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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Argentina
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alkyl
hglp
aib
acc
ala
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ARP100101943A
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English (en)
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Ipsen Pharma Sas
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Publication of AR076950A2 publication Critical patent/AR076950A2/es

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Zoology (AREA)
  • Otolaryngology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)

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
CA2552526A1 (en) 2004-01-08 2005-07-21 Theratechnologies Inc. Glucagon-like peptide-1 analogs with long duration of action
KR101593158B1 (ko) 2008-08-07 2016-02-12 입센 파마 에스.에이.에스. Ｎ-말단이 변형된 포도당 의존적인 인슐린 분비 자극성 폴리펩타이드(ｇｉｐ)의 유사체
KR20130133104A (ko) 2008-08-07 2013-12-05 입센 파마 에스.에이.에스 포도당 의존적인 인슐린 분비 자극성 폴리펩타이드 유사체
WO2014096179A1 (en) * 2012-12-19 2014-06-26 Novo Nordisk A/S Novel glp-1 receptor agonists with cholesterol efflux activity
TWI700291B (zh) * 2015-06-22 2020-08-01 美國禮來大藥廠 升糖素及glp-1共激動劑化合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991011457A1 (en) * 1990-01-24 1991-08-08 Buckley Douglas I Glp-1 analogs useful for diabetes treatment
HU227021B1 (en) * 1996-08-30 2010-05-28 Novo Nordisk As Glp-1 derivatives
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

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

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