JP2018503650A5 - - Google Patents
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- Publication number
- JP2018503650A5 JP2018503650A5 JP2017539604A JP2017539604A JP2018503650A5 JP 2018503650 A5 JP2018503650 A5 JP 2018503650A5 JP 2017539604 A JP2017539604 A JP 2017539604A JP 2017539604 A JP2017539604 A JP 2017539604A JP 2018503650 A5 JP2018503650 A5 JP 2018503650A5
- Authority
- JP
- Japan
- Prior art keywords
- item
- subject
- crystalline
- xrpd
- mammal
- 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.)
- Granted
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- 238000000634 powder X-ray diffraction Methods 0.000 claims description 33
- 241000124008 Mammalia Species 0.000 claims description 18
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 17
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 12
- -1 Chloro-2-isopropylaminopyridin-4-yl Chemical group 0.000 claims description 9
- 241000282412 Homo Species 0.000 claims description 6
- 238000004566 IR spectroscopy Methods 0.000 claims description 6
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 6
- 241001465754 Metazoa Species 0.000 claims description 6
- 241000288906 Primates Species 0.000 claims description 6
- 239000002246 antineoplastic agent Substances 0.000 claims description 6
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims description 6
- 238000002329 infrared spectrum Methods 0.000 claims description 6
- 244000144972 livestock Species 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 3
- 238000001228 spectrum Methods 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims 7
- 150000001735 carboxylic acids Chemical class 0.000 claims 2
- WRHZVMBBRYBTKZ-UHFFFAOYSA-N pyrrole-2-carboxylic acid Chemical compound OC(=O)C1=CC=CN1 WRHZVMBBRYBTKZ-UHFFFAOYSA-N 0.000 claims 2
- DOYOPBSXEIZLRE-UHFFFAOYSA-N pyrrole-3-carboxylic acid Natural products OC(=O)C=1C=CNC=1 DOYOPBSXEIZLRE-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 22
- NCBIFXNQFURYON-UHFFFAOYSA-N 4-[5-chloro-2-(propan-2-ylamino)pyridin-4-yl]-1h-pyrrole-2-carboxylic acid Chemical compound C1=NC(NC(C)C)=CC(C=2C=C(NC=2)C(O)=O)=C1Cl NCBIFXNQFURYON-UHFFFAOYSA-N 0.000 description 7
- 239000002253 acid Substances 0.000 description 5
- CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 description 2
- QWRFDTRCUUUHRA-UHFFFAOYSA-N 5-chloro-N-propan-2-yl-4-(1H-pyrrol-3-yl)pyridin-2-amine Chemical compound ClC=1C(=CC(=NC=1)NC(C)C)C=1C=CNC=1 QWRFDTRCUUUHRA-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
- 150000001408 amides Chemical class 0.000 description 1
- 150000002690 malonic acid derivatives Chemical class 0.000 description 1
- KSERXGMCDHOLSS-UHFFFAOYSA-N n-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-chloro-2-(propan-2-ylamino)pyridin-4-yl]-1h-pyrrole-2-carboxamide Chemical compound C1=NC(NC(C)C)=CC(C=2C=C(NC=2)C(=O)NC(CO)C=2C=C(Cl)C=CC=2)=C1Cl KSERXGMCDHOLSS-UHFFFAOYSA-N 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022135858A JP7469820B2 (ja) | 2015-01-30 | 2022-08-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2024056515A JP7701758B2 (ja) | 2015-01-30 | 2024-03-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2025099534A JP2025134802A (ja) | 2015-01-30 | 2025-06-13 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562110446P | 2015-01-30 | 2015-01-30 | |
| US62/110,446 | 2015-01-30 | ||
| PCT/US2016/015843 WO2016123581A1 (en) | 2015-01-30 | 2016-01-29 | Crystalline c21h22c12n4o2 malonate |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020166896A Division JP2021006560A (ja) | 2015-01-30 | 2020-10-01 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2022135858A Division JP7469820B2 (ja) | 2015-01-30 | 2022-08-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018503650A JP2018503650A (ja) | 2018-02-08 |
| JP2018503650A5 true JP2018503650A5 (https=) | 2019-03-14 |
| JP7180977B2 JP7180977B2 (ja) | 2022-11-30 |
Family
ID=56544446
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017539604A Active JP7180977B2 (ja) | 2015-01-30 | 2016-01-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2020166896A Pending JP2021006560A (ja) | 2015-01-30 | 2020-10-01 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2022135858A Active JP7469820B2 (ja) | 2015-01-30 | 2022-08-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2024056515A Active JP7701758B2 (ja) | 2015-01-30 | 2024-03-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2025099534A Pending JP2025134802A (ja) | 2015-01-30 | 2025-06-13 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020166896A Pending JP2021006560A (ja) | 2015-01-30 | 2020-10-01 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2022135858A Active JP7469820B2 (ja) | 2015-01-30 | 2022-08-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2024056515A Active JP7701758B2 (ja) | 2015-01-30 | 2024-03-29 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| JP2025099534A Pending JP2025134802A (ja) | 2015-01-30 | 2025-06-13 | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9670177B2 (https=) |
| EP (1) | EP3250291B1 (https=) |
| JP (5) | JP7180977B2 (https=) |
| CA (3) | CA3276518A1 (https=) |
| ES (1) | ES2830044T3 (https=) |
| WO (1) | WO2016123581A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015095842A2 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers |
| JP7180977B2 (ja) * | 2015-01-30 | 2022-11-30 | バイオメッド バレー ディスカバリーズ，インコーポレイティド | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
| WO2025264278A1 (en) * | 2024-06-18 | 2025-12-26 | Memorial Sloan-Kettering Cancer Center | Erk2 degraders |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4599331A (en) | 1984-12-24 | 1986-07-08 | Syntex (U.S.A.) Inc. | Etianic acids as antiangiogenics |
| JP2545522B2 (ja) | 1985-10-23 | 1996-10-23 | アルコン・ラボラトーリーズ，インコーポレイテッド | テトラヒドロ脈管形成抑制ステロイド |
| US4771042A (en) | 1985-11-25 | 1988-09-13 | The Upjohn Company | Inhibition of angiogenesis involving the coadministration of steroids with heparin or heparin fragments |
| EP0477195A1 (en) | 1989-06-16 | 1992-04-01 | The Upjohn Company | Suramin type compounds and angiostatic steroids to inhibit angiogenesis |
| WO1993010141A2 (en) | 1991-11-22 | 1993-05-27 | Alcon Laboratories, Inc. | Angiostatic steroids |
| US7927613B2 (en) | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
| LT3305776T (lt) | 2004-05-14 | 2020-01-10 | Vertex Pharmaceuticals Incorporated | Pirolo junginiai kaip erk baltymo kinazės inhibitoriai, ir farmacinės kompozicijos su šiais junginiais |
| US7582623B2 (en) | 2004-05-20 | 2009-09-01 | The Regents Of The University Of California | Photoactive metal nitrosyls for blood pressure regulation and cancer therapy |
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| JP7180977B2 (ja) * | 2015-01-30 | 2022-11-30 | バイオメッド バレー ディスカバリーズ，インコーポレイティド | 結晶性Ｃ２１Ｈ２２Ｃｌ２Ｎ４Ｏ２マロン酸塩 |
-
2016
- 2016-01-29 JP JP2017539604A patent/JP7180977B2/ja active Active
- 2016-01-29 CA CA3276518A patent/CA3276518A1/en active Pending
- 2016-01-29 ES ES16744245T patent/ES2830044T3/es active Active
- 2016-01-29 WO PCT/US2016/015843 patent/WO2016123581A1/en not_active Ceased
- 2016-01-29 EP EP16744245.8A patent/EP3250291B1/en active Active
- 2016-01-29 US US15/011,420 patent/US9670177B2/en active Active
- 2016-01-29 CA CA2975116A patent/CA2975116C/en active Active
- 2016-01-29 CA CA3168216A patent/CA3168216C/en active Active
-
2017
- 2017-05-17 US US15/598,160 patent/US9951041B2/en active Active
-
2020
- 2020-10-01 JP JP2020166896A patent/JP2021006560A/ja active Pending
-
2022
- 2022-08-29 JP JP2022135858A patent/JP7469820B2/ja active Active
-
2024
- 2024-03-29 JP JP2024056515A patent/JP7701758B2/ja active Active
-
2025
- 2025-06-13 JP JP2025099534A patent/JP2025134802A/ja active Pending
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