.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,514,646

« Back to Dashboard

Claims for Patent: 5,514,646

Title: Insulin analogs modified at position 29 of the B chain
Abstract:Analogs of human insulin modified at position 29 of the B chain thereof and, optionally, at other positions, have modified physico-chemical and pharmacokinetic properties and are useful in the treatment of hyperglycemia.
Inventor(s): Chance; Ronald E. (Westfield, IN), DiMarchi; Richard D. (Carmel, IN), Frank; Bruce H. (Indianapolis, IN), Shields; James E. (Noblesville, IN)
Assignee:
Application Number:08/057,201
Patent Claims: 1. An insulin analog of the formula ##STR11## or a pharmaceutically acceptable salt thereof, wherein A.sub.21 is Asn, or Ala;

B.sub.1 is Phe, or is absent;

B.sub.2 is Val, or is absent;

B.sub.10 is His, or Asp;

B.sub.28 is any amino acid;

B.sub.29 is L-Pro, D-Pro, L-hydroxyproline, D-hydroxyproline;

and,

B.sub.30 is Thr, Ala, or is absent.

2. The insulin analog of claim 1 wherein B.sub.28 is Asp, Val, Leu, Ile, Pro, Arg, His, Lys, Phe, Ala, Gly, norisoleucine, citrulline, or ornithine.

3. The insulin analog of claim 1 wherein B.sub.28 is Lys.

4. The insulin analog of claim 1 wherein A.sub.21 is Ala.

5. The insulin analog of claim 1 wherein B.sub.1 is absent.

6. The insulin analog of claim 5 wherein B.sub.10 is Asp.

7. The insulin analog of claim 5 wherein B.sub.2 is absent.

8. The insulin analog of claim 6 wherein B.sub.2 is absent.

9. The insulin analog of claim 1 wherein B.sub.30 is absent.

10. The insulin analog of claim 1 wherein B.sub.30 is Ala.

11. An insulin analog of the formula ##STR12##

12. The insulin analog of claim 1 wherein A.sub.21 is Ala, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is Thr.

13. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is Thr.

14. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is Val, B.sub.10 is Asp, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is Thr.

15. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is absent, B.sub.10 is His, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is Thr.

16. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is absent, B.sub.10 is Asp, B.sub.28 is Lys, B29 is Pro, and B.sub.30 is Thr.

17. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is absent.

18. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Lys, B.sub.29 is Pro, and B.sub.30 is Ala.

19. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

20. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), and D-lysine.

21. The insulin analog of claim 1 wherein A.sub.21 is Ala, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

22. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

23. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is Val, B.sub.10 is Asp, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

24. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is absent, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

25. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is absent, B.sub.2 is absent, B.sub.10 is Asp, B.sub.28 is Pro, B.sub.30 is Thr, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

26. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is absent, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

27. The insulin analog of claim 1 wherein A.sub.21 is Asn, B.sub.1 is Phe, B.sub.2 is Val, B.sub.10 is His, B.sub.28 is Pro, B.sub.30 is Ala, and B.sub.29 is selected from the group consisting of L-(N-methyllysine), D-lysine, L-(N-methylarginine), and D-arginine.

28. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 1.

29. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 2.

30. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 3.

31. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 4.

32. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 5.

33. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 6.

34. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 7.

35. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 8.

36. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 9.

37. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 10.

38. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog of the formula ##STR13##

39. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 12.

40. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 13.

41. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 14.

42. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 15.

43. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 16.

44. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 17.

45. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 18.

46. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 19.

47. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 20.

48. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 21.

49. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 22.

50. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 23.

51. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 24.

52. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 25.

53. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an, insulin analog according to claim 26.

54. A method of treating hyperglycemia which comprises administering, to a patient in need thereof, an effective amount of an insulin analog according to claim 27.

55. A pharmaceutical composition which comprises an insulin analog according to claim 1 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

56. A pharmaceutical composition which comprises an insulin analog according to claim 2 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

57. A pharmaceutical composition which comprises an insulin analog according to claim 3 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

58. A pharmaceutical composition which comprises an insulin analog according to claim 4 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

59. A pharmaceutical composition which comprises an insulin analog according to claim 5 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

60. A pharmaceutical composition which comprises an insulin analog according to claim 6 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

61. A pharmaceutical composition which comprises an insulin analog according to claim 7 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

62. A pharmaceutical composition which comprises an insulin analog according to claim 8 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

63. A pharmaceutical composition which comprises an insulin analog according to claim 9 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

64. A pharmaceutical composition which comprises an insulin analog according to claim 10 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

65. A pharmaceutical composition which comprises an insulin analog of the formula ##STR14## in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

66. A pharmaceutical composition which comprises an insulin analog according to claim 12 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

67. A pharmaceutical composition which comprises an insulin analog according to claim 13 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

68. A pharmaceutical composition which comprises an insulin analog according to claim 14 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

69. A pharmaceutical composition which comprises an insulin analog according to claim 15 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

70. A pharmaceutical composition which comprises an insulin analog according to claim 16 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

71. A pharmaceutical composition which comprises an insulin analog according to claim 17 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

72. A pharmaceutical composition which comprises an insulin analog according to claim 18 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

73. A pharmaceutical composition which comprises an insulin analog according to claim 19 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

74. A pharmaceutical composition which comprises an insulin analog according to claim 20 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

75. A pharmaceutical composition which comprises an insulin analog according to claim 21 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

76. A pharmaceutical composition which comprises an insulin analog according to claim 22 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

77. A pharmaceutical composition which comprises an insulin analog according to claim 23 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

78. A pharmaceutical composition which comprises an insulin analog according to claim 24 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

79. A pharmaceutical composition which comprises an insulin analog according to claim 25 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

80. A pharmaceutical composition which comprises an insulin analog according to claim 26 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.

81. A pharmaceutical composition which comprises an insulin analog according to claim 27 in combination with a pharmaceutically acceptable carrier, diluent, or excipient.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc