SG11201806966SA - Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3- fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n- methylmethanamine salt - Google Patents
Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3- fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n- methylmethanamine saltInfo
- Publication number
- SG11201806966SA SG11201806966SA SG11201806966SA SG11201806966SA SG11201806966SA SG 11201806966S A SG11201806966S A SG 11201806966SA SG 11201806966S A SG11201806966S A SG 11201806966SA SG 11201806966S A SG11201806966S A SG 11201806966SA SG 11201806966S A SG11201806966S A SG 11201806966SA
- Authority
- SG
- Singapore
- Prior art keywords
- crystalline form
- international
- pyrrol
- difluorophenyl
- fluorophenyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
- C07D207/48—Sulfur atoms
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
WO 17 / 16 457 6 A8 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 11111111111111111111111111111111111 0M 011 100 IIHOO #10# (10) International Publication Number WO 2017/164576 A8 28 September 2017 (28.09.2017) WI PO I PCT (51) International Patent Classification: C07D 207/48 (2006.01) A61K 31/40 (2006.01) (21) International Application Number: PCT/KR2017/002914 (22) International Filing Date: 17 March 2017 (17.03.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 10-2016-0036080 25 March 2016 (25.03.2016) KR (71) Applicant: DAEWOONG PHARMACEUTICAL CO., LTD. [KR/KR]; 35-14, Jeyakgongdan 4-gil, Hyang- nam-eup, Hwaseong-si, Gyenoggi-do 18623 (KR). (72) Inventors: KIM, Aeri; 109-1701, 154, Yeongjung-ro, Yeongdeungpo-gu, Seoul, 07226 (KR). CHO, Kwan Hyung; 111-1902, 156, Hwamyeongsindosi-ro, Buk-gu, Busan, 46525 (KR). (74) Agent: YOU ME PATENT AND LAW FIRM; 115 Teheran-ro, Gangnam-gu, Seoul 06134 (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, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, (54) Title: NOVEL CRYSTALLINE FORM OF 1-(5-(2,4-DIFLUOROPHENYL)-1-((3- FLUOROPHENYL)SULFONYL)-4- METHOXY-1H-PYRROL-3-YL)-N- METHYLMETHANAMINE SALT FIG. 1 2-Theta (57) : The present invention provides a novel crystalline form I of hydrochloride, a crystalline form II of hydrochloride, a crystalline form of succinate, a crystalline form of tartrate, a crystalline form I of fumarate and a crystalline form II of fumarate of 1-(5- (2,4- difluorophenyl)- 1 ((3-fluorophenyl)sulfony1)-4-methoxy-1H-pyrrol-3-y1)-N- methylmetlianamine. The above-described novel crystalline forms have high solubility in water and excellent stability under moisture-proof conditions and high-humidity exposure conditions, and thus can be pharmaceutically used. [Continued on next page] WO 2017/164576 A8 MIDEDIMOMOIDEIROIDEMOMMINIVINEROMEME# 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)) (48) Date of publication of this corrected version: 09 August 2018 (09.08.2018) (15) Information about Correction: see Notice of 09 August 2018 (09.08.2018)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020160036080A KR102081920B1 (en) | 2016-03-25 | 2016-03-25 | Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n-methylmethanamine salt |
| PCT/KR2017/002914 WO2017164576A1 (en) | 2016-03-25 | 2017-03-17 | Novel crystalline form of 1-(5-(2,4-difluorophenyl)-l-((3- fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n- methylmethanamine salt |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201806966SA true SG11201806966SA (en) | 2018-09-27 |
Family
ID=59900401
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201806966SA SG11201806966SA (en) | 2016-03-25 | 2017-03-17 | Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3- fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n- methylmethanamine salt |
Country Status (32)
| Country | Link |
|---|---|
| US (6) | US10336695B2 (en) |
| EP (1) | EP3433233B1 (en) |
| JP (1) | JP6554617B2 (en) |
| KR (1) | KR102081920B1 (en) |
| CN (1) | CN108602772B (en) |
| AR (1) | AR107963A1 (en) |
| AU (1) | AU2017238918B2 (en) |
| BR (1) | BR112018069461A2 (en) |
| CA (1) | CA3014745C (en) |
| CL (3) | CL2018002416A1 (en) |
| CO (1) | CO2018008833A2 (en) |
| DO (1) | DOP2018000190A (en) |
| EA (1) | EA029995B1 (en) |
| ES (1) | ES2818902T3 (en) |
| HK (1) | HK1254393A1 (en) |
| HR (1) | HRP20201594T1 (en) |
| HU (1) | HUE053502T2 (en) |
| JO (1) | JOP20170070B1 (en) |
| MA (1) | MA43833B1 (en) |
| MX (1) | MX2018009219A (en) |
| MY (1) | MY196299A (en) |
| NZ (1) | NZ745266A (en) |
| PE (1) | PE20190170A1 (en) |
| PH (1) | PH12018501846B1 (en) |
| PL (1) | PL3433233T3 (en) |
| PT (1) | PT3433233T (en) |
| RS (1) | RS60884B1 (en) |
| SG (1) | SG11201806966SA (en) |
| SI (1) | SI3433233T1 (en) |
| TN (1) | TN2018000288A1 (en) |
| TW (1) | TWI626234B (en) |
| WO (1) | WO2017164576A1 (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102081920B1 (en) * | 2016-03-25 | 2020-02-26 | 주식회사 대웅제약 | Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n-methylmethanamine salt |
| KR102233456B1 (en) | 2017-05-31 | 2021-03-29 | 주식회사 대웅제약 | Method for preparation of intermediate of 4-methoxypyrrole derivative |
| KR102233455B1 (en) * | 2017-06-21 | 2021-03-29 | 주식회사 대웅제약 | Method for preparation of intermediate of 4-methoxypyrrole derivative |
| KR102126576B1 (en) * | 2018-09-19 | 2020-06-24 | 주식회사 대웅제약 | Manufacturing method for 4-methoxypyrrole derivatives |
| AU2020409932B2 (en) * | 2019-12-18 | 2023-09-07 | Daewoong Pharmaceutical Co., Ltd. | Liquid pharmaceutical composition of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrole-3-yl)-N-methylmethaneamine |
| CN117820193A (en) * | 2022-09-29 | 2024-04-05 | 安徽皓元药业有限公司 | non-Su Lazan hydrochloride crystal form A and preparation method thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2336107B1 (en) | 2004-09-30 | 2015-09-23 | Takeda Pharmaceutical Company Limited | Proton pump inhibitors |
| PL1919865T3 (en) | 2005-08-30 | 2011-09-30 | Takeda Pharmaceuticals Co | 1-heterocyclylsulfonyl, 2-aminomethyl, 5- (hetero-) aryl substituted 1-h-pyrrole derivatives as acid secretion inhibitors |
| WO2007114338A1 (en) * | 2006-03-31 | 2007-10-11 | Takeda Pharmaceutical Company Limited | Acid secretion inhibitor |
| WO2008036211A1 (en) * | 2006-09-19 | 2008-03-27 | Alevium Pharmaceuticals, Inc. | Prodrugs of proton pump inhibitors including the (1h-pyrrol-1-yl)-1h-benzimidazole moiety |
| US8933105B2 (en) * | 2007-02-28 | 2015-01-13 | Takeda Pharmaceutical Company Limited | Pyrrole compounds |
| CN104718189B (en) * | 2012-11-19 | 2017-03-15 | 江苏豪森药业集团有限公司 | Pyrroles's sulphonyl analog derivative, its preparation method and its in application pharmaceutically |
| KR102084185B1 (en) * | 2013-08-29 | 2020-03-04 | 주식회사 대웅제약 | Tetrahydrocyclopentapyrrole derivatives and method for preparation thereof |
| CN104447490B (en) * | 2014-11-19 | 2017-06-06 | 连云港恒运医药有限公司 | A kind of crystal formation of proton pump inhibitor, prepare intermediate and its synthetic method and medical usage |
| CN104447491B (en) * | 2014-11-19 | 2017-06-23 | 连云港恒运医药有限公司 | Hemifumarate and its intermediate and medical usage containing pyrrole ring proton pump inhibitor |
| KR101613245B1 (en) * | 2015-04-27 | 2016-04-18 | 주식회사 대웅제약 | Novel 4-methoxy pyrrole derivatives or salts thereof and pharmaceutical composition comprising the same |
| KR20170113040A (en) | 2016-03-25 | 2017-10-12 | 주식회사 대웅제약 | Novel acid addition salt of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n-methylmethanamine |
| KR102081920B1 (en) | 2016-03-25 | 2020-02-26 | 주식회사 대웅제약 | Novel crystalline form of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1h-pyrrol-3-yl)-n-methylmethanamine salt |
| KR102233456B1 (en) | 2017-05-31 | 2021-03-29 | 주식회사 대웅제약 | Method for preparation of intermediate of 4-methoxypyrrole derivative |
| KR102233455B1 (en) | 2017-06-21 | 2021-03-29 | 주식회사 대웅제약 | Method for preparation of intermediate of 4-methoxypyrrole derivative |
| KR102126576B1 (en) | 2018-09-19 | 2020-06-24 | 주식회사 대웅제약 | Manufacturing method for 4-methoxypyrrole derivatives |
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2016
- 2016-03-25 KR KR1020160036080A patent/KR102081920B1/en active IP Right Grant
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2017
- 2017-03-17 EP EP17770546.4A patent/EP3433233B1/en active Active
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- 2017-03-17 SI SI201730397T patent/SI3433233T1/en unknown
- 2017-03-17 HU HUE17770546A patent/HUE053502T2/en unknown
- 2017-03-17 MY MYPI2018703342A patent/MY196299A/en unknown
- 2017-03-17 CN CN201780008736.5A patent/CN108602772B/en active Active
- 2017-03-17 TN TNP/2018/000288A patent/TN2018000288A1/en unknown
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- 2017-03-17 NZ NZ745266A patent/NZ745266A/en unknown
- 2017-03-17 US US16/073,359 patent/US10336695B2/en active Active
- 2017-03-17 JP JP2018549562A patent/JP6554617B2/en active Active
- 2017-03-17 ES ES17770546T patent/ES2818902T3/en active Active
- 2017-03-17 PT PT177705464T patent/PT3433233T/en unknown
- 2017-03-17 WO PCT/KR2017/002914 patent/WO2017164576A1/en active Application Filing
- 2017-03-17 SG SG11201806966SA patent/SG11201806966SA/en unknown
- 2017-03-17 BR BR112018069461-4A patent/BR112018069461A2/en not_active Application Discontinuation
- 2017-03-21 TW TW106109339A patent/TWI626234B/en active
- 2017-03-22 JO JOP/2017/0070A patent/JOP20170070B1/en active
- 2017-03-23 EA EA201790454A patent/EA029995B1/en not_active IP Right Cessation
- 2017-03-23 AR ARP170100726A patent/AR107963A1/en unknown
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2018
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- 2018-08-24 CO CONC2018/0008833A patent/CO2018008833A2/en unknown
- 2018-08-30 PH PH12018501846A patent/PH12018501846B1/en unknown
- 2018-08-31 DO DO2018000190A patent/DOP2018000190A/en unknown
- 2018-10-19 HK HK18113470.2A patent/HK1254393A1/en unknown
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2019
- 2019-05-14 US US16/411,270 patent/US10683268B2/en active Active
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2020
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2021
- 2021-01-19 US US17/151,901 patent/US11459297B2/en active Active
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2022
- 2022-07-27 US US17/874,700 patent/US11858894B2/en active Active
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