Anti-diabetic peptides
First Claim
Patent Images
1. A compound of the formula:
- X1 -Xaa1 -X2 -Xaa2 -X3 -Xaa3 -X4 -Xaa4 -X5 -Xaa5 -X6 -NH2 wherein X1 is Lys, Arg or absent;
X2 is Xaa6 Xaa7 Xaa8 Xaa9 (SEQ. ID. NO.
47) or Z-Xaa10 SerThr, provided that if X2 is Z-Xaa10 Ser-Thr, then X1 and Xaa1 are both absent;
X3 is AlaThr, AlaSer, SerMet, GluThr or ValThr;
X4 is ArgLeuAla, HisLeuAla, ArgIleAla, LysIleAla, ArgMetAla, HisMetAla, LysMetAla or ArgLeuThr;
X5 is PheLeu, PheIle, PheMet, TyrLeu, TyrIle, TyrMet, TrpMet, TrpIle or TrpMet;
X6 is ArgSerSerGlyTyr (SEQ. ID. NO.
48), LysSerSerGlyTyr (SEQ. ID. NO.
49), HisSerSerGlyTyr (SEQ. ID. NO.
50), ProSerSerGlyTyr (SEQ. ID. NO.
51), ArgSerArgGlyTyr (SEQ. ID. NO.
52), ArgThrSerGlyTyr (SEQ. ID. NO.
53), ArgAlaSerGlyTyr (SEQ. ID. NO.
54), AlaSerSerGlyTyr (SEQ. ID. NO.
55), ArgSerAlaGlyTyr (SEQ. ID. NO.
56), HisSerAlaGlyTyr (SEQ. ID. NO.
57), ArgSerGlyTyr (SEQ. ID. NO.
58), ArgSer, LysSer, HisSer, ArgThr, ProSer or Arg;
Xaa1 is Cys or absent;
Xaa2 is Cys or Ala;
Xaa3 is Gln, Ala or Asn;
Xaa4 is Asn, Ala or Gln;
Xaa5 is Val, Ala, Ile, Met, Leu, PentylGly, or t-butylGly;
Xaa6 is Asn, Gln or Asp;
Xaa7 is Thr, Ser, Met, Val, Leu or Ile;
Xaa8 is Ala or Val;
Xaa9 is Thr or Ser;
Xaa10 is Leu, Val, Met or Ile; and
Z is an alkanoyl group of about 1 to about 8 carbon atoms or absent and pharmaceutically acceptable salts thereof.
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Accused Products
Abstract
Compounds of formula I which act as amylin agonists with respect to certain desired amylin activities and as calcitonin agonists with respect to certain desired calcitonin activities are provided. Such compounds are useful in treating disturbances in fuel metabolism in mammals, including, but not limited to diabetes mellitus, including Type I diabetes and Type II diabetes. The present invention also relates to methods of treating Type I diabetes, treating Type II diabetes and to methods of beneficially regulating gastrointestinal motility comprising administration of a therapeutically effective among of one of the compounds. Also provided are pharmaceutical composition comprising a compound of formula I and a pharmaceutically acceptable carrier.
99 Citations
82 Claims
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1. A compound of the formula:
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X1 -Xaa1 -X2 -Xaa2 -X3 -Xaa3 -X4 -Xaa4 -X5 -Xaa5 -X6 -NH2 wherein X1 is Lys, Arg or absent; X2 is Xaa6 Xaa7 Xaa8 Xaa9 (SEQ. ID. NO.
47) or Z-Xaa10 SerThr, provided that if X2 is Z-Xaa10 Ser-Thr, then X1 and Xaa1 are both absent;X3 is AlaThr, AlaSer, SerMet, GluThr or ValThr; X4 is ArgLeuAla, HisLeuAla, ArgIleAla, LysIleAla, ArgMetAla, HisMetAla, LysMetAla or ArgLeuThr; X5 is PheLeu, PheIle, PheMet, TyrLeu, TyrIle, TyrMet, TrpMet, TrpIle or TrpMet; X6 is ArgSerSerGlyTyr (SEQ. ID. NO.
48), LysSerSerGlyTyr (SEQ. ID. NO.
49), HisSerSerGlyTyr (SEQ. ID. NO.
50), ProSerSerGlyTyr (SEQ. ID. NO.
51), ArgSerArgGlyTyr (SEQ. ID. NO.
52), ArgThrSerGlyTyr (SEQ. ID. NO.
53), ArgAlaSerGlyTyr (SEQ. ID. NO.
54), AlaSerSerGlyTyr (SEQ. ID. NO.
55), ArgSerAlaGlyTyr (SEQ. ID. NO.
56), HisSerAlaGlyTyr (SEQ. ID. NO.
57), ArgSerGlyTyr (SEQ. ID. NO.
58), ArgSer, LysSer, HisSer, ArgThr, ProSer or Arg;Xaa1 is Cys or absent; Xaa2 is Cys or Ala; Xaa3 is Gln, Ala or Asn; Xaa4 is Asn, Ala or Gln; Xaa5 is Val, Ala, Ile, Met, Leu, PentylGly, or t-butylGly; Xaa6 is Asn, Gln or Asp; Xaa7 is Thr, Ser, Met, Val, Leu or Ile; Xaa8 is Ala or Val; Xaa9 is Thr or Ser; Xaa10 is Leu, Val, Met or Ile; and Z is an alkanoyl group of about 1 to about 8 carbon atoms or absent and pharmaceutically acceptable salts thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 74, 75, 76, 77, 78, 79, 80, 81, 82)
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72. A compound according to claim 72 wherein Xaa2 is Cys.
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73. A compound according to claim 73 wherein Xaa1 and Xaa2 form a disulfide bridge.
Specification
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Current AssigneeAstrazeneca Pharmaceuticals LP (Astrazeneca PLC)
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Original AssigneeAmylin Pharmaceuticals Incorporated (Bristol-Myers Squibb Company)
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InventorsBeeley, Nigel Robert Arnold, Prickett, Kathryn S.
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Primary Examiner(s)DAVENPORT, AVIS MICHELLE
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Application NumberUS09/138,056Time in Patent Office690 DaysField of Search530/300, 530/308, 530/326, 514/2, 514/13, 424/184.1, 424/185.1US Class Current514/6.9CPC Class CodesA61K 38/00 Medicinal preparations cont...A61P 1/00 Drugs for disorders of the ...A61P 3/10 for hyperglycaemia, e.g. an...C07K 14/575 Hormones derived from pro-o...
