[EN] RAS INHIBITORS, COMPOSITIONS AND METHODS OF USE THEREOF [FR] INHIBITEURS DE RAS, COMPOSITIONS ET PROCÉDÉS D'UTILISATION DE CEUX-CI
摘要:
There is provided a compound of formula (I), and its use for inhibiting RAS (wild type or mutant), for example HRAS, NRAS, and/or KRAS, and for the prevention or treatment of a disease or disorder associated with abnormal RAS activity, for example abnormal RAS activity caused by a mutation in RAS, including cancers with a mutated RAS. (I)
COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
申请人:Van Goor Fredrick F.
公开号:US20110098311A1
公开(公告)日:2011-04-28
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
[EN] SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS SUBSTITUÉS DE PYRAZOLO[1,5-A]PYRIDINES COMME INHIBITEURS DE LA KINASE RET
申请人:ARRAY BIOPHARMA INC
公开号:WO2017011776A1
公开(公告)日:2017-01-19
Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
[EN] 6,6-FUSED HETEROARYL PIPERIDINE ETHER ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR<br/>[FR] MODULATEURS ALLOSTÉRIQUES D'ÉTHER DE PIPÉRIDINE D'HÉTÉROARYLE 6,6-FUSIONNÉ DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE
申请人:MERCK SHARP & DOHME
公开号:WO2018118735A1
公开(公告)日:2018-06-28
The present invention is directed to 6,6-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
A compound of Formula I
in free or salt or solvate form, where R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, R
9
, R
10
and R
11
have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.