21571-66-4Relevant academic research and scientific papers
KCNT1 INHIBITORS AND METHODS OF USE
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Paragraph 000332, (2020/11/23)
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
PIPERAZINYL METHANONE NAAA INHIBITORS
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Paragraph 0215; 0304; 0322, (2017/12/16)
Disclosed herein, inter alia, are compositions and methods for modulating the activity of N-acylethanolamine acid amidase for the treatment of a pathological state, including pain, an inflammatory condition, or a neurodegenerative disorder.
Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis
Migliore, Marco,Pontis, Silvia,Fuentes de Arriba, Angel Luis,Realini, Natalia,Torrente, Esther,Armirotti, Andrea,Romeo, Elisa,Di Martino, Simona,Russo, Debora,Pizzirani, Daniela,Summa, Maria,Lanfranco, Massimiliano,Ottonello, Giuliana,Busquet, Perrine,Jung, Kwang -Mook,Garcia-Guzman, Miguel,Heim, Roger,Scarpelli, Rita,Piomelli, Daniele
supporting information, p. 11193 - 11197 (2016/10/13)
Palmitoylethanolamide (PEA) and oleoylethanolamide (OEA) are endogenous lipid mediators that suppress inflammation. Their actions are terminated by the intracellular cysteine amidase, N-acylethanolamine acid amidase (NAAA). Even though NAAA may offer a new target for anti-inflammatory therapy, the lipid-like structures and reactive warheads of current NAAA inhibitors limit the use of these agents as oral drugs. A series of novel benzothiazole–piperazine derivatives that inhibit NAAA in a potent and selective manner by a non-covalent mechanism are described. A prototype member of this class (8) displays high oral bioavailability, access to the central nervous system (CNS), and strong activity in a mouse model of multiple sclerosis (MS). This compound exemplifies a second generation of non-covalent NAAA inhibitors that may be useful in the treatment of MS and other chronic CNS disorders.
PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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Paragraph 0388; 0389, (2013/03/26)
The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Triazolopyridine cannabinoid receptor 1 antagonists
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Page/Page column 84, (2008/06/13)
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
Gonadotropin releasing hormone receptor antagonists
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Page/Page column 77, (2010/02/15)
The present invention relates to Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists.
Triazolopyrimidine cannabinoid receptor 1 antagonists
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Page/Page column 48, (2010/11/25)
The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
Aryl sulfonic acids and derivatives as FSH antagonists
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, (2008/06/13)
This invention provides compounds of formula I having the structure wherein R1, Ar, Ar′, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful as contraceptive agents.
