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公开(公告)号：US20080171853A1
公开(公告)日：2008-07-17
申请号：US12075319
申请日：2008-03-11
CPC分类号： A61K38/08 , C07K14/655
摘要： The present invention is directed to a method for synthesizing a peptide using solid-state chemistry in which at least one amide bond is N-methylated, wherein said method of synthesis utilizes N-Boc protected amino acids. For example, the a peptide is first synthesized using N-BOC protected amino acids and 4-methylbenzylhydrylamine functionalized 1% cross linked polystyrene resin until reaching the amide bond to be N-methylated. Then, the amino group at the desired methylation site is methylated. If desired, the synthesis of additional peptide using N-BOC protected amino acids may continued until the desired peptide is complete.
摘要翻译： 本发明涉及使用其中至少一个酰胺键被N-甲基化的固态化学合成肽的方法，其中所述合成方法使用N-Boc保护的氨基酸。 例如，首先使用N-BOC保护的氨基酸和4-甲基苄基氢化胺官能化的1％交联聚苯乙烯树脂合成肽，直至达到酰胺键为N-甲基化。 然后，将所需甲基化位点处的氨基甲基化。 如果需要，可以继续使用N-BOC保护的氨基酸合成另外的肽，直到所需肽完成。
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公开(公告)号：US07378488B2
公开(公告)日：2008-05-27
申请号：US10469836
申请日：2002-03-05
CPC分类号： A61K38/08 , C07K14/655
摘要： The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ∝-amino acid; A2 is an optionally substituted aromatic ∝-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is β-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic -amino acid; and Y1 is OH, NH2 or NHR1, or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic -amino acid is optionally substituted with one or more substituents substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10, where R9 ad R10 each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.
摘要翻译： 本发明涉及式（I）的生长抑素拮抗剂，其中A 1为任选取代的芳族α-氨基酸; A 2是任选取代的芳族α-氨基酸; Dab，Dap，Lys或Orn; Aβ4是β-羟基缬氨酸，Ser，Hser或Thr; A 5是任选取代的D-或L-芳族 - 氨基酸; 和Y 1是OH，NH 2或NHR 1或NHR 1，其中R 1 是（C 1-6）烷基; 其中每个所述任选取代的芳族 - 氨基酸任选地被一个或多个取代基取代，所述取代基各自独立地选自卤素，NO 2，OH，CN，（C 1-6） （C 2-6）烯基，（C 2-6 - ）炔基，（C 1-6 - ）烷基，（C 2-6） 烷氧基，Bzl，O-Bzl和NR 9 R 10，其中R 9和R 10各自为 独立地是H，O或（C 1-6 - ）烷基; 并且其中酰胺肽键和式（I）的A 1的氨基的胺氮任选被甲基取代，条件是存在至少一个所述甲基; 或其药学上可接受的盐，及其用途。
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公开(公告)号：US07312304B2
公开(公告)日：2007-12-25
申请号：US10474248
申请日：2002-04-08
CPC分类号： C07K14/6555 , A61K38/00
摘要： Claimed are a series of somatostatin agonists and uses thereof, according to formula (I), A1-cyclo[Cys-A2-D-Trp-A3-A4-Cys]-A5-Y1, (I) wherein A1, A2, A3, A4, A5 and Y1 are as defined in specification provided that the amine nitrogen of at least one peptide bond is substituted with a methyl group or pharmaceutically acceptable salts thereof.
摘要翻译： 根据式（I），所述是一系列生长抑素激动剂及其用途，<？在线公式描述=“在线公式”end =“lead”？> A 环[Cys-A 2-D-Trp-A 3 -S-4-Cys] -A 5 -I <1>，（I）<？in-line-formula description =“In-line formula”end =“tail”？>其中A 1， > 2 ，A 3，A 4，A 5和Y 1如下所定义。 规定，至少一个肽键的胺氮被甲基取代或其药学上可接受的盐。
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公开(公告)号：US06262229B1
公开(公告)日：2001-07-17
申请号：US08855204
申请日：1997-05-13
申请人： David H. Coy , Barry Morgan , William Murphy
发明人： David H. Coy , Barry Morgan , William Murphy
IPC分类号： C07K700
CPC分类号： C07K14/6555
摘要： The invention features somatostatin antagonists having a D-amino acid at the second residue.
摘要翻译： 本发明具有在第二残基具有D-氨基酸的生长抑素拮抗剂
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公开(公告)号：US5847066A
公开(公告)日：1998-12-08
申请号：US631421
申请日：1996-04-12
申请人： David H. Coy , William Murphy
发明人： David H. Coy , William Murphy
摘要： A peptide which is a variant of the human growth hormone-releasing factor. The peptide, containing 23-28 amino acid residues, differs from its native counterpart at least at positions 8, 9, 16, 18, 24, 25, 27, and 28, and is potent in stimulating the release of growth hormone.
摘要翻译： 作为人生长激素释放因子的变体的肽。 含有23-28个氨基酸残基的肽至少在第8,9,16,18,24,25,27和28位与其天然对应物不同，并且有效刺激生长激素的释放。
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公开(公告)号：US5569741A
公开(公告)日：1996-10-29
申请号：US352392
申请日：1994-12-08
申请人： David H. Coy , John E. Taylor
发明人： David H. Coy , John E. Taylor
IPC分类号： A61K38/00 , A61K38/31 , A61P43/00 , C07K7/06 , C07K7/52 , C07K14/655 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A61K38/31 , C07K14/6555
摘要： A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp;A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH;A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6);A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;A.sup.8 is Nal or Trp;m is 1, 2, or 3;n is 1, 2, 3, 4 or 5;each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H;R.sub.4 is C.sub.6 H.sub.4 or absent;R.sub.7 is .dbd.NR.sub.8, .dbd.S, or .dbd.O; andeach of R.sub.3, R.sub.5, R.sub.6, and R.sub.8, independently, is H or E.
摘要翻译： 下式的环状八肽：其中：A1为D-Nal或D-Trp; A3是Phe，F5-Phe或X-Phe，其中X是卤素，NO 2，CH 3或OH; A5是-NH-CH（Y）-CO-，其中Y是（CH2）m-R4-N（R5）（R6）或（CH2）n-R4-NH-C（R7）-N（R5） ）; A6是Thr，Leu，Ile，Nle，Val和Abu的D-或L-异构体; A8是Nal或Trp; m为1,2或3; n为1,2,3,4或5; R 1和R 2各自独立地是H，E，COE或COOE，其中E是C 1-12烷基，C 2-12烯基，C 2-12炔基，苯基，萘基，C 7-12苯基烷基或烷基苯基，C 8-12苯基烯基 或烯基苯基，C 8-12苯基炔基或炔基苯基，C 11-20萘基烷基或烷基萘基，C 12-20萘基烯基或链烯基萘基，或C 12-20萘基炔基或炔基萘基，条件是当R 1或R 2中的一个为COE或COOE时，另一个必须为H ; R4为C6H4或不存在; R 7 = NR 8，= S或= O; R 3，R 5，R 6和R 8各自独立地为H或E.
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公开(公告)号：US5462927A
公开(公告)日：1995-10-31
申请号：US990555
申请日：1992-12-14
IPC分类号： A61K38/00 , A61K38/08 , C07K14/685 , C07K14/695 , C07K7/00 , C07K7/06 , C07K14/68
CPC分类号： C07K14/685 , A61K38/08 , C07K14/6955
摘要： Biologically active peptides are disclosed of the formula: A.sup.1 --A.sup.2 --A.sup.3 --A.sup.4 --Phe--Arg--TrP--A.sup.5, or a pharmaceutically acceptable salt thereof; A.sup.1 is H or acetyl; A.sup.2 is Ala, or D--Ala; A.sup.3 is Glu or Gln; and A.sup.4 is His or Tyr; A.sup.5 is NH.sub.2, Gly--NH.sub.2, or D--Ala--NH.sub.2. Pharmaceutical compositions containing these peptides are capable of promoting nerve regeneration and increasing muscle mass or preventing muscle atrophy following an injury.
摘要翻译： 公开了具有下式的生物活性肽：A1-A2-A3-A4-Phe-Arg-TrP-A5或其药学上可接受的盐; A1是H或乙酰基; A2是Ala或D-Ala; A3是Glu或Gln; 而A4是His或Tyr; A5是NH2，Gly-NH2或D-Ala-NH2。 含有这些肽的药物组合物能够促进神经再生和增加肌肉量，或者在损伤后防止肌肉萎缩。
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公开(公告)号：US5462926A
公开(公告)日：1995-10-31
申请号：US78419
申请日：1993-06-17
申请人： David H. Coy , John E. Taylor
发明人： David H. Coy , John E. Taylor
IPC分类号： A61K38/00 , A61K38/31 , A61P43/00 , C07K7/06 , C07K7/52 , C07K14/655 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A61K38/31 , C07K14/6555
摘要： A method of selectively inhibiting biochemical activity of cells induced by neuromedin B. The method includes the step of contacting cells which contain neuromedin B receptor with a cyclic octapeptide, D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH.sub.2, or an analog thereof.
摘要翻译： 一种选择性抑制由神经介肽B诱导的细胞生化活性的方法。该方法包括使含有神经介肽B受体的细胞与环状八肽D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys- Nal-NH 2，或其类似物。
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公开(公告)号：US5162497A
公开(公告)日：1992-11-10
申请号：US282328
申请日：1988-12-09
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685
CPC分类号： C07K7/086 , C07K14/57572 , C07K14/685 , C07K7/02 , C07K7/18 , A61K38/00 , Y10S514/803
摘要： A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.
摘要翻译： 包含9或10个氨基酸残基和至少一个[CH 2 N H]假肽键的缓激肽类似物，该类似物可用作天然存在的缓激肽的拮抗剂或激动剂。
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公开(公告)号：US5073624A
公开(公告)日：1991-12-17
申请号：US352140
申请日：1989-05-15
CPC分类号： C07K7/06 , C07K7/23 , A61K38/00 , Y10S514/80
摘要： A decapeptide of the formula: N-AC-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A-.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.9 is D-Ala, D-Ala-NH.sub.2, Ala-NH.sub.2, aminoisobutyric acid amide, or Gly-NH.sub.2 ; provided that at least one of A.sup.2 or A.sup.3 must be D-Phe or D-Tyr, and provided further that when A.sup.4 is Lys or Arg, A.sup.5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-.epsilon.-NH-R, or a pharmaceutically acceptable salt thereof.The invention also features a method of treating T-cell-deficient patients, e.g., those suffering from Acquired Immune Dificiency Syndrome, by administering a therapeutically effective amount of an LH-RH antagonist.
摘要翻译： 下式的十肽：N-AC-A1-A2-A3-Ser-A-4-A5-A6-A7-A8-A9，其中每个A1，A2和A3独立地是D-β-Nal， DpX-Phe（其中X是卤素，H，NH 2，NO 2，OH或C 1-3烷基），D-苯并噻吩基（2）-Ala或D-苯并噻吩基（1）-Ala; A4是p-X-Phe（其中X是卤素，H，NH 2，NO 2或C 1-3烷基），Tyr，Lys，Arg，Leu，Trp或Nal; A5是D-Lys，D-Tyr，D-Arg，D-Phe，D-β-Nal，D-Trp，D-均一Arg，D-二乙基均一Arg，DpX-Phe（其中X是卤素 ，H，NH 2，NO 2或C 1-3烷基）或D-Lys-ε--NH-R（其中R为H，支链或直链C 1 -C 10烷基或芳基）; A6是Leu，β-Nal，p-X-Phe（其中X是卤素，H，NH2，NO2，OH，C2F5，C1-3烷基）或Trp; A7是Arg，Lys或Lysε--NH-R（其中R是H，支链或直链的C 1 -C 6烷基或芳基）; A8是Pro A9为D-Ala，D-Ala-NH2，Ala-NH2，氨基异丁酸酰胺或Gly-NH2; 条件是A2或A3中的至少一个必须是D-Phe或D-Tyr，并且进一步提供当A4是Lys或Arg时，A5不得是D-Arg，D-Lys，D-均聚-Gly，D- 二乙基均一Arg或D-Lys-ε--NH-R或其药学上可接受的盐。 本发明还涉及通过施用治疗有效量的LH-RH拮抗剂来治疗T细胞缺陷患者，例如患有获得性免疫性综合征的患者的方法。
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