BR112022010599A2 - Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina - Google Patents
Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-aminaInfo
- Publication number
- BR112022010599A2 BR112022010599A2 BR112022010599A BR112022010599A BR112022010599A2 BR 112022010599 A2 BR112022010599 A2 BR 112022010599A2 BR 112022010599 A BR112022010599 A BR 112022010599A BR 112022010599 A BR112022010599 A BR 112022010599A BR 112022010599 A2 BR112022010599 A2 BR 112022010599A2
- Authority
- BR
- Brazil
- Prior art keywords
- methyl
- methylbenzo
- oxetan
- chloropyridin
- dioxol
- Prior art date
Links
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical class OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 title abstract 3
- 239000011973 solid acid Substances 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- SVPYZAJTWFQTSM-UGDMGKLASA-N 2-[[4-[(2S)-2-(5-chloropyridin-2-yl)-2-methyl-1,3-benzodioxol-4-yl]piperidin-1-yl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid Chemical compound ClC=1C=CC(=NC=1)[C@@]1(OC2=C(O1)C=CC=C2C1CCN(CC1)CC1=NC2=C(N1C[C@H]1OCC1)C=C(C=C2)C(=O)O)C SVPYZAJTWFQTSM-UGDMGKLASA-N 0.000 abstract 1
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 abstract 1
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 abstract 1
- 150000004682 monohydrates Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962946084P | 2019-12-10 | 2019-12-10 | |
| PCT/IB2020/061585 WO2021116874A1 (en) | 2019-12-10 | 2020-12-07 | Solid forms of 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d] [1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d] imidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022010599A2 true BR112022010599A2 (pt) | 2022-08-16 |
Family
ID=73835650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022010599A BR112022010599A2 (pt) | 2019-12-10 | 2020-12-07 | Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20230045419A1 (enExample) |
| EP (1) | EP4073028A1 (enExample) |
| JP (1) | JP2021091683A (enExample) |
| KR (1) | KR20220112811A (enExample) |
| CN (1) | CN115175893A (enExample) |
| AR (1) | AR120703A1 (enExample) |
| AU (1) | AU2020402177A1 (enExample) |
| BR (1) | BR112022010599A2 (enExample) |
| CA (1) | CA3163979A1 (enExample) |
| MX (1) | MX2022007105A (enExample) |
| TW (1) | TWI809334B (enExample) |
| WO (1) | WO2021116874A1 (enExample) |
| ZA (1) | ZA202207589B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA202191432A1 (ru) | 2018-11-22 | 2021-10-14 | Цилу Регор Терапьютикс Инк. | Агонисты glp-1r и их применения |
| AU2020256647B2 (en) | 2019-04-12 | 2025-07-31 | Qilu Regor Therapeutics Inc. | GLP-1R agonists and uses thereof |
| US20220193063A1 (en) * | 2020-12-15 | 2022-06-23 | Pfizer Inc. | Metabolites of glp1r agonists |
| US12065434B2 (en) | 2020-12-15 | 2024-08-20 | Pfizer Inc. | Metabolites of GLP1R agonists |
| SI4408840T1 (sl) | 2021-09-27 | 2025-12-31 | Terns Pharmaceuticals, Inc. | Benzimidazolne karboksilne kisline kot agonisti GLP-1R |
| 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 |
| US20250236627A1 (en) | 2021-10-05 | 2025-07-24 | Astrazeneca Ab | Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators |
| WO2023057427A1 (en) | 2021-10-05 | 2023-04-13 | Astrazeneca Ab | Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators |
| US12024507B2 (en) | 2021-10-25 | 2024-07-02 | Terns Pharmaceuticals, Inc. | Compounds as GLP-1R agonists |
| US20250066338A1 (en) | 2021-12-16 | 2025-02-27 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| US20250042882A1 (en) | 2021-12-16 | 2025-02-06 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| AU2023224854A1 (en) | 2022-02-23 | 2024-10-03 | Terns Pharmaceuticals, Inc. | Compounds as glp-1r agonists |
| CA3246495A1 (en) * | 2022-03-25 | 2023-09-28 | Ildong Pharmaceutical Co., Ltd. | NEW GLP-1 RECEPTOR AGONIST COMPOUND SALT, ITS PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITION INCLUDING IT |
| WO2023228023A1 (en) | 2022-05-23 | 2023-11-30 | Pfizer Inc. | Treatment of type 2 diabetes or weight management control with 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d]imidazole-6-carboxylic acid or a pharmaceutically salt thereof |
| CN117362282B (zh) * | 2022-07-07 | 2026-04-21 | 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 |
| CN116217522B (zh) * | 2023-02-22 | 2025-06-24 | 广东莱佛士制药技术有限公司 | Glp-1受体激动剂关键中间体的手性纯化方法 |
| PE20252787A1 (es) | 2023-04-07 | 2025-12-22 | Terns Pharmaceuticals Inc | Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica |
| CN118812522A (zh) * | 2023-04-21 | 2024-10-22 | 苏州闻泰医药科技有限公司 | 一种glp-1r受体激动剂化合物盐、其晶型、其制备方法和应用 |
| EP4777197A2 (en) | 2023-09-14 | 2026-07-22 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
| WO2025109387A1 (en) | 2023-11-24 | 2025-05-30 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
Family Cites Families (12)
| 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 |
| WO2008012623A1 (en) * | 2006-07-25 | 2008-01-31 | Pfizer Products Inc. | Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor |
| DK2621493T3 (en) | 2010-09-30 | 2016-10-24 | Pfizer | N1 PYRAZOLOSPIROKETON-ACETYL-CoA carboxylase INHIBITORS |
| CU24152B1 (es) | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| TN2018000198A1 (en) | 2015-12-29 | 2019-10-04 | Pfizer | Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| WO2018109607A1 (en) * | 2016-12-16 | 2018-06-21 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| CA3045644C (en) * | 2018-06-13 | 2024-01-16 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| CA3140972C (en) * | 2019-05-20 | 2024-06-18 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
-
2020
- 2020-12-07 CA CA3163979A patent/CA3163979A1/en active Pending
- 2020-12-07 MX MX2022007105A patent/MX2022007105A/es unknown
- 2020-12-07 US US17/782,478 patent/US20230045419A1/en not_active Abandoned
- 2020-12-07 AU AU2020402177A patent/AU2020402177A1/en not_active Abandoned
- 2020-12-07 BR BR112022010599A patent/BR112022010599A2/pt not_active Application Discontinuation
- 2020-12-07 CN CN202080095964.2A patent/CN115175893A/zh active Pending
- 2020-12-07 WO PCT/IB2020/061585 patent/WO2021116874A1/en not_active Ceased
- 2020-12-07 KR KR1020227023147A patent/KR20220112811A/ko not_active Withdrawn
- 2020-12-07 EP EP20824663.7A patent/EP4073028A1/en not_active Withdrawn
- 2020-12-07 TW TW109143088A patent/TWI809334B/zh not_active IP Right Cessation
- 2020-12-07 JP JP2020202383A patent/JP2021091683A/ja not_active Withdrawn
- 2020-12-09 AR ARP200103424A patent/AR120703A1/es unknown
-
2022
- 2022-07-08 ZA ZA2022/07589A patent/ZA202207589B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2021091683A (ja) | 2021-06-17 |
| TW202136247A (zh) | 2021-10-01 |
| US20230045419A1 (en) | 2023-02-09 |
| CN115175893A (zh) | 2022-10-11 |
| CA3163979A1 (en) | 2021-06-17 |
| ZA202207589B (en) | 2023-04-26 |
| MX2022007105A (es) | 2022-07-11 |
| TWI809334B (zh) | 2023-07-21 |
| EP4073028A1 (en) | 2022-10-19 |
| AR120703A1 (es) | 2022-03-09 |
| AU2020402177A1 (en) | 2022-06-16 |
| WO2021116874A1 (en) | 2021-06-17 |
| KR20220112811A (ko) | 2022-08-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25G | Requested change of headquarter approved |
Owner name: PFIZER, INC. (US) |
|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |