[EN] NOVEL COMPOUNDS FOR USE IN CANCER<br/>[FR] NOUVEAUX COMPOSÉS DESTINÉS À ÊTRE UTILISÉS POUR LE CANCER
申请人:FUNDACION PARA LA INVESTIG MEDICA APLICADA
公开号:WO2018229139A1
公开(公告)日:2018-12-20
It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein X, L,R1, R 2, and R 3 are as defined herein, which are cancer cell differentiation inducing agents. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, in particular by cell differentiation therapy.
The present invention relates to compounds of formula I
wherein R
1a
to R
1e
and R
2
to R
5
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
本发明涉及以下式I的化合物
其中R
1a
至R
1e
和R
2
至R
5
如描述和权利要求中所定义,并且其药学上可接受的盐。这些化合物是糖皮质激素受体拮抗剂,可用于治疗和/或预防疾病,如糖尿病、血脂异常、肥胖、高血压、心血管疾病、肾上腺失调或抑郁症。
[DE] NEUE PYRIMIDIN-4,6-DICARBONSÄUREDIAMIDE ZUR SELEKTIVEN INHIBIERUNG VON KOLLAGENASEN<br/>[EN] NOVEL PYRIMIDINE-4,6-DICARBOXAMIDES FOR THE SELECTIVE INHIBITION OF COLLAGENASES<br/>[FR] NOUVEAUX DIAMIDES D'ACIDE PYRIMIDINE-4,6-DICARBOXYLIQUE POUR L'INHIBITION SELECTIVE DE COLLAGENASES
申请人:AVENTIS PHARMA GMBH
公开号:WO2004041788A1
公开(公告)日:2004-05-21
Pyrimidin-4.6-dicarbonsäurediamide der Formel (I), eignen sich zur selektiven Inhibition der Kollagenase (MMP 13). Die Pyrimidin-4,6-dicarbonsäurediamide können daher zur Behandlung degenerativer Gelenkerkrankungen eingesetzt werden.
Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --, R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one), R.sub.2 is hydrogen or C.sub.1-3 alkyl; R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl; m is zero or an integer from 1 to 4; and n is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof. The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.
Substituted benzene compounds as modulators of the glucocorticoid receptor
申请人:Hoffman-La Roche Inc.
公开号:US08138189B2
公开(公告)日:2012-03-20
The present invention relates to compounds of formula I
wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.