Regioselective synthesis of 1-alkyl-5-(indol-3-yl- and -2-yl)pyrrolidin-2-ones from available reagents
摘要:
The reaction under mild conditions of 1-alkyl-5-hydroxypyrrolidin-2-ones with different indoles having a free 3 position leads exclusively to 1-alkyl-5-(indol-3-yl)pyrrolidin-2-ones but if position 3 is occupied to 1-alkyl-5-(indol-2-yl)pyrrolidin-2-ones.
Regioselective synthesis of 1-alkyl-5-(indol-3-yl- and -2-yl)pyrrolidin-2-ones from available reagents
摘要:
The reaction under mild conditions of 1-alkyl-5-hydroxypyrrolidin-2-ones with different indoles having a free 3 position leads exclusively to 1-alkyl-5-(indol-3-yl)pyrrolidin-2-ones but if position 3 is occupied to 1-alkyl-5-(indol-2-yl)pyrrolidin-2-ones.
[EN] PROCESSES FOR MAKING, AND METHODS OF USING, GLYCOPYRRONIUM COMPOUNDS<br/>[FR] PROCÉDÉS DE FABRICATION ET PROCÉDÉS D'UTILISATION DE COMPOSÉS GLYCOPYRRONIUM
申请人:DERMIRA INC
公开号:WO2018026869A1
公开(公告)日:2018-02-08
Provided herein are processes for making and methods of using salts of glycopyrronium, including solid forms and forms suitable for use as topicals. Disclosed here are processes for making salts of glycopyrronium, also processes for making compositions comprising salts of glycopyrronium, and methods of treating hyperhidrosis with salts of glycopyrronium as well as with compositions comprising salts of glycopyrronium such as, but not limited to, topical compositions. Disclosed herein are methods of treating hyperhidrosis including administering salts of glycopyrronium to subjects in need thereof.
Versatile and Sustainable Synthesis of Cyclic Imides from Dicarboxylic Acids and Amines by Nb<sub>2</sub>O<sub>5</sub>as a Base-Tolerant Heterogeneous Lewis Acid Catalyst
作者:Md. Ayub Ali、S. M. A. Hakim Siddiki、Kenichi Kon、Junya Hasegawa、Ken-ichi Shimizu
DOI:10.1002/chem.201404538
日期:2014.10.27
Catalytic condensation of dicarboxylicsacid and amines without excess amount of activating reagents is the most atom‐efficient but unprecedented synthetic method of cyclicimides. Here we present the first general catalytic method, proceeding selectively and efficiently in the presence of a commercial Nb2O5 as a reusable and base‐tolerant heterogeneousLewisacidcatalyst. The method is effective for
二羧酸和胺的催化缩合反应没有过量的活化剂是最高效,最空前的环状酰亚胺合成方法。在这里,我们介绍了第一种通用催化方法,该方法在作为可重用和耐碱多相路易斯酸催化剂的商业Nb 2 O 5的存在下选择性而有效地进行。该方法可有效地从二羧酸或酸酐与胺,羟胺或氨直接合成药学上或工业上重要的环状酰亚胺,例如苯甲酰亚胺,N-羟基邻苯二甲酰亚胺(NHPI)和未取代的环状酰亚胺。
[EN] HETEROCYCLIC SUBSTITUTED 4-(AMINOMETHYL)-PIPERIDINE BENZAMIDES AS 5HT4-ANTAGONISTS<br/>[FR] 4-(AMINOMETHYL)-PIPERIDINE BENZAMIDES SUBSTITUES PAR DES HETEROCYCLES, UTILISES COMME ANTAGONISTES DES RECEPTEURS 5HT4
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2005003124A1
公开(公告)日:2005-01-13
The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.
METHOD FOR STEREOSELECTIVELY PRODUCING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVE
申请人:Shionogi & Co., Ltd.
公开号:EP3693373A1
公开(公告)日:2020-08-12
The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity.
In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.
LINKER, ANTIBODY-DRUG CONJUGATE INCLUDING SAME, AND USE THEREOF
申请人:Academy of Military Medical Sciences
公开号:EP3838893A1
公开(公告)日:2021-06-23
Provided are a linker represented by Formula I or I', an antibody-drug conjugate containing the same, and use of thereof, a pharmaceutical composition comprising the antibody-drug conjugate, and use of the antibody-drug conjugate for treating and/or preventing a disease.
本文提供了一种由式 I 或式 I'表示的连接体、一种含有该连接体的抗体-药物共轭物及其用途、一种含有该抗体-药物共轭物的药物组合物,以及该抗体-药物共轭物在治疗和/或预防疾病方面的用途。