US2010331245A1PendingUtilityA1
Peptide yy analogs

Assignee: DONG ZHENG XINPriority: Jan 17, 2003Filed: Aug 31, 2010Published: Dec 30, 2010
Est. expiryJan 17, 2023(expired)· nominal 20-yr term from priority
Inventors:Zheng Xin Dong
A61P 3/10C07K 14/57545C07K 14/575A61P 3/00A61P 3/04A61K 38/00
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Claims
Abstract

The invention provides analogs of PYY. The invention also provides compositions and methods useful for controlling biological activities such as cell proliferation, nutrient transport, lipolysis, and intestinal water and electrolyte secretion.
Claims

exact text as granted — not AI-modified
1 . A method of regulating cell proliferation in a mammal in need thereof, said method comprising administering to said mammal an effective amount of a compound according to any one of the following compounds, or a pharmaceutically acceptable salt thereof:
 ((2,3,4,5,6-F)Phe 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 31)   ((2,3,4,5,6-F)Phe 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 32)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 33)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 34)   ((2,3,4,5,6-F)Phe 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 35)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 36)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 37)   ((2,3,4,5,6-F)Phe 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 38)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 39)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 40)   ((2,3,4,5,6-F)Phe 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 41)   ((3,4,5-F)Phe 20 )h PYY(3-36)NH 2 ; (SEQ ID NO. 42)   ((3,4,5-F)Phe 21 )h PYY(3-36)NH 2 ; (SEQ ID NO. 43)   Ac-((3,4,5-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 44)   Ac-((3,4,5-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 45)   ((3,4,5-F)Phe 26 )h PYY(3-36)NH 2 ; (SEQ ID NO. 46)   Ac-((3,4,5-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 15)   Ac-((3,4,5-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 47)   ((3,4,5-F)Phe 27 )h PYY(3-36)NH 2 ; (SEQ ID NO. 12)   Ac-((3,4,5-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 48)   Ac-((3,4,5-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 49)   ((3,4,5-F)Phe 36 )h PYY(3-36)NH 2 ; (SEQ ID NO. 50)   Ac-(D2Pal 26 )h PYY(22-36)NH 2 ; (SEQ ID NO. 26)   Ac-(2Pal 26 )h PYY(22-36)NH 2 ; (SEQ ID NO. 27)   Ac-(2Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 18)   Ac-(3Pal 26 )h PYY(22-36)NH 2 ; (SEQ ID NO. 14)   (3Pal 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 5)   Ac-(3Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 16)   Ac-(4Pal 26 )h PYY(22-36)NH 2 ; (SEQ ID NO. 13)   Ac-(4Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 17)   Ac-(A5c 22 )hPYY(22-36)NH 2  (SEQ ID NO. 4)   Ac-(A5c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 24)   Ac-(A5c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 51)   (A5c 31 )hPYY(3-36)NH 2  (SEQ ID NO. 3)   (A6c 10 )hPYY(3-36)NH 2 ; (SEQ ID NO. 52)   (A6c 11 )hPYY(3-36)NH 2 ; (SEQ ID NO. 53)   (A6c 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 54)   (A6c 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 55)   (A6c 15 )hPYY(3-36)NH 2 ; (SEQ ID NO. 56)   (A6c 16 )hPYY(3-36)NH 2 ; (SEQ ID NO. 57)   (A6c 17 )hPYY(3-36)NH 2 ; (SEQ ID NO. 58)   (A6c 18 )hPYY(3-36)NH 2 ; (SEQ ID NO. 59)   (A6c 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 60)   (A6c 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 61)   Ac-(A6c 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 62)   (A6c 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 63)   Ac-(A6c 24 )hPYY(22-36)NH 2 ; (SEQ ID NO. 25)   Ac-(A6c 24 )hPYY(24-36)NH 2 ; (SEQ ID NO. 64)   (A6C 24 )hPYY(3-36)NH 2 ; (SEQ ID NO. 10)   Ac-(A6c 24 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 28)   Ac-(A6c 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 65)   Ac-(A6c 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 66)   (A6c 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 67)   Ac-(A6c 28 )hPYY(22-36)NH 2 ; (SEQ ID NO. 23)   Ac-(A6c 28 )hPYY(24-36)NH 2 ; (SEQ ID NO. 68)   (A6c 28 )hPYY(3-36)NH 2 ; (SEQ ID NO. 8)   Ac-(A6c 28 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 29)   Ac-(A6c 29 )hPYY(22-36)NH 2 ; (SEQ ID NO. 69)   Ac-(A6c 29 )hPYY(24-36)NH 2 ; (SEQ ID NO. 70)   (A6c 29 )hPYY(3-36)NH 2 ; (SEQ ID NO. 71)   (A6c 3 )hPYY(3-36)NH 2 ; (SEQ ID NO. 72)   Ac-(A6c 30 )hPYY(22-36)NH 2 ; (SEQ ID NO. 22)   Ac-(A6c 30 )hPYY(24-36)NH 2 ; (SEQ ID NO. 73)   (A6c 30 )hPYY(3-36)NH 2 ; (SEQ ID NO. 9)   Ac-(A6c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 21)   Ac-(A6c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 30)   (A6c 31 )hPYY(3-36)NH 2 ; (SEQ ID NO. 74)   Ac-(A6c 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 75)   Ac-(A6c 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 76)   (A6c 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 77)   (A6c 6 )hPYY(3-36)NH 2 ; (SEQ ID NO. 78)   (A6c 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 79)   (A6c 9 )hPYY(3-36)NH 2 ; (SEQ ID NO. 80)   (Act 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 81)   (Act 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 82)   Ac-(Act 23 )hPYY(22-36)NH 2 ; (SEQ ID NO. 83)   (Act 23 )hPYY(3-36)NH 2 ; (SEQ ID NO. 84)   Ac-(Act 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 85)   Ac-(Act 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 86)   (Act 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 87)   (Act 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 88)   Ac-(Aib 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 89)   (Aib 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 11)   (Apc 16 )hPYY(3-36)NH 2 ; (SEQ ID NO. 90)   Ac-(Apc 25 )hPYY(22-36)NH 2 ; (SEQ ID NO. 91)   Ac-(Apc 25 )hPYY(24-36)NH 2 ; (SEQ ID NO. 92)   (Apc 25 )hPYY(3-36)NH 2 ; (SEQ ID NO. 93)   Ac-(Apc 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 94)   Ac-(Apc 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 95)   (Apc 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 96)   Ac-(Apc 33 )hPYY(22-36)NH 2 ; (SEQ ID NO. 97)   Ac-(Apc 33 )hPYY(24-36)NH 2 ; (SEQ ID NO. 98)   (Apc 33 )hPYY(3-36)NH 2 ; (SEQ ID NO. 99)   Ac-(Apc 34 )hPYY(22-36)NH 2 ; (SEQ ID NO. 100)   Ac-(Apc 34 )hPYY(24-36)NH 2 ; (SEQ ID NO. 101)   (Apc 34 )hPYY(3-36)NH 2 ; (SEQ ID NO. 102)   Ac-(Apc 35 )hPYY(22-36)NH 2 ; (SEQ ID NO. 103)   Ac-(Apc 35 )hPYY(24-36)NH 2 ; (SEQ ID NO. 104)   (Apc 35 )hPYY(3-36)NH 2 ; (SEQ ID NO. 7)   Ac-(Apc 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 105)   Ac-(Apc 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 106)   (Apc 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 107)   (Apc 4 )hPYY(3-36)NH 2 ; (SEQ ID NO. 108)   (Taz 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 6)   Ac-(Taz 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 20)   Ac-(Taz 26 , Leu 31 )hPPY(24-36)NH 2.  (SEQ ID NO. 19)   
     
     
         2 . A method of  claim 1 , wherein said cell is a gastrointestinal cell. 
     
     
         3 . A method of  claim 1 , wherein said cell is an epithelial cell. 
     
     
         4 . A method of facilitating weight loss, appetite decrease, weight maintenance, treating obesity, treating diabetes, treating complications of diabetes including retinopathy, or treating cardiovascular disorders in a mammal in need thereof, said method comprising administering to said mammal an effective amount of a compound according to any one of the following compounds, or a pharmaceutically acceptable salt thereof:
 ((2,3,4,5,6-F)Phe 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 31)   ((2,3,4,5,6-F)Phe 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 32)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 33)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 34)   ((2,3,4,5,6-F)Phe 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 35)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 36)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 37)   ((2,3,4,5,6-F)Phe 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 38)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 39)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 40)   ((2,3,4,5,6-F)Phe 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 41)   ((3,4,5-F)Phe 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 42)   ((3,4,5-F)Phe 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 43)   Ac-((3,4,5-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 44)   Ac-((3,4,5-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 45)   ((3,4,5-F)Phe 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 46)   Ac-((3,4,5-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 15)   Ac-((3,4,5-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 47)   ((3,4,5-F)Phe 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 12)   Ac-((3,4,5-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 48)   Ac-((3,4,5-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 49)   ((3,4,5-F)Phe 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 50)   Ac-(D2Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 26)   Ac-(2Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 27)   Ac-(2Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 18)   Ac-(3Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 14)   (3Pal 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 5)   Ac-(3Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 16)   Ac-(4Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 13)   Ac-(4Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 17)   Ac-(A5c 22 )hPYY(22-36)NH 2  (SEQ ID NO. 4)   Ac-(A5c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 24)   Ac-(A5c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 51)   (A5c 31 )hPYY(3-36)NH 2  (SEQ ID NO. 3)   (A6c 10 )hPYY(3-36)NH 2 ; (SEQ ID NO. 52)   (A6c 11 )hPYY(3-36)NH 2 ; (SEQ ID NO. 53)   (A6c 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 54)   (A6c 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 55)   (A6c 15 )hPYY(3-36)NH 2 ; (SEQ ID NO. 56)   (A6c 16 )hPYY(3-36)NH 2 ; (SEQ ID NO. 57)   (A6c 17 )hPYY(3-36)NH 2 ; (SEQ ID NO. 58)   (A6c 18 )hPYY(3-36)NH 2 ; (SEQ ID NO. 59)   (A6c 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 60)   (A6c 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 61)   Ac-(A6c 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 62)   (A6c 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 63)   Ac-(A6c 24 )hPYY(22-36)NH 2 ; (SEQ ID NO. 25)   Ac-(A6c 24 )hPYY(24-36)NH 2 ; (SEQ ID NO. 64)   (A6C 24 )hPYY(3-36)NH 2 ; (SEQ ID NO. 10)   Ac-(A6c 24 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 28)   Ac-(A6c 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 65)   Ac-(A6c 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 66)   (A6c 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 67)   Ac-(A6c 28 )hPYY(22-36)NH 2 ; (SEQ ID NO. 23)   Ac-(A6c 28 )hPYY(24-36)NH 2 ; (SEQ ID NO. 68)   (A6c 28 )hPYY(3-36)NH 2 ; (SEQ ID NO. 8)   Ac-(A6c 28 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 29)   Ac-(A6c 29 )hPYY(22-36)NH 2 ; (SEQ ID NO. 69)   Ac-(A6c 29 )hPYY(24-36)NH 2 ; (SEQ ID NO. 70)   (A6c 29 )hPYY(3-36)NH 2 ; (SEQ ID NO. 71)   (A6c 3 )hPYY(3-36)NH 2 ; (SEQ ID NO. 72)   Ac-(A6c 30 )hPYY(22-36)NH 2 ; (SEQ ID NO. 22)   Ac-(A6c 30 )hPYY(24-36)NH 2 ; (SEQ ID NO. 73)   (A6c 30 )hPYY(3-36)NH 2 ; (SEQ ID NO. 9)   Ac-(A6c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 21)   Ac-(A6c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 30)   (A6c 31 )hPYY(3-36)NH 2 ; (SEQ ID NO. 74)   Ac-(A6c 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 75)   Ac-(A6c 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 76)   (A6c 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 77)   (A6c 6 )hPYY(3-36)NH 2 ; (SEQ ID NO. 78)   (A6c 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 79)   (A6c 9 )hPYY(3-36)NH 2 ; (SEQ ID NO. 80)   (Act 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 81)   (Act 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 82)   Ac-(Act 23 )hPYY(22-36)NH 2 ; (SEQ ID NO. 83)   (Act 23 )hPYY(3-36)NH 2 ; (SEQ ID NO. 84)   Ac-(Act 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 85)   Ac-(Act 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 86)   (Act 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 87)   (Act 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 88)   Ac-(Aib 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 89)   (Aib 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 11)   (Apc 19 )hPYY(3-36)NH 2 ; (SEQ ID NO. 90)   Ac-(Apc 25 )hPYY(22-36)NH 2 ; (SEQ ID NO. 91)   Ac-(Apc 25 )hPYY(24-36)NH 2 ; (SEQ ID NO. 92)   (Apc 25 )hPYY(3-36)NH 2 ; (SEQ ID NO. 93)   Ac-(Apc 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 94)   Ac-(Apc 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 95)   (Apc 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 96)   Ac-(Apc 33 )hPYY(22-36)NH 2 ; (SEQ ID NO. 97)   Ac-(Apc 33 )hPYY(24-36)NH 2 ; (SEQ ID NO. 98)   (Apc 33 )hPYY(3-36)NH 2 ; (SEQ ID NO. 99)   Ac-(Apc 34 )hPYY(22-36)NH 2 ; (SEQ ID NO. 100)   Ac-(Apc 34 )hPYY(24-36)NH 2 ; (SEQ ID NO. 101)   (Apc 34 )hPYY(3-36)NH 2 ; (SEQ ID NO. 102)   Ac-(Apc 35 )hPYY(22-36)NH 2 ; (SEQ ID NO. 103)   Ac-(Apc 35 )hPYY(24-36)NH 2 ; (SEQ ID NO. 104)   (Apc 35 )hPYY(3-36)NH 2 ; (SEQ ID NO. 7)   Ac-(Apc 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 105)   Ac-(Apc 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 106)   (Apc 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 107)   (Apc 4 )hPYY(3-36)NH 2 ; (SEQ ID NO. 108)   (Taz 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 6)   Ac-(Taz 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 20)   Ac-(Taz 26 , Leu 31 )hPPY(24-36)NH 2  (SEQ ID NO. 19)   
     
     
         5 . A method according to  claim 4 , wherein excessive weight is a contributing factor to a disease or condition including hypertension, diabetes, dyslipidemia, cardiovascular disease, gall stones, osteoarthritis and cancers. 
     
     
         6 . A method according to  claim 5 , wherein said facilitation of weight loss reduces the likelihood of such diseases or conditions or where said facilitation of weight loss comprises at least part of a treatment for such diseases or conditions. 
     
     
         7 . A method of antagonizing the effects of PYY(3-36) in a mammal in need thereof, said method comprising administering to said mammal an effective amount of a compound according to any one of the following compounds, or a pharmaceutically acceptable salt thereof:
 ((2,3,4,5,6-F)Phe 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 31)   ((2,3,4,5,6-F)Phe 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 32)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 33)   Ac-((2,3,4,5,6-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 34)   ((2,3,4,5,6-F)Phe 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 35)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 36)   Ac-((2,3,4,5,6-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 37)   ((2,3,4,5,6-F)Phe 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 38)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 39)   Ac-((2,3,4,5,6-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 40)   ((2,3,4,5,6-F)Phe 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 41)   ((3,4,5-F)Phe 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 42)   ((3,4,5-F)Phe 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 43)   Ac-((3,4,5-F)Phe 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 44)   Ac-((3,4,5-F)Phe 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 45)   ((3,4,5-F)Phe 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 46)   Ac-((3,4,5-F)Phe 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 15)   Ac-((3,4,5-F)Phe 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 47)   ((3,4,5-F)Phe 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 12)   Ac-((3,4,5-F)Phe 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 48)   Ac-((3,4,5-F)Phe 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 49)   ((3,4,5-F)Phe 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 50)   Ac-(D2Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 26)   Ac-(2Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 27)   Ac-(2Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 18)   Ac-(3Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 14)   (3Pal 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 5)   Ac-(3Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 16)   Ac-(4Pal 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 13)   Ac-(4Pal 26 , Leu 31 )hPPY(24-36)NH 2 ; (SEQ ID NO. 17)   Ac-(A5c 22 )hPYY(22-36)NH 2  (SEQ ID NO. 4)   Ac-(A5c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 24)   Ac-(A5c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 51)   (A5c 31 )1 - 1 PYY(3-36)NH 2  (SEQ ID NO. 3)   (A6c 10 )hPYY(3-36)NH 2 ; (SEQ ID NO. 52)   (A6c 11 )hPYY(3 - 36)NH 2 ; (SEQ ID NO. 53)   (A6c 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 54)   (A6c 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 55)   (A6c 15 )hPYY(3-36)NH 2 ; (SEQ ID NO. 56)   (A6c 16 )hPYY(3-36)NH 2 ; (SEQ ID NO. 57)   (A6c 17 )hPYY(3-36)NH 2 ; (SEQ ID NO. 58)   (A6c 18 )hPYY(3-36)NH 2 ; (SEQ ID NO. 59)   (A6c 20 )hPYY(3-36)NH 2 ; (SEQ ID NO. 60)   (A6c 21 )hPYY(3-36)NH 2 ; (SEQ ID NO. 61)   Ac-(A6c 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 62)   (A6c 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 63)   Ac-(A6c 24 )hPYY(22-36)NH 2 ; (SEQ ID NO. 25)   Ac-(A6c 24 )hPYY(24-36)NH 2 ; (SEQ ID NO. 64)   (A6C 24 )hPYY(3-36)NH  2 ; (SEQ ID NO. 10)   Ac-(A6c 24 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 28)   Ac-(A6c 27 )hPYY(22-36)NH 2 ; (SEQ ID NO. 65)   Ac-(A6c 27 )hPYY(24-36)NH 2 ; (SEQ ID NO. 66)   (A6c 27 )hPYY(3-36)NH 2 ; (SEQ ID NO. 67)   Ac-(A6c 28 )hPYY(22-36)NH 2 ; (SEQ ID NO. 23)   Ac-(A6c 28 )hPYY(24-36)NH 2 ; (SEQ ID NO. 68)   (A6c 28 )hPYY(3-36)NH 2 ; (SEQ ID NO. 8)   Ac-(A6c 28 , Leu 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 29)   Ac-(A6c 29 )hPYY(22-36)NH 2 ; (SEQ ID NO. 69)   Ac-(A6c 29 )hPYY(24-36)NH 2 ; (SEQ ID NO. 70)   (A6c 29 )hPYY(3-36)NH 2 ; (SEQ ID NO. 71)   (A6c 3 )hPYY(3-36)NH 2 ; (SEQ ID NO. 72)   Ac-(A6c 30 )hPYY(22-36)NH 2 ; (SEQ ID NO. 22)   Ac-(A6c 30 )hPYY(24-36)NH 2 ; (SEQ ID NO. 73)   (A6c 30 )hPYY(3-36)NH 2 ; (SEQ ID NO. 9)   Ac-(A6c 31 )hPYY(22-36)NH 2 ; (SEQ ID NO. 21)   Ac-(A6c 31 )hPYY(24-36)NH 2 ; (SEQ ID NO. 30)   (A6c 31 )hPYY(3-36)NH 2 ; (SEQ ID NO. 74)   Ac-(A6c 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 75)   Ac-(A6c 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 76)   (A6c 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 77)   (A6c 6 )hPYY(3-36)NH 2 ; (SEQ ID NO. 78)   (A6c 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 79)   (A6c 9 )hPYY(3-36)NH 2 ; (SEQ ID NO. 80)   (Act 12 )hPYY(3-36)NH 2 ; (SEQ ID NO. 81)   (Act 13 )hPYY(3-36)NH 2 ; (SEQ ID NO. 82)   Ac-(Act 23 )hPYY(22-36)NH 2 ; (SEQ ID NO. 83)   (Act 23 )hPYY(3-36)NH 2 ; (SEQ ID NO. 84)   Ac-(Act 32 )hPYY(22-36)NH 2 ; (SEQ ID NO. 85)   Ac-(Act 32 )hPYY(24-36)NH 2 ; (SEQ ID NO. 86)   (Act 32 )hPYY(3-36)NH 2 ; (SEQ ID NO. 87)   (Act 7 )hPYY(3-36)NH 2 ; (SEQ ID NO. 88)   Ac-(Aib 22 )hPYY(22-36)NH 2 ; (SEQ ID NO. 89)   (Aib 22 )hPYY(3-36)NH 2 ; (SEQ ID NO. 11)   (Apc 18 )hPYY(3-36)NH 2 ; (SEQ ID NO. 90)   Ac-(Apc 25 )hPYY(22-36)NH 2 ; (SEQ ID NO. 91)   Ac-(Apc 25 )hPYY(24-36)NH 2 ; (SEQ ID NO. 92)   (Apc 25 )hPYY(3-36)NH 2 ; (SEQ ID NO. 93)   Ac-(Apc 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 94)   Ac-(Apc 26 )hPYY(24-36)NH 2 ; (SEQ ID NO. 95)   (Apc 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 96)   Ac-(Apc 33 )hPYY(22-36)NH 2 ; (SEQ ID NO. 97)   Ac-(Apc 33 )hPYY(24-36)NH 2 ; (SEQ ID NO. 98)   (Apc 33 )hPYY(3-36)NH 2 ; (SEQ ID NO. 99)   Ac-(Apc 34 )hPYY(22-36)NH 2 ; (SEQ ID NO. 100)   Ac-(Apc 34 )hPYY(24-36)NH 2 ; (SEQ ID NO. 101)   (Apc 34 )hPYY(3-36)NH 2 ; (SEQ ID NO. 102)   Ac-(Apc 35 )hPYY(22-36)NH 2 ; (SEQ ID NO. 103)   Ac-(Apc 35 )hPYY(24-36)NH 2 ; (SEQ ID NO. 104)   (Apc 35 )hPYY(3-36)NH 2 ; (SEQ ID NO. 7)   Ac-(Apc 36 )hPYY(22-36)NH 2 ; (SEQ ID NO. 105)   Ac-(Apc 36 )hPYY(24-36)NH 2 ; (SEQ ID NO. 106)   (Apc 36 )hPYY(3-36)NH 2 ; (SEQ ID NO. 107)   (Apc 4 )hPYY(3-36)NH 2 ; (SEQ ID NO. 108)   (Taz 26 )hPYY(3-36)NH 2 ; (SEQ ID NO. 6)   Ac-(Taz 26 )hPYY(22-36)NH 2 ; (SEQ ID NO. 20)   Ac-(Taz 26 , Leu 31 )hPPY(24-36)NH 2 . (SEQ ID NO. 19)    
     
     
         8 . A method according to  claim 7 , wherein said antagonist effects in said mammal comprise facilitating weight gain, facilitating maintenance in weight, and/or facilitating appetite increase. 
     
     
         9 . A method according to  claim 8 , wherein said facilitating weight gain, facilitating maintenance in weight, and/or facilitating appetite increase is indicated in a mammal having a disease or disorder, or under going a treatment, accompanied by weight loss. 
     
     
         10 . A method according to  claim 9 , wherein said diseases or disorders accompanied by weight loss include anorexia, bulimia, cancer cachexia, AIDS, wasting, cachexia, and wasting in frail elderly. 
     
     
         11 . A method according to  claim 9 , wherein said treatment accompanied by weight loss comprises chemotherapy, radiation therapy, temporary or permanent immobilization, or dialysis.
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