CN107001276A - 一种尿酸转运蛋白抑制剂的钠盐及其结晶形式 - Google Patents
一种尿酸转运蛋白抑制剂的钠盐及其结晶形式 Download PDFInfo
- Publication number
- CN107001276A CN107001276A CN201680003846.8A CN201680003846A CN107001276A CN 107001276 A CN107001276 A CN 107001276A CN 201680003846 A CN201680003846 A CN 201680003846A CN 107001276 A CN107001276 A CN 107001276A
- Authority
- CN
- China
- Prior art keywords
- crystallization
- bromoquinoline
- sulfenyl
- bases
- formula
- 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
Links
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/36—Sulfur atoms
-
- 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
Description
Claims (8)
- 式(I)所示1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠,
- 根据权利要求1所述的式(I)所示1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠的I型结晶,其特征在于使用Cu-Ka辐射,得到以2θ角度和晶面间距表示的X-射线粉末衍射图谱,所述结晶具有如图1所示的X-射线粉末衍射图谱,其中在约9.08(9.73),11.73(7.54),12.19(7.26),15.59(5.68),16.28(5.44),17.73(5.00),18.16(4.88),18.80(4.72),19.48(4.55),20.80(4.27),23.16(3.84),27.54(3.24)和30.37(2.94)附近有特征峰。
- 一种制备根据权利要求1所述的式(I)所示1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠的方法,包括将1-((6-溴喹啉-4-基)硫基)环丁基甲酸和氢氧化钠反应的步骤。
- 一种制备根据权利要求2所述的I型结晶的方法,所述方法包括下述步骤:1)将任意晶型或无定型的1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠固体加热溶解于适量的溶剂中,冷却、析晶,所述溶剂选自碳原子小于等于3的醇类、酮类的任意一种与水的混合溶剂;2)过滤结晶并洗涤,干燥。
- 根据权利要求4所述的方法,其特征在于在步骤1)中所述的溶剂优选为水/异丙醇、水/丙酮、丙酮/水/丙酮、丙酮/水/异丙醇。
- 一种药物组合物,其含有根据权利要求1所述的式(I)所示 1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠或权利要求2所述的I型结晶以及药学上可接受的载体。
- 根据权利要求1所述的式(I)所示1-((6-溴喹啉-4-基)硫基)环丁基甲酸钠、权利要求2所述的I型结晶或权利要求6所述的药物组合物在制备治疗与尿酸转运蛋白(URAT1)有关的疾病的药物中的用途。
- 根据权利要求7所述的用途,其中所述疾病为痛风。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201510280720 | 2015-05-27 | ||
CN2015102807202 | 2015-05-27 | ||
PCT/CN2016/083423 WO2016188444A1 (zh) | 2015-05-27 | 2016-05-26 | 一种尿酸转运蛋白抑制剂的钠盐及其结晶形式 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN107001276A true CN107001276A (zh) | 2017-08-01 |
CN107001276B CN107001276B (zh) | 2020-03-13 |
Family
ID=57393793
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201680003846.8A Active CN107001276B (zh) | 2015-05-27 | 2016-05-26 | 一种尿酸转运蛋白抑制剂的钠盐及其结晶形式 |
Country Status (21)
Country | Link |
---|---|
US (2) | US10196361B2 (zh) |
EP (1) | EP3305768B1 (zh) |
JP (1) | JP6738350B2 (zh) |
KR (1) | KR20180006441A (zh) |
CN (1) | CN107001276B (zh) |
AU (1) | AU2016269359B2 (zh) |
BR (1) | BR112017022505A2 (zh) |
CA (1) | CA2984961C (zh) |
CY (1) | CY1123262T1 (zh) |
DK (1) | DK3305768T3 (zh) |
ES (1) | ES2811325T3 (zh) |
HR (1) | HRP20201178T1 (zh) |
HU (1) | HUE051640T2 (zh) |
LT (1) | LT3305768T (zh) |
MX (1) | MX2017014319A (zh) |
PL (1) | PL3305768T3 (zh) |
PT (1) | PT3305768T (zh) |
RS (1) | RS60749B1 (zh) |
RU (1) | RU2719484C2 (zh) |
SI (1) | SI3305768T1 (zh) |
WO (1) | WO2016188444A1 (zh) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR112017022505A2 (zh) * | 2015-05-27 | 2018-07-17 | Jiangsu Hengrui Medicine Co., Ltd. | A sodium salt of uric acid transporter inhibitor and its crystalline form |
CN108201529B (zh) * | 2016-12-16 | 2021-10-08 | 江苏恒瑞医药股份有限公司 | 一种含有尿酸转运蛋白抑制剂的药物组合物及其制备方法 |
CN110467571B (zh) * | 2018-05-11 | 2021-02-26 | 江苏恒瑞医药股份有限公司 | 一种制备环烷基甲酸类衍生物或其可药用盐的方法 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1820515A1 (en) * | 2004-11-29 | 2007-08-22 | Japan Tobacco, Inc. | Nitrogen-containing fused ring compound and use thereof |
WO2014183555A1 (zh) * | 2013-05-13 | 2014-11-20 | 上海恒瑞医药有限公司 | 环烷基甲酸类衍生物、其制备方法及其在医药上的应用 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SA04250253B1 (ar) * | 2003-08-21 | 2009-11-10 | استرازينيكا ايه بي | احماض فينوكسي اسيتيك مستبدلة باعتبارها مركبات صيدلانية لعلاج الامراض التنفسية مثل الربو ومرض الانسداد الرئوي المزمن |
BR112017022505A2 (zh) * | 2015-05-27 | 2018-07-17 | Jiangsu Hengrui Medicine Co., Ltd. | A sodium salt of uric acid transporter inhibitor and its crystalline form |
-
2016
- 2016-05-26 BR BR112017022505-0A patent/BR112017022505A2/zh not_active Application Discontinuation
- 2016-05-26 WO PCT/CN2016/083423 patent/WO2016188444A1/zh active Application Filing
- 2016-05-26 RS RS20200924A patent/RS60749B1/sr unknown
- 2016-05-26 AU AU2016269359A patent/AU2016269359B2/en active Active
- 2016-05-26 ES ES16799331T patent/ES2811325T3/es active Active
- 2016-05-26 US US15/574,328 patent/US10196361B2/en active Active
- 2016-05-26 CN CN201680003846.8A patent/CN107001276B/zh active Active
- 2016-05-26 CA CA2984961A patent/CA2984961C/en active Active
- 2016-05-26 EP EP16799331.0A patent/EP3305768B1/en active Active
- 2016-05-26 SI SI201630871T patent/SI3305768T1/sl unknown
- 2016-05-26 PL PL16799331T patent/PL3305768T3/pl unknown
- 2016-05-26 JP JP2017555478A patent/JP6738350B2/ja active Active
- 2016-05-26 MX MX2017014319A patent/MX2017014319A/es unknown
- 2016-05-26 HU HUE16799331A patent/HUE051640T2/hu unknown
- 2016-05-26 PT PT167993310T patent/PT3305768T/pt unknown
- 2016-05-26 KR KR1020177035949A patent/KR20180006441A/ko not_active Application Discontinuation
- 2016-05-26 RU RU2017142996A patent/RU2719484C2/ru active
- 2016-05-26 LT LTEP16799331.0T patent/LT3305768T/lt unknown
- 2016-05-26 DK DK16799331.0T patent/DK3305768T3/da active
-
2018
- 2018-10-11 US US16/157,696 patent/US10358424B2/en active Active
-
2020
- 2020-07-28 HR HRP20201178TT patent/HRP20201178T1/hr unknown
- 2020-08-04 CY CY20201100720T patent/CY1123262T1/el unknown
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1820515A1 (en) * | 2004-11-29 | 2007-08-22 | Japan Tobacco, Inc. | Nitrogen-containing fused ring compound and use thereof |
WO2014183555A1 (zh) * | 2013-05-13 | 2014-11-20 | 上海恒瑞医药有限公司 | 环烷基甲酸类衍生物、其制备方法及其在医药上的应用 |
Non-Patent Citations (2)
Title |
---|
张超云、秦亚东主编: "《药剂学》", 31 October 2013, 辽宁大学出版社 * |
苏德森、王思玲主编: "《物理药剂学》", 31 July 2004, 化学工业出版社 * |
Also Published As
Publication number | Publication date |
---|---|
CN107001276B (zh) | 2020-03-13 |
RS60749B1 (sr) | 2020-10-30 |
CA2984961A1 (en) | 2016-12-01 |
RU2719484C2 (ru) | 2020-04-17 |
JP6738350B2 (ja) | 2020-08-12 |
PT3305768T (pt) | 2020-08-03 |
MX2017014319A (es) | 2018-03-07 |
ES2811325T3 (es) | 2021-03-11 |
CY1123262T1 (el) | 2021-12-31 |
AU2016269359B2 (en) | 2020-02-06 |
US20180134663A1 (en) | 2018-05-17 |
US20190040015A1 (en) | 2019-02-07 |
CA2984961C (en) | 2023-08-01 |
DK3305768T3 (da) | 2020-08-10 |
SI3305768T1 (sl) | 2020-10-30 |
WO2016188444A1 (zh) | 2016-12-01 |
EP3305768A1 (en) | 2018-04-11 |
EP3305768B1 (en) | 2020-07-01 |
HUE051640T2 (hu) | 2021-03-01 |
PL3305768T3 (pl) | 2020-12-28 |
US10196361B2 (en) | 2019-02-05 |
RU2017142996A (ru) | 2019-06-27 |
US10358424B2 (en) | 2019-07-23 |
BR112017022505A2 (zh) | 2018-07-17 |
HRP20201178T1 (hr) | 2020-11-13 |
EP3305768A4 (en) | 2019-02-13 |
AU2016269359A1 (en) | 2017-11-23 |
RU2017142996A3 (zh) | 2019-11-20 |
KR20180006441A (ko) | 2018-01-17 |
JP2018515454A (ja) | 2018-06-14 |
LT3305768T (lt) | 2020-08-25 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP2021105030A (ja) | ニコチンアミドリボシドの結晶形 | |
JP6166721B2 (ja) | 4−tert−ブチル−N−[4−クロロ−2−(1−オキシ−ピリジン−4−カルボニル)−フェニル]−ベンゼンスルホンアミドのナトリウム塩の多形 | |
CN100497337C (zh) | 叶酸二甲双胍及其制备方法 | |
US8946272B2 (en) | Plymorphic forms of deferasirox (ICL670A) | |
JP6122003B2 (ja) | 4−tert−ブチル−N−[4−クロロ−2−(1−オキシ−ピリジン−4−カルボニル)−フェニル]−ベンゼンスルホンアミドのナトリウム塩の結晶形 | |
CN106661025A (zh) | 一种周期素依赖性蛋白激酶抑制剂的羟乙基磺酸盐、其结晶形式及制备方法 | |
CN107001276A (zh) | 一种尿酸转运蛋白抑制剂的钠盐及其结晶形式 | |
JP6122002B2 (ja) | 4−tert−ブチル−N−[4−クロロ−2−(1−オキシ−ピリジン−4−カルボニル)−フェニル]−ベンゼンスルホンアミドのナトリウム塩の多形 | |
EP3279201B1 (en) | Cdk inhibitor, eutectic crystal of mek inhibitor, and preparation method therefor | |
JP2023071922A (ja) | 7h-ピロロ[2,3-d]ピリミジンjak-阻害剤 | |
WO2011023146A1 (en) | Imatinib mesylate polymorphs generated by crystallization in aqueous inorganic salt solutions | |
US9150982B2 (en) | Crystal form of (6S)-5-methyltetrahydrofolate salt and method for preparing same | |
US20100093820A1 (en) | Crystalline pyrazoles | |
CN104744464B (zh) | 伊曲茶碱晶型 | |
EP3792258A1 (en) | Addition salt of s1p1 receptor agonist and crystal form thereof, and pharmaceutical composition | |
CN105992769A (zh) | 一种钠-葡萄糖协同转运蛋白2抑制剂的l-脯氨酸复合物、其一水合物及晶体 | |
CN107001284A (zh) | 一种雄性激素受体抑制剂的结晶形式及其制备方法 | |
EP1927591A1 (en) | Polymorphic Forms of Deferasirox (ICL670) | |
CN106478616A (zh) | 一种gpr40激动剂的结晶形式及其制备方法 | |
CN104530051B (zh) | 稳定的(6r,s)-5-甲基四氢叶酸晶型及其制备方法 | |
CN106065016A (zh) | 一种周期素依赖性蛋白激酶抑制剂的结晶形式及其制备方法 | |
CN106518773A (zh) | 一种雄性激素受体抑制剂的结晶形式及其制备方法 | |
JP2018510173A (ja) | トピロキソスタットの新規結晶形及びその製造方法 | |
CN102731430A (zh) | 非布司他的新晶型和其制备方法以及应用 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
PB01 | Publication | ||
PB01 | Publication | ||
SE01 | Entry into force of request for substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1238636 Country of ref document: HK |
|
GR01 | Patent grant | ||
TR01 | Transfer of patent right | ||
TR01 | Transfer of patent right |
Effective date of registration: 20230921 Address after: 361026 room 53, floor 1, building A19, Xiamen biomedical industrial park, 2036 wengjiao West Road, Haicang District, Xiamen City, Fujian Province Patentee after: Fujian Shengdi Pharmaceutical Co.,Ltd. Patentee after: JIANGSU HENGRUI MEDICINE Co.,Ltd. Address before: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu Patentee before: JIANGSU HENGRUI MEDICINE Co.,Ltd. |