Synthèse et structure de dérivés amino-3 dihydro-4,5 1H-pyrazole; effets inhibiteurs sur la cyclooxygénase, la lipoxygénase, la thromboxane synthétase et l'agrégation plaquettaire
[EN] PYRAZOLYLAMINOBENZIMIDAZOLE DERIVATIVES AS JAK INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLYLAMINOBENZIMIDAZOLE EN TANT QU'INHIBITEURS DE JAK
申请人:LILLY CO ELI
公开号:WO2018013486A1
公开(公告)日:2018-01-18
The present invention provides compounds of the formula below (I'): where R, and R1-R3 are as described herein, methods of treating patients for certain types of autoimmune diseases and cancer, and processes for preparing the compounds.
Synthesis and Evaluation of the 2-Aminothiazoles as Anti-Tubercular Agents
作者:Edward A. Kesicki、Mai A. Bailey、Yulia Ovechkina、Julie V. Early、Torey Alling、Julie Bowman、Edison S. Zuniga、Suryakanta Dalai、Naresh Kumar、Thierry Masquelin、Philip A. Hipskind、Joshua O. Odingo、Tanya Parish
DOI:10.1371/journal.pone.0155209
日期:——
designing and synthesizing a large number of analogs and testing these for activity against M. tuberculosis, as well as eukaryotic cells. We determined that the C-2 position of the thiazole can accommodate a range of lipophilic substitutions, while both the C-4 position and the thiazole core are sensitive to change. The series has good activity against M. tuberculosis growth with sub-micromolar minimum
[EN] NITROGEN-CONTAINING HETEROARYL DERIVATIVES<br/>[FR] DÉRIVÉS HÉTÉROARYLIQUES CONTENANT DE L'AZOTE
申请人:HOFFMANN LA ROCHE
公开号:WO2011089132A1
公开(公告)日:2011-07-28
The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
[EN] 2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS<br/>[FR] INHIBITEURS DE TYROSINE KINASE DE LA RATE (SYK) CONTENANT UN 2-PYRIDYL CARBOXAMIDE
申请人:MERCK SHARP & DOHME
公开号:WO2013052394A1
公开(公告)日:2013-04-11
The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I)
wherein R
1
, R
2
, R
3
, R
4
, R
5
, A
1
, A
2
, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.