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21 条记录 (耗时 0.021 秒)

    Process for producing triglycyl-lysine vasopressin and intermediates therefor
    3.
    发明授权
    Process for producing triglycyl-lysine vasopressin and intermediates therefor 失效
    制备三甘氨酰赖氨酸加压素及其中间体的方法

    公开(公告)号：US4093610A

    公开(公告)日：1978-06-06

    申请号：US763772

    申请日：1977-01-31

    申请人： Nedumparambil A. Abraham ,  Hans U. Immer ,  Kazimir Sestanj

    发明人： Nedumparambil A. Abraham ,  Hans U. Immer ,  Kazimir Sestanj

    IPC分类号： A61K38/00 ,  C07K7/16 ,  C07C103/52 ,  C07G7/00

    CPC分类号： C07K7/16 ,  A61K38/00 ,  Y10S930/15

    摘要： A new process for preparing the cyclic dodecapeptide triglycyl-lysine vasopressin of the formula ##STR1## which comprises the preparation of a first hexapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--NHNH.sub.2 and a second hexapeptide of formula H--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxyl with an appropriately protected peptide having a free amino group. Subsequently, the first and second hexapeptides are condensed according to the azide coupling method to obtain the linear protected dodecapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 ; thereafter the linear protected dodecapeptide is transformed into the desired cyclic dodecapeptide, triglycyllysine vasopressin, by oxidizing and deprotecting processes.

    摘要翻译： 制备式“IMAGE”的环十二肽三缩水甘油基赖氨酸加压素的新方法，其包括制备式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-NHNH 2的第一六肽和第二个六肽 通过一系列缩合产生式H-Gln（Mbh）-Asn（Mbh）-Cys（Trt）-Pro-Lys（Boc）-Gly-NH 2）的反应，该缩合涉及适当保护的具有活性羧基的肽单元与适当的 具有游离氨基的保护肽。 随后，根据叠氮偶合法将第一和第二六肽缩合，得到式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-Gln（Mbh）-Asn（Mbh） - Cys（Trt）-Pro-Lys（Bo c）-Gly-NH 2; 此后，通过氧化和脱保护过程将线性保护的十二肽转化成所需的环十二肽，甘氨酰赖氨酸加压素。

    Process for preparing the releasing hormone of luteinizing hormone (LH) and of follicle stimulating hormone (FSH), salts and compositions thereof, and intermediates therefor
    4.
    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

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

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

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

    CPC分类号： C07K5/0821 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

    摘要： 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
    6.
    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

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

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

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

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16

    摘要： 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.

    摘要翻译： 式1或1a的化合物

    Novel hydrazinocarboxamide derivatives and preparation thereof
    8.
    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

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

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

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

    CPC分类号： C07C243/00 ,  C07D207/40

    摘要： .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.

    N-substituted dimeric cyclopeptide derivatives and preparation thereof
    9.
    发明授权
    N-substituted dimeric cyclopeptide derivatives and preparation thereof 失效
    N-取代二聚环肽衍生物及其制备方法

    公开(公告)号：US4252795A

    公开(公告)日：1981-02-24

    申请号：US941532

    申请日：1978-09-11

    申请人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    发明人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    IPC分类号： C07K5/12 ,  C07K7/64 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/64 ,  C07K5/12 ,  Y10S930/19 ,  Y10S930/27

    摘要： The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or pheny(lower) alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式（I）的N-取代二聚环肽衍生物，其中A是具有1-4个氨基酸残基的肽残基; R1是低级烷基，苯基或苯基（低级）亚烷基; R2是低级烷基，环（低级）烷基或低级烷氧基羰基（低级）亚烷基; R3是中性氨基酸侧链，并且公开了制备式I化合物的方法。 式I化合物可用于治疗微生物感染。 也公开了药物组合物。