Patent · US9018160B2 · B2 · US
Peptide tyrosine tyrosine analogues
- (11) Publication number
- US9018160B2
- (21) Application number
- 13/575,133
- (22) Filing date
- 2011-01-27
- (30) Priority date
- 2010-01-27
- (43) Publication date
- 2015-04-28
- (45) Date of grant
- 2015-04-28
- (51) IPC
- A61K 38/00; B65G 23/00; B66B 23/02; C07K 14/475; C07K 14/575
- (52) CPC
- C07K Peptides: 14/575, 14/435, 14/57545
- A61K Preparations for medical, dental or toiletry purposes: 38/00, 38/22
- A61P Specific therapeutic activity of chemical compounds or medicinal preparations: 3/04, 3/10
- B65G Transport or storage devices, e.g. conveyors for loading or tipping, shop conveyor systems or pneumatic tube conveyors: 23/00, 2812/02316
- (73) Assignee
- BLOOM STEPHEN ROBERT; IMP INNOVATIONS LTD
- (72) Inventors
- BLOOM STEPHEN ROBERT
- (54) Title
- Peptide tyrosine tyrosine analogues
- (57) Abstract
Peptide analogues of PYY, compositions comprising said analogues and methods of using said analogues for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as diabetes and obesity, and for a reduction in appetite, reduction in food intake or reduction of calorie intake in a subject.
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Claims (14)
- An analogue of Peptide Tyrosine Tyrosine (PYY) comprising an amino acid sequence represented by formula (I) (SEQ ID NO: 1) Xaa 2 -Ile-Xaa 4 -Pro-Xaa 6 -Ala-Pro-Gly-Glu-Asp-Ala- Ser-Pro-Glu-Xaa 16 -Xaa 17 -Xaa 18 -Xaa 19 -Tyr-Xaa 21 - Xaa 22 -Ala-Leu-Xaa 25 -His-Tyr-Leu-Asn-Xaa 30 -Val- Thr-Arg-Gln-Arg-Tyr-NH 2 (I) wherein Xaa 2 is Pro; Xaa 4 is selected from the group consisting of His and Lys; Xaa 6 is selected from the group consisting of Asp, Glu, His, Lys, Ser, Thr and Val; Xaa 16 is selected from the group consisting of Gln and Glu; Xaa 17 is selected from the group consisting of Ile and Leu; Xaa 18 is selected from the group consisting of Ala, Asn, Asp and Val; Xaa 19 is selected from the group consisting of Arg and His; Xaa 21 is selected from the group consisting of His, Phe and Tyr; Xaa 22 is selected from the group consisting of Ala and Ile; Xaa 25 is selected from the group consisting of Arg, Gln and His; and Xaa 30 is His; or an analogue of PYY of formula (I) that has been modified by one or more processes selected from the group consisting of amidation, glycosylation, carbamylation, acylation, sulfation, phosphylation, cyclization, lipidization, and pegylation; or a salt and/or solvate thereof.
- An analogue of PYY as claimed in claim 1, wherein Xaa 16 is Glu.
- An analogue of PYY as claimed in claim 2, wherein Xaa 25 is Arg.
- An analogue of PYY as claimed in claim 1, wherein Xaa 4 is Lys; Xaa 6 is selected from the group consisting of Glu and Ser; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 21 is Tyr; and Xaa 22 is Ala.
- An analogue of PYY as claimed in claim 4, wherein Xaa 19 is His.
- An analogue of PYY as claimed in claim 5, wherein Xaa 6 is Glu.
- An analogue of PYY as claimed in claim 1, wherein Xaa 4 is His; Xaa 6 is His; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 21 is Tyr; and Xaa 22 is Ala.
- An analogue of PPY as claim 7, wherein Xaa 19 is His.
- An analogue of PYY as claimed in claim 1, wherein the analogue is produced by a recombinant method.
- An analogue of PYY as claimed in claim 1, wherein the analogue is produced by a synthetic method.
- A pharmaceutical composition comprising an analogue of PYY as claimed in claim 1 together with a pharmaceutically acceptable carrier and optionally other therapeutic ingredients.
- A pharmaceutical composition as claimed in claim 11, which is present in a syringe or other administration device for subcutaneous administration to humans.
- An analogue of PPY as claimed in claim 1, wherein Xaa 4 is His; Xaa 6 is His; Xaa 16 is Glu; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 19 is His; Xaa 21 is Tyr; Xaa 22 is Ala; and Xaa 25 is Arg.
- An analogue of Peptide Tyrosine Tyrosine (PPY) comprising an amino acid sequence represented by formula (I) (SEQ ID NO: 1) Xaa 2 -Ile-Xaa 4 -Pro-Xaa 6 -Ala-Pro-Gly-Glu-Asp-Ala- Ser-Pro-Glu-Xaa 16 -Xaa 17 -Xaa 18 -Xaa 19 -Tyr-Xaa 21 - Xaa 22 -Ala-Leu-Xaa 25 -His-Tyr-Leu-Asn-Xaa 30 -Val- Thr-Arg-Gln-Arg-Tyr-NH 2 (I) wherein Xaa 2 is Pro; Xaa 4 is selected from the group consisting of His and Lys; Xaa 6 is selected from the group consisting of Asp, Glu, His, Lys, Ser, Thr and Val; Xaa 16 is selected from the group consisting of Gln and Glu; Xaa 17 is selected from the group consisting of Ile and Leu; Xaa 18 is selected from the group consisting of Ala, Asn, Asp and Val; Xaa 19 is selected from the group consisting of Arg and His; Xaa 21 is selected from the group consisting of His, Phe and Tyr; Xaa 22 is selected from the group consisting of Ala and Ile; Xaa 25 is selected from the group consisting of Arg, Gln and His; and Xaa 30 is His; or a salt and/or solvate thereof.
Description
This application is the U.S. national phased of International Application No. PCT/GB2011/000110, filed 27 Jan. 2011, which designated the U.S. and claims priority to GB 100333.2 filed 27 Jan. 2010; the entire contents of each of which are hereby incorporated by reference. 1. FIELD OF THE INVENTION This application relates to the use of agents to control appetite, feeding, food intake, energy expenditure and calorie intake, particularly in the field of obesity. 2. BACKGROUND OF THE INVENTION According to the National Health and Nutrition Examination Survey (NHANES III, 1988 to 1994), between one third and one half of men and women in the United States are overweight. In the United States, sixty percent of men and fifty-one percent of women, of the age of 20 or older, are either overweight or obese. In addition, a large percentage of children in the United States are overweight or obese. The cause of obesity is complex and multi-factorial. Increasing evidence suggests that obesity is not a simple problem of self-control but is a complex disorder involving appetite regulation and energy metabolism. In addition, obesity is associated with a variety of conditions associated with increased morbidity and mortality in a population. Although the etiology of obesity is not definitively established, genetic, metabolic, biochemical, cultural and psychosocial factors are believed to contribute. In general, obesity has been described as a condition in which excess body fat puts an individual at a health risk.
Citations (34)
- US2005002927A1
- US2006094652A1
- US2006094653A1
- US2006135747A1
- US2006243232A1
- US2009186811A1
- US2009215682A1
- US2009318347A1
- US2010279930A1
- US4179337A
- US5936092A
- US6093692A
- US6225445B1
- US6355478B1
- US6410707B2
- US6420352B1
- US7723471B2
- US7928060B2
- US8076288B2
- US8114958B2
- US8202836B2
- US8263736B2
- WO03026591A2
- WO2005077072A2
- WO2005077094A2
- WO2005089786A2
- WO2005089789A2
- WO2005089790A2
- WO2006066024A2
- WO2007008778A2
- WO2007022123A2
- WO2008003947A1
- WO9309227A1
- WO9505848A1
Record as JSON
{
"publication_number": "US9018160B2",
"country": "US",
"kind": "B2",
"title": "Peptide tyrosine tyrosine analogues",
"abstract": "Peptide analogues of PYY, compositions comprising said analogues and methods of using said analogues for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as diabetes and obesity, and for a reduction in appetite, reduction in food intake or reduction of calorie intake in a subject.",
"claims": [
"1. An analogue of Peptide Tyrosine Tyrosine (PYY) comprising an amino acid sequence represented by formula (I) (SEQ ID NO: 1) Xaa 2 -Ile-Xaa 4 -Pro-Xaa 6 -Ala-Pro-Gly-Glu-Asp-Ala- Ser-Pro-Glu-Xaa 16 -Xaa 17 -Xaa 18 -Xaa 19 -Tyr-Xaa 21 - Xaa 22 -Ala-Leu-Xaa 25 -His-Tyr-Leu-Asn-Xaa 30 -Val- Thr-Arg-Gln-Arg-Tyr-NH 2 (I) wherein Xaa 2 is Pro; Xaa 4 is selected from the group consisting of His and Lys; Xaa 6 is selected from the group consisting of Asp, Glu, His, Lys, Ser, Thr and Val; Xaa 16 is selected from the group consisting of Gln and Glu; Xaa 17 is selected from the group consisting of Ile and Leu; Xaa 18 is selected from the group consisting of Ala, Asn, Asp and Val; Xaa 19 is selected from the group consisting of Arg and His; Xaa 21 is selected from the group consisting of His, Phe and Tyr; Xaa 22 is selected from the group consisting of Ala and Ile; Xaa 25 is selected from the group consisting of Arg, Gln and His; and Xaa 30 is His; or an analogue of PYY of formula (I) that has been modified by one or more processes selected from the group consisting of amidation, glycosylation, carbamylation, acylation, sulfation, phosphylation, cyclization, lipidization, and pegylation; or a salt and/or solvate thereof.",
"2. An analogue of PYY as claimed in claim 1, wherein Xaa 16 is Glu.",
"3. An analogue of PYY as claimed in claim 2, wherein Xaa 25 is Arg.",
"4. An analogue of PYY as claimed in claim 1, wherein Xaa 4 is Lys; Xaa 6 is selected from the group consisting of Glu and Ser; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 21 is Tyr; and Xaa 22 is Ala.",
"5. An analogue of PYY as claimed in claim 4, wherein Xaa 19 is His.",
"6. An analogue of PYY as claimed in claim 5, wherein Xaa 6 is Glu.",
"7. An analogue of PYY as claimed in claim 1, wherein Xaa 4 is His; Xaa 6 is His; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 21 is Tyr; and Xaa 22 is Ala.",
"8. An analogue of PPY as claim 7, wherein Xaa 19 is His.",
"9. An analogue of PYY as claimed in claim 1, wherein the analogue is produced by a recombinant method.",
"10. An analogue of PYY as claimed in claim 1, wherein the analogue is produced by a synthetic method.",
"11. A pharmaceutical composition comprising an analogue of PYY as claimed in claim 1 together with a pharmaceutically acceptable carrier and optionally other therapeutic ingredients.",
"12. A pharmaceutical composition as claimed in claim 11, which is present in a syringe or other administration device for subcutaneous administration to humans.",
"13. An analogue of PPY as claimed in claim 1, wherein Xaa 4 is His; Xaa 6 is His; Xaa 16 is Glu; Xaa 17 is Leu; Xaa 18 is Asn; Xaa 19 is His; Xaa 21 is Tyr; Xaa 22 is Ala; and Xaa 25 is Arg.",
"14. An analogue of Peptide Tyrosine Tyrosine (PPY) comprising an amino acid sequence represented by formula (I) (SEQ ID NO: 1) Xaa 2 -Ile-Xaa 4 -Pro-Xaa 6 -Ala-Pro-Gly-Glu-Asp-Ala- Ser-Pro-Glu-Xaa 16 -Xaa 17 -Xaa 18 -Xaa 19 -Tyr-Xaa 21 - Xaa 22 -Ala-Leu-Xaa 25 -His-Tyr-Leu-Asn-Xaa 30 -Val- Thr-Arg-Gln-Arg-Tyr-NH 2 (I) wherein Xaa 2 is Pro; Xaa 4 is selected from the group consisting of His and Lys; Xaa 6 is selected from the group consisting of Asp, Glu, His, Lys, Ser, Thr and Val; Xaa 16 is selected from the group consisting of Gln and Glu; Xaa 17 is selected from the group consisting of Ile and Leu; Xaa 18 is selected from the group consisting of Ala, Asn, Asp and Val; Xaa 19 is selected from the group consisting of Arg and His; Xaa 21 is selected from the group consisting of His, Phe and Tyr; Xaa 22 is selected from the group consisting of Ala and Ile; Xaa 25 is selected from the group consisting of Arg, Gln and His; and Xaa 30 is His; or a salt and/or solvate thereof."
],
"description_excerpt": "This application is the U.S. national phased of International Application No. PCT/GB2011/000110, filed 27 Jan. 2011, which designated the U.S. and claims priority to GB 100333.2 filed 27 Jan. 2010; the entire contents of each of which are hereby incorporated by reference. 1. FIELD OF THE INVENTION This application relates to the use of agents to control appetite, feeding, food intake, energy expenditure and calorie intake, particularly in the field of obesity. 2. BACKGROUND OF THE INVENTION According to the National Health and Nutrition Examination Survey (NHANES III, 1988 to 1994), between one third and one half of men and women in the United States are overweight. In the United States, sixty percent of men and fifty-one percent of women, of the age of 20 or older, are either overweight or obese. In addition, a large percentage of children in the United States are overweight or obese. The cause of obesity is complex and multi-factorial. Increasing evidence suggests that obesity is not a simple problem of self-control but is a complex disorder involving appetite regulation and energy metabolism. In addition, obesity is associated with a variety of conditions associated with increased morbidity and mortality in a population. Although the etiology of obesity is not definitively established, genetic, metabolic, biochemical, cultural and psychosocial factors are believed to contribute. In general, obesity has been described as a condition in which excess body fat puts an individual at a health risk.",
"cpc": [
"C07K 14/575",
"A61K 38/00",
"A61K 38/22",
"A61P 3/04",
"A61P 3/10",
"B65G 23/00",
"B65G 2812/02316",
"C07K 14/435",
"C07K 14/57545"
],
"ipc": [
"A61K 38/00",
"B65G 23/00",
"B66B 23/02",
"C07K 14/475",
"C07K 14/575"
],
"assignees": [
"BLOOM STEPHEN ROBERT",
"IMP INNOVATIONS LTD"
],
"inventors": [
"BLOOM STEPHEN ROBERT"
],
"filing_date": "2011-01-27",
"publication_date": "2015-04-28",
"grant_date": "2015-04-28",
"priority_date": "2010-01-27",
"application_number": "US-201113575133-A",
"family_id": "42084054",
"citations": [
"US2005002927A1",
"US2006094652A1",
"US2006094653A1",
"US2006135747A1",
"US2006243232A1",
"US2009186811A1",
"US2009215682A1",
"US2009318347A1",
"US2010279930A1",
"US4179337A",
"US5936092A",
"US6093692A",
"US6225445B1",
"US6355478B1",
"US6410707B2",
"US6420352B1",
"US7723471B2",
"US7928060B2",
"US8076288B2",
"US8114958B2",
"US8202836B2",
"US8263736B2",
"WO03026591A2",
"WO2005077072A2",
"WO2005077094A2",
"WO2005089786A2",
"WO2005089789A2",
"WO2005089790A2",
"WO2006066024A2",
"WO2007008778A2",
"WO2007022123A2",
"WO2008003947A1",
"WO9309227A1",
"WO9505848A1"
]
}
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