SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
申请人:BlinkBio, Inc.
公开号:US20170202970A1
公开(公告)日:2017-07-20
Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.
N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
申请人:Rodgers James D.
公开号:US20100298334A1
公开(公告)日:2010-11-25
The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I:
which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
[EN] 4-FLUOROPIPERIDINE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DE L'OREXINE DE TYPE COMPOSÉS DE 4-FLUOROPIPÉRIDINE
申请人:MERCK SHARP & DOHME
公开号:WO2014113303A1
公开(公告)日:2014-07-24
The present invention is directed to 4-fluoropiperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
[EN] CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS<br/>[FR] CARBOXAMIDES UTILISÉES EN TANT QU'INHIBITEURS DE PROTÉASE SPÉCIFIQUE DE L'UBIQUITINE
申请人:FORMA THERAPEUTICS INC
公开号:WO2019032863A1
公开(公告)日:2019-02-14
The present disclosure relates to modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors, and methods of using the inhibitors. The modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25 can be useful in the treatment of cancers, among other ailments.
[EN] DECAHYDROQUINOXALINE DERIVATIVES AND ANALOGS THEREOF<br/>[FR] DÉRIVÉS DE DÉCAHYDROQUINOXALINE ET LEURS ANALOGUES
申请人:OTSUKA PHARMA CO LTD
公开号:WO2013137479A1
公开(公告)日:2013-09-19
A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).