JPWO2020247643A5 - - Google Patents
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- Publication number
- JPWO2020247643A5 JPWO2020247643A5 JP2021571896A JP2021571896A JPWO2020247643A5 JP WO2020247643 A5 JPWO2020247643 A5 JP WO2020247643A5 JP 2021571896 A JP2021571896 A JP 2021571896A JP 2021571896 A JP2021571896 A JP 2021571896A JP WO2020247643 A5 JPWO2020247643 A5 JP WO2020247643A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- crystalline form
- acceptable salt
- compound
- ray powder
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000003839 salts Chemical class 0.000 claims 20
- 229940125904 compound 1 Drugs 0.000 claims 18
- 238000000634 powder X-ray diffraction Methods 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 239000003937 drug carrier Substances 0.000 claims 9
- -1 2-amino-3-chloropyridin-4-yl Chemical group 0.000 claims 4
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010029748 Noonan syndrome Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims 1
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims 1
- HISJAYUQVHMWTA-BLLLJJGKSA-N [6-(2-amino-3-chloropyridin-4-yl)sulfanyl-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl]methanol Chemical group NC1=NC=CC(=C1Cl)SC1=C(N=C(C(=N1)CO)N1CCC2([C@@H]([C@@H](OC2)C)N)CC1)C HISJAYUQVHMWTA-BLLLJJGKSA-N 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025101917A JP2025138706A (ja) | 2019-06-07 | 2025-06-18 | Shp2阻害物質である{6-[(2-アミノ-3-クロロピリジン-4-イル)スルファニル]-3-[(3s,4s)-4-アミノ-3-メチル-2-オキサ-8-アザスピロ[4.5]デカン-8-イル]-5-メチルピラジン-2-イル}メタノールの固体形態 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962858837P | 2019-06-07 | 2019-06-07 | |
| US62/858,837 | 2019-06-07 | ||
| PCT/US2020/036137 WO2020247643A1 (en) | 2019-06-07 | 2020-06-04 | Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025101917A Division JP2025138706A (ja) | 2019-06-07 | 2025-06-18 | Shp2阻害物質である{6-[(2-アミノ-3-クロロピリジン-4-イル)スルファニル]-3-[(3s,4s)-4-アミノ-3-メチル-2-オキサ-8-アザスピロ[4.5]デカン-8-イル]-5-メチルピラジン-2-イル}メタノールの固体形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022534788A JP2022534788A (ja) | 2022-08-03 |
| JP2022534788A5 JP2022534788A5 (https=) | 2023-06-07 |
| JPWO2020247643A5 true JPWO2020247643A5 (https=) | 2023-06-07 |
Family
ID=71787182
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021571896A Pending JP2022534788A (ja) | 2019-06-07 | 2020-06-04 | Shp2阻害物質である{6-[(2-アミノ-3-クロロピリジン-4-イル)スルファニル]-3-[(3s,4s)-4-アミノ-3-メチル-2-オキサ-8-アザスピロ[4.5]デカン-8-イル]-5-メチルピラジン-2-イル}メタノールの固体形態 |
| JP2025101917A Pending JP2025138706A (ja) | 2019-06-07 | 2025-06-18 | Shp2阻害物質である{6-[(2-アミノ-3-クロロピリジン-4-イル)スルファニル]-3-[(3s,4s)-4-アミノ-3-メチル-2-オキサ-8-アザスピロ[4.5]デカン-8-イル]-5-メチルピラジン-2-イル}メタノールの固体形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025101917A Pending JP2025138706A (ja) | 2019-06-07 | 2025-06-18 | Shp2阻害物質である{6-[(2-アミノ-3-クロロピリジン-4-イル)スルファニル]-3-[(3s,4s)-4-アミノ-3-メチル-2-オキサ-8-アザスピロ[4.5]デカン-8-イル]-5-メチルピラジン-2-イル}メタノールの固体形態 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11220501B2 (https=) |
| EP (1) | EP3980128A1 (https=) |
| JP (2) | JP2022534788A (https=) |
| KR (1) | KR20220019017A (https=) |
| CN (2) | CN115141205A (https=) |
| AU (1) | AU2020288631A1 (https=) |
| BR (1) | BR112021022635A2 (https=) |
| CA (1) | CA3142430A1 (https=) |
| IL (1) | IL288568A (https=) |
| MA (1) | MA56113A (https=) |
| MX (1) | MX2021014855A (https=) |
| PH (1) | PH12021552902A1 (https=) |
| SG (1) | SG11202112461QA (https=) |
| TW (1) | TW202112785A (https=) |
| WO (1) | WO2020247643A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3074690A1 (en) | 2017-09-07 | 2019-03-14 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
| EP3980128A1 (en) | 2019-06-07 | 2022-04-13 | Revolution Medicines, Inc. | Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途 |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| CA2606288A1 (en) * | 2005-04-18 | 2006-10-26 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
| KR101906146B1 (ko) * | 2009-08-17 | 2018-10-10 | 메모리얼 슬로안-케터링 캔서 센터 | 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법 |
| JO3517B1 (ar) * | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| JP6523303B2 (ja) * | 2014-01-17 | 2019-05-29 | ノバルティス アーゲー | Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物 |
| KR102598895B1 (ko) * | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| CA3074690A1 (en) | 2017-09-07 | 2019-03-14 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
| SG11202009793TA (en) | 2018-04-10 | 2020-10-29 | Revolution Medicines Inc | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
| EP3980128A1 (en) * | 2019-06-07 | 2022-04-13 | Revolution Medicines, Inc. | Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor |
-
2020
- 2020-06-04 EP EP20746488.4A patent/EP3980128A1/en active Pending
- 2020-06-04 CN CN202210564150.XA patent/CN115141205A/zh active Pending
- 2020-06-04 AU AU2020288631A patent/AU2020288631A1/en not_active Abandoned
- 2020-06-04 MX MX2021014855A patent/MX2021014855A/es unknown
- 2020-06-04 CA CA3142430A patent/CA3142430A1/en active Pending
- 2020-06-04 MA MA056113A patent/MA56113A/fr unknown
- 2020-06-04 JP JP2021571896A patent/JP2022534788A/ja active Pending
- 2020-06-04 BR BR112021022635A patent/BR112021022635A2/pt not_active IP Right Cessation
- 2020-06-04 CN CN202080054905.0A patent/CN114190090A/zh active Pending
- 2020-06-04 TW TW109118750A patent/TW202112785A/zh unknown
- 2020-06-04 SG SG11202112461QA patent/SG11202112461QA/en unknown
- 2020-06-04 WO PCT/US2020/036137 patent/WO2020247643A1/en not_active Ceased
- 2020-06-04 KR KR1020227000184A patent/KR20220019017A/ko not_active Ceased
- 2020-06-04 PH PH1/2021/552902A patent/PH12021552902A1/en unknown
-
2021
- 2021-02-26 US US17/187,504 patent/US11220501B2/en active Active
- 2021-11-29 US US17/537,113 patent/US12528807B2/en active Active
- 2021-12-01 IL IL288568A patent/IL288568A/en unknown
-
2025
- 2025-06-18 JP JP2025101917A patent/JP2025138706A/ja active Pending
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