Tartrate salt of a substituted dipeptide as growth hormone secretagogue

本发明涉及2-氨基-N-{1-(R)-(2，4-二氟-卞氧甲基)-2-氧代-2-[3-氧代-3a-(R)-吡啶-2-基甲基-2-(2，2，2-三氟-乙基)-2，3，3a，4，6，7-六氢化-吡唑子基[4，3-c]吡啶-5-基]-乙基}-2-甲基-丙酰胺的(L)-(+)-酒石酸盐，它是一种生长激素促分泌素，并且可用于提高内源性生长激素水平。另一方面，本发明提供可用于合成上述化合物的某些中间体。本发明化合物的(L)-酒石酸盐可用于治疗和/或预防骨质疏松症、胰岛素抵抗以及其他与生长激素缺乏有关的状态或疾病。当本发明化合物的(L)-酒石酸盐与一种双膦酸盐化合物；雌激素或妊马雌酮和可任意选择的孕酮；一种雌激素兴奋剂或对抗剂；或降钙素联合使用时，还可用于治疗骨质疏松症。而且，本发明涉及药物组合物。本发明还涉及包括给予人或其他动物一种α-2肾上腺素能兴奋剂和本发明化合物的(L)-酒石酸盐的方法。 This invention is directed to the (L)-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo{4,3-c}pyridin-5-yl]-ethyl]-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compound. The (L)-tartaric acid salt of the compound of this invention is useful in the treatment and/or prevention of osteoporosis, insulin resistance and other conditions or diseases associated with growth hormone deficiency. The (L)-tartaric acid salt of the compound of the present invention is also useful in treating osteoporosis when used in combination with: a bisphosphonate compound; estrogen, Premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin. Further, the present invention is directed to pharmaceutical compositions. This invention is further directed to methods comprising administering to a human or other animal a combination of an alpha-2 adrenergic agonist and the (L)-tartaric acid salt of the compound of this invention.