Novel compounds and their effects on feeding behaviour

An amino acid and sequence technology, applied in animal/human peptides, chemical instruments and methods, animal/human proteins, etc., can solve problems such as increasing treatment costs, reducing patient compliance, and inconvenience

Inactive Publication Date: 2009-11-11
IMPERIAL INNOVATIONS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, high clearance or rapid degradation of therapeutic agents is inconvenient in cases where it is desired to maintain high blood levels over an extended period of time, since repeated dosing would be required, reducing patient compliance and increasing treatment costs

Method used

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  • Novel compounds and their effects on feeding behaviour
  • Novel compounds and their effects on feeding behaviour
  • Novel compounds and their effects on feeding behaviour

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0507] Preparations for administration may be suitably formulated so as to administer controlled release of the compounds of the invention. For example, the pharmaceutical composition may be in the form of particles comprising one or more biodegradable polymers, polysaccharide gelling polymers and / or bioadhesive polymers, amphiphilic polymers, particles capable of modifying particles of compounds of the invention Reagents for interface features. These compositions exhibit certain biocompatibility features which allow controlled release of active substances. See US Patent No. 5,700,486.

[0508] The compounds of the invention can be delivered by pumps (see Langer, Science 249:1527-1533, 1990; Sefton, CRCCrit.Ref.Biomed.Eng.14:201, 1987; Buchwald et al., Surgery 88:507, 1980; et al., N. Engl. J. Med. 321:574, 1989) or by continuous subcutaneous infusion (eg using a mini-pump). Intravenous bag solutions are also available. A key factor in selecting an appropriate dosage is th...

Embodiment 1

[0545] Embodiment 1 (comparative example)

[0546] The fed efficacy (human) of natural oxyntomodulin was studied by intraperitoneal injection of 1400 nmol / kg into groups of fasted mice. Another group of mice was administered saline (control group). The mean cumulative food absorption over a continuous 24-hour period compared to saline is shown in figure 2 . High doses are given due to the relatively low activity of natural oxyntomodulin. Less pronounced results were observed with lower doses.

Embodiment 2

[0547] Embodiment 2 (comparative example)

[0548] The fed efficacy of natural oxyntomodulin (human) was studied by subcutaneous injection of 1400 nmol / kg into groups of fasted rats. Another group of rats was administered saline (control group). The mean cumulative food absorption over a continuous 6-hour period compared to saline is shown in image 3 . It can be seen that even at a high dose of 1400 nmol / kg, the natural oxyntomodulin fails to reduce food absorption in fasted rats in this case. At lower doses, the same lack of efficacy was observed.

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Abstract

The invention provides a peptide comprising the amino acid sequence given below, together with use of the peptide and methods associated therewith. The peptide finds particular use as an appetite suppressant and in the treatment of obesity. Xaa1 Xaa2 Xaa3 Gly4 Thr5 Phe6 Thr7 Ser8 Asp9 Tyr1O Ser1 1 Lys12 Tyr13 Leu14 Xaa15 Xaa16 Xaa17 Xaa18 Xaa19 Xaa20 Xaa21 Xaa22 Xaa23 Xaa24 Trp25 Leu26 Xaa27 Xaa28Xaa29 Xaa30 Xaa31 Xaa32 Lys33 Asn34 Asn35 Ue36 Ala37; wherein: Xaa1 is His1 or D-His1, Xaa2 is Ser2 or Ala2, Xaa3 is Gln3 or Asp3; Xaa15 Xaa16 Xaa17 Xaa18 Xaa19 Xaa20 Xaa21 Xaa22 Xaa23 Xaa24 is: G1u1 5 Glu16 G1u17 Leu18 Val19 Lys20 Tyr21 Phe22 Leu23 Glu24, Glu15 Glu16 Glu17 Leu18 Val19 Lys20 Tyr21 Phe22 Leu23 Gln24, Glu15 Glu16 Glu17 Leul18 Val19 Lys20 Tyr21 Phe22 Ile23 Glu24, Glu15 Glu16 Glu17 Leul18 Val19 Lys20 Tyr21 Phe22 Ile23 Gln24, Glu15 Glu16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Leu23 Glu24, Glu15 Glu16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Leu23 Gln24, Glu15 Glu16 Glu17 Ilel18 Val19 Lys20Tyr21 Phe22 Ile23 Glu24, Glu15 Glu16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Ile23 Gln24, Glu15 Gln16 Glu17 Leu18 Val19 Lys20 Tyr21 Phe22 Leu23 Glu24, Glu15 Gln16 G1u17 Leu18 Val19 Lys20 Tyr21 Phe22 Leu2 3 Gln24, Glu15 Gln16 Glu17 Leu18 Val19 Lys20 Tyr21 Phe22 Ile23 Glu24, Glu15 Gln16 Glu17 Leu18 Val19 Lys20 Tyr21 Phe22 Ue23 Gln24, Glu15 Gln16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Leu23 Glu24, Glu15 Gln16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Leu23 Gln24, Glu15 Gln16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Ile23 Glu24, Glu15 Gln16 Glu17 Ile18 Val19 Lys20 Tyr21 Phe22 Ile23 Gln24, or Asp15 Ser16 Arg17 Arg18Ala19 Gln20 Asp21 Phe22 Val23 Gln24; Xaa27 Xaa28 Xaa29 Xaa30 Xaa31 Xaa32 is: Met27 Asn28 Thr29 Lys30 Arg31 Asn32, Lys27 Asn28 Ala29 Gly30 Pro31 Ser32, or Lys27 Asn28 Gly29 Gly30 Pro31 Ser32 or a pept ide as set out above in which residue Asn34 is replaced with Asp34; or a peptide as set out above in which Xaa3 is Glu3.

Description

technical field [0001] This application relates to the use of agents to control appetite, food intake, food intake, energy expenditure and calorie intake, treatment of overweight, obesity, and prevention and treatment of co-morbidity of obesity. Background technique [0002] According to the World Health Organization (WHO), obesity represents a global epidemic in which more than one billion adults are overweight, and among the overweight individuals at least 3 million are clinically diagnosed as obese. Furthermore, WHO estimates that 250,000 deaths per year in Europe and more than 2.5 million worldwide are weight-related (World Health Organization, Global Strategy on Diet, Physical Activity and Health, 2004). [0003] The causes of obesity are complex and multifactorial. Mounting evidence suggests that obesity is not a simple matter of self-control, but a complex disorder involving appetite regulation and energy metabolism. Furthermore, obesity is associated with various c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26C07K14/435
CPCA61K38/00C07K14/605
Inventor 史第芬·罗伯特·布罗姆
Owner IMPERIAL INNOVATIONS LTD
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