BR112017007953A2 - forma cristalina de um bissulfato inibidor de jak quinase e método de preparação desse - Google Patents
forma cristalina de um bissulfato inibidor de jak quinase e método de preparação desseInfo
- Publication number
- BR112017007953A2 BR112017007953A2 BR112017007953A BR112017007953A BR112017007953A2 BR 112017007953 A2 BR112017007953 A2 BR 112017007953A2 BR 112017007953 A BR112017007953 A BR 112017007953A BR 112017007953 A BR112017007953 A BR 112017007953A BR 112017007953 A2 BR112017007953 A2 BR 112017007953A2
- Authority
- BR
- Brazil
- Prior art keywords
- crystalline form
- preparation
- formula
- kinase inhibitor
- jak kinase
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 3-methoxy-1,2,4-thiadiazol-5-yl Chemical group 0.000 abstract 2
- 239000013078 crystal Substances 0.000 abstract 2
- 239000003960 organic solvent Substances 0.000 abstract 2
- ZHNUHDYFZUAESO-UHFFFAOYSA-N formamide Substances NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
a presente invenção refere-se à forma cristalina de um bissulfato inibidor de jak quinase e seu método de preparação. em particular, a presente invenção refere-se à forma cristalina tipo ii do bissulfato de (3ar,5s,6as)-n-(3-metoxil-1,2,4-tiadiazol-5-il)-5-(metil(7h-pirrolo[2,3-d] pirimidino-4-il)amino)hexa-hidrociclopenta[c]pirrol-2(1h)-formamida e seu método de preparação. o método de preparação compreende cristalizar qualquer uma das formas cristalina ou amorfa do composto sólido da fórmula (i) em um solvente orgânico ou solvente orgânico misto para obter a forma cristalina do tipo ii do composto da fórmula (i). fórmula (i) a forma cristalina do tipo ii do composto da fórmula (i) obtida pela presente invenção tem uma boa estabilidade do cristal e estabilidade química e o solvente usado no cristal tem baixa toxicidade e pouco resíduo, o que pode ser melhor usado no tratamento clínico.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410617808.4 | 2014-11-05 | ||
| CN201410617808 | 2014-11-05 | ||
| PCT/CN2015/091527 WO2016070697A1 (zh) | 2014-11-05 | 2015-10-09 | 一种jak激酶抑制剂的硫酸氢盐的结晶形式及其制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112017007953A2 true BR112017007953A2 (pt) | 2017-12-19 |
| BR112017007953B1 BR112017007953B1 (pt) | 2023-12-05 |
Family
ID=55908546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017007953-4A BR112017007953B1 (pt) | 2014-11-05 | 2015-10-09 | Forma cristalina ii do bissulfato inibidor de jak quinase, seu uso e seu método de preparação, e composição farmacêutica |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US10023577B2 (pt) |
| EP (1) | EP3216790B1 (pt) |
| JP (1) | JP6851572B2 (pt) |
| KR (1) | KR102522895B1 (pt) |
| CN (1) | CN105980390B (pt) |
| AU (1) | AU2015342444B2 (pt) |
| BR (1) | BR112017007953B1 (pt) |
| CA (1) | CA2965716C (pt) |
| CY (1) | CY1122468T1 (pt) |
| DK (1) | DK3216790T3 (pt) |
| ES (1) | ES2754548T3 (pt) |
| HR (1) | HRP20192030T1 (pt) |
| HU (1) | HUE047404T2 (pt) |
| PL (1) | PL3216790T3 (pt) |
| PT (1) | PT3216790T (pt) |
| RS (1) | RS59669B1 (pt) |
| RU (1) | RU2716260C2 (pt) |
| SI (1) | SI3216790T1 (pt) |
| TW (1) | TWI672305B (pt) |
| WO (1) | WO2016070697A1 (pt) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3014090A1 (en) | 2016-02-19 | 2017-08-24 | Jiangsu Hengrui Medicine Co., Ltd. | Pharmaceutical composition containing jak kinase inhibitor or pharmaceutically acceptable salt thereof |
| TW201827436A (zh) * | 2017-01-20 | 2018-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種ｊａｋ激酶抑制劑的硫酸氫鹽的晶型及其製備方法 |
| CN111205290B (zh) * | 2018-11-22 | 2021-10-08 | 江苏恒瑞医药股份有限公司 | 一种jak激酶抑制剂的结晶形式及其制备方法 |
| AU2021318201A1 (en) | 2020-07-28 | 2023-02-02 | Arcutis Biotherapeutics, Inc. | Topical formulation containing jak inhibitor and laureth-4 |
| JP2023550363A (ja) | 2020-11-17 | 2023-12-01 | アーキュティス・バイオセラピューティクス・インコーポレーテッド | 深部皮膚薬物送達のための組成物および方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE423120T1 (de) * | 2000-06-26 | 2009-03-15 | Pfizer Prod Inc | Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe |
| PT1613315E (pt) * | 2003-04-04 | 2009-04-22 | Novartis Ag | Derivados da quinolina-2-ona para o tratamento de doenças das vias aéreas respiratórias |
| CN101142218B (zh) * | 2005-02-03 | 2013-02-06 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡咯并嘧啶 |
| EP2721025B1 (en) * | 2011-06-16 | 2015-11-25 | Boehringer Ingelheim International Gmbh | New selective ccr2 antagonists |
| AU2012357296B2 (en) * | 2011-12-21 | 2017-04-13 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof |
| KR102275326B1 (ko) * | 2013-06-07 | 2021-07-12 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 야누스 키나제(jak) 억제제의 바이설페이트 및 그의 제조 방법 |
| CN105566327A (zh) | 2014-10-09 | 2016-05-11 | 江苏恒瑞医药股份有限公司 | 一种jak激酶抑制剂的硫酸氢盐的i型结晶及其制备方法 |
-
2015
- 2015-10-09 EP EP15857844.3A patent/EP3216790B1/en active Active
- 2015-10-09 RU RU2017118193A patent/RU2716260C2/ru active
- 2015-10-09 SI SI201530982T patent/SI3216790T1/sl unknown
- 2015-10-09 WO PCT/CN2015/091527 patent/WO2016070697A1/zh active Application Filing
- 2015-10-09 HU HUE15857844A patent/HUE047404T2/hu unknown
- 2015-10-09 BR BR112017007953-4A patent/BR112017007953B1/pt active IP Right Grant
- 2015-10-09 RS RS20191420A patent/RS59669B1/sr unknown
- 2015-10-09 CA CA2965716A patent/CA2965716C/en active Active
- 2015-10-09 KR KR1020177013839A patent/KR102522895B1/ko active IP Right Grant
- 2015-10-09 US US15/522,991 patent/US10023577B2/en active Active
- 2015-10-09 JP JP2017518183A patent/JP6851572B2/ja active Active
- 2015-10-09 AU AU2015342444A patent/AU2015342444B2/en active Active
- 2015-10-09 PL PL15857844T patent/PL3216790T3/pl unknown
- 2015-10-09 PT PT158578443T patent/PT3216790T/pt unknown
- 2015-10-09 DK DK15857844T patent/DK3216790T3/da active
- 2015-10-09 ES ES15857844T patent/ES2754548T3/es active Active
- 2015-10-09 CN CN201580008169.4A patent/CN105980390B/zh active Active
- 2015-10-22 TW TW104134655A patent/TWI672305B/zh active
-
2019
- 2019-11-04 CY CY20191101146T patent/CY1122468T1/el unknown
- 2019-11-08 HR HRP20192030TT patent/HRP20192030T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RS59669B1 (sr) | 2020-01-31 |
| TWI672305B (zh) | 2019-09-21 |
| CN105980390B (zh) | 2017-07-07 |
| HRP20192030T1 (hr) | 2020-02-07 |
| EP3216790A1 (en) | 2017-09-13 |
| JP2017532327A (ja) | 2017-11-02 |
| RU2716260C2 (ru) | 2020-03-11 |
| RU2017118193A3 (pt) | 2019-05-08 |
| CA2965716C (en) | 2023-03-21 |
| PT3216790T (pt) | 2019-11-19 |
| DK3216790T3 (da) | 2019-11-25 |
| KR102522895B1 (ko) | 2023-04-17 |
| KR20170078710A (ko) | 2017-07-07 |
| SI3216790T1 (sl) | 2020-02-28 |
| JP6851572B2 (ja) | 2021-03-31 |
| HUE047404T2 (hu) | 2020-04-28 |
| CY1122468T1 (el) | 2021-01-27 |
| US20170313709A1 (en) | 2017-11-02 |
| AU2015342444A1 (en) | 2017-05-18 |
| CN105980390A (zh) | 2016-09-28 |
| US10023577B2 (en) | 2018-07-17 |
| EP3216790B1 (en) | 2019-10-02 |
| PL3216790T3 (pl) | 2020-05-18 |
| BR112017007953B1 (pt) | 2023-12-05 |
| WO2016070697A1 (zh) | 2016-05-12 |
| EP3216790A4 (en) | 2018-04-25 |
| TW201617347A (zh) | 2016-05-16 |
| RU2017118193A (ru) | 2018-12-05 |
| ES2754548T3 (es) | 2020-04-20 |
| CA2965716A1 (en) | 2016-05-12 |
| AU2015342444B2 (en) | 2019-12-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
|
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 09/10/2015, OBSERVADAS AS CONDICOES LEGAIS |