AU2021255488B2 - Crystalline RET inhibitor - Google Patents
Crystalline RET inhibitor Download PDFInfo
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- AU2021255488B2 AU2021255488B2 AU2021255488A AU2021255488A AU2021255488B2 AU 2021255488 B2 AU2021255488 B2 AU 2021255488B2 AU 2021255488 A AU2021255488 A AU 2021255488A AU 2021255488 A AU2021255488 A AU 2021255488A AU 2021255488 B2 AU2021255488 B2 AU 2021255488B2
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- Prior art keywords
- selpercatinib
- acid
- slurry
- cancer
- water
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- 101000579425 Homo sapiens Proto-oncogene tyrosine-protein kinase receptor Ret Proteins 0.000 title claims abstract description 43
- 102100028286 Proto-oncogene tyrosine-protein kinase receptor Ret Human genes 0.000 title claims abstract description 43
- 239000003112 inhibitor Substances 0.000 title description 4
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- 238000000034 method Methods 0.000 claims abstract description 153
- 229940121610 selpercatinib Drugs 0.000 claims abstract description 54
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- 150000001875 compounds Chemical class 0.000 claims description 94
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- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 8
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- 150000008648 triflates Chemical class 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- IARSSOVWSJAVSZ-UHFFFAOYSA-N tris(dimethylamino)sulfanium Chemical compound CN(C)[S+](N(C)C)N(C)C IARSSOVWSJAVSZ-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- 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
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- 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
- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Semiconductor Lasers (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063011701P | 2020-04-17 | 2020-04-17 | |
| US63/011,701 | 2020-04-17 | ||
| US202163151354P | 2021-02-19 | 2021-02-19 | |
| US63/151,354 | 2021-02-19 | ||
| PCT/US2021/026611 WO2021211380A1 (en) | 2020-04-17 | 2021-04-09 | Crystalline ret inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2021255488A1 AU2021255488A1 (en) | 2022-11-10 |
| AU2021255488B2 true AU2021255488B2 (en) | 2024-05-30 |
Family
ID=75747118
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2021255488A Active AU2021255488B2 (en) | 2020-04-17 | 2021-04-09 | Crystalline RET inhibitor |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP4136090A1 (es) |
| JP (1) | JP2023522012A (es) |
| KR (1) | KR20230002706A (es) |
| CN (1) | CN115916791A (es) |
| AU (1) | AU2021255488B2 (es) |
| BR (1) | BR112022020446A2 (es) |
| CA (1) | CA3174316A1 (es) |
| CL (1) | CL2022002849A1 (es) |
| CO (1) | CO2022014882A2 (es) |
| CR (1) | CR20220520A (es) |
| DO (1) | DOP2022000221A (es) |
| EC (1) | ECSP22080982A (es) |
| IL (1) | IL297212A (es) |
| MX (1) | MX2022012952A (es) |
| PE (1) | PE20230388A1 (es) |
| TW (1) | TW202202501A (es) |
| WO (1) | WO2021211380A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022069357A1 (en) * | 2020-10-01 | 2022-04-07 | Sandoz Ag | Crystalline form of selpercatinib |
| US20230183266A1 (en) | 2021-12-13 | 2023-06-15 | Loxo Oncology, Inc. | Crystalline forms of ret inhibitor and preparation thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI704148B (zh) * | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI812649B (zh) * | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI783057B (zh) * | 2017-10-10 | 2022-11-11 | 美商絡速藥業公司 | 製備6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈的方法 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| CN114380825B (zh) * | 2018-09-30 | 2024-02-13 | 北京志健金瑞生物医药科技有限公司 | 取代吡唑稠环类衍生物及其制备方法和应用 |
| CN111004257B (zh) * | 2019-12-24 | 2021-06-29 | 武汉九州钰民医药科技有限公司 | 制备RET抑制剂Selpercatinib的方法 |
-
2021
- 2021-04-07 TW TW110112512A patent/TW202202501A/zh unknown
- 2021-04-09 KR KR1020227039684A patent/KR20230002706A/ko active Search and Examination
- 2021-04-09 AU AU2021255488A patent/AU2021255488B2/en active Active
- 2021-04-09 MX MX2022012952A patent/MX2022012952A/es unknown
- 2021-04-09 PE PE2022002417A patent/PE20230388A1/es unknown
- 2021-04-09 JP JP2022562612A patent/JP2023522012A/ja active Pending
- 2021-04-09 CN CN202180043101.5A patent/CN115916791A/zh active Pending
- 2021-04-09 IL IL297212A patent/IL297212A/en unknown
- 2021-04-09 EP EP21722702.4A patent/EP4136090A1/en active Pending
- 2021-04-09 WO PCT/US2021/026611 patent/WO2021211380A1/en active Application Filing
- 2021-04-09 CA CA3174316A patent/CA3174316A1/en active Pending
- 2021-04-09 CR CR20220520A patent/CR20220520A/es unknown
- 2021-04-09 BR BR112022020446A patent/BR112022020446A2/pt unknown
-
2022
- 2022-10-14 CL CL2022002849A patent/CL2022002849A1/es unknown
- 2022-10-17 DO DO2022000221A patent/DOP2022000221A/es unknown
- 2022-10-17 EC ECSENADI202280982A patent/ECSP22080982A/es unknown
- 2022-10-19 CO CONC2022/0014882A patent/CO2022014882A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20230388A1 (es) | 2023-03-06 |
| EP4136090A1 (en) | 2023-02-22 |
| CL2022002849A1 (es) | 2023-06-16 |
| CN115916791A (zh) | 2023-04-04 |
| ECSP22080982A (es) | 2023-01-31 |
| IL297212A (en) | 2022-12-01 |
| KR20230002706A (ko) | 2023-01-05 |
| MX2022012952A (es) | 2023-01-11 |
| CA3174316A1 (en) | 2021-10-21 |
| DOP2022000221A (es) | 2023-01-15 |
| JP2023522012A (ja) | 2023-05-26 |
| TW202202501A (zh) | 2022-01-16 |
| BR112022020446A2 (pt) | 2022-11-29 |
| AU2021255488A1 (en) | 2022-11-10 |
| CO2022014882A2 (es) | 2022-10-31 |
| CR20220520A (es) | 2022-11-15 |
| WO2021211380A1 (en) | 2021-10-21 |
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