67704-17-0Relevant academic research and scientific papers
Discovery of histone deacetylase 8 selective inhibitors
Tang, Weiping,Luo, Tuoping,Greenberg, Edward F.,Bradner, James E.,Schreiber, Stuart L.
supporting information; experimental part, p. 2601 - 2605 (2011/06/22)
We have developed an efficient method for synthesizing candidate histone deacetylase (HDAC) inhibitors in 96-well plates, which are used directly in high-throughput screening. We selected building blocks having hydrazide, aldehyde and hydroxamic acid functionalities. The hydrazides were coupled with different aldehydes in DMSO. The resulting products have the previously identified 'cap/linker/biasing element' structure known to favor inhibition of HDACs. These compounds were assayed without further purification. HDAC8-selective inhibitors were discovered from this novel collection of compounds.
SINGLE ENANTIOMER BETA-AGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THE USE THEREOF AS MEDICATION
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Page/Page column 8, (2010/09/07)
The present invention relates to single enantiomer compounds of formula (1), where the moieties n, A, R1, R2, R3, m, and Y can have the meanings stated in the claims and in the description, methods for the production there
DRUG COMBINATIONS FOR THE TREATMENT OF RESPIRATORY TRACT DISEASES
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, (2010/01/31)
The present invention relates to novel drug combinations which, besides one or more, preferably on compound of the general formula (1), wherein remainder n, A, R1, R2, and R3 can have the meanings given in the claims and in the description comprise at least one further active ingredient 2 and method for the production thereof and the use thereof as drugs.
Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors
Vegas, Arturo J.,Bradner, James E.,Tang, Weiping,McPherson, Olivia M.,Greenberg, Edward F.,Koehler, Angela N.,Schreiber, Stuart L.
, p. 7960 - 7964 (2008/09/19)
(Figure Presented) Noncovalent immobilization is an attractive method for identifying inhibitors of histone deacetylases (HDACs). Fluorous-based small-molecule microarrays were validated as an effective method. Three enzymes and three assays (microarray, biochemical activity, and surface plasmon resonance) were used to identify inhibitors of HDACs and to compare them.
Long-acting betamimetics for the treatment of respiratory complaints
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Page/Page column 8, (2008/06/13)
The present invention relates to compounds of formula 1, wherein n, A, R1, R2 and R3 may have the meanings specified in the description and claims, processes for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
New long acting beta-2 agonists and their use as medicaments
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Page/Page column 7, (2010/02/13)
A compound of formula 1 wherein the groups R1, R2, R3, R4 and n may have the meanings given in the claims and in the specification, and methods for preparing a pharmaceutical composition for the treatment of inf
1, 3, 4-BENZOTRIAZEPIN-2-ONE SALTS AND THEIR USE AS CCK RECEPTOR LIGANDS
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Page 47, (2008/06/13)
This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+-O-; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is -(CR11R12)m-X-(CR13R14)p-R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR15=CR16-, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H ; C1 to C6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.
