Univalent and Bivalent Ligands of Butorphan: Characteristics of the Linking Chain Determine the Affinity and Potency of Such Opioid Ligands
摘要:
Bivalent morphinan compounds containing ester linkers were synthesized and their binding affinities at the mu, delta, and kappa opioid receptors determined. Addition of methyl groups adjacent to the hydrolytically labile ester linkage increased stability while only partially affecting binding affinity. The resulting bivalent ligands with optimized spacer length and structure show potent binding profiles with the most potent compound (4b), having K-i values of 0.47 nM for both the mu and kappa opioid receptors, and 4a, having K-i values of 0.95 and 0.62 nM for the mu and kappa receptors, respectively. Both 4a and 4b were partial agonists at the kappa and mu receptors in the [S-35]GTP gamma S binding assay.
[EN] LIPID PRODRUGS OF JAK INHIBITORS AND USES THEREOF<br/>[FR] PROMÉDICAMENTS LIPIDIQUES D'INHIBITEURS DE JAK ET LEURS UTILISATIONS
申请人:PURETECH LYT INC
公开号:WO2020176859A1
公开(公告)日:2020-09-03
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
[EN] LIPID PRODRUGS OF GLUCOCORTICOIDS AND USES THEREOF<br/>[FR] PROMÉDICAMENTS LIPIDIQUES DE GLUCOCORTICOÏDES ET LEURS UTILISATIONS
申请人:PURETECH LYT INC
公开号:WO2020176856A1
公开(公告)日:2020-09-03
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
The regiospecific palladium catalysed hydrocarboxylation of alkenes under mild conditions
作者:Howard Alper、James B. Woell、Bertrand Despeyroux、David J. H. Smith
DOI:10.1039/c39830001270
日期:——
Alkenes react with carbon monoxide, water, oxygen, hydrochloric acid, and palladium and copper chlorides, to give branched chain acids in good yields.
烯烃与一氧化碳,水,氧气,盐酸以及钯和氯化铜反应,以高收率得到支链酸。
REUSABLE PRINT MEDIUM AND METHOD OF MANUFACTURING THEREOF
申请人:OCE TECHNOLOGIES B.V.
公开号:US20130137805A1
公开(公告)日:2013-05-30
The present invention relates to a reusable print medium comprising a substrate and a sacrificial layer. The sacrificial layer contains a hotmelt composition at least comprising an amorphous material. The amorphous material is a resin being a reaction product of a first monomer A, said first monomer A being a polyhydroxyl alcohol comprising X hydroxyl functional groups, wherein X≧2, monomer A optionally comprises a primary or secondary amine functionality; a second monomer B, being an aromatic monocarboxylic acid; a third monomer C, said third monomer C being able to form an ester linkage with an alcohol and/or an amide linkage with a primary or secondary amine; and optionally, a fourth monomer D, being an aromatic monocarboxylic acid different from the second monomer B. The sacrificial layer including the printed image may be removed from the substrate by applying heat. A new sacrificial layer may be applied such that the reusable print medium is ready to be reused.
The present invention also relates to a method of manufacturing a reusable print medium according to the present invention, a method of printing and recycling such a print medium and an apparatus for printing and recycling such a print medium.
Reusable print medium and method of manufacturing thereof
申请人:Océ-Technologies B.V.
公开号:EP2596960A2
公开(公告)日:2013-05-29
The present invention relates to a reusable print medium (200) comprising a substrate (201) and a sacrificial layer (202). The sacrificial layer contains a hotmelt composition at least comprising an amorphous material. The amorphous material is a resin being a reaction product of a first monomer A, said first monomer A being a polyhydroxyl alcohol comprising X hydroxyl functional groups, wherein X ≥ 2, monomer A optionally comprises a primary or secondary amine functionality; a second monomer B, being an aromatic monocarboxylic acid; a third monomer C, said third monomer C being able to form an ester linkage with an alcohol and/or an amide linkage with a primary or secondary amine; and optionally, a fourth monomer D, being an aromatic monocarboxylic acid different from the second monomer B. The sacrificial layer including the printed image may be removed from the substrate by applying heat. A new sacrificial layer may be applied such that the reusable print medium is ready to be reused.
The present invention also relates to a method of manufacturing a reusable print medium according to the present invention and a method of printing and recycling such a print medium.
本发明涉及一种可重复使用的打印介质(200),它包括一个基底(201)和一个牺牲层(202)。牺牲层包含一种热熔胶组合物,至少包括一种非晶材料。无定形材料是一种树脂,是第一单体 A 的反应产物,所述第一单体 A 是一种多羟基醇,包含 X 个羟基官能团,其中 X ≥ 2,单体 A 可选择包含伯胺或仲胺官能团;第二单体 B,为芳香族单羧酸; 第三单体 C,所述第三单体 C 能与醇形成酯连接和/或与伯胺或仲胺形成酰胺连接;以及 第四单体 D,为不同于第二单体 B 的芳香族单羧酸。可通过加热将包括印刷图像的牺牲层从基底上去除。然后再涂上一层新的牺牲层,这样可重复使用的打印介质就可以重复使用了。
本发明还涉及根据本发明制造可重复使用打印介质的方法,以及打印和回收这种打印介质的方法。