(3AR,6AS)-5-羟基六氢环戊二烯并[C]吡咯-2(1H)-羧酸叔丁酯 、 盐酸 在
乙酸乙酯 作用下,
反应 2.0h,
以to afford the title compound as an off-white solid (2.84 g, 91%)的产率得到(3aalpha,5beta,6aalpha)-八氢环戊二烯并[c]吡咯-5-醇盐酸盐
CYCLOPENTA[C]PYRROLE-2-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
申请人:Abouabdellah Ahmed
公开号:US20120095040A1
公开(公告)日:2012-04-19
The invention relates to compounds of the general formula (I) where: R
2
is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C
1-6
-alkyl, C
1-6
-alkoxy, or NR
8
R
9
group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C
1-6
-alkylene group or a —O—C
1-6
-alkylene group in which the end that is an oxygen atom is bonded to the R
1
group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R
1
is an optionally substituted aryl or heteroaryl group; R
3
is a hydrogen or fluorine atom or a C
1-6
-alkyl or trifluoromethyl group; R
4
is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.
Cyclopenta[C]pyrrole-2-carboxylate derivatives, preparation thereof and therapeutic use thereof
申请人:Abouabdellah Ahmed
公开号:US08697883B2
公开(公告)日:2014-04-15
The invention relates to cyclopenta[c]pyrrole-2-carboxylate derivatives, to their preparation and to their therapeutic use.
本发明涉及环戊[c]吡咯-2-羧酸酯衍生物的制备及其治疗用途。
3H-thieno[3,4]pyrimidin-4-one and pyrrolopyrimidone as gram-positive antibacterial agents
申请人:LABORATOIRE BIODIM
公开号:EP2913333A1
公开(公告)日:2015-09-02
The invention relates to novel heteroaromatic derivatives of formula (I) and their addition salts thereof with acids and bases; their preparation, their use as drugs and pharmaceutical compositions and associations containing them.
wherein A, B, T, V, X and Y represent organic substituents as defined herein,
The compounds of formula (I) are able to inhibit the activity of the Gram-positive bacterial DltA enzyme and they are used to prevent and/or treat Gram-positive bacterial infections in humans or animals, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity,
本发明涉及式(I)的新型杂芳香族衍生物及其与酸和碱的加成盐;它们的制备、作为药物和药物组合物的用途以及含有它们的组合物。
其中 A、B、T、V、X 和 Y 代表本文定义的有机取代基、
式(I)化合物能够抑制革兰氏阳性菌 DltA 酶的活性,它们可单独或与抗菌剂、抗病毒剂或增强宿主先天免疫力的药物一起用于预防和/或治疗人或动物的革兰氏阳性菌感染、
Bicyclic derivatives
申请人:Hoffmann-La Roche Inc.
公开号:US10669268B2
公开(公告)日:2020-06-02
The invention provides novel compounds having the general formula (I)
wherein R1, Y, A, W, R2, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds.
[EN] 3H-THIENO[3,4]PYRIMIDIN-4-ONEAND PYRROLOPYRIMID-4-ONE AS GRAM-POSITIVE ANTIBACTERIAL AGENTS<br/>[FR] 3H-THIÉNO[3,4]PYRIMIDIN-4-ONE ET PYRROLOPYRIMID-4-ONE UTILISÉES COMME AGENTS ANTIBACTÉRIENS CONTRE LES BACTÉRIES À GRAM POSITIF