- EP300/CREBBP INHIBITOR
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The present invention provides a compound having excellent histone acetyltransferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.
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- Stereoselective radiosynthesis of L- and D-3-[18F]fluoro-α-methyltyrosine
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A three-step radiosynthesis is described which allows for the first time the preparation of L- and D-3-[18F]fluoro-α-methyltyrosine starting from [18F]fluoride. Corresponding 3-fluoro-4-formyl-benzylated Sch?llkopf derivatives were
- Castillo Meleán, Johnny,Humpert, Sven,Ermert, Johannes,Coenen, Heinz H.
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p. 202 - 207
(2015/08/19)
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- AROMATASE INHIBITOR
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There is provided a compound of formula (I) wherein Z is selected from N and CR22, wherein R22 is H or a bond with D, wherein D is selected from a bond, C=O, and linear or branched hydrocarbon groups having a carbon chain of from 1 t
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- PHARMACEUTICAL COMPOSITION COMPRISING A PYRAZOLE-O-GLUCOSIDE DERIVATIVE
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The invention relates toa pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the trea
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- Dual aromatase-steroid sulfatase inhibitors
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By introducting the steroid sulfatase inhibitory pharmacophore into aromatase inhibitor 1 (YM511), two series of single agent dual aromatase-sulfatase inhibitors (DASIs) were generated. The best DASIs in'vitro (JEG-3 cells) are 5, (IC50(aromatase) = 0.82 nM; IC 50(sulfatase) = 39 nM), and 14, (IC50(aromatase) = 0.77 nM; IC50(sulfatase) = 590 nM). X-ray crystallography of 5, and docking studies of selected compounds into an aromatase homology model and the steroid sulfatase crystal structure are presented. Both 5 and 14 inhibit aromatase and sulfatase in PMSG pretreated adult female Wistar rats potently 3 h after a single oral 10 mg/kg dose. Almost complete dual inhibition is observed for 5 but the levels were reduced to 85% (aromatase) and 72% (sulfatase) after 24 h. DASI 5 did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed.
- Woo, L. W. Lawrence,Bubert, Christian,Sutcliffe, Oliver-B.,Smith, Andrew,Chander, Surinder K.,Mahon, Mary F.,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
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p. 3540 - 3560
(2008/02/09)
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- METHODS FOR PREVENTING AND TREATING METABOLIC DISORDERS AND NEW PYRAZOLE-O-GLYCOSIDE DERIVATIVES
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The invention relates to methods for preventing or treating metabolic disorders, for improving glycemic control, for preventing progression from impaired glucose tolerance, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, for
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Page/Page column 33
(2010/11/25)
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- Compound
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There is provided a compound of Formula I 1 wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C═O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.
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Page/Page column 60
(2008/06/13)
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