PE20231066A1 - Agonistas heterociclicos de glp-1 - Google Patents
Agonistas heterociclicos de glp-1Info
- Publication number
- PE20231066A1 PE20231066A1 PE2022001553A PE2022001553A PE20231066A1 PE 20231066 A1 PE20231066 A1 PE 20231066A1 PE 2022001553 A PE2022001553 A PE 2022001553A PE 2022001553 A PE2022001553 A PE 2022001553A PE 20231066 A1 PE20231066 A1 PE 20231066A1
- Authority
- PE
- Peru
- Prior art keywords
- ring
- alkyl
- alkylene
- bond
- cycloalkyl
- Prior art date
Links
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 title abstract 2
- 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
- 239000000556 agonist Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000002947 alkylene group Chemical group 0.000 abstract 3
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 abstract 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- -1 RLa is H Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6568—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
- C07F9/65685—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
- C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Zoology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Refiere a agonistas de GLP-1 de Formula (I), o una sal o solvato farmaceuticamente aceptable de los mismos, en donde Q1, Q2, Q3, Q4 y Q5, forman parte de un anillo con enlaces simples o dobles, siempre que este sea aromatico, y se seleccionan, de acuerdo con (AA) o (BB), de N, CH, CRQA, CRQB, entre otros; R1, R2 y R3 se seleccionan de H y C1-6 alquilo y se sustituyen con 1-6 sustituyentes del grupo de halo, -OH y C1-6 alcoxi; L1 es -C(=O)-, -CH2-, -CH(C1-6 alquil)- y -S(=O)2; en L2, aa es el punto de union al anillo de Q1-Q5, L2A es un enlace o C1-10 alquileno, RLa es H, C1-6 alquilo y C(=O)(C1-6 alquilo), y n1 es 1-3; el anillo A es C6-10 arilo, C5-7 cicloalquilo, heterociclilo de 5-7 miembros o un heteroarilo de 5-10 miembros; en el anillo B, bb es el punto de union a L1., R4, R5, R6 y R7 se seleccionan de H, halo y C1-6 alquilo, R8a y R8b forman un anillo C3-15 cicloalquilo, L3 es un enlace o C1-3 alquileno y L4 es un enlace o C1-5 alquileno; y el anillo C se selecciona del grupo conformado por un heterociclilo de 3-12 miembros; C3-15 cicloalquilo; y un heteroarilo de 5-10 miembros. Tambien, refiere a una composicion farmaceutica que comprende al compuesto y un excipiente farmaceuticamente aceptable y un metodo para el tratamiento de la diabetes mellitus tipo 2.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2020074537 | 2020-02-07 | ||
CN2020109304 | 2020-08-14 | ||
PCT/CN2021/075488 WO2021155841A1 (en) | 2020-02-07 | 2021-02-05 | Heterocyclic glp-1 agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20231066A1 true PE20231066A1 (es) | 2023-07-17 |
Family
ID=77199190
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022001553A PE20231066A1 (es) | 2020-02-07 | 2021-02-05 | Agonistas heterociclicos de glp-1 |
Country Status (30)
Country | Link |
---|---|
US (2) | US11492365B2 (es) |
EP (2) | EP4458834A3 (es) |
JP (1) | JP2023513272A (es) |
KR (1) | KR20220156535A (es) |
CN (1) | CN115698003B (es) |
AU (1) | AU2021216324B2 (es) |
CA (1) | CA3169975A1 (es) |
CL (1) | CL2022002105A1 (es) |
CO (1) | CO2022011065A2 (es) |
CR (1) | CR20220371A (es) |
DK (1) | DK4097099T3 (es) |
DO (1) | DOP2022000158A (es) |
ES (1) | ES2986788T3 (es) |
FI (1) | FI4097099T3 (es) |
HR (1) | HRP20241159T1 (es) |
HU (1) | HUE068174T2 (es) |
IL (1) | IL295281A (es) |
LT (1) | LT4097099T (es) |
MA (1) | MA58498B1 (es) |
MD (1) | MD4097099T2 (es) |
MX (1) | MX2022009524A (es) |
PE (1) | PE20231066A1 (es) |
PH (1) | PH12022552056A1 (es) |
PL (1) | PL4097099T3 (es) |
PT (1) | PT4097099T (es) |
RS (1) | RS65877B1 (es) |
SI (1) | SI4097099T1 (es) |
SM (1) | SMT202400344T1 (es) |
TW (1) | TW202142538A (es) |
WO (1) | WO2021155841A1 (es) |
Families Citing this family (28)
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US10954221B2 (en) | 2019-04-12 | 2021-03-23 | Qilu Regor Therapeutics Inc. | GLP-1R agonists and uses thereof |
KR20220092909A (ko) | 2019-10-25 | 2022-07-04 | 길리애드 사이언시즈, 인코포레이티드 | Glp-1r 조절 화합물 |
EP4097097B1 (en) | 2020-01-29 | 2025-01-15 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
TW202142538A (zh) | 2020-02-07 | 2021-11-16 | 美商迦舒布魯姆生物有限公司 | 雜環glp-1促效劑 |
CN116368140A (zh) * | 2020-09-10 | 2023-06-30 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
EP4247804A1 (en) | 2020-11-20 | 2023-09-27 | Gilead Sciences, Inc. | Polyheterocyclic glp-1 r modulating compounds |
WO2022192430A1 (en) | 2021-03-11 | 2022-09-15 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
EP4304711A1 (en) | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
US20240217966A1 (en) | 2021-03-24 | 2024-07-04 | Shionogi & Co., Ltd. | Pharmaceutical composition containing glp-1 receptor agonist having fused ring |
PE20240362A1 (es) | 2021-04-21 | 2024-03-04 | Gilead Sciences Inc | Compuestos moduladores del glp-ir carboxibenzimidazolicos |
US20240366639A1 (en) * | 2021-08-12 | 2024-11-07 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
CN118215478A (zh) | 2021-09-08 | 2024-06-18 | 盐野义制药株式会社 | 用于预防和治疗与抗肥胖作用有关的疾病的药物 |
WO2023169456A1 (en) | 2022-03-09 | 2023-09-14 | Gasherbrum Bio , Inc. | Heterocyclic glp-1 agonists |
WO2024063143A1 (ja) | 2022-09-22 | 2024-03-28 | 塩野義製薬株式会社 | Glp-1受容体アゴニスト作用を有する縮合環化合物 |
CN116003403B (zh) * | 2022-11-20 | 2024-07-23 | 药康众拓(北京)医药科技有限公司 | 一种氘代吲唑类化合物、药物组合物及其应用 |
WO2024125602A1 (en) | 2022-12-15 | 2024-06-20 | Gasherbrum Bio, Inc. | Salts and solid forms of a compound having glp-1 agonist activity |
WO2024153070A1 (en) * | 2023-01-17 | 2024-07-25 | Fochon Biosciences, Ltd. | Glp-1r agonists and uses thereof |
WO2025002326A1 (zh) * | 2023-06-30 | 2025-01-02 | 正大天晴药业集团股份有限公司 | 含多稠环结构的化合物 |
US20250019389A1 (en) | 2023-06-30 | 2025-01-16 | Gasherbrum Bio, Inc. | Heterocyclic agonists |
WO2025011664A1 (zh) * | 2023-07-12 | 2025-01-16 | 歌礼制药(中国)有限公司 | Glp-1r激动剂的制剂及其制备方法 |
WO2025015269A1 (en) | 2023-07-13 | 2025-01-16 | Aconcagua Bio, Inc. | Compounds, compositions, and methods |
WO2025015268A1 (en) | 2023-07-13 | 2025-01-16 | Aconcagua Bio, Inc. | Modulators of calcitonin receptor and/or amylin receptor activity |
WO2025026270A1 (zh) * | 2023-07-28 | 2025-02-06 | 上海翰森生物医药科技有限公司 | 一种苯并含氮杂环类衍生物调节剂、其制备方法和应用 |
WO2025026436A1 (zh) * | 2023-08-02 | 2025-02-06 | 韦恩生物科技有限公司 | 一种含氮并环化合物及其制备方法和用途 |
WO2025045208A1 (en) * | 2023-08-31 | 2025-03-06 | Gasherbrum Bio, Inc. | Heteroaryl-heterocycloalkyl-based glp-1 agonists |
WO2025057134A2 (en) | 2023-09-14 | 2025-03-20 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
CN117447493A (zh) * | 2023-12-25 | 2024-01-26 | 药康众拓(北京)医药科技有限公司 | 氘代吲哚嗪类化合物、药物组合物及其应用 |
CN119176808A (zh) * | 2024-11-25 | 2024-12-24 | 山东法恩新材料科技有限公司 | 一种glp-1激动剂及其制备方法和应用 |
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