PE20191083A1 - Agonistas duales acilados de glp-1/glp-2 - Google Patents
Agonistas duales acilados de glp-1/glp-2Info
- Publication number
- PE20191083A1 PE20191083A1 PE2019001207A PE2019001207A PE20191083A1 PE 20191083 A1 PE20191083 A1 PE 20191083A1 PE 2019001207 A PE2019001207 A PE 2019001207A PE 2019001207 A PE2019001207 A PE 2019001207A PE 20191083 A1 PE20191083 A1 PE 20191083A1
- Authority
- PE
- Peru
- Prior art keywords
- glp
- formula
- psi
- dual
- accylated
- Prior art date
Links
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 title abstract 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 title abstract 2
- 102400000326 Glucagon-like peptide 2 Human genes 0.000 title abstract 2
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title abstract 2
- TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 title abstract 2
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 title 1
- 230000009977 dual effect Effects 0.000 title 1
- 229940125542 dual agonist Drugs 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 101500028775 Homo sapiens Glucagon Proteins 0.000 abstract 1
- 102100040918 Pro-glucagon Human genes 0.000 abstract 1
- 101100353123 Rattus norvegicus Ppp1r15a gene Proteins 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 230000006583 body weight regulation Effects 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000000968 intestinal effect Effects 0.000 abstract 1
- 230000003818 metabolic dysfunction Effects 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se refiere a un agonista dual de GLP-1/GLP-2 (peptido similar al glucagon tipos 1 y 2 humano) representado por la formula: R1-X -U-R2, en la que: R1 es hidrogeno, acetilo, formilo, entre otros; R2 es NH2 u OH; X es un peptido de formula: H-X2-EG-X5-F-X7-X8-E-X10-X11-TIL-X15-X16-X17-A-X19-X20-X21-FI-X24-WL-X27-X28-X29-KIT-X33 (formula I), en la que: X2 es Aib o G; X5 y X7 son T o S; X8 es S, E o D; X10 es L, M, entre otros; X11 es A, N o S; X15 es D o E; X16 es G, E, entre otros; X17 es Q, E, entre otros; X19 es A, V o S; X20 es R, K o psi; X21 es D, L o E; X24 es A, N o S; X27 es I, Q, entre otros; X28 es Q, E, entre otros; X29 es H, Y, entre otros; X33 es D o E; U esta ausente o es una secuencia de 1 a 15 residuos seleccionados de K, k, E, A, T, I, L y psi. La molecula contiene solo un psi, en la que spsi es un residuo K, k, R, Orn, Dap o Dab en la que la cadena lateral esta conjugada a un sustituyente que tiene la formula Z1 o Z1-Z2, en la que Z1 es CH3-(CH2)10-22-(CO)- o HOOC-(CH2)10-22-(CO)-; Z2 es ZS1-, -ZS2-, entre otros; ZS1 es isoGlu, isoLys, entre otros; Z2 es -(Peg3)m; m es 1, 2 o 3 y en la que al menos uno de X5 y X7 es T. Tambien se refiere a una composicion que comprende al agonista dual. Dicho agonista es util para la profilaxis o el tratamiento del dano y la disfuncion intestinal, la regulacion del peso corporal y la profilaxis o el tratamiento de la disfuncion metabolica
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DKPA201600757 | 2016-12-09 | ||
PCT/EP2017/082290 WO2018104561A1 (en) | 2016-12-09 | 2017-12-11 | Acylated glp-1/glp-2 dual agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20191083A1 true PE20191083A1 (es) | 2019-08-20 |
Family
ID=61005766
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2019001207A PE20191083A1 (es) | 2016-12-09 | 2017-12-11 | Agonistas duales acilados de glp-1/glp-2 |
Country Status (17)
Country | Link |
---|---|
US (4) | US20190142904A1 (es) |
EP (1) | EP3551651B1 (es) |
JP (2) | JP6563614B1 (es) |
KR (1) | KR102502040B1 (es) |
CN (2) | CN110088125B (es) |
AU (1) | AU2017371516C1 (es) |
BR (1) | BR112019010624A2 (es) |
CA (1) | CA3043151A1 (es) |
CL (1) | CL2019001552A1 (es) |
CO (1) | CO2019005924A2 (es) |
DK (1) | DK3551651T3 (es) |
IL (1) | IL266219B2 (es) |
MX (1) | MX2019006486A (es) |
PE (1) | PE20191083A1 (es) |
RU (1) | RU2753193C2 (es) |
SG (2) | SG10201911851VA (es) |
WO (1) | WO2018104561A1 (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK3551651T3 (da) | 2016-12-09 | 2024-05-13 | Zealand Pharma As | Acylerede glp-1/glp-2-dobbeltagonister |
CA3138715A1 (en) * | 2019-06-14 | 2020-12-17 | Zealand Pharma A/S | Pharmaceutical parenteral composition of dual glp1/2 agonist |
AU2020363377A1 (en) | 2019-10-07 | 2022-04-21 | Kallyope, Inc. | GPR119 agonists |
EP4126004A1 (en) | 2020-03-30 | 2023-02-08 | Zealand Pharma A/S | Agonist combination |
EP4126003A1 (en) | 2020-03-30 | 2023-02-08 | Zealand Pharma A/S | Glp-1/glp-2 dual agonists |
EP4153589A4 (en) | 2020-05-19 | 2024-06-12 | Kallyope, Inc. | AMPK ACTIVATORS |
WO2021263039A1 (en) | 2020-06-26 | 2021-12-30 | Kallyope, Inc. | Ampk activators |
AU2021399904A1 (en) | 2020-12-16 | 2023-06-08 | Zealand Pharma A/S | Pharmaceutical composition of glp-1/glp-2 dual agonists |
CA3200526A1 (en) | 2020-12-16 | 2022-06-23 | Jesper Skodborg VILLADSEN | Pharmaceutical composition of glp-1/glp-2 dual agonists |
KR20230121824A (ko) | 2020-12-16 | 2023-08-21 | 질랜드 파마 에이/에스 | Glp-1/glp-2 이중 효능제의 약학적 조성물 |
EP4294424A1 (en) | 2021-02-18 | 2023-12-27 | Zealand Pharma A/S | Composition for treating short bowel syndrome |
CA3228429A1 (en) | 2021-09-03 | 2023-03-09 | Mikkel Askjar Agersnap | Dosage regime |
WO2023111273A1 (en) * | 2021-12-17 | 2023-06-22 | Bainan Biotech Aps | Peptide dual agonists of gipr and glp2r |
WO2023132609A1 (ko) * | 2022-01-05 | 2023-07-13 | 주식회사 휴온스랩 | 지속형 지방산-펩타이드 유도체 및 이의 용도 |
CN116655772A (zh) * | 2022-02-18 | 2023-08-29 | 成都奥达生物科技有限公司 | 一种长效的glp-1/glp-2双激动剂化合物 |
WO2024061919A1 (en) | 2022-09-19 | 2024-03-28 | Zealand Pharma A/S | Combination therapy |
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