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AR076950A2 - Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen - Google Patents

Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen

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Publication number
AR076950A2
AR076950A2 ARP100101943A ARP100101943A AR076950A2 AR 076950 A2 AR076950 A2 AR 076950A2 AR P100101943 A ARP100101943 A AR P100101943A AR P100101943 A ARP100101943 A AR P100101943A AR 076950 A2 AR076950 A2 AR 076950A2
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AR
Argentina
Prior art keywords
alkyl
hglp
aib
acc
ala
Prior art date
Application number
ARP100101943A
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English (en)
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Ipsen Pharma Sas
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Publication date
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Publication of AR076950A2 publication Critical patent/AR076950A2/es

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    • 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
    • C07K14/605Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
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  • Gastroenterology & Hepatology (AREA)
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  • Psychiatry (AREA)
  • Immunology (AREA)
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Abstract

Análogos del péptido 1-similar al glucagon, que comprende un compuesto de la siguiente formula (1): (R2R3)-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A12-A23-A24-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-R1 (1) en la cual A7 es L-His, Ura, Paa, Pta, Amp, Tma-his, des-amino-His, o suprimido; A8 es Ala, D-Ala, Aib, Acc, N-Me-Ala, N-Me-D-Ala o N-Me-Gly; A9 es Glu, N-Me-Glu, N-Me.Asp o Asp; A10 es Gly, Acc, b-Ala o Aib; A11 es Thr o Ser; A12 es Phe, Acc, Aic, Aib, 3-Pal, 4-Pal, b-Nal, Cha, Trp o X1-Phe; A13 es Thr o Ser; A14 es Ser o Aib; A15 es Aspp Glu; A16 es Val, Acc, Aib, Leu, Ile, TIe, NIe, Abu, Ala o Cha; A17 es Ser o Thr; A18 es Ser o Thr; A19 es Tyr, Cha, Phe, 3-Pal, 4-Pal, Acc, b-Nal o X1-Phe; A20 es Leu, Acc, Aib, NIe, Ile, Cha, TIe, Val, Phe o X1-Phe; A21 es Glu o Asp; A22 es Gly, Acc, b-Ala, Glu o Aib; A23 es Gln, Asp, Asn o Glu; A24 es Ala, Aib, Val, Abu, TIe o Acc; A25 es Ala, Aib, Val, Abu, TIe, Acc, Lys, Arg, hArg, Orn, HN-CH((CH2)n-N(R10R11))-C(O) o HN-CH((CH2)e-X3)-C(O); A26 es Lys, Arg, hArg, Orn, HN-CH((CH2)n-N(R10R11))-C(O) o HN-CH((CH2)e-X3)-C(O); A27 es Glu Asp, Leu, Aib o Lys; A28 es Phe, Pal, b-Nal, X1-Phe, Aic, Acc, Aib, Cha o Trp; A29 es Ile, Acc, Aib, Leu, NIe, Cha, TIe, Val, Abu, Ala o Phe; A30 es Ala, Aib o Acc; A31 es Trp, b-Nal, 3-Pal, 4-Pal, Phe, Acc, Aib o Cha; A32 es Leu, Acc, Aib, NIe, Ile, Cha, Tle, Phe, X1-Phe o Ala; A33 es Val, Acc, Aib, Leu, Ile, Tle, Nle, Cha, Ala, Phe, Abu, Lys o X1-Phe; A34 es Lys, Arg, hArg, Orn, HN-CH((CH2)n-N(R10R11))-C(O) o HN-CH((CH2)e-X3)-C(O); A35 es Gly, b-Ala, D-Ala, Gaba, Ava, HN-(CH2)m-C(O), Aib, Acc o a D-amino ácido; A36 es L- o D-Arg, D- o L-Lys, D- o L-hArg, D- o L-Orn, HN-CH((CH2)n-N(R10R11))-C(O), HN-CH((CH2)e-X3)-C(O) o suprimido; A37 es Gly, b-Ala, Gaba, Ava, Aib, Acc, Ado, Arg, Asp, Aun, Aec, HN-(CH2)m-C(O), HN-CH((CH2)n-N(R10R11))-C(O), a D-amino ácido, o suprimido; A38 es D- o L-Lys, D- o L-Arg, D- o L-hArg, D- o L-Orn, HN-CH((CH2)n-N(R10R11))-C(O), HN-CH((CH2)e-X3)-C(O), Ava, Ado, Aec o suprimido; A39 es D- o L-Lys, D- o L-Arg, HN-CH((CH2)n-N(R10R11))-C(O), Ava, Ado o Aec; X1 para cada ocurrencia es independientemente entre sí, seleccionado de entre el grupo consistente en: alquilo C1-6, OH y halo; R1 es OH, NH2, alcoxi C1-30, o NH-X2-CH2-Z0, en lo cual X2 es una parte hidrocarburo de 1 a 12 átomos de carbono, y Z0 es H, OH, CH2H o CONH2; X3 es un compuesto de formula (2), de formula (3) o -C(O)-NHR12, en lo cual X4 para cada ocurrencia es independientemente entre sí -C-(O)-, -NH-C(O)- o -CH2-, y f para cada ocurrencia es independientemente entre sí, un numero entero de 1 a 29 inclusive; cada uno de los R2 y R3 es independientemente entre sí, seleccionado de entre el grupo consistente en: H, alquilo C1-30, alquenilo C2-30, fenil-alquilo C1-30, naftil-alquilo C1-30, hidroxi-alquilo C1-30, hidroxi-alquenilo C2-30, hidroxifenil-alquilo C1-30, e hidroxinaftil-alquilo C1-30; o uno de R2 y R3 es un resto de formula (4), acilo C1-30, alquil C1-30sulfonilo, C(O)X5, un resto de formula (5) o de formula (6); en lo cual Y es H, O o NH2; r vale de 0 a 4; q vale de 0 a 4; y X5 es alquilo C1-30, alquenilo C2-30, fenil-alquilo C1-30, naftil-alquilo C1-30, hidroxi-alquilo C1-30, hidroxi-alquenilo C2-30, hidroxifenil-alquilo C1-30, o hidroxinaftil-alquilo C1-30; e es, independientemente entre sí, en cada ocurrencia un numero entero de 1 a 4 inclusive; m es, independientemente entre sí, en cada ocurrencia un numero entero de 5 a 24 inclusive; n es, independientemente entre sí, en cada ocurrencia un numero entero de 1 a 5 inclusive; R10 y R11 para cada ocurrencia es, cada uno de ellos e independientemente entre sí, H, alquilo C1-30, acilo C1-30, alquil C1-30sulfonilo, -C((NH)(NH2)) o un resto de formula (7) y, R12 y R13 son, cada uno de ellos e independientemente entre sí, alquilo C1-30, con la condicion que cuando A7 es Ura, Paa o Pta, entonces R2 y R3 están suprimidos; cuando R10 es acilo C1-30, alquil C1-30sulfonilo, -C((NH)(NH2)) o el resto de formula (7) entonces R11 es H o alquilo C1-30; (i) por lo menos un amino ácido de un compuesto de la formula (1) no es el mismo que la secuencia nativa de hGLP-1(7-36, -37 o -38)NH2 o hGLP-1(7-36, -37 o -38)OH; (ii) un compuesto de la formula (1) no es un análogo de hGLP-1(7-36, -37 o -38)NH2 o hGLP-1(7-36, -37 o -38)OH en lo cual una unica posicion ha sido sustituida por Ala; (iii) un compuesto de la formula (1) no es (Arg26,34, Lys38)hGLP-1(7-38)-E, (Lys26(Ne-alcanoil))hGLP-1(7-36, -37 o -38)-E, (Lys34(Ne-alcanoil))hGLP-1(7-36, -37 o -38)-E, (Lys26,34-bis(Ne-alcanoil))hGLP-1(7-36, -37 o -38)-E, Arg26, Lys34(Ne-alcanoil))hGLP-1(8-36, -37 o -38)-E, (Arg26,34,Lys36(Ne-alcanoil))hGLP-1(7-36, -37 o -38)-E o Arg26,34,Lys38(Ne-alcanoil))hGLP-1(7-38)-E, siendo E, -OH o -NH2; (iv) un compuesto de la formula (1) no es Z1-hGLP-1(7-36, -37 o -38)-OH, Z1-hGLP-1(7-36, -37 o -38)-NH2, estando Z1 seleccionado de entre el grupo consistente en: (e) (Arg26), (Arg34), (Arg26,34), (Lys36), (Arg26, Lys36), (Arg34, Lys36), (D-Lys36), (Arg36), (D-Arg36), (Arg26,34, Lys36), o (Arg26,36, Lys34); (f) [Asp21]; (g) por lo menos uno de los siguientes: (Aib8), (D-Ala8) y (Asp9); y (h) (Tyr7), (N-acil-His7), (N-alquil-His7), (N-acil-D-His7) o (N-alquil-D-His7); (v) un compuesto de la formula (1) no es una combinacion de dos cualesquiera de las sustituciones enumeradas en los grupos (a) a (d); y (vi) un compuesto de la formula (1) no es (N-Me-AIa8)hGLP-1(8-36 o -37), (Glu15)hGLP-1(7-36 o -37), (Asp21)hGLP-1(7-36 o -37) o (Phe31)hGLP-1(7-36 o -37) o una sal farmacéuticamente aceptable del mismo; con la condicion que el compuesto no es (Aib8,35)hGLP-1(7-36)NH2, uso de los mismos para la manufactura de un medicamento y composiciones farmacéuticas que los contienen.
ARP100101943A 1998-12-07 2010-06-02 Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen AR076950A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20660198A 1998-12-07 1998-12-07

Publications (1)

Publication Number Publication Date
AR076950A2 true AR076950A2 (es) 2011-07-20

Family

ID=32592693

Family Applications (4)

Application Number Title Priority Date Filing Date
ARP990106236A AR021576A1 (es) 1998-12-07 1999-12-07 Analogos del peptido 1-similar al glucagon, uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen.
ARP030101524A AR040228A2 (es) 1998-12-07 2003-04-30 Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen
ARP070101341A AR057639A2 (es) 1998-12-07 2007-03-29 Analogos del peptido 1- similar al glucagon uso de los mismos par ala manufactura de un medicamento y composiciones farmaceuticas que los contienen
ARP100101943A AR076950A2 (es) 1998-12-07 2010-06-02 Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen

Family Applications Before (3)

Application Number Title Priority Date Filing Date
ARP990106236A AR021576A1 (es) 1998-12-07 1999-12-07 Analogos del peptido 1-similar al glucagon, uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen.
ARP030101524A AR040228A2 (es) 1998-12-07 2003-04-30 Analogos del peptido 1-similar al glucagon uso de los mismos para la manufactura de un medicamento y composiciones farmaceuticas que los contienen
ARP070101341A AR057639A2 (es) 1998-12-07 2007-03-29 Analogos del peptido 1- similar al glucagon uso de los mismos par ala manufactura de un medicamento y composiciones farmaceuticas que los contienen

Country Status (7)

Country Link
EP (1) EP1359159A3 (es)
CN (1) CN1935839B (es)
AR (4) AR021576A1 (es)
CA (1) CA2778047A1 (es)
DK (1) DK1137667T3 (es)
PL (1) PL189664B1 (es)
ZA (2) ZA200304047B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1709071A4 (en) * 2004-01-08 2007-05-30 Theratechnologies Inc GLUCAGON LIKE PEPTIDE-1 ANALOGS WITH LONG PERFORMANCE
EP2769986A3 (en) 2008-08-07 2014-11-26 Ipsen Pharma S.A.S. Analogues of glucose-dependent insulinotropic polypeptide (GIP) modified at N-terminal
EA020005B1 (ru) 2008-08-07 2014-07-30 Ипсен Фарма С.А.С. Аналоги глюкозазависимого инсулинотропного полипептида
US20150344540A1 (en) * 2012-12-19 2015-12-03 Novo Nordisk A/S Novel glp-1 receptor agonists with cholesterol efflux activity
AR104932A1 (es) * 2015-06-22 2017-08-23 Lilly Co Eli Compuestos co-agonistas del glucagón y péptido-1 similar al glugacón (glp-1)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2073856C (en) * 1990-01-24 2002-12-03 Douglas I. Buckley Glp-1 analogs useful for diabetes treatment
UA72181C2 (uk) * 1996-08-30 2005-02-15 Ново Нордіск А/С Похідна глюкагоноподібного пептиду-1 (варіанти), фармацевтична композиція та спосіб одержання лікувального засобу (варіанти), спосіб лікування діабету (варіанти) і ожиріння
UA65549C2 (uk) * 1996-11-05 2004-04-15 Елі Ліллі Енд Компані Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція

Also Published As

Publication number Publication date
AR057639A2 (es) 2007-12-12
ZA200104478B (en) 2003-12-01
EP1359159A2 (en) 2003-11-05
DK1137667T3 (da) 2005-02-14
CN1935839A (zh) 2007-03-28
AR021576A1 (es) 2002-07-24
AR040228A2 (es) 2005-03-23
CA2778047A1 (en) 2000-06-15
ZA200304047B (en) 2004-04-28
PL189664B1 (pl) 2005-09-30
EP1359159A3 (en) 2004-07-21
CN1935839B (zh) 2012-06-06

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