DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
申请人:ALTENBURGER Jean-Michel
公开号:US20110294788A1
公开(公告)日:2011-12-01
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
本发明涉及新型取代二氢吡唑酮衍生物,其制备以及作为转录因子HIF激活剂的治疗用途。
NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
申请人:FUJIFILM Corporation
公开号:US20160168139A1
公开(公告)日:2016-06-16
There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof.
(In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z
2
represents CH or the like; Z
1
represents CR
6
or the like; R
6
represents a hydrogen atom or the like; X
1
represents CHR
7
or the like; R
7
represents a hydrogen atom or the like; X
2
represents CH
2
or the like; R
1
and R
2
are the same as or different from each other, and each of R
1
and R
2
represents a hydrogen atom or the like; R
3
, R
4
, and R
5
are the same as or different from each other, and each of R
3
, R
4
, and R
5
represents a hydrogen atom, NR
a
R
b
, or the like; and each of R
a
and R
b
represents a hydrogen atom, a C
1-8
alkyl group which may have a substituent, or the like.)
提供一种由通用式[1A]表示的吗啉衍生物或其盐。
(在该式中,环A代表由通用式[I]表示的环;*代表连接位置;Z
2
代表CH或类似物;Z
1
代表CR
6
或类似物;R
6
代表氢原子或类似物;X
1
代表CHR
7
或类似物;R
7
代表氢原子或类似物;X
2
代表CH
2
或类似物;R
1
和R
2
相同或不同,且R
1
和R
2
中的每一个代表氢原子或类似物;R
3
,R
4
和R
5
相同或不同,且R
3
,R
4
和R
5
中的每一个代表氢原子,NR
a
R
b
或类似物;R
a
和R
b
中的每一个代表氢原子,可能具有取代基的C
1-8
烷基基团,或类似物。)
AMINES OR AMINO ALCOHOLS AS GLYT1 INHIBITORS
申请人:Kolczewski Sabine
公开号:US20100210592A1
公开(公告)日:2010-08-19
The invention relates to the use of compounds of formula I
wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
Cp*Rh<sup>III</sup>-Catalyzed Arylation of C(sp<sup>3</sup>)H Bonds
作者:Xiaoming Wang、Da-Gang Yu、Frank Glorius
DOI:10.1002/anie.201503888
日期:2015.8.24
The first Cp*RhIII‐catalyzed arylation of unactivated C(sp3)Hbonds is presented. The unactivated primary C(sp3)H bond of 2‐alkylpyridines can be activated by RhIII and further reacts with triarylboroxines to efficiently build new C(sp3)aryl bonds. The methodology also provides a facile and efficient synthesis of unsymmetrical triarylmethanes by RhIII‐catalyzed C(sp3)Harylation of diarylmethanes
FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
申请人:Gilead Sciences, Inc.
公开号:US20130184255A1
公开(公告)日:2013-07-18
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:
wherein Z
1
, Z
2
, Z
3
, Z
4
, X, Y, R
2
, R
3
and R
4
are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.