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1. 发明公开

EP0427458A2 Use of heptapeptides in the treatment or prophylaxis of muscle wasting 失效
标题翻译： Verwendung von Heptapeptiden zur Behandlung oder Prophylaxe von Muskelschwund。
公开(公告)号：EP0427458A2
公开(公告)日：1991-05-15
申请号：EP90311969.1
申请日：1990-11-01
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： A61K37/02 , A61K37/40
CPC分类号： C07K14/6955 , A61K38/08
摘要： Muscle wasting is treated by administering a composition comprising a heptapeptide of the formula:
A¹-A²-A³-A⁴-Phe-Arg-Trp-A⁵
wherein
A¹ is H or acetyl;
A² is Ala, D-Ala, Nle, or Met;
A³ is Glu or Gln;
A⁴ is His or Tyr; and
A⁵ is NH₂, Gly-NH₂ or D-Ala-NH₂;
provided that when A³ is Glu and A⁴ is His, A² cannot be Met or Nle, or a pharmaceutically acceptable salt thereof.
摘要翻译：通过施用包含下式的七肽的组合物来治疗肌肉消耗：A 1 -A 2 -A 3 -A 4 -Phe-Arg-Trp-A 5其中A 1，是H或乙酰基; A 2是Ala，D-Ala，Nle或Met; A 3是Glu或Gln; A 4是His或Tyr; A 5是NH 2，Gly-NH 2或D-Ala-NH 2; 条件是当A 3为Glu且A 4为His时，A 2不能为Met或Nle，或其药学上可接受的盐。

2. 发明公开

EP0225746A3 Therapeutic decapeptides 失效
标题翻译：治疗方法
公开(公告)号：EP0225746A3
公开(公告)日：1989-12-20
申请号：EP86308905.8
申请日：1986-11-14
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： C07K7/06 , C07K7/20 , A61K37/02
CPC分类号： C07K7/23 , A61K38/00
摘要： A decapeptide of the formula:
A 9 , wherein each A 1 , A2, and A3, independently, is D-β-Nal, D-p-X-Phe (where X is halogen, H, NH 2 , NO 2 , OH, or C 1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A4 is p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A 5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-β-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), or D-Lys-ε-NH-R (where R is H, a branched or straight chain C 1 -C 10 akyl group, or an aryl group); A 6 is Leu, β-Nal, p-X-Phe (where X is halogen, H, NH 2 , N0 2 , OH, C 2 F 5 , C 1-3 alkyl), or Trp; A 7 is Arg, Lys, or Lys-e-NH-R (where R is H, a branched or straight chain C 1 -C 6 alkyl group, or an aryl group); As is Pro; and A 9 is D-Ala, D-Ala-NH 2 , Ala-NH 2 , aminoisobutyric acid amide, or Gly-NH 2 ; provided that at least one of A 2 or A3 must be D-Phe or D-Tyr, and provided further that when A4 is Lys or Arg, A 5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-ε-NH-R, or a pharmaceutically acceptable salt thereof, can be used to inhibit the release of sex hormones in the treatment or prophylaxis of various sex hormone-released conditions. They may also be used as female contraceptives.

3. 发明公开

EP0427458A3 Use of heptapeptides in the treatment or prophylaxis of muscle wasting 失效
标题翻译：使用抗生素治疗或预防肌肉损伤
公开(公告)号：EP0427458A3
公开(公告)日：1991-09-25
申请号：EP90311969.1
申请日：1990-11-01
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： A61K37/02 , A61K37/40
CPC分类号： C07K14/6955 , A61K38/08
摘要： Muscle wasting is treated by administering a composition comprising a heptapeptide of the formula:
A¹-A²-A³-A⁴-Phe-Arg-Trp-A⁵
wherein
A¹ is H or acetyl;
A² is Ala, D-Ala, Nle, or Met;
A³ is Glu or Gln;
A⁴ is His or Tyr; and
A⁵ is NH₂, Gly-NH₂ or D-Ala-NH₂;
provided that when A³ is Glu and A⁴ is His, A² cannot be Met or Nle, or a pharmaceutically acceptable salt thereof.

4. 发明公开

EP0225746A2 Therapeutic decapeptides 失效
标题翻译：治疗脱卡肽
公开(公告)号：EP0225746A2
公开(公告)日：1987-06-16
申请号：EP86308905.8
申请日：1986-11-14
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： C07K7/06 , C07K7/20 , A61K37/02
CPC分类号： C07K7/23 , A61K38/00
摘要： A decapeptide of the formula:
A 9 , wherein each A 1 , A2, and A3, independently, is D-β-Nal, D-p-X-Phe (where X is halogen, H, NH 2 , NO 2 , OH, or C 1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A4 is p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A 5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-β-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH 2 , N0 2 , or C 1-3 alkyl), or D-Lys-ε-NH-R (where R is H, a branched or straight chain C 1 -C 10 akyl group, or an aryl group); A 6 is Leu, β-Nal, p-X-Phe (where X is halogen, H, NH 2 , N0 2 , OH, C 2 F 5 , C 1-3 alkyl), or Trp; A 7 is Arg, Lys, or Lys-e-NH-R (where R is H, a branched or straight chain C 1 -C 6 alkyl group, or an aryl group); As is Pro; and A 9 is D-Ala, D-Ala-NH 2 , Ala-NH 2 , aminoisobutyric acid amide, or Gly-NH 2 ; provided that at least one of A 2 or A3 must be D-Phe or D-Tyr, and provided further that when A4 is Lys or Arg, A 5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-ε-NH-R, or a pharmaceutically acceptable salt thereof, can be used to inhibit the release of sex hormones in the treatment or prophylaxis of various sex hormone-released conditions. They may also be used as female contraceptives.
摘要翻译：下式的十肽：N-Ac-A 1 -A 2 -A 3 -Ser-A 4 -A 5 -A 6 -7 -A -A 8 > -A <9>，其中每个A 1，A 2和A 3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-Trp，D-苯并噻吩基（2）-Ala或D-苯并噻吩基（1）-Ala; A 4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; A 5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是H，支链或直链C 1 -C 10烷基或芳基）。 A 6是Leu，β-Nal，p-X-Phe（其中X是卤素，H，NH 2，NO 2，OH，C 2 F 5，C 1-3烷基）或Trp; A 7是Arg，Lys或Lys-ε--NH-R（其中R是H，支链或直链的C 1 -C 6烷基或芳基）; A <8>是Pro A 9为D-Ala，D-Ala-NH 2，Ala-NH 2，氨基异丁酸酰胺或Gly-NH 2; 条件是A 2或A 3中的至少一个必须是D-Phe或D-Tyr，并且进一步提供当A 4为Lys或Arg时，A 5不得为D-Arg， D-Lys，D-homo-Arg，D-二乙基高-Arg或D-Lys-ε--NH-R或其药学上可接受的盐可用于抑制性激素在治疗或预防中的释放各种性激素释放条件。它们也可以用作女性避孕药。

5. 发明公开

EP0309297A2 Therapeutic peptides 失效
标题翻译：治疗肽
公开(公告)号：EP0309297A2
公开(公告)日：1989-03-29
申请号：EP88308916.1
申请日：1988-09-26
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： C07K7/00 , A61K37/02 , C07K7/02
CPC分类号： C07K7/086 , A61K38/00 , C07K7/02
摘要： A linear peptide which is an analog of a naturally occurring, biologically active bombesin having an active site and a binding site responsible for binding of bombesin to a receptor on a target cell, cleavage of a peptide bond in the active site of the naturally occurring peptide being unnecessary for in vivo biological activity, the analog having a non-peptide bond instead of a peptide bond between an amino acid of the active site and an adjacent amino acid, and having the same binding site as the naturally occurring peptide, so that the analog, is capable of acting as a competitive inhibitor of naturally occurring bombesin by binding to the receptor and, by virtue of the non-peptide bond, failing to exhibit the in vivo activity of naturally occurring bombesin.
摘要翻译：线性肽，其是具有活性位点的天然存在的，生物活性的铃蟾肽的类似物，并且负责将铃蟾肽与靶细胞上的受体结合的结合位点，天然存在的肽的活性位点中的肽键的切割对于体内生物活性是不必要的，所述类似物具有非肽键而不是活性位点的氨基酸与相邻氨基酸之间的肽键，并且具有与天然存在的肽相同的结合位点，使得类似物能够通过结合受体而作为天然存在的铃蟾肽的竞争性抑制剂，并且由于非肽键，不能表现出天然存在的铃蟾肽的体内活性。

6. 发明授权

EP0309297B1 Therapeutic peptides 失效
标题翻译：治疗性多肽。
公开(公告)号：EP0309297B1
公开(公告)日：1994-11-09
申请号：EP88308916.1
申请日：1988-09-26
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： C07K7/00 , A61K37/02 , C07K7/02
CPC分类号： C07K7/086 , A61K38/00 , C07K7/02

7. 发明公开

EP0309297A3 Therapeutic peptides 失效
标题翻译：治疗肽
公开(公告)号：EP0309297A3
公开(公告)日：1990-07-04
申请号：EP88308916.1
申请日：1988-09-26
申请人： The Administrators of The Tulane Educational Fund
发明人： Coy, David H. , Moreau, Jacques-Pierre
IPC分类号： C07K7/00 , A61K37/02 , C07K7/02
CPC分类号： C07K7/086 , A61K38/00 , C07K7/02
摘要： A linear peptide which is an analog of a naturally occurring, biologically active bombesin having an active site and a binding site responsible for binding of bombesin to a receptor on a target cell, cleavage of a peptide bond in the active site of the naturally occurring peptide being unnecessary for in vivo biological activity, the analog having a non-peptide bond instead of a peptide bond between an amino acid of the active site and an adjacent amino acid, and having the same binding site as the naturally occurring peptide, so that the analog, is capable of acting as a competitive inhibitor of naturally occurring bombesin by binding to the receptor and, by virtue of the non-peptide bond, failing to exhibit the in vivo activity of naturally occurring bombesin.

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