Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors
摘要:
Monoglyceride lipase (MGL) inhibition may offer an approach in treating diseases in which higher 2-arachidonoyglycerol activity would be beneficial. We report here the synthesis and pharmacological evaluation of bis(dialkylaminethiocarbonyl)disulfide derivatives as irreversible MGL inhibitors. Inhibition occurs through interactions with MGL C208 and C242 residues, and these derivatives exhibit high inhibition selectivity over fatty acid amide hydrolase, another endocannabinoid-hydrolyzing enzyme.
Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors
摘要:
Monoglyceride lipase (MGL) inhibition may offer an approach in treating diseases in which higher 2-arachidonoyglycerol activity would be beneficial. We report here the synthesis and pharmacological evaluation of bis(dialkylaminethiocarbonyl)disulfide derivatives as irreversible MGL inhibitors. Inhibition occurs through interactions with MGL C208 and C242 residues, and these derivatives exhibit high inhibition selectivity over fatty acid amide hydrolase, another endocannabinoid-hydrolyzing enzyme.
The present invention provides a novel complex lipid having a cationic functional group derived from an amino acid. Namely, the present invention provides a cationic acid amino acid type lipid represented by the following formula:
wherein, R
1
is a hydrocarbon group having a cationic functional group derived from an amino acid, R
2
and R
3
are each independently a chain hydrocarbon group, A
1
and A
2
are each independently a linkage group selected from the group consisting of —COO—, —OCO—, —CONH— and NHCO—, and n is an integer of 2 to 4.
CARBOXYLIC ACID-TYPE LIPID, AND LIPID PARTICLE AND LIPID MEMBRANE EACH COMPRISING CARBOXYLIC ACID-TYPE LIPID
申请人:Toray Industries, Inc.
公开号:US20210387943A1
公开(公告)日:2021-12-16
A carboxylic acid-type lipid can accelerate adhesion or aggregation of platelets even if the carboxylic acid-type lipid does not carry a protein involved in adhesion or aggregation of platelets or a peptide corresponding to an active site of the protein; a lipid particle and a lipid membrane each include the carboxylic acid-type lipid; and a platelet aggregation accelerating agent, a platelet adhesion accelerating agent, a hemostatic agent and a platelet substitute each include the carboxylic acid-type lipid, the lipid particle or the lipid membrane. A carboxylic acid-type lipid is selected from carboxylic acid-type lipids represented by formulas (I) to (VI), a lipid particle includes the carboxylic acid-type lipid, a lipid membrane includes the carboxylic acid-type lipid, and a platelet aggregation accelerating agent, a platelet adhesion accelerating agent, a hemostatic agent and a platelet substitute each include the carboxylic acid-type lipid, the lipid particle or the lipid membrane.
The present invention provides a reagent for introducing a protein or gene into a cell. The reagent of the present invention is, for example, a reagent for introducing a protein or gene into a cell, which comprises a composition comprising a cationic amino acid type lipid represented by the following formula (I)-1:
(wherein in formula (I)-1: L is a single bond, —CONH—, or —S—S—; M
1
is —(CH
2
)
k
— or —(CH
2
CH
2
O)
k
— (wherein k is an integer between 0 and 14); and m1 and m2 are each independently an integer between 11 and 21 (in this regard, when providing a reagent for introducing a gene into a cell, the case where both m1 and m2 are 15 is excluded)).
Pentaerythritol-spiro-bis-phosphite compositions having improved hydrolytic stability
申请人:Argus Chemical Corporation
公开号:EP0143464A2
公开(公告)日:1985-06-05
Pentaerythritol-spiro-bis-phosphite compositions are provided having an improved hydrolytic stability, comprising (1) a pentaerythritol-spiro-bis-phosphite of the formula:
wherein:
R, and R2 are selected from the group consisting of alkyl and alkylaryl groups having at least fourteen carbon atoms up to about thirty-six carbon atoms; and
(2) a long-chain aliphatic amine in an amount to improve the hydrolytic stability of the phosphite and having the formula:
wherein:
R3, R4, and R5 are selected from the group consisting of hydrogen; aliphatic (including alkyl and alkenyl) groups having from one to about thirty-six carbon atoms; and hydroxyalkyl having from two to about six carbon atoms; one of R3, R4 and R5 is an aliphatic group having at least fourteen carbon atoms, and the remaining of R3, R4 and R5 are selected from hydrogen, alkyl having from one to four carbon atoms and hydroxyalkyl; and preferably at least one of R3, R4 and R5 is hydroxyalkyl.
Novel perfluoropolyether derivatives, and lubricants and magnetic recording medium using the same
申请人:SONY CORPORATION
公开号:EP0519406A2
公开(公告)日:1992-12-23
Novel perfluoropolyether derivatives are described which are obtained from perfluoropolyethers having a carboxyl group at one or both ends and monoamines or diamines. The derivative is useful as a lubricant owing to its significantly improved lubricity. The lubricity is shown under severe high or low temperature and humidity conditions over a long term. The derivative is especially useful as a lubricant for magnetic recording mediums of the coating and metal thin film types.