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93. (GB2427550) Y2/Y4 selective receptor agonists for therapeutic interventions

Application Number: 0618812 Application Date: 17.03.2005
Publication Number: 2427550 Publication Date: 08.11.2006
Publication Kind : B
IPC:
A61K 38/17
A61K 8/00
A61P 3/04
C07K 14/705
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17
from animals; from humans
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
8
Cosmetics or similar toilet preparations
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
705
Receptors; Cell surface antigens; Cell surface determinants
CPC:
C07K 14/70571
A61K 38/00
A61K 38/22
Applicants: 7TM PHARMA AS
Inventors: SCHWARTZ THUE
Priority Data: 200400436 17.03.2004 DK
2005002982 17.03.2005 EP
0503111 14.02.2005 GB
55893204 01.04.2004 US
58596404 06.07.2004 US
Title: (EN) Y2/Y4 selective receptor agonists for therapeutic interventions
Abstract:
(EN) Y receptor agonists which are selective for Y2 and Y4 receptors over the Y1 receptor are useful for treatment of, for example obesity, are (a) PP-fold peptides or PP-fold peptides mimics which have (i) a C-terminal Y receptor-recognition amino acid sequence represented by -X-Thr-Arg-X<3>-Arg-Tyr-C(=0)NR<1>R<2> wherein R<1> and R<1> are independently hydrogen or C1-C6 alkyl X is Val, lle, Leu or Ala, and X<3> is Gln or Asn, or a conservatively substituted variant thereof in which Thr is replaced by His or Asn and/or Tyr is replaced by Trp or Phe; and/or Arg is replaced by Lys, and (ii) an N-terminal Y receptor-recognition amino acid sequence represented by H2N-X<1>-Pro-X<2>-(Glu or Asp)- wherein X<1> is not present or is amino acid residue, and X<2> is Leu or Ser or conservative substitutions of Leu or Ser, or (b) the said comprise a C-terminal Y receptor-recognition amino acid sequence as defined in (i) above, said Y receptor-recognition sequence being fused to an amphiphilic amino acid sequence domain comprising at least one alpha helical turn adjacent the N-terminus of the said hexapeptide sequence, said turn being constrained in a helical configuration by a covalent intramolecular link, and optionally an N-terminal sequence which commences with a Y receptor-recognition amino acid sequence as defined in (ii) above.