1313176-45-2Relevant articles and documents
AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 51, (2011/08/08)
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
Synthesis of hGRF (somatocrinin) in liquid phase and intermediate peptides
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, (2008/06/13)
A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF, (1) on the one hand, the following fragments: ______________________________________H--Ala--Arg--Ala--Arg--Leu--NH2 called hGRF Frag- (40-44) or ment A alaninamide (40)H--Gln--Glu--Arg--Gly--OH called hGRF Frag- (36-39) ment B'1H--Glu--Ser--Asn--OH called hGRF Frag- (33-35) ment B'2H--Ser--Arg--Gln--Gln--Gly--OH called hGRF Frag- (28-32) ment CH--Leu--Gln--Asp--Ile--Met--OH called hGRF Frag- (23-27) ment D'H--Arg--Lys--Leu--OH called hGRF Frag- (20-22) ment E'1______________________________________ to obtain the peptide K1 [(hGRF (20-44)] on the corresponding peptide having the sequence (20-40) and (2) on the other hand, the following fragments:______________________________________H--Gln--Leu--Ser--Ala called hGRF Frag- (16-19) ment F1H--Tyr--Arg--Lys--Val--Leu--Gly OH called hGRF Frag- (10-15) ment G1H--Ile--Phe--Thr--Asn--Ser--OH called hGRF Frag- (5-9) ment H1______________________________________ to obtain the peptide J [hGRF (5-19)] and thereafter to couple together the peptides J and K1 in order to form the peptide having the sequence hGRF (5-44) or hGRF (5-40) and finally to couple the resulting peptide with the peptide H-Tyr-Ala-Asp-Ala-H, called fragment I hGRF (1-4).
Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides
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, (2008/06/13)
The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
SYNTHESIS AND ABSOLUTE CONFIGURATION OF SUBSTITUTED MORPHOLINES
Bettoni, Giancarlo,Franchini, Carlo,Perrone, Roberto,Tortorella, Vincenzo
, p. 409 - 415 (2007/10/02)
We studied methods of stereospecific synthesis that enabled us to obtain variously substituted morpholinic compounds and to determine their absolute configuration.From a study of the chiroptical properties of synthetic N-(2-pyridyl-N-oxide) derivatives of optically active morpholines, it was possible to correlate the sign of the Cotton effect with the absolute configuration.This correlation agrees with that previously established for derivatives of the piperidine type.By evaluating the various contributions to the Cotton effect of substituents in positions 2 and 3, we established the absolute configuration of bicyclic compounds condensed in the two positions mentioned above.
Method of recovering primary and secondary amines
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, (2008/06/13)
A method of recovering primary or secondary amines from aqueous, organic or aquo-organic solutions of said amines by subjecting these solutions to distillation or rectification in the presence of carbonic acid.