PE20211871A1 - Agonistas de glp-1r y usos de los mismos - Google Patents
Agonistas de glp-1r y usos de los mismosInfo
- Publication number
- PE20211871A1 PE20211871A1 PE2021000746A PE2021000746A PE20211871A1 PE 20211871 A1 PE20211871 A1 PE 20211871A1 PE 2021000746 A PE2021000746 A PE 2021000746A PE 2021000746 A PE2021000746 A PE 2021000746A PE 20211871 A1 PE20211871 A1 PE 20211871A1
- Authority
- PE
- Peru
- Prior art keywords
- ring
- halogen
- alkyl
- contain
- acid
- Prior art date
Links
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 title abstract 2
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- -1 6- (4-chloro-2-fluorobenzylamino) pyridin-2-yl Chemical group 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000001280 Prediabetic State Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052805 deuterium Inorganic materials 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 201000009104 prediabetes syndrome Diseases 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Steroid Compounds (AREA)
Abstract
Esta referido a un compuesto de Formula I, en donde: EE es -COOH o un sustituto del grupo carboxilico; Anillo A no contiene 3 N en el anillo en 3 posiciones contiguas; Anillo B no contiene 3 N en el anillo en 3 posiciones contiguas; Anillo C no contiene mas de dos dobles enlaces; R1 es halogeno, CN, OH, alquilo, alcoxi, entre otros; R2 es halogeno, CN; OH, oxo, alquilo, entre otros; R3 es halogeno, CN, OH, alquilo, alcoxi, arilo, entre otros; W es O, S, SR5R6, NR5; X1, X2, X3, X4, X5 son N, CH; Y1, Y3, Y4, Y5 son N, NH, CN, CH2; Y2, Y6 son N, C, CH; Z1, Z2 son H, C, CH; Z3, Z4 es un enlace, CH, CH2, CH=CH, CH2CH2, CH2CH y CHCH2; T2, T3, T4 son N, NR4, O, S, C y CR4; T6, T7, T8 son N, CR4; Ra, Rb, Rc, Rd son H, deuterio, halogeno, CN, alquilo, entre otros; m es 0, 1, 2, 3, 4; n es 0, 1, 2, 3, 4, 5; o es 0, 1, 2, 3, 4, 5. Entre los compuestos preferidos tenemos los siguientes: acido (S)-2-((4-(6-(4-cloro-2-fluorobencilamino) piridin-2-il) piperazin-1-il) metil)-1-(oxetan-2-ilmetil)-1H-benzo[d] imidazol-6-carboxilico; acido (S)-2-((4-(4-(4-cloro-2-fluorobencil)-3,4-dihidro-2H-pirido[3,2- b][1,4]oxazin-6-ilo)piperazin-1-il)metil)-1-(oxetan-2-ilmetil)-1H-benzo[d]imidazol-6- carboxilico; entre otros. Estos compuestos son agonistas de GLP-1R y se emplean en el tratamiento de la diabetes mellitus tipo 2, prediabetes, obesidad, enfermedad del higado graso no alcoholico, esteatohepatitis no alcoholica y enfermedades cardiovasculares.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018117047 | 2018-11-22 | ||
| PCT/CN2019/119373 WO2020103815A1 (en) | 2018-11-22 | 2019-11-19 | Glp-1r agonists and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211871A1 true PE20211871A1 (es) | 2021-09-21 |
Family
ID=70774321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000746A PE20211871A1 (es) | 2018-11-22 | 2019-11-19 | Agonistas de glp-1r y usos de los mismos |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US20220024901A1 (es) |
| EP (1) | EP3883928A4 (es) |
| JP (1) | JP2022508203A (es) |
| KR (1) | KR20210106447A (es) |
| CN (1) | CN113227068B (es) |
| AU (1) | AU2019382642A1 (es) |
| BR (1) | BR112021009877A2 (es) |
| CA (1) | CA3120499A1 (es) |
| CL (1) | CL2021001332A1 (es) |
| CO (1) | CO2021008089A2 (es) |
| CR (1) | CR20210341A (es) |
| CU (1) | CU20210042A7 (es) |
| EA (1) | EA202191432A1 (es) |
| IL (1) | IL283322A (es) |
| MA (1) | MA54555A (es) |
| MX (1) | MX2021006034A (es) |
| PE (1) | PE20211871A1 (es) |
| PH (1) | PH12021551165A1 (es) |
| SA (1) | SA521422068B1 (es) |
| SG (1) | SG11202105241YA (es) |
| TW (1) | TWI839416B (es) |
| WO (1) | WO2020103815A1 (es) |
Families Citing this family (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2943510T3 (es) * | 2018-06-15 | 2023-06-13 | Pfizer | Agonistas del receptor GLP-1 y usos del mismo |
| UA127629C2 (uk) | 2018-08-13 | 2023-11-08 | Ф. Хоффманн-Ля Рош Аг | Нові гетероциклічні сполуки як інгібітори моноацилгліцеролліпази |
| PE20211871A1 (es) * | 2018-11-22 | 2021-09-21 | Qilu Regor Therapeutics Inc | Agonistas de glp-1r y usos de los mismos |
| PH12021552557A1 (en) | 2019-04-12 | 2022-07-04 | Qilu Regor Therapeutics Inc | Glp-1r agonists and uses thereof |
| US10954221B2 (en) | 2019-04-12 | 2021-03-23 | Qilu Regor Therapeutics Inc. | GLP-1R agonists and uses thereof |
| TWI751585B (zh) * | 2019-06-28 | 2022-01-01 | 美商美國禮來大藥廠 | 類升糖素肽1受體促效劑 |
| WO2021018023A1 (zh) * | 2019-08-01 | 2021-02-04 | 济南泰达领创医药技术有限公司 | 小分子glp-1受体调节剂 |
| WO2021048242A1 (en) | 2019-09-12 | 2021-03-18 | F. Hoffmann-La Roche Ag | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
| PE20221040A1 (es) * | 2019-10-25 | 2022-06-17 | Gilead Sciences Inc | Compuestos moduladores de glp-1r |
| PE20221422A1 (es) | 2019-11-15 | 2022-09-20 | Ildong Pharmaceutical Co Ltd | Agonista del receptor glp-1 y uso de este |
| US12121511B2 (en) | 2020-01-29 | 2024-10-22 | Gilead Sciences, Inc. | GLP-1R modulating compounds |
| ES2986788T3 (es) | 2020-02-07 | 2024-11-12 | Gasherbrum Bio Inc | Agonistas heterocíclicos de GLP-1 |
| CN115697999A (zh) * | 2020-02-13 | 2023-02-03 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
| TW202144340A (zh) * | 2020-04-03 | 2021-12-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合咪唑類衍生物、其製備方法及其在醫藥上的應用 |
| HUE068535T2 (hu) * | 2020-05-27 | 2025-01-28 | Qilu Regor Therapeutics Inc | GLP-1R agonisták sója és kristályformái és azok felhasználásai |
| KR102588241B1 (ko) * | 2020-06-04 | 2023-10-11 | 항저우 사이윈드 바이오사이언시즈 컴퍼니 리미티드 | 5원 헤테로방향족 이미다졸 화합물 및 이의 용도 |
| CN117645601A (zh) * | 2020-06-10 | 2024-03-05 | 重庆康丁医药技术有限公司 | 一种具有心血管益处的glp-1小分子 |
| CN113816948B (zh) * | 2020-06-19 | 2023-08-11 | 江苏恒瑞医药股份有限公司 | 稠合咪唑类衍生物、其制备方法及其在医药上的应用 |
| CN113831337B (zh) * | 2020-06-24 | 2023-03-24 | 广州市恒诺康医药科技有限公司 | Glp-1受体激动剂及其药物组合物和用途 |
| IL300155A (en) | 2020-08-06 | 2023-03-01 | Gasherbrum Bio Inc | Heterocyclic GLP-1 agonists |
| WO2022031994A1 (en) * | 2020-08-06 | 2022-02-10 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| MX2023002108A (es) * | 2020-08-21 | 2023-07-11 | Terns Pharmaceuticals Inc | Compuestos como agonistas de glp-1r. |
| CN116406360A (zh) | 2020-08-28 | 2023-07-07 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
| WO2022007979A1 (zh) * | 2020-09-01 | 2022-01-13 | 江苏恒瑞医药股份有限公司 | 稠合咪唑类衍生物、其制备方法及其在医药上的应用 |
| WO2022051317A1 (en) | 2020-09-03 | 2022-03-10 | Amgen Inc. | Diol desymmetrization by nucleophilic aromatic substitution |
| WO2022068772A1 (zh) * | 2020-09-29 | 2022-04-07 | 深圳信立泰药业股份有限公司 | 一种苯并咪唑类衍生物及其制备方法和医药用途 |
| EP4227299A1 (en) | 2020-10-12 | 2023-08-16 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | Benzimidazolone glp-1 receptor agonist and use thereof |
| EP4229050A4 (en) * | 2020-10-13 | 2024-12-11 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| WO2022078380A1 (en) * | 2020-10-13 | 2022-04-21 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| WO2022078352A1 (en) * | 2020-10-14 | 2022-04-21 | Qilu Regor Therapeutics Inc. | Crystal forms of glp-1r agonists and uses thereof |
| CN114478497B (zh) * | 2020-11-12 | 2023-10-20 | 杭州中美华东制药有限公司 | 芳基烷基酸类glp-1受体激动剂及其用途 |
| EP4247804A1 (en) * | 2020-11-20 | 2023-09-27 | Gilead Sciences, Inc. | Polyheterocyclic glp-1 r modulating compounds |
| US20240246959A1 (en) * | 2020-11-27 | 2024-07-25 | Shenzhen Salubris Pharmaceuticals Co., Ltd. | Benzimidazole derivative and preparation method therefor and medical use thereof |
| CN114591308B (zh) * | 2020-12-03 | 2024-03-08 | 苏州闻泰医药科技有限公司 | 一类glp-1r受体激动剂化合物及其用途 |
| US20240124470A1 (en) * | 2020-12-25 | 2024-04-18 | Sichuan Haisco Pharmaceutical Co., Ltd. | Five-membered ring derivative and medical use thereof |
| WO2022165076A1 (en) * | 2021-01-28 | 2022-08-04 | Carmot Therapeutics, Inc. | Gpcr receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
| WO2022184849A1 (en) | 2021-03-04 | 2022-09-09 | Les Laboratoires Servier | Glp-1r agonists, uses and pharmaceutical compositions thereof |
| EP4304711A1 (en) * | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| EP4304712A1 (en) | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| US20240208952A1 (en) | 2021-03-22 | 2024-06-27 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | Thiophene glp-1 receptor agonist and use thereof |
| JPWO2022202864A1 (es) | 2021-03-24 | 2022-09-29 | ||
| EP4271672A1 (en) | 2021-04-21 | 2023-11-08 | Gilead Sciences, Inc. | Carboxy-benzimidazole glp-1r modulating compounds |
| WO2022228490A1 (zh) * | 2021-04-30 | 2022-11-03 | 上海翰森生物医药科技有限公司 | 多环类衍生物调节剂、其制备方法和应用 |
| CA3217720A1 (en) * | 2021-05-03 | 2022-11-10 | Xiaohui Du | Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
| TWI843104B (zh) | 2021-05-20 | 2024-05-21 | 美商美國禮來大藥廠 | 類升糖素肽1受體促效劑 |
| EP4361145A1 (en) | 2021-06-24 | 2024-05-01 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | Glp-1 receptor agonist and composition and use thereof |
| JP2024525900A (ja) * | 2021-07-21 | 2024-07-12 | ヘパジーン セラピューティクス（エイチケー）リミティド | グルカゴン様ペプチド－１受容体モジュレーター及びその使用 |
| CN113480534B (zh) * | 2021-07-23 | 2022-05-13 | 广州必贝特医药股份有限公司 | 苯并咪唑或氮杂苯并咪唑-6-羧酸类化合物及其应用 |
| US20240360109A1 (en) * | 2021-08-04 | 2024-10-31 | Shanghai Hansoh Biomedical Co., Ltd. | Cycloalkene derivative regulator, preparation method therefor, and application thereof |
| CN117242067B (zh) * | 2021-08-30 | 2025-03-25 | 杭州德睿智药科技有限公司 | 作为glp1r激动剂的新型芳醚取代杂环类化合物 |
| EP4400105A1 (en) | 2021-09-08 | 2024-07-17 | Shionogi & Co., Ltd | Medicine for prevention and treatment of diseases linked to anti-obesity activity |
| EP4412707A1 (en) | 2021-10-05 | 2024-08-14 | Astrazeneca AB | Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators |
| WO2023057429A1 (en) | 2021-10-05 | 2023-04-13 | Astrazeneca Ab | Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators |
| WO2023057414A1 (en) | 2021-10-05 | 2023-04-13 | Astrazeneca Ab | Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators |
| TWI843243B (zh) * | 2021-10-22 | 2024-05-21 | 大陸商盛世泰科生物醫藥技術（蘇州）股份有限公司 | 作為glp-1受體激動劑的化合物、包含其的藥物組成物及其用途 |
| IL312364A (en) * | 2021-10-25 | 2024-06-01 | Luehr Gary W | Compounds as GLP-1R agonists |
| AU2022401795A1 (en) * | 2021-12-03 | 2024-07-04 | Hangzhou Sciwind Biosciences Co., Ltd. | Crystal forms of thienoimidazole compound and preparation method thereof |
| CN114163438A (zh) * | 2021-12-13 | 2022-03-11 | 无锡捷化医药科技有限公司 | 一种2-甲基-3-羰基吡唑并[4,3-c]吡啶-7-羧酸盐酸盐的制备方法 |
| WO2023111145A1 (en) | 2021-12-16 | 2023-06-22 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| WO2023111144A1 (en) | 2021-12-16 | 2023-06-22 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| AU2022418658A1 (en) * | 2021-12-23 | 2024-07-11 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Pharmaceutically acceptable salt and crystalline form of glp-1 receptor agonist and preparation method therefor |
| CN116354945B (zh) * | 2021-12-27 | 2024-08-30 | 长春金赛药业有限责任公司 | 一种稠合咪唑羧酸类化合物及其制备方法和应用 |
| CN118613476A (zh) * | 2022-01-10 | 2024-09-06 | 西藏海思科制药有限公司 | 一种glp-1激动剂盐及其晶型及在医药上的应用 |
| WO2023151575A1 (en) * | 2022-02-09 | 2023-08-17 | Gasherbrum Bio Inc. | Heterocyclic glp-1 agonists |
| JP2025508097A (ja) | 2022-03-08 | 2025-03-21 | 広州市聯瑞制葯有限公司 | ベンゾビシクロ系化合物及びその製造方法と応用 |
| CN119137124A (zh) * | 2022-03-09 | 2024-12-13 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
| EP4508047A1 (en) * | 2022-04-14 | 2025-02-19 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| CN117362282A (zh) * | 2022-07-07 | 2024-01-09 | 杭州德睿智药科技有限公司 | Glp-1r激动剂的盐及其制备方法和应用 |
| WO2024026338A1 (en) * | 2022-07-27 | 2024-02-01 | Carmot Therapeutics, Inc. | N-heterocylic gpcr receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
| WO2024051749A1 (zh) * | 2022-09-06 | 2024-03-14 | 德睿智药(苏州)新药研发有限公司 | 一种glp-1r激动剂化合物的多晶型物及其制备方法与用途 |
| 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 |
| CN116102543A (zh) * | 2022-10-21 | 2023-05-12 | 江南大学 | 一种glp-1r激动剂、合成方法及其用途 |
| WO2024102625A1 (en) | 2022-11-11 | 2024-05-16 | Eli Lilly And Company | Glucagon-like peptide 1 receptor agonists |
| WO2024107781A1 (en) | 2022-11-16 | 2024-05-23 | Eli Lilly And Company | Glucagon-like peptide 1 receptor agonists |
| CN118184637A (zh) * | 2022-12-13 | 2024-06-14 | 杭州中美华东制药有限公司 | Glp-1受体激动剂的新晶型和制备方法及其药物组合物和用途 |
| TW202440556A (zh) * | 2022-12-13 | 2024-10-16 | 中國大陸商杭州中美華東製藥有限公司 | 鹽型的glp-1受體激動劑、其晶型和製備方法及其藥物組合物和用途 |
| WO2024153070A1 (en) * | 2023-01-17 | 2024-07-25 | Fochon Biosciences, Ltd. | Glp-1r agonists and uses thereof |
| WO2024160271A1 (zh) * | 2023-02-02 | 2024-08-08 | 江苏豪森药业集团有限公司 | 一种环烯类化合物的盐、晶型及其制备方法和应用 |
| WO2024212742A1 (zh) * | 2023-04-10 | 2024-10-17 | 上海研健新药研发有限公司 | 一种glp-1r激动剂，其制备方法和应用 |
| WO2025007836A1 (zh) * | 2023-07-04 | 2025-01-09 | 杭州中美华东制药有限公司 | 一种glp1r激动剂及其中间体的制备方法 |
| US12234236B1 (en) | 2023-09-14 | 2025-02-25 | Ascletis Pharma (China) Co., Limited | GLP-1R agonist and therapeutic method thereof |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| US5013556A (en) | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| US20040127504A1 (en) | 2002-09-06 | 2004-07-01 | Cowart Marlon D. | Benzimidazoles that are useful in treating sexual dysfunction |
| WO2004099192A2 (en) | 2003-04-30 | 2004-11-18 | The Institutes Of Pharmaceutical Discovery, Llc | Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b |
| CN101775013A (zh) | 2004-09-13 | 2010-07-14 | 小野药品工业株式会社 | 含氮杂环衍生物及含有其作为活性成分的药物 |
| US20060122222A1 (en) | 2004-11-18 | 2006-06-08 | The Institutes For Pharmaceutical Discovery, Llc | Heterocycle substituted carboxylic acids |
| WO2007082264A2 (en) | 2006-01-11 | 2007-07-19 | Bristol-Myers Squibb Company | Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions |
| CA2785410A1 (en) | 2009-12-23 | 2011-06-30 | Carlos F. Barbas, Iii | Tyrosine bioconjugation through aqueous ene-like reactions |
| NZ603876A (en) * | 2010-05-13 | 2015-02-27 | Amgen Inc | Nitrogen heterocyclic compounds useful as pde10 inhibitors |
| JP2013530963A (ja) | 2010-06-09 | 2013-08-01 | レセプトス インコーポレイテッド | 新規のｇｌｐ−１受容体安定化薬および調節薬 |
| PE20140859A1 (es) * | 2011-02-25 | 2014-07-25 | Merck Sharp & Dohme | Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos |
| US9464065B2 (en) | 2011-03-24 | 2016-10-11 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| KR20140107340A (ko) * | 2011-12-12 | 2014-09-04 | 레셉토스, 인코포레이티드 | 당뇨병과 같은 치료를 위한 glp-1 수용체 조절제로서 작용하는 4 개의 사이클을 포함하는 카르복실산 유도체 |
| EP3954685A1 (en) | 2014-12-29 | 2022-02-16 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Small molecule inhibitors of lactate dehydrogenase and methods of use thereof |
| BR112018068703B1 (pt) | 2016-03-16 | 2024-02-06 | Kura Oncology, Inc. | Inibidores substituídos de menin-mll e métodos de uso |
| UA122035C2 (uk) | 2016-12-16 | 2020-08-25 | Пфайзер Інк. | Агоністи рецептора glp-1 та їх застосування |
| US10934279B2 (en) * | 2018-06-13 | 2021-03-02 | Pfizer Inc. | GLP-1 receptor agonists and uses thereof |
| ES2943510T3 (es) * | 2018-06-15 | 2023-06-13 | Pfizer | Agonistas del receptor GLP-1 y usos del mismo |
| WO2020033413A2 (en) | 2018-08-07 | 2020-02-13 | Tosk, Inc. | Modulators of ras gtpase |
| BR112021003039A2 (pt) * | 2018-08-31 | 2021-05-18 | Pfizer Inc. | combinações para o tratamento de nash/nafld e doenças relacionadas |
| PE20211871A1 (es) * | 2018-11-22 | 2021-09-21 | Qilu Regor Therapeutics Inc | Agonistas de glp-1r y usos de los mismos |
| HUE068535T2 (hu) * | 2020-05-27 | 2025-01-28 | Qilu Regor Therapeutics Inc | GLP-1R agonisták sója és kristályformái és azok felhasználásai |
-
2019
- 2019-11-19 PE PE2021000746A patent/PE20211871A1/es unknown
- 2019-11-19 KR KR1020217019126A patent/KR20210106447A/ko active Pending
- 2019-11-19 SG SG11202105241YA patent/SG11202105241YA/en unknown
- 2019-11-19 CN CN201980087385.0A patent/CN113227068B/zh active Active
- 2019-11-19 EP EP19887901.7A patent/EP3883928A4/en active Pending
- 2019-11-19 CA CA3120499A patent/CA3120499A1/en active Pending
- 2019-11-19 MA MA054555A patent/MA54555A/fr unknown
- 2019-11-19 WO PCT/CN2019/119373 patent/WO2020103815A1/en active Application Filing
- 2019-11-19 US US17/296,078 patent/US20220024901A1/en active Pending
- 2019-11-19 EA EA202191432A patent/EA202191432A1/ru unknown
- 2019-11-19 MX MX2021006034A patent/MX2021006034A/es unknown
- 2019-11-19 CR CR20210341A patent/CR20210341A/es unknown
- 2019-11-19 BR BR112021009877-1A patent/BR112021009877A2/pt unknown
- 2019-11-19 CU CU2021000042A patent/CU20210042A7/es unknown
- 2019-11-19 JP JP2021529110A patent/JP2022508203A/ja active Pending
- 2019-11-19 AU AU2019382642A patent/AU2019382642A1/en active Pending
- 2019-11-22 TW TW108142555A patent/TWI839416B/zh active
-
2020
- 2020-05-15 US US16/874,908 patent/US10844049B2/en active Active
-
2021
- 2021-05-20 SA SA521422068A patent/SA521422068B1/ar unknown
- 2021-05-20 IL IL283322A patent/IL283322A/en unknown
- 2021-05-20 CL CL2021001332A patent/CL2021001332A1/es unknown
- 2021-05-21 PH PH12021551165A patent/PH12021551165A1/en unknown
- 2021-06-21 CO CONC2021/0008089A patent/CO2021008089A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3120499A1 (en) | 2020-05-28 |
| BR112021009877A2 (pt) | 2021-08-17 |
| EP3883928A4 (en) | 2022-06-29 |
| EA202191432A1 (ru) | 2021-10-14 |
| CN113227068B (zh) | 2023-06-13 |
| CL2021001332A1 (es) | 2021-11-05 |
| PH12021551165A1 (en) | 2021-10-25 |
| US20200283424A1 (en) | 2020-09-10 |
| WO2020103815A1 (en) | 2020-05-28 |
| TWI839416B (zh) | 2024-04-21 |
| CN113227068A (zh) | 2021-08-06 |
| CU20210042A7 (es) | 2022-01-13 |
| SG11202105241YA (en) | 2021-06-29 |
| US10844049B2 (en) | 2020-11-24 |
| IL283322A (en) | 2021-07-29 |
| MA54555A (fr) | 2021-09-29 |
| TW202039458A (zh) | 2020-11-01 |
| MX2021006034A (es) | 2021-09-21 |
| CO2021008089A2 (es) | 2021-09-09 |
| AU2019382642A1 (en) | 2021-06-10 |
| EP3883928A1 (en) | 2021-09-29 |
| SA521422068B1 (ar) | 2024-04-24 |
| JP2022508203A (ja) | 2022-01-19 |
| CR20210341A (es) | 2021-11-25 |
| KR20210106447A (ko) | 2021-08-30 |
| US20220024901A1 (en) | 2022-01-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20211871A1 (es) | Agonistas de glp-1r y usos de los mismos | |
| PE20220143A1 (es) | Agonistas de glp-1r y usos de los mismos | |
| PE20220931A1 (es) | Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina | |
| PE20221336A1 (es) | Compuestos triciclicos sustituidos | |
| AR053415A1 (es) | Inhibidores dipeptidil peptidasa iv, composiciones farmaceuticas que los contienen y procesos para la preparacion de los compuestos y de la composicion | |
| UY29393A1 (es) | Nuevos derivados de amidas, sales farmacéuticas aceptables, composiciones que los contienen, procedimientos de preparación y aplicaciones. | |
| AR076551A1 (es) | Compuestos de 1-cianoetilheterociclilcarboxamida sustituida, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por dppi | |
| AR053548A1 (es) | Derivados de oxiindol | |
| PE20100138A1 (es) | Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k | |
| AR064452A1 (es) | Derivados de 1,2,4 oxadiazol-indol,composiciones farmaceuticas que los comprenden y usos en trastornos asociados a receptores s1p1. | |
| AR052902A1 (es) | Derivados de piridazina, composicion farmaceutica que los contiene y su uso como agentes terapeuticos para enfermedades mediadas por la estearoil-coa desaturasa | |
| PE20181144A1 (es) | Derivados de heteroarilo como inhibidores de parp | |
| AR068496A1 (es) | Piperidinas sustituidas, una composicion farmaceutica que las comprende y su uso para el tratamiento de enfermedades mediadas por la modulacion de la actividad de gpr119. | |
| PE20050951A1 (es) | Compuestos mimeticos de glucocorticoides, metodos de preparacion y composiciones farmaceuticas | |
| PE20091204A1 (es) | Derivados de 2-aminoquinolina como antagonistas del receptor de 5-ht5a | |
| AR054799A1 (es) | Derivados de oxindol | |
| AR051920A1 (es) | Derivados de quinazolinona como inhibidores del parp, un procedimiento de preparacion, composicion farmaceutica y proceso de preparacion de esta | |
| PE20060150A1 (es) | Antagonistas de cgrp seleccionados, composiciones farmaceuticas y procedimiento para su preparacion | |
| PE20120321A1 (es) | Indazoles sustituidos con oxazol como inhibidores de pi3-quinasa | |
| PE20011166A1 (es) | Piridinas, pirimidinas, purinonas, pirrolopirimidinonas y pirrolopiridinonas como antagonistas del factor liberador de corticotropina | |
| PA8581401A1 (es) | Compuestos de imedazopiridina como agonistas del receptor 5-ht4 | |
| ES2564010T3 (es) | Composición farmacéutica para tratar o prevenir el glaucoma | |
| AR079260A1 (es) | Inhibidores de bencimidazol de la produccion de leucotrienos, un procedimiento para su preparacion, composiciones farmaceuticas que los comprenden y su empleo como medicamentos en el tratamiento de trastornos mediados por leucotrienos | |
| PE20081472A1 (es) | Compuestos de pirazolina | |
| AR056103A1 (es) | Compuestos de(piran-piperidinil)benzimidazol, composiciones farmaceuticas que los comprenden, proceso de preparacion y usos en el tratamiento de afecciones mediadas por agonistas del receptor muscarinico m1 |