INHIBITORS OF CRUZIPAIN AND OTHER CYSTEINE PROTEASES
申请人:Quibell Martin
公开号:US20090247471A1
公开(公告)日:2009-10-01
Compounds of general formula (I) or general formula (II):—
wherein R
1
, P
1
, P
2
, Q, Y, (X)
o
, (W)
n
, (V)
m
, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
BUNTYAKOV, A. S.;BUNTYAKOVA, N. A.;ZAXAROV, V. G.;LASHEK, N. A., XIMIYA I TEXNOL. FURANOV. SOED., KRASNODAR,(1987) 84-88
作者:BUNTYAKOV, A. S.、BUNTYAKOVA, N. A.、ZAXAROV, V. G.、LASHEK, N. A.
DOI:——
日期:——
US7425562B2
申请人:——
公开号:US7425562B2
公开(公告)日:2008-09-16
[EN] THIOTRIAZOLYL DERIVATIVES<br/>[FR] DERIVES DE THIOTRIAZOLYLE
申请人:EPIX DELAWARE INC
公开号:WO2007047394A2
公开(公告)日:2007-04-26
[EN] The invention relates to KvI.5 ion channel antagonists. Novel thiotriazolyl derivative compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by KvI.5 ion channels, are disclosed. Such conditions include numerous heart conditions including atrial fibrillation and other diseases; as well as epilepsy, anxiety, depression, age-related memory loss, migraine, obesity, Parkinson's disease or Alzheimer's disease. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided. [FR] L'invention concerne des antagonistes des canaux ioniques Kv1.5. Elle concerne notamment de nouveaux dérivés de thiotriazolyle représentés par la formule (I) ainsi que la synthèse et les utilisations de ceux-ci pour traiter des maladies médiées directement ou indirectement par les canaux ioniques Kv1.5. Ces maladies incluent diverses affections cardiaques, telles que la fibrillation auriculaire et d'autres maladies, ainsi que l'épilepsie, l'anxiété, la dépression, la perte de mémoire liée à l'âge, la migraine, l'obésité, la maladie de Parkinson ou la maladie d'Alzheimer. L'invention concerne en outre des procédés de préparation ainsi que de nouveaux produits intermédiaires et des sels pharmaceutiques correspondants.
Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow
作者:Yiding Chen、Marco Leonardi、Paul Dingwall、Ricardo Labes、Patrick Pasau、David C. Blakemore、Steven V. Ley
DOI:10.1021/acs.joc.8b02721
日期:2018.12.21
formaldehyde was used as a formylating reagent in a homologation reaction with nonstabilized diazo compounds, enabled by UV photolysis of bench-stable oxadiazolines in a flow photoreactor. Various aliphatic aldehydes were synthesized along with the corresponding derivatized alcohols and benzimidazoles. No transition-metal catalyst or additive was required to affect the reaction, which proceeded at room temperature