BR112022001002A2 - Solvato de dmf, forma a, forma c, processos para a preparação do solvato de dmf, para a preparação da forma a de relugolix anidra, para a preparação da forma b de relugolix anidra e para a preparação da forma c de relugolix anidra, composição farmacêutica, e, método de tratamento de doença - Google Patents
Solvato de dmf, forma a, forma c, processos para a preparação do solvato de dmf, para a preparação da forma a de relugolix anidra, para a preparação da forma b de relugolix anidra e para a preparação da forma c de relugolix anidra, composição farmacêutica, e, método de tratamento de doençaInfo
- Publication number
- BR112022001002A2 BR112022001002A2 BR112022001002A BR112022001002A BR112022001002A2 BR 112022001002 A2 BR112022001002 A2 BR 112022001002A2 BR 112022001002 A BR112022001002 A BR 112022001002A BR 112022001002 A BR112022001002 A BR 112022001002A BR 112022001002 A2 BR112022001002 A2 BR 112022001002A2
- Authority
- BR
- Brazil
- Prior art keywords
- relugolix
- preparing
- anhydrous
- dmf solvate
- anhydrous form
- Prior art date
Links
- AOMXMOCNKJTRQP-UHFFFAOYSA-N 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea Chemical compound C1=CC(NC(=O)NOC)=CC=C1C1=C(CN(C)C)C(C(=O)N(C=2N=NC(OC)=CC=2)C(=O)N2CC=3C(=CC=CC=3F)F)=C2S1 AOMXMOCNKJTRQP-UHFFFAOYSA-N 0.000 title abstract 16
- 229950004238 relugolix Drugs 0.000 title abstract 12
- 239000012453 solvate Substances 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 6
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000007787 solid Substances 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/03—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to hydrogen atoms
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962882297P | 2019-08-02 | 2019-08-02 | |
| PCT/US2020/044553 WO2021026011A1 (en) | 2019-08-02 | 2020-07-31 | Solid-state forms of relugolix |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022001002A2 true BR112022001002A2 (pt) | 2022-04-12 |
Family
ID=72145496
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022001002A BR112022001002A2 (pt) | 2019-08-02 | 2020-07-31 | Solvato de dmf, forma a, forma c, processos para a preparação do solvato de dmf, para a preparação da forma a de relugolix anidra, para a preparação da forma b de relugolix anidra e para a preparação da forma c de relugolix anidra, composição farmacêutica, e, método de tratamento de doença |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20230374030A1 (https=) |
| EP (1) | EP4007760A1 (https=) |
| JP (1) | JP2022542159A (https=) |
| KR (1) | KR20220047972A (https=) |
| CN (1) | CN114174302A (https=) |
| BR (1) | BR112022001002A2 (https=) |
| CA (1) | CA3145993A1 (https=) |
| WO (1) | WO2021026011A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12441738B2 (en) | 2018-03-14 | 2025-10-14 | Assia Chemical Industries Ltd. | Solid state forms of Relugolix |
| WO2021031148A1 (zh) * | 2019-08-21 | 2021-02-25 | 深圳仁泰医药科技有限公司 | 促性腺素释放激素拮抗剂的晶型及其制备方法和用途 |
| JP2022551316A (ja) | 2019-10-10 | 2022-12-08 | ミオバント サイエンシズ ゲーエムベーハー | Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶形 |
| CN113620972A (zh) * | 2021-02-02 | 2021-11-09 | 奥锐特药业(天津)有限公司 | 瑞卢戈利新晶型及其制备方法 |
| CN114031626A (zh) * | 2021-12-09 | 2022-02-11 | 成都科圣原医药科技有限公司 | 一种瑞卢戈利的合成方法 |
| WO2025037218A1 (en) * | 2023-08-11 | 2025-02-20 | Glenmark Life Sciences Limited | Crystalline solvate of relugolix and a process for its preparation |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7300935B2 (en) * | 2003-01-29 | 2007-11-27 | Takeda Pharmaceutical Company | Thienopyrimidine compounds and use thereof |
| WO2010026993A1 (ja) | 2008-09-03 | 2010-03-11 | 武田薬品工業株式会社 | 製剤における吸収性改善方法および吸収性が改善された製剤 |
| AR092707A1 (es) * | 2012-09-28 | 2015-04-29 | Takeda Pharmaceuticals Co | Metodo de produccion de derivado de tienopirimidina |
| TWI744224B (zh) | 2015-02-26 | 2021-11-01 | 日商武田藥品工業股份有限公司 | 固形製劑 |
| US11306104B2 (en) * | 2018-03-14 | 2022-04-19 | Teva Pharmaceuticals International Gmbh | Solid state forms of Relugolix |
| EP3666776A1 (en) * | 2018-12-11 | 2020-06-17 | Sandoz AG | Hydrate of a gonadotropin-releasing hormone receptor antagonist |
-
2020
- 2020-07-31 CN CN202080054641.9A patent/CN114174302A/zh active Pending
- 2020-07-31 WO PCT/US2020/044553 patent/WO2021026011A1/en not_active Ceased
- 2020-07-31 US US17/597,998 patent/US20230374030A1/en not_active Abandoned
- 2020-07-31 KR KR1020227003478A patent/KR20220047972A/ko active Pending
- 2020-07-31 JP JP2022505338A patent/JP2022542159A/ja active Pending
- 2020-07-31 EP EP20758031.7A patent/EP4007760A1/en not_active Withdrawn
- 2020-07-31 BR BR112022001002A patent/BR112022001002A2/pt not_active Application Discontinuation
- 2020-07-31 CA CA3145993A patent/CA3145993A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20220047972A (ko) | 2022-04-19 |
| EP4007760A1 (en) | 2022-06-08 |
| CA3145993A1 (en) | 2021-02-11 |
| WO2021026011A1 (en) | 2021-02-11 |
| US20230374030A1 (en) | 2023-11-23 |
| JP2022542159A (ja) | 2022-09-29 |
| CN114174302A (zh) | 2022-03-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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] |