EA201270676A1 - Полиморфная, кристаллическая и мезофазная формы 2-(5-бром-4-(4-циклопропилнафталинил-1-ил)-4н-1,2,4-триазол-3- илтио)ацетата натрия и их применение - Google Patents
Полиморфная, кристаллическая и мезофазная формы 2-(5-бром-4-(4-циклопропилнафталинил-1-ил)-4н-1,2,4-триазол-3- илтио)ацетата натрия и их применениеInfo
- Publication number
- EA201270676A1 EA201270676A1 EA201270676A EA201270676A EA201270676A1 EA 201270676 A1 EA201270676 A1 EA 201270676A1 EA 201270676 A EA201270676 A EA 201270676A EA 201270676 A EA201270676 A EA 201270676A EA 201270676 A1 EA201270676 A1 EA 201270676A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- triazol
- cyclopropylnaftalinyl
- iltio
- brom
- polymorphic
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
- C07D249/12—Oxygen or sulfur atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
Abstract
Описаны кристаллические полиморфы и твёрдые мезофазные формы 2-(5-бром-4-(4-циклопропилнафталин-1-ил)-4Н-1,2,4-триазол-3-илтио)ацетата натрия. Кроме того, предусмотрены фармацевтические композиции и применение таких композиций для лечения различных болезней и состояний.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US29360210P | 2010-01-08 | 2010-01-08 | |
PCT/US2011/020233 WO2011085009A2 (en) | 2010-01-08 | 2011-01-05 | Polymorphic, crystalline and mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio)acetate, and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201270676A1 true EA201270676A1 (ru) | 2013-01-30 |
EA020183B1 EA020183B1 (ru) | 2014-09-30 |
Family
ID=44306123
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201270676A EA020183B1 (ru) | 2010-01-08 | 2011-01-05 | Полиморфная, кристаллическая и мезофазная формы 2-(5-бром-4-(4-циклопропилнафталинил-1-ил)-4н-1,2,4-триазол-3-илтио)ацетата натрия и их применение |
Country Status (20)
Country | Link |
---|---|
US (2) | US8524754B2 (ru) |
EP (1) | EP2521716B1 (ru) |
JP (1) | JP5696346B2 (ru) |
KR (1) | KR20120104627A (ru) |
CN (1) | CN102741234B (ru) |
AU (1) | AU2011203708B2 (ru) |
BR (1) | BR112012016795A2 (ru) |
CA (1) | CA2785200C (ru) |
CL (1) | CL2012001841A1 (ru) |
CO (1) | CO6561780A2 (ru) |
EA (1) | EA020183B1 (ru) |
ES (1) | ES2563207T3 (ru) |
HK (1) | HK1172622A1 (ru) |
MX (1) | MX2012007925A (ru) |
MY (1) | MY161482A (ru) |
NZ (1) | NZ600984A (ru) |
SG (1) | SG182404A1 (ru) |
TW (1) | TWI451867B (ru) |
WO (1) | WO2011085009A2 (ru) |
ZA (1) | ZA201204938B (ru) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2011126852A2 (en) * | 2010-03-30 | 2011-10-13 | Ardea Biosciences, Inc. | Treatment of gout |
ES2670700T3 (es) | 2010-06-15 | 2018-05-31 | Ardea Biosciences, Inc. | Tratamiento de gota e hiperuricemia |
EA022301B1 (ru) | 2010-12-30 | 2015-12-30 | Ардеа Биосайнсиз, Инк. | Полиморфные формы 2-(5-бром-4-(4-циклопропилнафталин-1-ил)-4h-1,2,4-триазол-3-илтио)уксусной кислоты и их применение |
JP6025853B2 (ja) | 2011-11-03 | 2016-11-16 | アルデア バイオサイエンシーズ インク. | 3,4−二置換ピリジン化合物、その使用方法、および、該化合物を含む組成物 |
AR091651A1 (es) * | 2012-07-03 | 2015-02-18 | Ardea Biosciences Inc | Elaboracion de acido 2-(5-bromo-4-(4-ciclopropilnaftalen-1-il)-4h-1,2,4-triazol-3-iltio)acetico |
CN103524440B (zh) * | 2013-10-15 | 2015-09-09 | 苏州鹏旭医药科技有限公司 | 痛风治疗药Lesinurad的制备方法及Lesinurad中间体 |
CN103613552A (zh) * | 2013-12-02 | 2014-03-05 | 苏州晶云药物科技有限公司 | 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1,2,4-三唑-3-基硫基)乙酸钠的新晶型及其制备方法 |
CA2931430A1 (en) * | 2013-11-22 | 2015-05-28 | Crystal Pharmatech Co., Ltd. | Crystalline forms of lesinurad and its sodium salt |
CN103588716A (zh) * | 2013-11-22 | 2014-02-19 | 苏州晶云药物科技有限公司 | 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1,2,4-三唑-3-基硫基)乙酸的新晶型及其制备方法 |
CN103755651A (zh) * | 2013-12-23 | 2014-04-30 | 苏州晶云药物科技有限公司 | 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1,2,4-三唑-3-基硫基)乙酸的盐的新晶型及其制备方法 |
WO2015095703A1 (en) | 2013-12-20 | 2015-06-25 | Crystal Pharmatech, Inc. | Novel salts and co-crystals of lesinurad |
CN103626710A (zh) * | 2013-12-20 | 2014-03-12 | 苏州晶云药物科技有限公司 | 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1,2,4-三唑-3-基硫基)乙酸的共晶及其制备方法 |
CN105315218A (zh) * | 2014-07-17 | 2016-02-10 | 天津药物研究院 | 一种制备lesinurad中间体1-萘基三唑硫酮的方法 |
CN105622427A (zh) * | 2014-10-31 | 2016-06-01 | 天津药物研究院有限公司 | 一种制备lesinurad中间体4-环丙基-1-萘胺的方法 |
CN105820130B (zh) * | 2015-01-08 | 2018-06-22 | 天津药物研究院有限公司 | 三氮唑正丙酸类urat1抑制剂、制备方法及其在高尿酸血症和痛风治疗上的用途 |
CN105985296B (zh) * | 2015-02-13 | 2018-10-16 | 天津药物研究院有限公司 | 一种可以工业化的lesinurad中间体1-萘基三唑硫酮的精制工艺 |
CN105622531A (zh) | 2015-04-03 | 2016-06-01 | 南京明德新药研发股份有限公司 | 轴手性异构体及其制备方法和制药用途 |
CN104817509B (zh) * | 2015-04-13 | 2019-05-17 | 安徽省逸欣铭医药科技有限公司 | Lesinurad类似物及其制备方法和医药用途 |
CN106187926B (zh) | 2015-04-30 | 2018-11-27 | 天津药物研究院有限公司 | 含二芳基甲烷结构的羧酸类urat1抑制剂、制备方法及其在高尿酸血症和痛风治疗上的用途 |
EP3112334A1 (en) * | 2015-06-29 | 2017-01-04 | DPx Fine Chemicals Austria GmbH & CoKG | Process for manufacturing 1-cyclopropyl-naphthalenes |
CN104987311A (zh) * | 2015-06-30 | 2015-10-21 | 安徽万邦医药科技有限公司 | 一种[4-(4-环丙基萘-1-基)-5-硝基- 4h-[1,2,4]三唑-3-基硫烷基]-乙酸乙酯的制备方法及其中间体(5-硝基-4h-[1,2,4]三唑-3-基硫基)-乙酸乙酯 |
CN105153056A (zh) * | 2015-07-01 | 2015-12-16 | 安徽万邦医药科技有限公司 | 一种[5-溴-4-(4-环丙基萘-1-基)-4h-[1,2,4]三唑-3-基硫烷基]-乙酸甲酯的新制备方法 |
CN105017168A (zh) * | 2015-07-01 | 2015-11-04 | 安徽万邦医药科技有限公司 | 一种[5-溴-4-(4-环丙基萘-1-基)-4h-[1,2,4]三唑-3-基硫烷基]-乙酸甲酯的新制备方法 |
WO2017036884A1 (en) | 2015-08-28 | 2017-03-09 | Sandoz Ag | A lesinurad, free form / lesinurad ethyl ester co-crystal |
CN105566237B (zh) * | 2016-03-01 | 2018-05-18 | 山东大学 | 一种治疗痛风的三唑巯乙酸类化合物的制备方法 |
CN107337649B (zh) * | 2016-04-29 | 2020-10-16 | 四川科伦药物研究院有限公司 | 一种乙酸钠水合物无定型及其制备方法和用途 |
EP3281941B1 (en) | 2016-08-11 | 2019-07-24 | Zentiva K.S. | Process for preparing 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid |
US10513500B2 (en) | 2016-11-10 | 2019-12-24 | Apotex Inc. | Crystalline forms of Lesinurad |
CN106632108A (zh) * | 2016-12-14 | 2017-05-10 | 湖南欧亚生物有限公司 | 一种来司诺雷的制备方法 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG155246A1 (en) | 2004-08-25 | 2009-09-30 | Ardea Biosciences Inc | S-TRIAZOLYL α-MERCAPTOACETANILIDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE |
WO2007050087A1 (en) | 2004-08-25 | 2007-05-03 | Ardea Biosciences, Inc. | N[S(4-aryl-triazol-3-yl)α -mercaptoacetyl]-p-amino benozoic acids AS HIV REVERSE TRANSCRIPTASE INHIBITORS |
TWI415840B (zh) | 2007-11-27 | 2013-11-21 | Ardea Biosciences Inc | 新穎化合物、組合物及使用方法 |
JP2012502050A (ja) * | 2008-09-04 | 2012-01-26 | アルディア バイオサイエンス,インク. | 尿酸値を調節するための化合物、組成物及びそれを使用する方法。 |
EA022301B1 (ru) | 2010-12-30 | 2015-12-30 | Ардеа Биосайнсиз, Инк. | Полиморфные формы 2-(5-бром-4-(4-циклопропилнафталин-1-ил)-4h-1,2,4-триазол-3-илтио)уксусной кислоты и их применение |
-
2011
- 2011-01-05 SG SG2012050100A patent/SG182404A1/en unknown
- 2011-01-05 WO PCT/US2011/020233 patent/WO2011085009A2/en active Application Filing
- 2011-01-05 CA CA2785200A patent/CA2785200C/en not_active Expired - Fee Related
- 2011-01-05 EA EA201270676A patent/EA020183B1/ru not_active IP Right Cessation
- 2011-01-05 KR KR1020127020834A patent/KR20120104627A/ko active Search and Examination
- 2011-01-05 JP JP2012548092A patent/JP5696346B2/ja not_active Expired - Fee Related
- 2011-01-05 EP EP11732089.5A patent/EP2521716B1/en active Active
- 2011-01-05 ES ES11732089.5T patent/ES2563207T3/es active Active
- 2011-01-05 CN CN201180005688.7A patent/CN102741234B/zh not_active Expired - Fee Related
- 2011-01-05 NZ NZ600984A patent/NZ600984A/xx not_active IP Right Cessation
- 2011-01-05 US US13/375,607 patent/US8524754B2/en not_active Expired - Fee Related
- 2011-01-05 MX MX2012007925A patent/MX2012007925A/es active IP Right Grant
- 2011-01-05 MY MYPI2012003108A patent/MY161482A/en unknown
- 2011-01-05 BR BR112012016795-2A patent/BR112012016795A2/pt not_active Application Discontinuation
- 2011-01-05 AU AU2011203708A patent/AU2011203708B2/en not_active Ceased
- 2011-01-07 TW TW100100688A patent/TWI451867B/zh not_active IP Right Cessation
-
2012
- 2012-06-29 CO CO12109744A patent/CO6561780A2/es not_active Application Discontinuation
- 2012-07-02 ZA ZA2012/04938A patent/ZA201204938B/en unknown
- 2012-07-06 CL CL2012001841A patent/CL2012001841A1/es unknown
- 2012-12-28 HK HK12113508.4A patent/HK1172622A1/zh not_active IP Right Cessation
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2013
- 2013-07-30 US US13/954,736 patent/US20130345271A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
AU2011203708A1 (en) | 2012-07-26 |
EA020183B1 (ru) | 2014-09-30 |
US20130345271A1 (en) | 2013-12-26 |
EP2521716A4 (en) | 2013-07-10 |
EP2521716A2 (en) | 2012-11-14 |
ZA201204938B (en) | 2014-12-23 |
US20120129903A1 (en) | 2012-05-24 |
CN102741234B (zh) | 2015-11-25 |
NZ600984A (en) | 2013-10-25 |
AU2011203708B2 (en) | 2013-08-01 |
US8524754B2 (en) | 2013-09-03 |
CO6561780A2 (es) | 2012-11-15 |
SG182404A1 (en) | 2012-08-30 |
CN102741234A (zh) | 2012-10-17 |
CA2785200C (en) | 2015-02-24 |
JP2013516473A (ja) | 2013-05-13 |
TWI451867B (zh) | 2014-09-11 |
TW201143767A (en) | 2011-12-16 |
ES2563207T3 (es) | 2016-03-11 |
WO2011085009A2 (en) | 2011-07-14 |
EP2521716B1 (en) | 2015-12-30 |
WO2011085009A3 (en) | 2011-11-10 |
MX2012007925A (es) | 2012-08-03 |
HK1172622A1 (zh) | 2013-04-26 |
KR20120104627A (ko) | 2012-09-21 |
MY161482A (en) | 2017-04-14 |
CL2012001841A1 (es) | 2013-08-23 |
CA2785200A1 (en) | 2011-07-14 |
BR112012016795A2 (pt) | 2020-09-01 |
JP5696346B2 (ja) | 2015-04-08 |
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