SG11201909615YA - Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same - Google Patents
Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the sameInfo
- Publication number
- SG11201909615YA SG11201909615YA SG11201909615YA SG11201909615YA SG 11201909615Y A SG11201909615Y A SG 11201909615YA SG 11201909615Y A SG11201909615Y A SG 11201909615YA SG 11201909615Y A SG11201909615Y A SG 11201909615YA
- Authority
- SG
- Singapore
- Prior art keywords
- gyeonggi
- gil
- international
- preparing
- crystalline form
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 4
- 150000003927 aminopyridines Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 title abstract 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 230000036642 wellbeing Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/02—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
- C07C303/22—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids, by reactions not involving the formation of sulfo or halosulfonyl groups; from sulfonic halides by reactions not involving the formation of halosulfonyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
-
- 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
Abstract
O O (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 25 October 2018 (25.10.2018) WIP0 I PCT oimitia °nolo Oil mum iflo oimIE (10) International Publication Number WO 2018/194356 Al (51) International Patent Classification: CO7D 413/14 (2006.01) A61K 31/5377 (2006.01) (21) International Application Number: PCT/KR2018/004473 (22) International Filing Date: 18 April 2018 (18.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 10-2017-0051687 21 April 2017 (21.04.2017) KR (71) Applicant: YUHAN CORPORATION [KR/KR]; 74, No- ryangjin-ro, Dongjak-gu, Seoul 06927 (KR). (72) Inventors: OH, Sang Ho; 967-2004, 6, Gosan-ro 539beon- gil, Gunpo-si, Gyeonggi-do 15821 (KR). KIM, Jong Gyun; 102-1302, 44, Podowon-ro 27beon-gil, Don- gan-gu, Anyang-si, Gyeonggi-do 14128 (KR). OH, Se- Woong; 120-1201, 85, Hwasan-ro, Jangan-gu, Suwon-si, Gyeonggi-do 16420 (KR). HAN, Tae Dong; 103-1601, 1842, Yonggu-daero, Giheung-gu, Yongin-si, Gyeonggi-do 17080 (KR). CHUNG, Soo Yong; 1401-1003, 19, Dong- tandaerosibeom-gil, Hwaseong-si, Gyeonggi-do 18477 (KR). LEE, Seong Ran; 326-902, 132, Cheongmyeong- ro, Yeongtong-gu, Suwon-si, Gyeonggi-do 16707 (KR). KIM, Kyeong Bae; 410-404, 45, Jagok-ro 3-gil, Gang- nam-gu, Seoul 06374 (KR). LEE, Young Sung; 103-603, 107, Seoun-ro, Seocho-gu, Seoul 06624 (KR). SHIN, Woo Seob; 542-802, 12, Maeyeong-ro 310beon-gil, Yeong- tong-gu, Suwon-si, Gyeonggi-do 16697 (KR). JU, Hyun; 403-802, 55, Dongtansunhwan-daero 26-gil, Hwaseong-si, Gyeonggi-do 18466 (KR). KANG, Jeong Ki; 8409-202, 46-23, Wellbeing town-ro 36beon-gil, Yeongtong-gu, Su- won-si, Gyeonggi-do 16223 (KR). PARK, Su Min; 108-401, 64, Gagyeong-ro, Heungdeok-gu, Cheongju-si, Chungcheongbuk-do 28408 (KR). KIM, Dong Kyun; 402-ho, 51-16, Sangbong-gil, Bongdam-eup, Hwaseong-si, Gyeonggi-do 18316 (KR). (74) Agent: FIRSTLAW P.C.; 60 Mabang-Ro, Seocho-Ku, Seoul 06775 (KR). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (54) Title: SALT OF AN AMINOPYRIDINE DERIVATIVE COMPOUND, A CRYSTALLINE FORM THEREOF, AND A PRO- CESS FOR PREPARING THE SAME O 9000 8000 7000 6000 5000 4000 :3000 2000 1000 - c7.1 II 2-Theta-Scale (57) : The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyra- zol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenypacrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phe ny1-1H-pyrazol-1-y1)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same. [Continued on next page] WO 2018/194356 Al MIDEDIMOMOIDEIREEMOMOHMOIMIOMMOIMMIS PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3))
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20170051687 | 2017-04-21 | ||
| PCT/KR2018/004473 WO2018194356A1 (en) | 2017-04-21 | 2018-04-18 | Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201909615YA true SG11201909615YA (en) | 2019-11-28 |
Family
ID=63857137
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201909615Y SG11201909615YA (en) | 2017-04-21 | 2018-04-18 | Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US11453656B2 (en) |
| EP (1) | EP3612529A4 (en) |
| JP (2) | JP7126514B2 (en) |
| KR (2) | KR102629654B1 (en) |
| CN (1) | CN110869367B (en) |
| AR (1) | AR111469A1 (en) |
| AU (2) | AU2018256227B2 (en) |
| BR (1) | BR112019021868A2 (en) |
| CA (1) | CA3059543A1 (en) |
| CO (1) | CO2019011578A2 (en) |
| EA (1) | EA201992501A1 (en) |
| IL (2) | IL270018B (en) |
| MA (1) | MA49696A (en) |
| MX (1) | MX2022006357A (en) |
| NZ (1) | NZ758443A (en) |
| PH (1) | PH12019502370A1 (en) |
| SA (1) | SA519410342B1 (en) |
| SG (1) | SG11201909615YA (en) |
| TW (1) | TWI776882B (en) |
| UA (1) | UA124364C2 (en) |
| WO (1) | WO2018194356A1 (en) |
| ZA (1) | ZA201907687B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR111469A1 (en) | 2017-04-21 | 2019-07-17 | Yuhan Corp | COME OUT OF AN AMINOPIRIDINE DERIVATIVE COMPOUND, A CRYSTAL FORM OF THE SAME, AND A PROCESS TO PREPARE THE SAME |
| KR20200043618A (en) * | 2018-10-18 | 2020-04-28 | 주식회사유한양행 | Pharmaceutical composition for oral administration comprising an aminopyrimidine derivative or its salt |
| CN111349084B (en) * | 2018-12-21 | 2022-11-25 | 深圳市塔吉瑞生物医药有限公司 | Aminopyrimidines useful for inhibiting protein kinase activity |
| JP2022521610A (en) | 2019-02-26 | 2022-04-11 | ヤンセン バイオテツク，インコーポレーテツド | Combination therapy with bispecific anti-EGFR / C-MET antibody and patient stratification |
| US11879013B2 (en) | 2019-05-14 | 2024-01-23 | Janssen Biotech, Inc. | Combination therapies with bispecific anti-EGFR/c-Met antibodies and third generation EGFR tyrosine kinase inhibitors |
| US11850248B2 (en) * | 2019-05-14 | 2023-12-26 | Yuhan Corporation | Therapies with 3rd generation EGFR tyrosine kinase inhibitors |
| EA202193117A1 (en) * | 2019-05-14 | 2022-02-11 | Янссен Байотек, Инк. | COMBINATION THERAPIES USING BISPECIFIC EGFR/c-MET ANTIBODIES AND 3rd GENERATION EGFR TYROSINE KINASE INHIBITORS |
| TW202207940A (en) | 2020-04-14 | 2022-03-01 | 美商健生生物科技公司 | Pharmaceutical composition for oral administration comprising aminopyrimidine derivative or pharmaceutically acceptable salt, hydrate, or solvate thereof |
| EP4349835A1 (en) | 2021-06-01 | 2024-04-10 | Hangzhou Solipharma Co., Ltd. | Hydrate crystal form of lazertinib methanesulfonate, preparation method therefor and use thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS54033B1 (en) | 2003-12-25 | 2015-10-30 | Eisai R&D Management Co. Ltd. | Crystal of salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)amino-phenoxy)-7-methoxy-6-quinolinecarboxamide or of solvate thereof and processes for producing these |
| PL1720853T3 (en) | 2004-02-11 | 2016-06-30 | Natco Pharma Ltd | Novel polymorphic form of imatinib mesylate and a process for its preparation |
| JP2011526299A (en) * | 2008-06-27 | 2011-10-06 | アビラ セラピューティクス， インコーポレイテッド | Heteroaryl compounds and their use |
| CZ2009570A3 (en) | 2009-08-26 | 2011-03-09 | Zentiva, K. S. | Preparation, stabilization and use of imatinib mesylate polymorphs for development of medicinal forms |
| MX2012005332A (en) * | 2009-11-13 | 2012-10-15 | Oscotec Inc | Kinase inhibitors. |
| US9006448B2 (en) * | 2010-12-06 | 2015-04-14 | Msn Laboratories Private Limited | Process for the preparation of benzimidazole derivatives and its salts |
| CN104109161B (en) * | 2011-07-27 | 2016-08-17 | 阿斯利康(瑞典)有限公司 | 2-(2,4,5-substituted aniline) pyrimidine derivatives is used for treating cancer as EGFR modulator |
| CN104540822B (en) | 2013-07-08 | 2016-08-31 | 杭州普晒医药科技有限公司 | Crystal formation of dabrafenib mesylate and preparation method thereof |
| JP6468611B2 (en) | 2014-05-13 | 2019-02-13 | アリアド ファーマシューティカルズ， インコーポレイテッド | Heteroaryl compounds for kinase inhibition |
| EP3604294B1 (en) | 2014-10-13 | 2021-05-05 | Yuhan Corporation | Compounds and compositions for modulating egfr mutant kinase activities |
| CN104788427B (en) * | 2015-02-05 | 2017-05-31 | 上海泓博智源医药股份有限公司 | 3 (2 pyrimdinyl-amino) phenylacryloyl amine compounds and its application |
| AR111469A1 (en) | 2017-04-21 | 2019-07-17 | Yuhan Corp | COME OUT OF AN AMINOPIRIDINE DERIVATIVE COMPOUND, A CRYSTAL FORM OF THE SAME, AND A PROCESS TO PREPARE THE SAME |
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2018
- 2018-04-13 AR ARP180100945A patent/AR111469A1/en unknown
- 2018-04-18 AU AU2018256227A patent/AU2018256227B2/en active Active
- 2018-04-18 EA EA201992501A patent/EA201992501A1/en unknown
- 2018-04-18 IL IL270018A patent/IL270018B/en unknown
- 2018-04-18 WO PCT/KR2018/004473 patent/WO2018194356A1/en active Application Filing
- 2018-04-18 UA UAA201911263A patent/UA124364C2/en unknown
- 2018-04-18 BR BR112019021868-8A patent/BR112019021868A2/en active Search and Examination
- 2018-04-18 TW TW107113234A patent/TWI776882B/en active
- 2018-04-18 NZ NZ758443A patent/NZ758443A/en unknown
- 2018-04-18 IL IL294666A patent/IL294666B1/en unknown
- 2018-04-18 CA CA3059543A patent/CA3059543A1/en active Pending
- 2018-04-18 KR KR1020180044850A patent/KR102629654B1/en active IP Right Grant
- 2018-04-18 SG SG11201909615Y patent/SG11201909615YA/en unknown
- 2018-04-18 EP EP18787260.1A patent/EP3612529A4/en active Pending
- 2018-04-18 CN CN201880026342.7A patent/CN110869367B/en active Active
- 2018-04-18 US US16/605,944 patent/US11453656B2/en active Active
- 2018-04-18 MA MA049696A patent/MA49696A/en unknown
- 2018-04-18 JP JP2019556610A patent/JP7126514B2/en active Active
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2019
- 2019-10-18 PH PH12019502370A patent/PH12019502370A1/en unknown
- 2019-10-18 CO CONC2019/0011578A patent/CO2019011578A2/en unknown
- 2019-10-20 SA SA519410342A patent/SA519410342B1/en unknown
- 2019-10-21 MX MX2022006357A patent/MX2022006357A/en unknown
- 2019-11-20 ZA ZA2019/07687A patent/ZA201907687B/en unknown
-
2022
- 2022-03-17 US US17/697,655 patent/US20230021395A1/en active Pending
- 2022-05-23 AU AU2022203486A patent/AU2022203486A1/en active Pending
- 2022-08-16 JP JP2022129468A patent/JP7390444B2/en active Active
-
2023
- 2023-12-18 KR KR1020230184208A patent/KR20230175161A/en not_active Application Discontinuation
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