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Use of compounds for the elevation of pyruvate dehydrogenase activity
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A compound and active technology, applied in the application field of compounds in enhancing the activity of pyruvate dehydrogenase, can solve the problem of increased availability of lactic acid
Inactive Publication Date: 2009-04-29
ASTRAZENECA AB
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Alternatively, a further effect of reduced PDH activity may be an increase in pyruvate concentration, with consequent increased availability of lactate, a substrate for hepatic gluconeogenesis
Method used
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[0747] In (R)-N-[2-chloro-4-(2-fluorobenzenesulfonyl)phenyl]-2-hydroxy-2-methyl-3,3,3-trifluoropropionamide (Method 63) ( Sodium methyl mercaptan (49.5 mg) was added to a solution of 0.15 g) in NMP (1.5 ml), the resulting mixture was heated at 120°C for 18 nitric acid, and then cooled. A saturated aqueous solution of ammoniumchloride (15ml) was added, and the mixture was extracted with ethyl acetate (2 x 50ml). The organic extracts were combined, washed with brine and dried. The volatile substances were removed by evaporation, and the residue was purified by chromatography on a silica gelMega Bond E1ur column using 0-20% ethyl acetate / hexane to obtain the title compound as a solid (0.10 g). NMR: (CDCl 3 ): 1.75(s, 3H), 2.4(s, 3H), 3.6(brs, 1H), 7.3(t, 1H), 7.35(t, 1H), 7.55(m, 1H), 7.9(dd, 1H) , 8.05 (d, 1H), 8.25 (dd, 1H), 8.6 (d, 1H), 9.25 (brs, 1H); MS (ESP - ): 45...
Embodiment 2-12
[0749] According to the method of Example 1, the following compounds were prepared using appropriate starting materials.
[0750] Example Compound NMR(CDCl 3 ) MS SM 2
[0751] 8
[0752] 1 Add three equivalents of sodium methyl mercaptan.
[0755] In (R)-N-[2-chloro-4-(2-methylthiobenzenesulfonyl)phenyl]-2-hydroxy-2-methyl-3,3,3-trifluoropropionamide (Example 1) Add m-chloroperbenzoic acid (50%, 0.293g) to a solution of (0.384g) in DCM (40ml). Stir the mixture at room temperature for 6 hours, and then use saturated aqueous sodiumbicarbonate (3 x 100ml), water ( 100ml) and brine, and then dried. The volatiles were removed by evaporation, and the residue was purified by chromatography on a silica gelMega Bond Elur column, eluting with 50-70% ethyl acetate / hexane to obtain the title compound as a solid (0.26 g). Mp 118-120℃; NMR(CDCl 3 ): 1.70 (s, 3H), 3.0 (m, 3H), 4.85 (brs, 1H), 7.75 (t, IH), 7.85 (m, 2H), 8.0 (m, 1H), 8.15 (d, 1H) , 8.3 (d, 1H), 8.65 (dd, 1H), 9.40 (brs, 1H); MS (ESP - ): 468; EA: Measured value: C, 44.3; H, 3.7; N, 2.6%; C 17 H 16 ClF 3 NO 5 S 2 ·0.125 C 4 H 8 O 2 ·0.3C 4 H 10 Ca...
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Abstract
The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R<1> is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R<2> and R<3> are as defined within; R<4> is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
Description
[0001] This application is a divisional application of Chinese patent application 99806754.7 (International application PCT / GB99 / 01669 entered the Chinese national phase) with the filing date of May 26, 1999. Technical field [0002] The present invention relates to compounds capable of enhancing the activity of pyruvate dehydrogenase (PDH), preparation methods thereof, pharmaceutical compositions containing them as active ingredients, methods for treating diseases related to reduced PDH activity, their application as medicines and their preparation The application of medicines for enhancing the activity of PDH in warm-blooded animals such as humans. Background technique [0003] In tissues, adenosine triphosphate (ATP) provides energy for the synthesis of complex molecules and produces muscle contraction. ATP is produced by the cleavage of energy-rich substrates such as glucose and long-chain free fatty acids. In oxidative tissues such as muscle, most of ATP is produced by acetyl...
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