[EN] IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES [FR] DÉRIVÉS D'IMIDAZO[4, 5-C]PYRIDINES UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES
To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2–27 showed binding affinity (IC50 = 4.2–418 nM) and antagonist activity (EC50 = 4.0–889 nM). Compound 5
为了鉴定结构上新颖的CRF1受体拮抗剂,使用了一系列双环核心拮抗剂,吡唑并[1,5-a]嘧啶,三唑并[1,5- a ]嘧啶,咪唑并[1,2- a ]嘧啶和吡唑并[1,5]。 -设计,合成和评价a ] [1,3,5]三嗪作为CRF1受体拮抗剂。化合物2 – 27表现出结合亲和力(IC 50 = 4.2–418 nM)和拮抗剂活性(EC 50 = 4.0–889 nM)。在大鼠的Elevated Plus Maze测试中,发现化合物5显示出口服功效。它们的进一步化学修饰使我们发现了三环核心拮抗剂吡唑并[1,5- a ]吡咯并[3,2- e]嘧啶。介绍了这些化合物的发现过程,以及对结构与活性关系的研究。
Method for producing oligomer and catalyst
申请人:ENEOS Corporation
公开号:US10815317B2
公开(公告)日:2020-10-27
The present invention provides a method for preparing an oligomer and a catalyst comprising a step of oligomerizing a polymerizable monomer containing an olefin in the presence of a catalyst, which comprises (A) a complex of a diimine compound and at least one metal selected from the group consisting of Group 8 elements, Group 9 elements and Group 10 elements, (B) a mixture of a pyridine diimine compound and an iron salt and/or an iron complex, (C) methylaluminoxane and/or a boron compound, and (D) an organoaluminum compound other than methylaluminoxane and/or an organozinc compound. The components (A), (B), (C) and (D) described above are respectively as defined in the present Description.
Catalytic enantioselective directed methylene C(sp3 )-H amidation reactions of 8-alkylquinolines using a Cp*RhIII /chiralcarboxylicacid (CCA) hybrid catalytic system are described. A binaphthyl-based chiralcarboxylicacid efficiently differentiates between the enantiotopic methylene C-H bonds, which leads to the formation of C-N bonds with good enantioselectivity.
[EN] SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRAZINONES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE<br/>[FR] ARYLE POLYCYCLIQUE SUBSTITUTE ET PYRAZINONES D'HETEROARYLE UTILISES DANS L'INHIBITION SELECTIVE DE LA COAGULATION
申请人:PHARMACIA CORP
公开号:WO2001087854A1
公开(公告)日:2001-11-22
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.