AR095986A1 - MODIFIED PROTEINS THAT REGULATE GLUCOSE IN BLOOD WITH ALTERED PROFILE OF PHARMACOLOGICAL ACTIVITY AND PREPARATION OF THE SAME - Google Patents

MODIFIED PROTEINS THAT REGULATE GLUCOSE IN BLOOD WITH ALTERED PROFILE OF PHARMACOLOGICAL ACTIVITY AND PREPARATION OF THE SAME

Info

Publication number
AR095986A1
AR095986A1 ARP140101464A ARP140101464A AR095986A1 AR 095986 A1 AR095986 A1 AR 095986A1 AR P140101464 A ARP140101464 A AR P140101464A AR P140101464 A ARP140101464 A AR P140101464A AR 095986 A1 AR095986 A1 AR 095986A1
Authority
AR
Argentina
Prior art keywords
amino acid
arg
absent
seq
chain
Prior art date
Application number
ARP140101464A
Other languages
Spanish (es)
Original Assignee
Sanofi Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of AR095986A1 publication Critical patent/AR095986A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/62Insulins
    • C07K14/622Insulins at least 1 amino acid in D-form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Abstract

Métodos para preparar estas moléculas, formulaciones farmacéuticas de las mismas, así como su uso en terapia. Además, la solicitud se refiere a métodos para inhibir la degradación de proteasas en suero y/o el aumento de la estabilidad en suero de una proteína. Reivindicación 1: Un análogo de insulina modificada o una sal del mismo de fórmula (1) en donde (a) A0 está ausente o es Arg, (b) (A1 - A5) son restos de aminoácidos en las posiciones A1 a A5 en la cadena A del ser humano (SEC ID Nº 1) o insulina animal, (c) (A8 - A10) son restos de aminoácidos en las posiciones A8 a A10 en la cadena A del ser humano (SEC ID Nº 1) o insulina animal, (d) (A12 - A19) son restos de aminoácidos en las posiciones A12 a A19 en la cadena A del ser humano (SEC ID Nº 1) o insulina animal, (e) A21 es Asn o Gly, (f) B1 es Phe o His, (g) B3 es Asn o His, (h) B2 y (B4 - B6) son restos de aminoácidos en las posiciones B2 y B4 a B6 en la cadena B del ser humano (SEC ID Nº 2) o insulina animal, (i) (B8 - B18) son restos de aminoácidos en las posiciones B8 a B18 en la cadena B del ser humano (SEC ID Nº 2) o insulina animal, (j) (B20 - B27) son restos de aminoácidos en las posiciones B20 a B27 en la cadena B del ser humano (SEC ID Nº 2) o insulina animal, (k) B28 es Pro o Lys, (l) B29 es Lys o está ausente, (m) B30 es Thr o está ausente, (n) B31 está ausente, es Arg o un D-aminoácido básico, particularmente D-Arg, D-His, D-Lys, D-Hyl, D-Ornitina, o D-Citrulina, (o) B32 es un D-aminoácido básico, particularmente D-Arg, con la condición de que si B31 es Arg, entonces A21 es Gly, o si B31 está ausente, entonces A0 es Arg, y con la condición de que si B28 es Lys y B29, B30 y B31 están ausentes, entonces A0 es Arg.Methods to prepare these molecules, pharmaceutical formulations thereof, as well as their use in therapy. In addition, the application relates to methods for inhibiting the degradation of serum proteases and / or increasing the stability in serum of a protein. Claim 1: A modified insulin analogue or a salt thereof of formula (1) wherein (a) A0 is absent or is Arg, (b) (A1-A5) are amino acid residues at positions A1 to A5 in the human A chain (SEQ ID No. 1) or animal insulin, (c) (A8 - A10) are amino acid residues at positions A8 to A10 in human A chain (SEQ ID No. 1) or animal insulin, (d) (A12 - A19) are amino acid residues at positions A12 to A19 in the human chain A (SEQ ID No. 1) or animal insulin, (e) A21 is Asn or Gly, (f) B1 is Phe or His, (g) B3 is Asn or His, (h) B2 and (B4-B6) are amino acid residues at positions B2 and B4 through B6 in the human B chain (SEQ ID NO: 2) or animal insulin , (i) (B8 - B18) are amino acid residues at positions B8 to B18 in the human B chain (SEQ ID No. 2) or animal insulin, (j) (B20 - B27) are amino acid residues in positions B20 to B27 in the human B chain (SEQ ID No. 2) or animal insulin , (k) B28 is Pro or Lys, (l) B29 is Lys or is absent, (m) B30 is Thr or is absent, (n) B31 is absent, is Arg or a basic D-amino acid, particularly D-Arg , D-His, D-Lys, D-Hyl, D-Ornithine, or D-Citrulline, (o) B32 is a basic D-amino acid, particularly D-Arg, with the proviso that if B31 is Arg, then A21 is Gly, or if B31 is absent, then A0 is Arg, and with the proviso that if B28 is Lys and B29, B30 and B31 are absent, then A0 is Arg.

ARP140101464A 2013-04-03 2014-04-01 MODIFIED PROTEINS THAT REGULATE GLUCOSE IN BLOOD WITH ALTERED PROFILE OF PHARMACOLOGICAL ACTIVITY AND PREPARATION OF THE SAME AR095986A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13305431 2013-04-03

Publications (1)

Publication Number Publication Date
AR095986A1 true AR095986A1 (en) 2015-11-25

Family

ID=48083085

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140101464A AR095986A1 (en) 2013-04-03 2014-04-01 MODIFIED PROTEINS THAT REGULATE GLUCOSE IN BLOOD WITH ALTERED PROFILE OF PHARMACOLOGICAL ACTIVITY AND PREPARATION OF THE SAME

Country Status (2)

Country Link
AR (1) AR095986A1 (en)
WO (1) WO2014161835A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6914844B2 (en) * 2015-03-13 2021-08-04 ケース ウェスタン リザーブ ユニバーシティCase Western Reserve University Insulin analogs including glucose-controlled conformational switch

Family Cites Families (26)

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DE3327709A1 (en) * 1983-07-29 1985-02-07 Hoechst Ag, 6230 Frankfurt INSULIN DERIVATIVE CRYSTAL SUSPENSIONS, METHOD FOR THE PRODUCTION AND USE THEREOF
NZ232375A (en) * 1989-02-09 1992-04-28 Lilly Co Eli Insulin analogues modified at b29
US5514646A (en) * 1989-02-09 1996-05-07 Chance; Ronald E. Insulin analogs modified at position 29 of the B chain
EA003922B1 (en) * 1999-05-17 2003-10-30 Конджачем, Инк. Long lasting insulinotropic peptides
KR101135244B1 (en) * 2007-11-29 2012-04-24 한미사이언스 주식회사 A pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate
TWI428346B (en) 2006-12-13 2014-03-01 Imp Innovations Ltd Novel compounds and their effects on feeding behaviour
AU2008216265B2 (en) 2007-02-15 2014-04-03 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
JP5385266B2 (en) 2007-06-15 2014-01-08 ジーランド ファーマ アクティーゼルスカブ Glucagon analog
CL2009001424A1 (en) 2008-06-17 2010-04-30 Univ Indiana Res & Tech Corp Glucagon-like peptide; dimer comprising two of said peptides; pharmaceutical composition comprising it; and its use to treat diabetes or induce weight loss.
EA020326B9 (en) 2008-06-17 2015-03-31 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Gip-based mixed agonists for treatment of metabolic disorders and obesity
CN102282167B (en) 2008-12-15 2014-08-13 西兰制药公司 Glucagon analogues
EA020520B1 (en) 2008-12-15 2014-11-28 Зилэнд Фарма А/С Glucagon analogues
DK2370462T3 (en) 2008-12-15 2014-09-08 Zealand Pharma As Glucagon-ANALOGS
DK2370461T3 (en) 2008-12-15 2013-12-16 Zealand Pharma As glucagon
WO2010096052A1 (en) 2009-02-19 2010-08-26 Merck Sharp & Dohme Corp. Oxyntomodulin analogs
MX2011013625A (en) 2009-06-16 2012-01-20 Univ Indiana Res & Tech Corp Gip receptor-active glucagon compounds.
SG177609A1 (en) 2009-07-13 2012-02-28 Zealand Pharma As Acylated glucagon analogues
US8703701B2 (en) 2009-12-18 2014-04-22 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
RU2012136450A (en) 2010-01-27 2014-03-10 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн CONJUGATES GLUCAGON ANTAGONIST - GIP AGONIST AND COMPOSITIONS FOR TREATMENT OF METABOLIC DISORDERS AND OBESITY
AR080592A1 (en) 2010-03-26 2012-04-18 Lilly Co Eli PEPTIDE WITH ACTIVITY FOR GIP-R AND GLP-1-R, FAMILY FORMULATION THAT UNDERSTANDS IT, ITS USE TO PREPARE A USEFUL MEDICINAL PRODUCT FOR THE TREATMENT OF MELLITUS DIABETES AND TO INDICATE WEIGHT LOSS
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EP2578726B1 (en) 2010-05-31 2018-10-17 JTEKT Corporation Method for manufacturing a coated member
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SG191194A1 (en) 2010-12-22 2013-07-31 Univ Indiana Res & Tech Corp Glucagon analogs exhibiting gip receptor activity
EP2694095B1 (en) 2011-04-05 2018-03-07 Longevity Biotech, Inc. Compositions comprising glucagon analogs and methods of making and using the same

Also Published As

Publication number Publication date
WO2014161835A1 (en) 2014-10-09

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