —CR.sup.1R.sup.2R.sup.3 group, or any of its pharmaceutically acceptable salt.
PYRIDIN-2-ONE COMPOUNDS USEFUL AS SMARCA2 ANTAGONISTS
This disclosure generally relates to pyridine-2-one compounds of formula (I) and methods of using them in the treatment of a disorder, such as cancer or a SMARCA2-associated disorder, including as antagonists (e.g., inhibitors) of SMARCA2. The present disclosure provides treatment modalities, e.g., strategies, treatment methods, patient stratification methods, compounds, combinations, and compositions that are useful for the treatment of disorders, e.g., proliferative disorders, such as certain cancers. Some aspects of this disclosure provide treatment modalities, methods, strategies, compounds, compositions, combinations, and dosage forms for the treatment of cell proliferative disorders, e.g., cancers with decreased activity or function, or loss of function, of SMARCA4 with a SMARCA2 antagonist.
##STR00001##
PYRIDIN-2-ONE COMPOUNDS USEFUL AS SMARCA2 ANTAGONISTS
This disclosure generally relates to pyridine-2-one compounds of formula (I) and methods of using them in the treatment of a disorder, such as cancer or a SMARCA2-associated disorder, including as antagonists (e.g., inhibitors) of SMARCA2. The present disclosure provides treatment modalities, e.g., strategies, treatment methods, patient stratification methods, compounds, combinations, and compositions that are useful for the treatment of disorders, e.g., proliferative disorders, such as certain cancers. Some aspects of this disclosure provide treatment modalities, methods, strategies, compounds, compositions, combinations, and dosage forms for the treatment of cell proliferative disorders, e.g., cancers with decreased activity or function, or loss of function, of SMARCA4 with a SMARCA2 antagonist.
##STR00001##
Kv11.1-3.1 INHIBITING METHODS AND COMPOSITIONS
##STR00001##
Compounds of formula (I), formula (II), or formula (III) and their use with a neurological or psychiatric disorder, mediated by Kv11.1-3.1 containing potassium channels, including schizophrenia, are disclosed.
SALT OF OMECAMTIV MECARBIL AND PROCESS FOR PREPARING SALT
Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.
SALT OF OMECAMTIV MECARBIL AND PROCESS FOR PREPARING SALT
Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.
COMPOUND AS CYCLIN-DEPENDENT KINASE 9 INHIBITOR AND USE THEREOF
Disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt, a stereoisomer, an isotope derivative or a prodrug thereof. The compound has an excellent activity as a cyclin-dependent kinase 9 (CDK9) inhibitor for treating hyperproliferative diseases. The experimental research on in vitro inhibition of cell proliferation and in vivo suppression of tumors shows that such compounds have a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and have a good selectivity and a low toxicity and few side effects, thereby possessing a good clinical value as novel anti-tumor drugs.
##STR00001##
SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF
The presented invention relates to Omecamtiv mecarbil salts with methane sulfonic acid, benzene sulfonic acid and p-toluene sulfonic acid and to processes for preparation thereof.