SI2864350T1 - Analogi glukagona z aktivnostjo gip-receptorja - Google Patents
Analogi glukagona z aktivnostjo gip-receptorja Download PDFInfo
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- SI2864350T1 SI2864350T1 SI201331079T SI201331079T SI2864350T1 SI 2864350 T1 SI2864350 T1 SI 2864350T1 SI 201331079 T SI201331079 T SI 201331079T SI 201331079 T SI201331079 T SI 201331079T SI 2864350 T1 SI2864350 T1 SI 2864350T1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
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- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Genetics & Genomics (AREA)
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- Biophysics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measurement And Recording Of Electrical Phenomena And Electrical Characteristics Of The Living Body (AREA)
- Measuring Pulse, Heart Rate, Blood Pressure Or Blood Flow (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (15)
- ANALOGI GLUKAGONA Z AKTIVNOSTJO GIP-RECEPTORJA Patentni zahtevki1. Peptid, ki obsega zaporedje XlX2X3GTFTSDXl0SKYLXl5Xl6Xl7Xl8Xl9X20X2lFVQWLX27X28X29X30PSSGX35PPPS (SEQ ID NO: 140), v katerem i) Xi ustreza položaju 1 nativnega glukagona in Xi je izbran iz skupine, ki sestoji iz: acetil D-His, acetil D-Tyr, acetil D-Phe, desamino Tyr, D-His in D-Tyr; Χ2 je Ala, Gly, Pro, sarkozin, Ser in Val, Χ3 je Gin, aminokislina, ki obsega stransko verigo s strukturo I, II ali III, hidrofobna aminokislina, kisla aminokislina ali bazična aminokislina ali je aminokislina, izbrana iz skupine, ki sestoji iz: Glu, Ala, Leu, lle, Nle, Val, NorVal, homoserina, Met, metionin sulfoksida, metionin sulfona, acetil-Orn, acetil-diaminobutanojske kisline in acetil-Lys; pri čemer je struktura I, II in lil:struktura Istruktura IIstruktura III v kateri je R1 Co-3-alkil ali Co-3-heteroalkil; R2 je NHR4 ali Ci-3-alkil; R3 je C-i-3-alkil; R4 je H ali Ci-3-alkil; X je NH, O ali S; in Y je NHR4, SR3 ali OR3; Χ10 je Tyr ali aminokislina, kovalentno vezana na C12- do C18-acilno ali alkilno skupino;Xi5 je kisla aminokislina, po izbiri Glu ali Asp; Χ16 je katera koli aminokislina, po izbiri katera koli aminokislina razen Gly, Pro in Ser; npr. Glu, Ala, alfa, alfa-disubstituirana aminokislina (npr. AIB), His, Lys Χ17 je Arg, His, Gin; Χ18 je Arg ali Ala; Χ19 je Ala ali alfa, alfa disubstituirana aminokislina; Χ20 je izbran iz skupine, ki sestoji iz: alfa, alfa-disubstituirane aminokisline (npr. AIB) ali Gin ali His, Lys ali Ala; Χ21 je kisla aminokislina, po izbiri Asp ali Glu; X27je Leu, Ala, Nle ali Met; Χ28 je Ala ali kisla aminokislina (po izbiri Asp ali Glu); Χ29 je alifatski, npr. Ala ali Leu ali Gly ali AIB ali Val; X3oje majhna alifatska aminokislina, npr. Ala ali Gly Χ35 je Ala ali bazična aminokislina (po izbiri Arg ali Lys); pri čemer, kadar je Χ28 kisla aminokislina, je Χ35 bazična aminokislina; pri čemer, po izbiri, kadar je Χ28 Asp, potem Χ29 ni Gly pri čemer, kadar je XioTyr, peptid obsega pri položaju 40 aminokislino, kije kovalentno vezana na C12- do C18-acilno ali alkilno skupino, in pri čemer, po izbiri, peptid obsega Gly pri položaju 41, pri čemer je aminokislina na C-koncu peptida amidirana; ali ii) Χ1 ustreza položaju 1 nativnega glukagona in Χ1 je izbran iz skupine, ki sestoji iz: acetil D-His, acetil D-Tyr, acetil D-Phe, desamino Tyr, D-His in D-Tyr; Χ2 je Ala ali Gly, Χ3 je Gin; Xioje aminokislina, kije kovalentno vezana na C12-C18-acilno ali -alkilno skupino; Χ15 je Asp; Χ16 je Glu; Χ17 je Arg, His ali Gin; Χ18 je Ala; Χ19 je Ala; Χ20 je Gin; Χ21 je Asp; Χ27 je Leu; Χ28 je Glu; Χ29 je Gly; Χ30 je Gly Χ35 je Ala; pri čemer ima peptid agonistično aktivnost pri humanem GlP-receptorju in humanem GLP-1-receptorju in/ali humanem glukagonskem receptorju, po izbiri pri čemer ima analog glukagona manj kot 100-kratno selektivnost za humani GLP-1-receptor v primerjavi z GlP-receptorjem.
- 2. Peptid po zahtevku 1, ki obsega pri položajih 1 in 2 par aminokislin, izbranih iz skupine, ki sestoji iz:dalje pri čemer Χ10 je aminokislina, kovalentno vezana na C12-C18-acilno ali -alkilno skupino, ali kadar je Χ10 Tyr, peptid obsega pri položaju 40 aminokislino, ki je kovalentno vezana na C12-C18-acilno ali -alkilno skupino in peptid po izbiri obsega Gly pri položaju 41.
- 3. Peptid po zahtevku 1 (ii), pri čemeri) aminokislina pri položaju 1 je izbrana izmed acetil D-Tyr, acetil D-His, desamino Tyr, D-Tyr, D-His in acetil D-Phe; ii) aminokislina pri položaju 2 je Ala ali Gly. iii) aminokislina pri položaju 10 je kovalentno vezana na C12-C18-acilno ali -alkilno skupino. iv) Χ20 je Gin; v) Χ16 in Χ28 sta oba Glu; vi) Χ18 je Ala; vii) Χ27 je Leu, Χ29 je Gly in peptid obsega amidiran Gly na C-koncu.
- 4. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 11.
- 5. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 12.
- 6. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 13
- 7. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 15.
- 8. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 16.
- 9. Peptid po zahtevku 1, ki obsega zaporedje s SEQ ID NO: 22.
- 10. Analog peptida po zahtevku 1, ki obsega a. zaporedje s SEQ ID NO: 11 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 11; b. zaporedje s SEQ ID NO: 12 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 12, c. zaporedje s SEQ ID NO: 13 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 13, d. zaporedje s SEQ ID NO: 15 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 15, e. zaporedje s SEQ ID NO: 16 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 16 ali f zaporedje s SEQ ID NO: 22 z do 3 aminokislinskimi modifikacijami v primerjavi s SEQ ID NO: 22, pri čemer ima peptid agonistično aktivnost pri humanem GlP-receptorju in humanem GLP-1-receptorju in peptid ima manj kot 100-kratno selektivnost za humani GLP-1 -receptor v primerjavi z GlP-receptorjem.
- 11. Dimer ali multimer, ki obsega dva ali več peptidov ali peptidnih analogov po katerem koli od predhodnih zahtevkov.
- 12. Konjugat, ki obsega peptid ali peptidni analog po katerem koli od predhodnih zahtevkov in konjugatni del.
- 13. Farmacevtski sestavek, ki obsega peptid ali peptidni analog po katerem koli od zahtevkov 1-10, dimer ali multimer po zahtevku 11, konjugat po zahtevku 12 ali kombinacijo le-teh in farmacevtsko sprejemljiv nosilec, razredčilo ali pomožno snov.
- 14. Peptid ali peptidni analog po katerem koli od zahtevkov 1-10, dimer ali multimer po zahtevku 11 ali konjugat po zahtevku 12 za uporabo pri zmanjšanju pridobivanja telesne teže ali pri induciranju zgubljanja telesne teže pri posamezniku, ki to potrebuje, ali uporaba peptida ali peptidnega analoga po katerem koli od zahtevkov 1-10, dimera ali multimera po zahtevku 11 ali konjugata po zahtevku 12 pri pripravi zdravila za zmanjšanje pridobivanja telesne teže ali induciranju zgubljanja telesne teže.
- 15. Peptid ali peptidni analog po katerem koli od zahtevkov 1-10, dimer ali multimer po zahtevku 11, konjugat po zahtevku 12 za uporabo pri zdravljenju diabetesa.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261662874P | 2012-06-21 | 2012-06-21 | |
US201361787973P | 2013-03-15 | 2013-03-15 | |
PCT/US2013/046229 WO2013192130A1 (en) | 2012-06-21 | 2013-06-18 | Analogs of glucagon exhibiting gip receptor activity |
EP13731246.8A EP2864350B1 (en) | 2012-06-21 | 2013-06-18 | Analogs of glucagon exhibiting gip receptor activity |
Publications (1)
Publication Number | Publication Date |
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SI2864350T1 true SI2864350T1 (sl) | 2018-08-31 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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SI201331079T SI2864350T1 (sl) | 2012-06-21 | 2013-06-18 | Analogi glukagona z aktivnostjo gip-receptorja |
Country Status (30)
Country | Link |
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US (2) | US9868772B2 (sl) |
EP (1) | EP2864350B1 (sl) |
JP (1) | JP6300239B2 (sl) |
KR (1) | KR20150039748A (sl) |
CN (1) | CN104583233B (sl) |
AR (1) | AR091478A1 (sl) |
AU (1) | AU2013277372B2 (sl) |
BR (1) | BR112014031671A2 (sl) |
CA (1) | CA2877127A1 (sl) |
CL (1) | CL2014003421A1 (sl) |
CO (1) | CO7170125A2 (sl) |
CR (1) | CR20150015A (sl) |
DK (1) | DK2864350T3 (sl) |
EA (1) | EA029025B1 (sl) |
ES (1) | ES2674946T3 (sl) |
HR (1) | HRP20180936T1 (sl) |
HU (1) | HUE039267T2 (sl) |
IL (1) | IL236386B (sl) |
MX (1) | MX356000B (sl) |
MY (1) | MY185217A (sl) |
PE (1) | PE20150863A1 (sl) |
PH (1) | PH12014502857A1 (sl) |
PL (1) | PL2864350T3 (sl) |
PT (1) | PT2864350T (sl) |
RS (1) | RS57347B1 (sl) |
SG (1) | SG11201408491SA (sl) |
SI (1) | SI2864350T1 (sl) |
TR (1) | TR201808818T4 (sl) |
TW (1) | TWI644920B (sl) |
WO (1) | WO2013192130A1 (sl) |
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