KINETIC RESOLUTION REACTION OF A (1RS,2SR)-(2-HYDROXY-3,5,5-TRIMETHYL-3-CYCLOPENTENYL)METHYL CARBOXYLATE COMPOUND, A PROCESS FOR PREPARING OPTICALLY ACTIVE TRANS-alpha-NECRODYL ISOBUTYRATE, AND A PROCESS FOR PREPARING OPTICALLY ACTIVE gamma-NECRODYL ISOBUTYRATE
[EN] IMIDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH<br/>[FR] DÉRIVÉS IMIDAZOLE UTILES COMME INHIBITEURS DE LA FAAH
申请人:MERCK & CO INC
公开号:WO2009152025A1
公开(公告)日:2009-12-17
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
[EN] PYRAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH<br/>[FR] DÉRIVÉS DE PYRAZOLE UTILES COMME INHIBITEURS DE FAAH
申请人:MERCK & CO INC
公开号:WO2009151991A1
公开(公告)日:2009-12-17
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease
The present invention relates to compounds of formula
1
wherein A is an unsubstituted or substituted cyclic group; and
R is hydrogen or lower alkyl;
or a pharmaceutically acceptable acid addition salt thereof.
These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.
NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
申请人:Ryono Denis E.
公开号:US20080009465A1
公开(公告)日:2008-01-10
Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure
wherein
is a heteroaryl ring;
R
4
is —(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
), —(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
, —(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
, —(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10
), or —(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10
);
R
5
and R
6
are independently selected from H, alkyl and halogen;
Y is R
7
(CH
2
)
s
or is absent; and
X, n, Z, m, R
4
, R
5
, R
6
, R
7
, and s are as defined herein; or a pharmaceutically acceptable salt thereof.
A method for treating diabetes and related diseases employing the above compounds is also provided.
提供了磷酸酯和磷酸酯激活剂,因此在治疗糖尿病和相关疾病方面非常有用,并具有以下结构:
其中
是杂环芳基环;
R
4
为—(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
)、—(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
、—(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
、—(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10)
或—(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10)
;
R
5
和R
6
分别选择自H、烷基和卤素;
Y为R
7
(CH
2
)
s
或不存在;以及
X、n、Z、m、R
4
、R
5
、R
6
、R
7
和s如本文所定义;或其药用盐。
还提供了一种利用上述化合物治疗糖尿病和相关疾病的方法。
[EN] ROR-GAMMA INHIBITORS<br/>[FR] INHIBITEURS DE ROR-GAMMA
申请人:GLAXOSMITHKLINE IP DEV LTD
公开号:WO2019063748A1
公开(公告)日:2019-04-04
The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.