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    Process for preparing the releasing hormone of luteinizing hormone (LH) and of follicle stimulating hormone (FSH), salts and compositions thereof, and intermediates therefor
    2.
    发明授权
    Process for preparing the releasing hormone of luteinizing hormone (LH) and of follicle stimulating hormone (FSH), salts and compositions thereof, and intermediates therefor 失效
    制备促黄体激素（LH）和促卵泡激素（FSH）的释放激素及其盐及其组合物及其中间体的方法

    公开(公告)号：US4159980A

    公开(公告)日：1979-07-03

    申请号：US456343

    申请日：1974-03-29

    Applicant: Hans U. Immer ,  Verner R. Nelson ,  Manfred K. Gotz

    Inventor： Hans U. Immer ,  Verner R. Nelson ,  Manfred K. Gotz

    IPC: A61K38/00 ,  C07K5/097 ,  C07C103/52

    CPC classification number: C07K5/0821 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

    Abstract: A process for preparing the LH- and FSH-releasing hormone of the formula Ih-- pyr-- His-- Trp-- Ser-- Tyr-- Gly-- Leu-- Arg-- Pro-- Gly-- NH.sub.2which comprises the following steps: Condensing N-(5-oxo-L-prolyl)-L-histidine hydrazide by means of the azide method with L-tryptophan benzyl ester and treating the resulting compound with hydrazine hydrate to obtain N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophan hydrazide (II); treating N-[O-benzyl-N-carboxy-L-tyrosyl]glycine N-benzyl ester with ethyl chloroformate to obtain the corresponding mixed anhydride which is reacted with t-butyl carbazate to obtain the corresponding 2-carboxyhydrazide t-butyl ester which is hydrogenolyzed to N-L-tyrosylglycine 2-carboxyhydrazide t-butyl ester, and condensing the latter with N-carboxy-L-seryl N-benzyl ester 2,4-dinitrophenyl ester followed by hydrogenolysis of the reaction product to obtain N-(N-L-seryl-L-tyrosyl)glycine 2-carboxyhydrazide t-butyl ester (III); condensing N-carboxy-L-proline N-benzyl ester with glycine ethyl ester in the presence of dicyclohexylcarbodiimide, treating the resulting product with ammonia and then hydrogenolyzing, to obtain 2-[(L-prolyl)amino]acetamide, which is condensed with N-carboxy-N.sup.G -nitro-L-arginine N-t-butyl ester in the presence of dicyclohexylcarbodiimide and N-hydroxysuccinimide to obtain N-[N-(N-carboxy-N.sup.G -nitro-L-arginyl)-L-prolyl)]glycinamide N-t-butyl ester (IV); or alternatively condensing L-proline methyl ester with N-carboxy-N.sup.G -nitro-arginine N-t-butyl ester in the presence of dicyclohexylcarbodiimide, condensing the resulting product with glycine ethyl ester in the presence of dicyclohexylcarbodiimide, and treating the resulting product with ammonia to obtain the same compound IV as above; treating said compound IV with acid and then with N-carboxy-L-leucine N-benzyl ester 2,4,5-trichlorophenyl ester and hydrogenolyzing the resulting product in acetic acid, to obtain N-[N-[N-(N-L-leucyl)-L-arginyl]-L-prolyl]-glycinamide diacetate (V); condensing compound II with compound III by means of the azide method to obtain the hexapeptide N-[N-[N-[N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophyl]-L-seryl]-L-tyrosyl]glycine 2-carboxyhydrazide t-butyl ester, or condensing N-[N-(5-oxo-L-prolyl)-L-histidyl]-L-tryptophan with compound III in the presence of dicyclohexylcarbodiimide to obtain the same hexapeptide as above, and deprotecting and converting the latter to its trifluoroacetate salt (VI); and condensing compound V with compound VI by means of the azide method, to obtain the decapeptide of formula I which is isolated as the diacetate salt and optionally converted to other pharmaceutically acceptable salts.

    Derivatives of retro-enantio-somatostatin, intermediates therefor, and process therefor
    4.
    发明授权
    Derivatives of retro-enantio-somatostatin, intermediates therefor, and process therefor 失效
    复方生长抑素的衍生物，其中间体及其制备方法

    公开(公告)号：US4010260A

    公开(公告)日：1977-03-01

    申请号：US599448

    申请日：1975-07-28

    Applicant: Hans U. Immer ,  Nedumparambil A. Abraham ,  Verner R. Nelson

    Inventor： Hans U. Immer ,  Nedumparambil A. Abraham ,  Verner R. Nelson

    IPC: A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16

    Abstract: Compounds of the formula 1 or 1a ##STR1## IN WHICH R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 are disclosed. The compounds are obtained by a process which comprises the following step: preparing peptide fragments II, III, V and VII see below, by a series of condensations involving the reaction of an appropriately protected peptide having an activated ester group with an appropriately protected peptide having a free amino group; condensing ##STR2## by means of the azide method with ##STR3## followed by hydrogenolysis of the reaction product to obtain ##STR4## condensing the latter by means of the azide method with ##STR5## followed by treating the resulting compound with hydrazine hydrate to obtain ##STR6## condensing the latter by means of the azide method with ##STR7## in which R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 to obtain the linear protected peptide ##STR8## in which R is as defined herein; thereafter said linear peptide is transformed into the desired cyclic peptide of formula 1 by deprotecting and oxidizing processes. In addition, the linear, reduced form of the peptide of formula 1a is obtained by deprotection of the aforementioned linear peptide or by reduction of the cyclic peptide. The peptides of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed.

    Abstract translation: 式1或1a的化合物

    Novel hydrazinocarboxamide derivatives and preparation thereof
    7.
    发明授权
    Novel hydrazinocarboxamide derivatives and preparation thereof 失效
    新型氢氯氰菊酯衍生物及其制备方法

    公开(公告)号：US4000122A

    公开(公告)日：1976-12-28

    申请号：US565332

    申请日：1975-04-07

    Applicant: Amedeo Failli ,  Verner R. Nelson ,  Hans U. Immer ,  Manfred K. Gotz

    Inventor： Amedeo Failli ,  Verner R. Nelson ,  Hans U. Immer ,  Manfred K. Gotz

    IPC: C07D207/40 ,  C07K5/04 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07C243/00 ,  C07D207/40

    Abstract: .alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.8 is hydrogen, that when Y is lower alkoxy than R.sup.8 is lower alkyl and that when Y is amino R.sup.4 is lower alkyl, are disclosed herein along with the related .alpha.-hydrazino-carboxamide and .alpha.-(.alpha.'-acylhydrazino)carboxamide compounds of formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3 , R.sup.5 and R.sup.7 are as defind above and Y is lower alkoxy. These compounds possess antibacterial activity. Methods for their preparation and use are disclosed also.

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