- Synthesis method of multi-configuration long-chain phenyl amino acid compound
-
The invention relates to a method for synthesizing a multi-configuration long-chain phenyl amino acid compound. The method comprises the following steps: reacting a compound shown in a formula I witha compound shown in a formula II or an isomer thereof in
- -
-
Paragraph 0071-0077; 0078-0084
(2021/03/05)
-
- Effective synthesis of optically active 3-phenyl-3-(3-trifluoromethyl) diazirinyl bishomophenylalanine derivatives
-
Effective incorporation of phenyldiazirine moiety on the acyl residue of L- and D- glutamic acid by Friedel-Crafts reactions with triflic acid developed simple preparation of bishomophenylalanine (bhPhe) for aromatics, which added a
- Murai, Yuta,Hatanaka, Yasumaru,Kanaoka, Yuichi,Hashimoto, Makoto
-
body text
p. 359 - 364
(2009/12/03)
-
- STEREOSELECTIVE PROCESS FOR THE SYNTHESIS OF (D)-2-AMINO-5-PHENYLPENTANOIC OR ALKYL ESTER THEREOF
-
The present invention provides a process for preparing a compound of formula (I); wherein R is a C1-C6 alkyl; or a salt thereof; comprising:(c) hydrolyzing (D,L)-N-acetyl-2-amino-5-phenylpentanoic acid with a suitable base in the pre
- -
-
Page/Page column 9-10
(2010/02/07)
-
- Treatment of insulin resistance with growth hormone secretagogues
-
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are 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 compounds and certain processes useful for the synthesis of said intermediates and the compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
- -
-
-
- Heterocyclic compounds
-
This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula I.
- -
-
-
- Spiro piperidines and homologs promote release of growth hormone
-
There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
- -
-
-