BR112023003811A2 - Sal de 2-[3-({1-[2-(dimetilamino)etil]-2-(2,2-dimetilpropil)-1h1,3-benzodiazol-5-il}sulfonil)azetidin-1-il]etan-1-ol com ácido, forma cristalina, composição farmacêutica, processo de produção e método de tratamento e prevenção de doenças utilizando o mesmo - Google Patents
Sal de 2-[3-({1-[2-(dimetilamino)etil]-2-(2,2-dimetilpropil)-1h1,3-benzodiazol-5-il}sulfonil)azetidin-1-il]etan-1-ol com ácido, forma cristalina, composição farmacêutica, processo de produção e método de tratamento e prevenção de doenças utilizando o mesmoInfo
- Publication number
- BR112023003811A2 BR112023003811A2 BR112023003811A BR112023003811A BR112023003811A2 BR 112023003811 A2 BR112023003811 A2 BR 112023003811A2 BR 112023003811 A BR112023003811 A BR 112023003811A BR 112023003811 A BR112023003811 A BR 112023003811A BR 112023003811 A2 BR112023003811 A2 BR 112023003811A2
- Authority
- BR
- Brazil
- Prior art keywords
- salt
- azetidin
- dimethylpropyl
- sulfonyl
- dimethylamino
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 4
- -1 CRYSTALLINE FORM Substances 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 230000002265 prevention Effects 0.000 title abstract 2
- 150000003839 salts Chemical group 0.000 abstract 4
- 229940126062 Compound A Drugs 0.000 abstract 3
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 abstract 3
- 239000013078 crystal Chemical group 0.000 abstract 2
- OAYGNQGEUIFBFA-UHFFFAOYSA-N 2-[3-[1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)benzimidazol-5-yl]sulfonylazetidin-1-yl]ethanol Chemical compound C=1C=C2N(CCN(C)C)C(CC(C)(C)C)=NC2=CC=1S(=O)(=O)C1CN(CCO)C1 OAYGNQGEUIFBFA-UHFFFAOYSA-N 0.000 abstract 1
- 239000003556 cannabinoid 2 receptor agonist Substances 0.000 abstract 1
- 238000002844 melting Methods 0.000 abstract 1
- 230000008018 melting Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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Abstract
SAL DE 2-[3-({1-[2-(DIMETILAMINO)ETIL]-2-(2,2-DIMETILPROPIL)-1H1,3-BENZODIAZOL-5-IL}SULFONIL)AZETIDIN-1-IL]ETAN-1-OL COM ÁCIDO, FORMA CRISTALINA, COMPOSIÇÃO FARMACÊUTICA, PROCESSO DE PRODUÇÃO E MÉTODO DE TRATAMENTO E PREVENÇÃO DE DOENÇAS UTILIZANDO O MESMO. Esta invenção refere-se a novos sais e formas de cristal de 2-[3-({1-[2-(dimetilamino)etil]-2-(2,2-dimetilpropil)-1H-1,3-benzodiazol-5-il}sulfonil)azetidin-1-il]etan-1-ol, simplesmente abreviado como Composto A,que é um agonista seletivo do receptor CB2. A presente invenção fornece um sal do Composto A, uma forma de cristal dele, um método para preparar o referido sal e uma composição farmacêutica dele e seu uso. Os sais do Composto A da presente invenção mostram boas propriedades de formulação farmacêutica, tais como alta solubilidade aquosa, boa cristalinidade, alto ponto de fusão, boa estabilidade química e física ou não deliquescente.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
BR122023023137-6A BR122023023137A2 (pt) | 2020-11-12 | 2021-11-11 | Forma cristalina de sal de hcl de 2-[3-({1-[2- (dimetilamino)etil]-2-(2,2- dimetilpropil)-1h-1,3-benzodiazol- 5-il}sulfonil)azetidin-1-il]etan-1-ol com ácido, uso da mesma para fabricação de um medicamento e processo de produção da mesma |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063112893P | 2020-11-12 | 2020-11-12 | |
US63/112,893 | 2020-11-12 | ||
PCT/JP2021/041552 WO2022102713A1 (en) | 2020-11-12 | 2021-11-11 | Stable salt and crystal forms of 2-[3-({1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)-1h-1,3-benzodiazol-5-yl}sulfonyl)azetidin-1-yl]ethan-1-ol |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112023003811A2 true BR112023003811A2 (pt) | 2023-03-28 |
BR112023003811B1 BR112023003811B1 (pt) | 2024-05-21 |
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Also Published As
Publication number | Publication date |
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BR122023023137A2 (pt) | 2024-01-16 |
CN116322672B (zh) | 2024-04-09 |
IL301333B1 (en) | 2024-09-01 |
US20230322737A1 (en) | 2023-10-12 |
US11964963B2 (en) | 2024-04-23 |
AU2021380315B2 (en) | 2023-04-13 |
KR102660003B1 (ko) | 2024-04-22 |
NZ797451A (en) | 2024-07-05 |
EP4244220A1 (en) | 2023-09-20 |
CN116322672A (zh) | 2023-06-23 |
CN118561820A (zh) | 2024-08-30 |
MX2023005430A (es) | 2023-11-14 |
CA3196706A1 (en) | 2022-05-19 |
CA3196706C (en) | 2024-06-25 |
WO2022102713A1 (en) | 2022-05-19 |
JP7427309B2 (ja) | 2024-02-05 |
KR20230093297A (ko) | 2023-06-27 |
EP4244220A4 (en) | 2024-10-23 |
IL301333A (en) | 2023-05-01 |
KR20240052885A (ko) | 2024-04-23 |
CA3238129A1 (en) | 2022-05-19 |
AU2021380315A1 (en) | 2023-03-23 |
JP2023544218A (ja) | 2023-10-20 |
US20240352004A1 (en) | 2024-10-24 |
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