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公开(公告)号：US07312334B2
公开(公告)日：2007-12-25
申请号：US10530465
申请日：2003-11-18
IPC分类号： C07D471/02
CPC分类号： C07D471/04
摘要： In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula (V), which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula (IX, IXa).
摘要翻译： 一方面，本发明涉及一种制备式（V）中间体的一锅法，其可用于制备磷酸二酯酶-4的抑制剂：本发明还涉及一种制备磷酸二酯酶抑制剂的方法，其包含式 （IX，IXa）。
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公开(公告)号：US06909002B2
公开(公告)日：2005-06-21
申请号：US10690118
申请日：2003-10-21
IPC分类号： A61K31/4745 , C07D471/02 , C07D471/04
CPC分类号： C07D471/04
摘要： In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula
摘要翻译： 一方面，本发明涉及制备式V中间体的一锅法，其可用于制备磷酸二酯酶-4的抑制剂：本发明还涉及制备磷酸二酯酶抑制剂的方法，其包含式
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3.发明授权公开(公告)号：US06248717B1
公开(公告)日：2001-06-19
申请号：US09380886
申请日：1999-09-07
IPC分类号： A61K3805
CPC分类号： C07D401/06 , A61K38/06 , C07D471/04 , C07K5/0202 , C07K5/06191 , Y02P20/55 , A61K2300/00
摘要： 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.
摘要翻译： 本发明涉及2-氨基-N- {1-（2,4-二氟 - 苄氧基甲基）-2-氧代-2- [3-氧代-3a-吡啶-2-基] （2,2,2-三氟 - 乙基）-2,3,3a，4,6,7-六氢 - 吡唑并[4,3-c]吡啶-5-基] - 乙基] -2- 作为生长激素促分泌素的甲基丙酰胺，因此可用于增加内源性生长激素的水平。 在另一方面，本发明提供了可用于合成前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/或预防与生长激素缺乏相关的骨质疏松症，胰岛素抵抗和其它病症或疾病。 本发明化合物的（L） - 酒石酸盐与二膦酸盐化合物组合使用时也可用于治疗骨质疏松症。 雌激素，孕激素，以及孕激素; 雌激素激动剂或拮抗剂; 或降钙素。 此外，本发明涉及药物组合物。 本发明进一步涉及包括向人或其他动物施用α-2肾上腺素能激动剂和本发明化合物的（L） - 酒石酸盐的组合的方法。
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4.发明授权公开(公告)号：US06596867B2
公开(公告)日：2003-07-22
申请号：US09734269
申请日：2000-12-11
IPC分类号： C07D47102
CPC分类号： C07D401/06 , A61K38/06 , C07D471/04 , C07K5/0202 , C07K5/06191 , Y02P20/55 , A61K2300/00
摘要： This application relates to processes for making compounds of formula I, and processes for making intermediates useful in the processes for making compounds of formula I.
摘要翻译： 本申请涉及制备式I化合物的方法和制备用于制备式I化合物的方法的中间体的方法。
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