C07D239/24

AMINE DERIVATIVES AS POTASSIUM CHANNEL BLOCKERS

The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

AMINE DERIVATIVES AS POTASSIUM CHANNEL BLOCKERS

The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

PYRIDINE OR PYRIMIDINE DERIVATIVES
20180258066 · 2018-09-13 · ·

The present invention relates to compounds of formula I

##STR00001##

wherein R.sup.1 is methyl; R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropylmethyl, or hydroxmethyl; R.sup.3 is Cl, F, CF.sub.3, methyl, methoxy, or cyclopropyl; R.sup.4 is hydrogen, methyl, F or Cl; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer.

The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING SAME

The present specification provides a heterocyclic compound and an organic light emitting device using the same.

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING SAME

The present specification provides a heterocyclic compound and an organic light emitting device using the same.

Compositions and methods for using fixed biological samples

The present disclosure provides compositions and methods for using fixed biological samples in partition-based assays. In at least one embodiment, the disclosure provides a composition comprising a fixed biological sample and an un-fixing agent contained in a partition, such as a discrete droplet. In some embodiments, the disclosure provides un-fixing agent compounds capable of catalytically cleaving crosslinks in fixed biological samples, particularly crosslinked nucleic acids, such as RNA.

Compositions and methods for using fixed biological samples

The present disclosure provides compositions and methods for using fixed biological samples in partition-based assays. In at least one embodiment, the disclosure provides a composition comprising a fixed biological sample and an un-fixing agent contained in a partition, such as a discrete droplet. In some embodiments, the disclosure provides un-fixing agent compounds capable of catalytically cleaving crosslinks in fixed biological samples, particularly crosslinked nucleic acids, such as RNA.

Pyridine and pyrimidine derivatives
10005736 · 2018-06-26 · ·

The present invention relates to compounds of formula I ##STR00001##
wherein R.sup.1 is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl or cyclopropyl; R.sup.3 is Cl, F, CF.sub.3, cyano, methyl, methoxy or cyclopropyl; R.sup.4 is hydrogen, methyl or F; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Pyridine and pyrimidine derivatives
10005736 · 2018-06-26 · ·

The present invention relates to compounds of formula I ##STR00001##
wherein R.sup.1 is CH.sub.3 R.sup.1 is methyl, ethyl, CF.sub.3, CH.sub.2OH, cyclopropyl or cyano, or R.sup.1 and R.sup.1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R.sup.2 is hydrogen, methyl, ethyl, isopropyl, tert-butyl or cyclopropyl; R.sup.3 is Cl, F, CF.sub.3, cyano, methyl, methoxy or cyclopropyl; R.sup.4 is hydrogen, methyl or F; X is N or CH; Y is N or CH; with the proviso that X and Y are not simultaneously CH;
or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

2-(PYRAZOLOPYRIDIN-3-YL)PYRIMIDINE DERIVATIVES AS JAK INHIBITORS

New 2-(pyrazolopyridin-3-yl)pyrimidine derivatives are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of Janus Kinases (JAK).