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公开(公告)号:US4159981A
公开(公告)日:1979-07-03
申请号:US842122
申请日:1977-10-04
申请人: Werner Rittel , Max Brugger , Bruno Kamber , Bernhard Riniker , Peter Sieber , Hendrik M. Greven
发明人: Werner Rittel , Max Brugger , Bruno Kamber , Bernhard Riniker , Peter Sieber , Hendrik M. Greven
IPC分类号: A61K38/00 , C07K14/585 , C07C103/52
CPC分类号: C07K14/585 , A61K38/00
摘要: The new hypocalcaemically active peptides of formula I ##STR1## and corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.
摘要翻译: 式I的新的低活性活性肽GlyThrTyrThrGlnAspPheAsnLysPhe HisThrPheProGlnThrAlaGleVal GlyAlaProOH和其中一个或多个天冬酰胺和谷氨酸基团被天冬氨酸或谷氨酸基团和/或天冬氨酸基团代替的相应化合物被替换为 天冬酰胺基团,它们的二聚体,特别是其中2个相同的肽序列(1-32和1'-32')通过半胱氨酸自由基1,7'和7,1'以反平行布置连接的那些,借助于 二硫键和衍生物可用作低钙血症药物,并且通过分离保护至少一个氨基或一个羧基的基团或将相应的硫化物氧化成二硫化物或将其合并在一起而制备。
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公开(公告)号:USRE32347E
公开(公告)日:1987-02-03
申请号:US644696
申请日:1984-08-27
申请人: Robert Neher , Bernhard Riniker
发明人: Robert Neher , Bernhard Riniker
IPC分类号: A61K38/00 , C07K14/585
CPC分类号: C07K14/585 , A61K38/00
摘要: Human calcitonin in the form of four components and process for their isolation from C-cells material.
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公开(公告)号:US4613676A
公开(公告)日:1986-09-23
申请号:US671261
申请日:1984-11-14
IPC分类号: C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00 , C07C101/30 , C07C69/74 , C07C101/72 , C07C61/08
CPC分类号: C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl- lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译: 式(I)的化合物,其中R 1表示氢或酰基,X 1表示任选N-烷基化的氨基酸残基,其N-末端与R 1和C-末端键合于X 2,X 2表示任选N-烷基化的 氨基酸残基,其N-末端与X1和C-末端键合在基团-NR2-上,R 2表示氢或低级烷基,R 3表示氢,烷基,环烷基,芳基 - 低级烷基或芳基,R 4表示羟基或醚化或 酯化羟基,R5代表烷基,环烷基,芳基 - 低级烷基或芳基,R6表示游离或取代的氨基或取代的羟基,这些具有成盐基团的化合物的盐抑制酶肾素的增压作用, 用作抗高血压药。
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公开(公告)号:US3994871A
公开(公告)日:1976-11-30
申请号:US471617
申请日:1974-05-20
申请人: Bruno Kamber , Peter Sieber , Bernhard Riniker , Albert Hartmann , Werner Rittel
发明人: Bruno Kamber , Peter Sieber , Bernhard Riniker , Albert Hartmann , Werner Rittel
IPC分类号: A61K38/00 , C07C231/00 , C07K1/00 , C07K1/06 , C07K1/113 , C07K1/12 , C07K14/575 , C07K14/62 , C07C103/52 , A61K37/26 , C07G7/00
摘要: Process for the manufacture of peptides which contain more than one disulphide bond characterized in that in one or two aminoacid sequences containing cysteine, in which disulphide bonds are to be produced, two cysteine radicals which are to be linked are protected by a mercapto-protective group R.sub.1 of the aralkyl type, two further cysteine radicals are protected by an acylaminomethyl group R.sub.2, the protective groups R.sub.1 are removed by treatment with iodine in the presence of a polyhalogenated lower aliphatic hydroxy compound or oxo compound, or a corresponding lower alkanoic acid lower alkyl ester, at the same time forming the disulphide bond between these cysteine radicals, which are protected by R.sub.1, and at any desired point after removal of the polyhalogenated compound the second disulphide bridge is formed in the usual manner.
摘要翻译: 用于制造含有多于一个二硫键的肽的方法,其特征在于在含有半胱氨酸的一个或两个氨基酸序列中,其中将产生二硫键,待连接的两个半胱氨酸基团被巯基保护基团保护 芳烷基类型的R1,两个另外的半胱氨酸基团被酰氨基甲基R2保护,保护基R1在多卤化低级脂族羟基化合物或氧代化合物或相应的低级链烷酸低级烷基存在下用碘处理除去 酯,同时形成由R1保护的这些半胱氨酸基团之间的二硫键,并且在去除多卤代化合物之后的任何所需点,以通常的方式形成第二二硫桥。
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公开(公告)号:US3934008A
公开(公告)日:1976-01-20
申请号:US271873
申请日:1972-07-14
申请人: Werner Rittel , Max Brugger , Bruno Kamber , Bernhard Riniker , Peter Sieber , Hendrik Marie Greven
发明人: Werner Rittel , Max Brugger , Bruno Kamber , Bernhard Riniker , Peter Sieber , Hendrik Marie Greven
IPC分类号: A61K38/00 , C07K14/585 , A61K37/00 , C07C103/52 , C07G7/00
CPC分类号: C07K14/585 , A61K38/00 , Y10S514/807
摘要: The new hypocalcaemically active peptides of formula Ih-cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Thr-Gln-Asp-Phe-Asn-Lys-Phe-His-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-val-Gly-Ala-Pro-OHand corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.
摘要翻译: 式I H-Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Thr-Gln-Asp-Phe-Asn-Lys-Phe-His-的新的低血清活性肽 Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-val-Gly-Ala-Pro-OH和其中一个或多个天冬酰胺和谷氨酸基被天冬氨酸或谷氨酸基团代替的相应化合物 特别是其中2个相同的肽序列(1-32和1'-32')通过半胱氨酸自由基1以反平行排列连接的那些,天冬酰胺基团和/或天冬氨酸基团被天冬酰胺基团替代, 7'和7,1',并且衍生物可用作低钙血症药物,并且通过分离保护至少一个氨基或一个羧基的基团或将相应的硫化物氧化成二硫化物或将其合并在一起而制备足够的肽 。
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公开(公告)号:US5324833A
公开(公告)日:1994-06-28
申请号:US509102
申请日:1990-04-13
申请人: Peter Sieber , Bernhard Riniker
发明人: Peter Sieber , Bernhard Riniker
IPC分类号: C07K1/04 , C07C237/06 , C07C237/22 , C07C271/22 , C07C271/54 , C07D253/08 , C07K1/06 , C07K1/08 , C07K1/113 , C07K7/06 , C07K7/08 , C07D253/04 , C07C229/24 , C07D487/04
CPC分类号: C07D253/08 , C07C237/06 , C07C271/22 , C07K1/064 , C07C2103/18 , Y02P20/55
摘要: Compounds of the formula I, ##STR1## in which 'R.sub.1 is an amino protective group, and n stands for 1 or 2, R.sub.1 denotes hydrogen or an amino protective group, R.sub.2 denotes hydrogen or a carboxyl protective group and R.sub.3 denotes triphenylmethyl, 4-monomethoxy-trityl or 4,4'-dimethoxy-trityl, and reactive carboxylic acid derivatives of such compounds of the formula I in which R.sub.2 stands for hydrogen, are described.These compounds can be used as starting materials for the preparation of peptides. They are more suitable for this than are analogous compounds of the formula I in which R.sub.3 denotes hydrogen or one of the carbamoyl protective groups hitherto customary.
摘要翻译: 式Ⅰ化合物,其中R1为氨基保护基,n为1或2,R1为氢或氨基保护基,R2为氢或羧基保护基,R3为 三苯基甲基,4-单甲氧基 - 三苯甲基或4,4'-二甲氧基三苯甲基,以及其中R2代表氢的式Ⅰ化合物的反应性羧酸衍生物。 这些化合物可以用作制备肽的起始材料。 它们比类似的式I化合物更适合于其中,R3表示氢或迄今为止常用的氨基甲酰基保护基之一。
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公开(公告)号:US4719288A
公开(公告)日:1988-01-12
申请号:US869800
申请日:1986-06-02
IPC分类号: C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00 , C07K5/08 , C07C103/34 , C07C103/12 , C07C103/20 , C07C101/30 , C07D277/20 , C07D209/18 , C07D233/64 , C07D207/12 , C07D211/70
CPC分类号: C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译: 式(I)的化合物,其中R 1表示氢或酰基,X 1表示任选N-烷基化的氨基酸残基,其N-末端与R 1和C-末端键合于X 2,X 2表示任选N-烷基化的 氨基酸残基,其N-末端与X1和C-末端键合在基团-NR2-上,R 2表示氢或低级烷基,R 3表示氢,烷基,环烷基,芳基 - 低级烷基或芳基,R 4表示羟基或醚化或 酯化羟基,R5代表烷基,环烷基,芳基 - 低级烷基或芳基,R6表示游离或取代的氨基或取代的羟基,这些具有成盐基团的化合物的盐抑制酶肾素的增压作用, 用作抗高血压药。
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公开(公告)号:US3956260A
公开(公告)日:1976-05-11
申请号:US206933
申请日:1971-12-10
申请人: Max Brugger , Friedrich Werner Kahnt , Bruno Kamber , Robert Neher , Bernhard Riniker , Werner Rittel , Peter Sieber , Herbert Zuber , Hendrik Marie Greven
发明人: Max Brugger , Friedrich Werner Kahnt , Bruno Kamber , Robert Neher , Bernhard Riniker , Werner Rittel , Peter Sieber , Herbert Zuber , Hendrik Marie Greven
IPC分类号: A61K38/00 , C07K1/06 , C07K5/06 , C07K5/072 , C07K5/083 , C07K5/103 , C07K5/107 , C07K7/08 , C07K14/585 , C07C103/52 , C07G7/00
CPC分类号: C07K7/08 , C07K1/067 , C07K14/585 , C07K5/06026 , C07K5/06052 , C07K5/06069 , C07K5/06113 , C07K5/0804 , C07K5/1005 , C07K5/1016 , A61K38/00 , Y10S514/808 , Y10S930/26
摘要: Synthetic hypocalcaemic dotriacontapeptide of the formulaH-Cys-Ser-Asn-Leu-Ser--Thr-Cys-Val-Leu-Ser-Ala-Tyr-Try-Arg-Asn-Leu-Asn-Asn-Phe-His-Arg-Phe-Ser-Gly-Met-Gly-Phe-Gly-Pro-Glu-Thr-Pro-OH Iand analogues and derivatives, salts and complexes thereof and process for their manufacture.
摘要翻译: 式H-Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Ser-Ala-Tyr-Try-Arg-Asn-Leu-Asn -Asn-Phe-His-Arg的合成低碳血症dotriacontapeptide -Phe-Ser-Gly-Met-Gly-Phe-Gly-Pro-Glu-Thr-Pro-OH I及其类似物及其衍生物,盐和络合物及其制备方法。
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公开(公告)号:US4863903A
公开(公告)日:1989-09-05
申请号:US112631
申请日:1987-10-26
IPC分类号: C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00
CPC分类号: C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group -NR.sub.2 -, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译: 式(I)的化合物,其中R 1表示氢或酰基,X 1表示任选N-烷基化的氨基酸残基,其N-末端与R 1和C-末端键合于X 2,X 2表示任选N-烷基化的 氨基酸残基,其N-末端与X1和C-末端键合在基团-NR2-上,R 2表示氢或低级烷基,R 3表示氢,烷基,环烷基,芳基 - 低级烷基或芳基,R 4表示羟基或醚化或 酯化羟基,R5代表烷基,环烷基,芳基 - 低级烷基或芳基,R6表示游离或取代的氨基或取代的羟基,这些具有成盐基团的化合物的盐抑制酶肾素的增压作用, 用作抗高血压药。
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公开(公告)号:US4595677A
公开(公告)日:1986-06-17
申请号:US554735
申请日:1983-11-23
申请人: Bernhard Riniker , Peter Buhlmayer , Walter Fuhrer
发明人: Bernhard Riniker , Peter Buhlmayer , Walter Fuhrer
CPC分类号: C07K5/0227 , C07K7/02 , C07K7/14 , A61K38/00 , Y10S530/86
摘要: Tetrapeptides of the formula I, ##STR1## in which R.sup.1 represents hydrogen or acyl, R.sup.2 represents alkyl or aralkyl, R.sup.3 represents free or functionally modified hydroxy, R.sup.4 represents free or substituted amino or free or etherified hydroxy, and -Pro-, -Phe- and -His- respectively represent the bivalent radicals of the amino acids proline, phenylalanine and histidine or the (D)-isomers thereof, salts of such compounds having salt-forming groups, and processes for their manufacture.The compounds inhibit the action of the enzyme renin and can be used as antihypertensives and for the treatment of cardiac insufficiency.
摘要翻译: 式I的四肽,其中R 1表示氢或酰基,R 2表示烷基或芳烷基,R 3表示游离或官能改性的羟基,R 4表示游离或取代的氨基或游离的或醚化的羟基,和-Pro- ,-Phe-和-His-分别表示氨基酸脯氨酸,苯丙氨酸和组氨酸或其(D)异构体的二价基团,这些具有成盐基团的化合物的盐及其制备方法。 该化合物抑制酶肾素的作用,可用作抗高血压药物和治疗心功能不全。
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