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US 4,487,761 AGranted
Dopamine .beta.-hydroxylase inhibitors
AssigneeMerck & Co., Inc.
InventorsLucille J. Cole, Leeyan Huang, Jerrold M. Liesch
Life of this patent
Estimating the term…
Abstract
Two fermentation isolates, C.sub.7 H.sub.9 NO.sub.4 and C.sub.6 H.sub.7 NO.sub.3, presumably trihydroxy, methyl-pyridine derivatives, are inhibitors of dopamine .beta.-hydroxylase. These natural product compounds are produced by fermentation of Streptoverticillium hiroshimense and each may prove useful as antihypertensive agents.
Claims6
A dopamine .beta.-hydroxylase inhibitor of structural formula I:
- ##STR4## empirical formula C.sub.7 H.sub.9 NO.sub.4, and physical chemical characteristics:
- a. colorless crystalline compound,
- b. acidic aqueous UV data:
- 276 nm 261 sh,
- c. basic aqueous UV data:
- 304 nm 227 sh,
- d. acidic NMR (D.sub.2 O) chemical shifts:
- 2.48 (s) 4.82 (s),
- e. basic NMR (D.sub.2 O) chemical shifts:
- 2.30 (s) 4.68 (s),
- f. mass spectral data:
- M.sup.+ 171.0525 (100%)
- 153. 0449 (54%)
- 125.0589 (32%)
- 112.0398 (74%),
- produced by the controlled aerobic fermentation of an aqueous nutrient medium by Streptoverticillium hiroshimense, ATCC 39070 at a temperature of 26.degree. to 30.degree. C. for at least 70 hours at pH 6.0 to 8.0.
13 more elements
A dopamine .beta.-hydroxylase inhibitor of structural formula II:
- ##STR5## empirical formula C.sub.6 H.sub.7 NO.sub.3, and physical chemical characteristics:
- a. colorless crystalline compound,
- b. acidic aqueous UV data:
- 276 nm 261 sh,
- c. basic aqueous UV data:
- 304 nm 228 sh,
- d. acidic NMR (D.sub.2 O) chemical shifts:
- 2.48 (s) 4.82 (s),
- e. basic NMR (D.sub.2 O) chemical shifts:
- 2.30 (s) 4.68 (s),
- f. mass spectral data:
- M.sup.+ 171.0525 (100%)
- 153. 0449 (54%)
- 125.0589 (32%)
- 112.0398 (74%),
- produced by the controlled aerobic fermentation of an aqueous nutrient medium by Streptoverticillium hiroshimense, ATCC 39070 at a temperature of 26.degree. to 30.degree. C. for a least 70 hours at pH 6.0 to 8.0.
13 more elements
Dependencies are inferred from the claim text.