Patent classifications
C07D401/14
SMALL MOLECULE MODULATORS OF SIGMA-1 AND SIGMA-2 RECEPTORS AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.
COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE AND METABOLIC DISORDERS
Compounds described herein may be used for the treatment of neurodegenerative diseases linked to protein misfolding, including prion diseases, Alzheimer's disease, Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS), and also other neurodegenerative, degenerative, metabolic and ischemic conditions. Indeed, NAD metabolism impairment is also a critical feature in brain ischemia/reperfusion injury, Wallerian degeneration, kidney failure, multiple sclerosis, aging, and metabolic disorders such as diabetes mellitus. Therapies that elevate or stabilize NAD levels may thus have broad potential for treating many severely debilitating neurological and metabolic conditions. Evidence is provided herein with compounds from 8 lead series for NAD restoring properties and for therapeutic efficacy in cellular and/or animal models of prion disease, PD and ALS.
COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE AND METABOLIC DISORDERS
Compounds described herein may be used for the treatment of neurodegenerative diseases linked to protein misfolding, including prion diseases, Alzheimer's disease, Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS), and also other neurodegenerative, degenerative, metabolic and ischemic conditions. Indeed, NAD metabolism impairment is also a critical feature in brain ischemia/reperfusion injury, Wallerian degeneration, kidney failure, multiple sclerosis, aging, and metabolic disorders such as diabetes mellitus. Therapies that elevate or stabilize NAD levels may thus have broad potential for treating many severely debilitating neurological and metabolic conditions. Evidence is provided herein with compounds from 8 lead series for NAD restoring properties and for therapeutic efficacy in cellular and/or animal models of prion disease, PD and ALS.
HETEROAROMATIC DERIVATIVES FOR USE AS REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.
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HETEROAROMATIC DERIVATIVES FOR USE AS REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.
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SUBSTITUTED ISOINDOLINONES AS MODULATORS OF CEREBLON-MEDIATED NEO-SUBSTRATE RECRUITMENT
Disclosed herein are isoindolinone compounds and methods for binding cereblon and for modulating cereblon neosubstrates. The isoindolinone compounds can have a structure of Formula (I).
SUBSTITUTED ISOINDOLINONES AS MODULATORS OF CEREBLON-MEDIATED NEO-SUBSTRATE RECRUITMENT
Disclosed herein are isoindolinone compounds and methods for binding cereblon and for modulating cereblon neosubstrates. The isoindolinone compounds can have a structure of Formula (I).
Compounds for the Treatment of Kinase-Dependent Disorders
Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Ax1 and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.
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Compounds for the Treatment of Kinase-Dependent Disorders
Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Ax1 and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.
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FLUORINATED QUINOLINE AND QUINOXALINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula (I) as follows:
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wherein R.sup.1a, R.sup.1b, R.sup.2, and R.sup.3, are defined herein.