Patent classifications
C07D401/06
PHARMACEUTICAL COMPOSITIONS COMPRISING N-[1-(5-CYANO-PYRIDIN-2-YLMETHYL)-1H-PYRAZOL-3-YL]-2-[4-(1-TRIFLUOROMETHYL-CYCLOPROPYL)-PHENYL]-ACETAMIDE
The present invention relates to solid pharmaceutical compositions comprising N-[1-(5-cyano-pyridin-2−ylmethyl)-1H-pyrazol-3-yl]-2-[4-(1-trifluoromethyl-cyclopropyl)-phenyl]-acetamide or pharmaceutically acceptable salt thereof. The invention further relates to methods for manufacturing said compositions and their uses for the treatment or prevention of diseases and disorders linked to T-type calcium channels such as epilepsy.
Chemical process for preparing phenylpiperidinyl indole derivatives
The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-(((2S,4S)-(4-ethoxy-1-(((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.
Chemical process for preparing phenylpiperidinyl indole derivatives
The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-(((2S,4S)-(4-ethoxy-1-(((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.
MATRIPTASE 2 INHIBITORS AND USES THEREOF
The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.
MATRIPTASE 2 INHIBITORS AND USES THEREOF
The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.
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.
HETEROCYCLIC COMPOUND
- Yuhei MIYANOHANA ,
- Yuichi KAJITA ,
- Tatsuki KOIKE ,
- Yasutaka HOASHI ,
- Yasushi Hattori ,
- Norihito Tokunaga ,
- Tsuneo ODA ,
- Tohru Miyazaki ,
- Dilhumar UYGHUR ,
- Yoshiteru ITO ,
- Kohei TAKEUCHI ,
- Keisuke IMAMURA ,
- Takahiro SUGIMOTO ,
- Koichiro FUKUDA ,
- Yasuhisa KOHARA ,
- Rei OKAMOTO ,
- Taiichi OHRA ,
- Naoki MIYAMOTO ,
- Jun CHIBA ,
- Yoshito Terao ,
- Masanori KAWASAKI
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.
A compound represented by the formula (I):
##STR00001## wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
HETEROCYCLIC COMPOUND
- Yuhei MIYANOHANA ,
- Yuichi KAJITA ,
- Tatsuki KOIKE ,
- Yasutaka HOASHI ,
- Yasushi Hattori ,
- Norihito Tokunaga ,
- Tsuneo ODA ,
- Tohru Miyazaki ,
- Dilhumar UYGHUR ,
- Yoshiteru ITO ,
- Kohei TAKEUCHI ,
- Keisuke IMAMURA ,
- Takahiro SUGIMOTO ,
- Koichiro FUKUDA ,
- Yasuhisa KOHARA ,
- Rei OKAMOTO ,
- Taiichi OHRA ,
- Naoki MIYAMOTO ,
- Jun CHIBA ,
- Yoshito Terao ,
- Masanori KAWASAKI
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.
A compound represented by the formula (I):
##STR00001## wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
SUBSTITUTED ARYLMETHYLUREAS AND HETEROARYLMETHYLUREAS, ANALOGUES THEREOF, AND METHODS USING SAME
The present invention includes substituted arylmethyl ureas and heteroarylmethyl-ureas, and compositions comprising the same, that can be used to treat and/or prevent hepatitis B virus (HBV) infections in a patient.