- SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
-
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
- -
-
Page/Page column 100
(2015/01/07)
-
- OLEFIN SUBSTITUTED OXINDOLES HAVING AMPK ACTIVITY
-
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
- -
-
Page/Page column 97
(2015/01/07)
-
- Convenient and practical synthesis of 6-chloro-2-(chloromethyl)- thiazolo[5,4-b]pyridine
-
(Chemical Equation Presented) A high-yielding and practical synthesis of 6-chloro-2-(chloromethyl)- thiazolo[5,4-b]pyridine starting from 2-amino-5-chloropyridine has been accomplished in a sequence of five steps. Copyright Taylor & Francis Group, LLC.
- Ding, Zi-Chun,Ma, Xiang,Zhou, Weicheng
-
experimental part
p. 2791 - 2796
(2012/07/28)
-
- HETEROARYL SULFONAMIDES AND CCR2
-
Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
- -
-
Page/Page column 91
(2008/06/13)
-
- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
-
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiv
- -
-
-
- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
-
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
- -
-
-
- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
-
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiv
- -
-
-
- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
-
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiv
- -
-
-
- Synthesis and SAR of 5-, 6-, 7- and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2(1H)-one as NMDA/glycine site antagonists
-
A series of 5-, 6-, 7- and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2(1H)-one was synthesized and assayed as NMDA/glycine receptor antagonists. The in vitro potency of these antagonists was determined by displacement of the glycine site radioligand [3H]5,7-dicholorokynurenic acid ([3H]DCKA) in rat brain cortical membranes. Selected compounds were also tested for functional antagonism using electrophysiological assays in Xenopus oocytes expressing cloned NMDA receptor (NR) 1A/2C subunits. Among the 5-, 6-, 7-, and 8-aza-3-aryl-4-hydroxyquinoline-2(1H)-ones investigated, 5-aza-7-chloro-4-hydroxy-3-(3-phenoxyphenyl)quinolin-2-(1H)-one (13i) is the most potent antagonist, having an IC50 value of 110 nM in [3H]DCKA binding and a Kb of 11 nM in the electrophysiology assay. Compound 13i is also an active anticonvulsant when administered systemically in the mouse maximum electroshock-induced seizure test (ED50 = 2.3 mg/kg, IP).
- Zhou, Zhang-Lin,Navratil, James M.,Cai, Sui Xiong,Whittemore, Edward R.,Espitia, Stephen A.,Hawkinson, Jon E.,Tran, Minhtam,Woodward, Richard M.,Weber, Eckard,Keana, John F.W.
-
p. 2061 - 2071
(2007/10/03)
-
