氧杂环丁烷是药物相关合成中的多功能构建基块,可诱导性能调节作用。尽管相关的氧杂环丁烷广泛用于与二氧化碳(CO 2)偶联的化学反应中,以提供增值的商品化学品,但是尽管这些四元杂环的合成取得了新进展,但氧杂环丁烷/ CO 2的偶联仍然极为有限。在这里,我们报告了一种有效的单锅三组分反应(3CR)策略,用于偶联(取代的)氧杂环丁烷,胺和CO 2可以提供具有出色的化学选择性和高收率的各种功能化氨基甲酸酯。该过程由铝基催化剂在相对温和的条件下介导,并且已开发的催化方法可用于两种药学上相关的氨基甲酸酯的正式合成,其中3CR是关键步骤。
氧杂环丁烷是药物相关合成中的多功能构建基块,可诱导性能调节作用。尽管相关的氧杂环丁烷广泛用于与二氧化碳(CO 2)偶联的化学反应中,以提供增值的商品化学品,但是尽管这些四元杂环的合成取得了新进展,但氧杂环丁烷/ CO 2的偶联仍然极为有限。在这里,我们报告了一种有效的单锅三组分反应(3CR)策略,用于偶联(取代的)氧杂环丁烷,胺和CO 2可以提供具有出色的化学选择性和高收率的各种功能化氨基甲酸酯。该过程由铝基催化剂在相对温和的条件下介导,并且已开发的催化方法可用于两种药学上相关的氨基甲酸酯的正式合成,其中3CR是关键步骤。
SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:OOST Thorsten
公开号:US20140057916A1
公开(公告)日:2014-02-27
This invention relates to substituted 4-pyridones of formula 1
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
[EN] NAMPT MODULATORS<br/>[FR] MODULATEURS DE NAMPT
申请人:CYTOKINETICS INC
公开号:WO2021159015A1
公开(公告)日:2021-08-12
Provided are compounds of Formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and p are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.
[EN] NOVEL INDAZOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION<br/>[FR] NOUVEAUX INDAZOLES POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION PAR LE VIRUS RESPIRATOIRE SYNCYTIAL
申请人:HOFFMANN LA ROCHE
公开号:WO2014009302A1
公开(公告)日:2014-01-16
The invention provides novel compounds having the general formula: formula (I) wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
申请人:Hoffmann-La Roche Inc.
公开号:US20160200741A1
公开(公告)日:2016-07-14
The invention provides novel compounds having the general formula:
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
7
, A
1
, A
2
and A
3
are as described herein, compositions including the compounds and methods of using the compounds.
[EN] PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE LA PIPÉRIDINONE EN TANT QU'INHIBITEURS DE MDM2 POUR LE TRAITEMENT DU CANCER
申请人:AMGEN INC
公开号:WO2011153509A1
公开(公告)日:2011-12-08
The present invention provides MDM2 inhibitor compounds of Formula (I), wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.