The present invention provides compounds of the Formula I and II:
1
wherein R
1
, R
3
, W, Z, X
1
, X
2
, Ar
1
, R
8
and R
9
are as defined herein, and methods and intermediates for their preparation and uses thereof.
[EN] PYRROLOPYRAZINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE PYRROLOPYRAZINE KINASE
申请人:HOFFMANN LA ROCHE
公开号:WO2013030138A1
公开(公告)日:2013-03-07
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Remote C(sp<sup>3</sup>)–H Oxygenation of Protonated Aliphatic Amines with Potassium Persulfate
作者:Melissa Lee、Melanie S. Sanford
DOI:10.1021/acs.orglett.6b03731
日期:2017.2.3
the development of a method for selective remoteC(sp3)–H oxygenation of protonated aliphatic amines using aqueous potassium persulfate. Protonation serves to deactivate the proximal C(sp3)–H bonds of the amine substrates and also renders the amines soluble in the aqueous medium. These reactions proceed under relatively mild conditions (within 2 h at 80 °C with amine as limiting reagent) and do not
This invention relates to the compounds represented by a general formula [I]:
1
[in which A
1
and A
2
represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C
3
-C
20
aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.