The synthesis of 2-morpholine carboxylic acid derivatives and their elaboration to 1-aza-4-oxabicyclo[3.3.1]nonan-6-one.
摘要:
Two syntheses of novel 2-morpholine carboxylic acid derivatives are described. The esters were converted into 1-aza-4-oxabicyclo[3.3.1]nonan-6-one, the first example of this ring system, which was further elaborated to the ortho-methoxy benzamide derivative (2).
[EN] NOVEL DIHYDROQUINOLIZINONES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION<br/>[FR] NOUVELLES DIHYDROQUINOLIZINONES POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION PAR LE VIRUS DE L'HÉPATITE B
申请人:HOFFMANN LA ROCHE
公开号:WO2015173164A1
公开(公告)日:2015-11-19
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, X and Y are as described in the description and in the claims, as well as or pharmaceutically acceptable salts, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
[EN] INDAZOLYL-SPIRO[2.3]HEXANE-CARBONITRILE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF<br/>[FR] DÉRIVÉS D'INDAZOLYL-SPIRO [2,3] HEXANE-CARBONITRILE COMME INHIBITEURS DE LRRK2, COMPOSITIONS PHARMACEUTIQUES, ET UTILISATIONS DE CEUX-CI
申请人:MERCK SHARP & DOHME
公开号:WO2019074810A1
公开(公告)日:2019-04-18
The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
[EN] SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE<br/>[FR] INHIBITEURS SPÉCIFIQUES DE LA MÉTHIONYL-TARN SYNTHÉTASE
申请人:UNIV WASHINGTON
公开号:WO2016029146A1
公开(公告)日:2016-02-25
The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
本公开涉及的是通常用于抑制MetRS的组合物和治疗通过抑制MetRS改善的疾病的方法。
4-Pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament
申请人:Boehringer Ingelheim International GmbH
公开号:US20200123140A1
公开(公告)日:2020-04-23
Disclosed are 4-pyrimidin-5-ylmethyl-morpholines of formula A
and pharmaceutically acceptable salts thereof, wherein R
1
and R
2
are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.
4-Pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament
申请人:Boehringer Ingelheim International GmbH
公开号:US20200121691A1
公开(公告)日:2020-04-23
Disclosed are 4-pyrazin-2-ylmethyl-morpholines of formula A
and pharmaceutically acceptable salts thereof, wherein R
1
and R
2
are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.