Convergent process for the preparation of a growth hormone secre

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D40100

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060463333

ABSTRACT:
The present invention is directed to a novel convergent process for the preparation of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.

REFERENCES:
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patent: 5723616 (1998-03-01), Houghton et al.
N. Sole, et al., Tetrahedron vol. 42, No. 1, pp. 193-198 (1986) "Mixed Anhydrides in Peptide Synthesis, Factors Affecting Urethane Formation and Racemization".
Sumitomo Seiyaku, Derwent Abst. 94-077374, (1994) "Cell Adhesion Peptide--for Suppression of Cancer Metastasis and Platelet Aggregation" (Japan).
Ioannis Houpis, et al., Presentation at Gordon Res. Conf. New Hmpton, NH, Jul. 14, 1996, "Synthesis of the Orally Active Nonpeptidal Growth Hormone Secretagogue, MK-677".
A. A. Patchett, et al., Proc. Natl. Acad, Sci., USA, vol. 92, pp. 7001-7005, (1995), "Design and Biological Activities of L-163-191 (MK-067): A Potent, Orally Active Growth Hormone Secretagogue".

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