- Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase
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A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.
- Tarver, James E.,Pabba, Praveen K.,Barbosa, Joseph,Han, Qiang,Gardyan, Michael W.,Brommage, Robert,Thompson, Andrea Y.,Schmidt, James M.,Wilson, Alan G.E.,He, Wei,Lombardo, Victoria K.,Carson, Kenneth G.
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p. 1525 - 1528
(2016/07/27)
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- AlCl3-induced (hetero)arylation of thienopyrimidine ring: a new synthesis of 4-substituted thieno[2,3-d]pyrimidines
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AlCl3 facilitated C-C bond forming reaction between 4-chloro-thieno[2,3-d]pyrimidines and (hetero)arenes affording a direct and single-step method for the synthesis of 4-(hetero)aryl substituted thieno[2,3-d]pyrimidines. A number of novel thien
- Kumar, K. Shiva,Chamakuri, Srinivas,Vishweshwar, Peddy,Iqbal, Javed,Pal, Manojit
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supporting information; experimental part
p. 3269 - 3273
(2010/07/18)
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- NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention relates to a novel thienopyrimidine derivative having an excellent anti? inflammatory and anti-cancer activity, or a pharmaceutically acceptable salt thereof, a process for the preparation thereof and a pharmaceutical composition comprising the same. The compound according to the present invention strongly inhibits IKB kinase-β (IKK-β) involved in the activation of a transcriptional factor, NF-κB, which is associated with inducing various immune and inflammatory diseases, whereby a composition comprising the compound is a useful therapeutic agent against inflammatory diseases, in particular, arthritis and cancer.
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- COMPOUND HAVING TGF-BETA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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The present invention provides compounds of formula (I) or compounds of formula (II) and pharmaceutically acceptable salts or solvates thereof. An objective of the present invention is to provide compounds having TGF2 inhibitory activity.
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Page/Page column 53
(2010/11/24)
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- SUBSTITUTED AMINOPYRIMIDINES AS NEUROKININ ANTAGONISTS
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The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central ner
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- THIENOPYRIMIDINE DERIVATIVES AS POTASSIUM CHANNEL INHIBITORS
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The present invention provides thienopyrimidine compounds which are potasium channels inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also provided.
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- INHIBITORS OF FUNGAL INVASION
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This invention relates to various anti-fungall agents including agents that are inhibitors of fungal invasion.
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Drawing sheet 30
(2010/02/09)
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- Thienopyrimidine derivatives
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4-Substituted-thieno[2,3-d], [3,2-d], and [3,4-d]pyrimidines having fungicidal, insecticidal, and miticidal utility are disclosed. Related 3-substituted-thieno[2,3-d], [3,2-d], and [3,4-d]pyrimidin-4-(3H)-imines are useful as fungicides, insecticides, and
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