[EN] 6-6 OR 5-6 FUSED BICYCLIC COMPOUNDS COMPRISING A PYRI(MI)DINE RING USEFUL IN THE|TREATMENT OF INFECTIOUS DISEASES [FR] COMPOSÉS BICYCLIQUES FUSIONNÉS EN 6-6 OU 5-6 COMPRENANT UN CYCLE PYRI(MI)DINE UTILES DANS LE TRAITEMENT DE MALADIES INFECTIEUSES
摘要:
The present invention relates to new specific 6-6 or 5-6 fused bicyclic compounds comprising pyrimidine or pyridine useful in the prevention and/or treatment of infectious diseases. In particular, the present invention relates to a compound of formula (I) wherein : Ar1is a (C5-C11)arylene or (C5-C11)heteroarylene group, X is -CH-, -S-, -NR5or -N-, Y is -CH-, -NR5-S- or -NR6-CH2-, T is -CH- and Q is -CH- or T is -N- and Q is -CR10- or -N-, provided that one or two of X, Q and Y comprise a heteroatom, and with the proviso that, at least one of R1, R2, and, if present, R5or R6, contains a group -NH-Alk-NR3R4. The inventors showed that compounds of formula (I) present an activity against both W2 and 3D7 Plasmodium falciparum strains, an activity against T. brucei brucei but also an activity against SARS-CoV-2 virus, and that they are positive for G4 recognition. The invention also relates to the preparation process and to the therapeutic uses of the compounds of formula (I).
[EN] SUBSTITUTED TETRACYCLINE COMPOUNDS<br/>[FR] COMPOSÉS À BASE DE TÉTRACYCLINES SUBSTITUÉES
申请人:PARATEK PHARM INNC
公开号:WO2009128913A1
公开(公告)日:2009-10-22
The present invention pertains, at least in part, to methods of treating a microorganism-associated infection in a subject comprising administering to said subject an effective amount of a tetracycline compound.
本发明至少部分涉及治疗宿主微生物相关感染的方法,包括向宿主施用有效量的四环素化合物。
[EN] MODULATORS OF THE ADENOSINE A2A RECEPTOR<br/>[FR] MODULATEURS DU RÉCEPTEUR A2A DE L'ADÉNOSINE
申请人:RYVU THERAPEUTICS S A
公开号:WO2020128036A1
公开(公告)日:2020-06-25
The present invention relates to the compounds of formula (I) and salts, stereoisomers, tautomers, isotopologues, or N-oxides thereof. The present invention is further concerned with the use of such a compounds or salt, stereoisomer, tautomer, isotopologues, or N- oxide thereof as modulators of the adenosine A2A receptor in the treatment of cancer and a pharmaceutical composition comprising said compounds.
[EN] TGFBETAR2 INHIBITOR-LRRC15 ANTIBODY CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS INHIBITEUR DE TGFBETAR2-ANTICORPS ANTI-LRRC15 ET LEURS UTILISATIONS
申请人:SILVERBACK THERAPEUTICS INC
公开号:WO2021102332A1
公开(公告)日:2021-05-27
Conjugates comprising a TGFβR2 inhibitor and an anti-LRRC15 antibody, compositions comprising the conjugates, and use of the conjugates in the treatment of disease, such as fibrosis and cancer, are disclosed herein. Also disclosed herein are anti-LRRC15 antibodies, including humanized anti-LRRC15 antibodies.
Pyridopyrazines and derivatives thereof as alk and c-Met inhibitors
申请人:Dorsey D. Bruce
公开号:US20080032972A1
公开(公告)日:2008-02-07
The present invention provides a compound of Formula I
or a pharmaceutically acceptable salt form thereof, wherein A, L
1
, R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.
PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS
申请人:Dorsey Bruce D.
公开号:US20100048576A1
公开(公告)日:2010-02-25
The present invention provides a compound of Formula I
or a pharmaceutically acceptable salt form thereof, wherein A, L
1
, R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.