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    Tripeptide derivatives with central nervous system activity and preparation thereof
    1.
    发明授权
    Tripeptide derivatives with central nervous system activity and preparation thereof 失效
    具有中枢神经系统活性的三肽衍生物及其制备方法

    公开(公告)号：US4018912A

    公开(公告)日：1977-04-19

    申请号：US599450

    申请日：1975-07-28

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

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

    IPC分类号： C07K5/08 ,  A61K38/00 ,  A61K38/06 ,  A61P25/00 ,  C07K1/02 ,  C07K1/113 ,  C07K5/097 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/0823 ,  Y02P20/55

    摘要： The tripeptide derivatives of formula 1H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

    摘要翻译： 式1的HL-Pro-N（R1）CH（R2）CO-Y-R3（1）的三肽衍生物，其中R 1是氢，低级烷基或NR 4 R 5，其中R 4和R 5各自是低级烷基，R 2是氢或更低 烷基，R3是氨基，低级烷基氨基，二（低级）烷基氨基或氨基（低级）烷基氨基，Y是氨基酸残基Gly或D-Ala之一，条件是当R 1是NR 4 R 5时，其中R 4和R 5如本文所定义 并且R 2和Y如本文所定义，R 3是低级烷基氨基，二（低级）烷基氨基或氨基（低级）烷基氨基，并且公开了其制备方法。 式1的三肽衍生物具有中枢神经系统活性，并给出了其使用方法。

    N-substituted dimeric cyclopeptide derivatives and preparation thereof
    2.
    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。

    Tripeptide derivatives with central nervous system activity and preparation thereof
    3.
    再颁专利
    Tripeptide derivatives with central nervous system activity and preparation thereof 失效
    具有中枢神经系统活性的三肽衍生物及其制备方法

    公开(公告)号：USRE30496E

    公开(公告)日：1981-01-27

    申请号：US15091

    申请日：1979-02-26

    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： C07K5/097

    CPC分类号： C07K5/0823

    摘要： The tripeptide derivatives of formulaH--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R' is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, .Iadd.and with the further proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen or lower alkyl and Y is Gly then R.sup.3 is amino(lower)alkylamino, .Iaddend.and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

    N-Substituted cyclopeptide derivatives
    5.
    发明授权
    N-Substituted cyclopeptide derivatives 失效
    N-取代的环肽衍生物

    公开(公告)号：US4351828A

    公开(公告)日：1982-09-28

    申请号：US164663

    申请日：1980-06-30

    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： A61K38/00 ,  C07K7/64 ,  A61K37/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27 ,  Y10S930/29

    摘要： The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式I的N-取代的环肽衍生物，其中R 1是低级烷基，R 2是低级烷基或环（低级）烷基，R 3是中性氨基酸侧链，Y是一个肽残基， 公开了9个氨基酸残基和制备式I化合物的方法。 式I的化合物是有用的抗菌和抗真菌剂。 也公开了药物组合物。

    N-Substituted dimeric cyclopeptide derivatives
    7.
    发明授权
    N-Substituted dimeric cyclopeptide derivatives 失效
    N-取代的二聚环肽衍生物

    公开(公告)号：US4401656A

    公开(公告)日：1983-08-30

    申请号：US189458

    申请日：1980-09-22

    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 phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and 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; 并且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。

    N-substituted cyclopeptide derivatives and preparation thereof
    8.
    发明授权
    N-substituted cyclopeptide derivatives and preparation thereof 失效
    N-取代的环肽衍生物及其制备

    公开(公告)号：US4237045A

    公开(公告)日：1980-12-02

    申请号：US941827

    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： A61K38/00 ,  C07K7/64 ,  C07C103/52 ,  A61K37/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27 ,  Y10S930/29

    摘要： The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式I的N-取代的环肽衍生物，其中R 1为低级烷基，R 2为低级烷基或环（低级）烷基，R 3为中性氨基酸侧链，Y为具有3至9个氨基酸的肽残基 公开了制备式I化合物的残基和方法。 式I的化合物是有用的抗菌和抗真菌剂。 也公开了药物组合物。

    Novel hydrazinocarboxamide derivatives and preparation thereof
    9.
    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.

    Process for preparing the releasing hormone of luteinizing hormone (LH) and of follicle stimulating hormone (FSH), salts and compositions thereof, and intermediates therefor
    10.
    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.