AR079134A1 - Procedimiento para la preparacion de (4,6-diamino -2-(1-(2- fluorobencil )-1h- pirazolo (3,4-b) piridin-3-il) pirimidin -5-il) metil carbamato de metilo y su purificacion para su uso como principio activo farmaceutico - Google Patents
Procedimiento para la preparacion de (4,6-diamino -2-(1-(2- fluorobencil )-1h- pirazolo (3,4-b) piridin-3-il) pirimidin -5-il) metil carbamato de metilo y su purificacion para su uso como principio activo farmaceuticoInfo
- Publication number
- AR079134A1 AR079134A1 ARP100104326A ARP100104326A AR079134A1 AR 079134 A1 AR079134 A1 AR 079134A1 AR P100104326 A ARP100104326 A AR P100104326A AR P100104326 A ARP100104326 A AR P100104326A AR 079134 A1 AR079134 A1 AR 079134A1
- Authority
- AR
- Argentina
- Prior art keywords
- purification
- diamino
- formula
- preparation
- procedure
- Prior art date
Links
- 238000000746 purification Methods 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 2
- GTCAXTIRRLKXRU-UHFFFAOYSA-N methyl carbamate Chemical compound COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 title 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- RCKYXYXLIJBCOE-UHFFFAOYSA-N 2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidine-4,5,6-triamine Chemical compound NC1=C(N)C(N)=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=N1 RCKYXYXLIJBCOE-UHFFFAOYSA-N 0.000 abstract 1
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000009903 catalytic hydrogenation reaction Methods 0.000 abstract 1
- 239000012043 crude product Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- -1 {4,6 -diamino-2- [1- (2-fluorobenzyl) -1H-pyrazolo [3,4-b] pyridin-3-yl] pyrimidin-5-yl} methylcarbamate methyl-sulfinyldimethane Chemical compound 0.000 abstract 1
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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- 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
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Abstract
Un procedimiento para la purificacion del producto bruto del compuesto de formula (1) para su uso como sustancia farmacéuticamente activa, aislándose para la purificacion como intermedio o produciéndose como intermedio en este procedimiento de purificacion, dado el caso presente en una mezcla {4,6-diamino-2-[1-(2-fluorobencil)-1H-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilcarbamato de metilo-sulfinildimetano (1:1), es decir, un compuesto de la formula (2). Reivindicacion 1: Procedimiento para la preparacion de {4,6-diamino-2-[1-(2-fluorobencil)-1H-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilcarbamato de metilo de la formula (1), caracterizado porque se disocia 2-[1-(2-fluorobencil)-1H-pirazolo[3,4-b]piridin-3-il]-5-[(E)-fenildiazenil]pirimidin-4,6-diamina de la formula (3) por hidrogenacion catalítica y porque se aísla 2-[1-(2-fluorobencil)-1H-pirazolo[3,4-b]piridin-3-il]-4,5,6-pirimidintriamina de la formula (4) sin formacion intermedia de sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09177371 | 2009-11-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079134A1 true AR079134A1 (es) | 2011-12-28 |
Family
ID=43536603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104326A AR079134A1 (es) | 2009-11-27 | 2010-11-24 | Procedimiento para la preparacion de (4,6-diamino -2-(1-(2- fluorobencil )-1h- pirazolo (3,4-b) piridin-3-il) pirimidin -5-il) metil carbamato de metilo y su purificacion para su uso como principio activo farmaceutico |
Country Status (43)
Families Citing this family (27)
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| MX381242B (es) | 2009-11-27 | 2025-03-12 | Genzyme Corp | Una forma amorfa y una cristalina de hemitartrato de genz 112638 como inhibidor de glucosilceramida sintasa. |
| KR101861981B1 (ko) * | 2009-11-27 | 2018-05-28 | 아드베리오 파마 게엠베하 | 제약상 물질로서 사용하기 위한 메틸-(4,6-디아미노-2-(1-(2-플루오로벤질)-1ｈ-피라졸로(3,4-ｂ)피리디노-3-일)피리미디노-5-일)메틸카르바메이트의 제조 방법 및 그의 정제 |
| DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| DE102010043379A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung |
| DE102010043380A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Benzyl-substituierte Carbamate und ihre Verwendung |
| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| LT3421470T (lt) * | 2011-11-25 | 2021-04-26 | Adverio Pharma Gmbh | Pakeistieji 5-fluor-1h-pirazolopiridinai kristalų pavidale |
| AU2014220801A1 (en) * | 2013-02-21 | 2015-09-10 | Adverio Pharma Gmbh | Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate |
| CN104327107A (zh) * | 2013-10-17 | 2015-02-04 | 广东东阳光药业有限公司 | 一种氟喹诺酮类抗菌药物的制备方法 |
| PE20170697A1 (es) | 2014-09-19 | 2017-06-24 | Bayer Pharma AG | Indazoles sustituidos con benzilo como inhibidores de bub1 |
| WO2016113415A1 (en) | 2015-01-16 | 2016-07-21 | Sandoz Ag | Process for the preparation of riociguat essentially free from genotoxic impurities |
| CN105367568B (zh) * | 2015-11-18 | 2019-08-20 | 浙江京新药业股份有限公司 | 一种制备利奥西呱的方法 |
| CN105294686B (zh) * | 2015-11-30 | 2017-03-22 | 郑州大明药物科技有限公司 | 一种利奥西呱的制备方法 |
| CA3006764A1 (en) | 2015-12-14 | 2017-06-22 | Ironwood Pharmaceuticals, Inc. | Use of sgc stimulators for the treatment of gastrointestinal sphincter dysfunction |
| US10414766B2 (en) * | 2015-12-15 | 2019-09-17 | Alembic Pharmaceuticals Limited | Polymorph of Riociguat and its process for the preparation |
| CN108069960A (zh) * | 2016-11-15 | 2018-05-25 | 江苏豪森药业集团有限公司 | 利奥西呱中间体的制备方法 |
| WO2018096550A1 (en) * | 2016-11-28 | 2018-05-31 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate and its polymorphs thereof |
| US20190381039A1 (en) | 2016-12-13 | 2019-12-19 | Cyclerion Therapeutics, Inc. | USE OF sGC STIMULATORS FOR THE TREATMENT OF ESOPHAGEAL MOTILITY DISORDERS |
| WO2018130226A1 (zh) * | 2017-01-16 | 2018-07-19 | 苏州科睿思制药有限公司 | 利奥西呱的新晶型及其制备方法和用途 |
| KR20210031931A (ko) | 2018-07-11 | 2021-03-23 | 사이클리온 테라퓨틱스, 인크. | 미토콘드리아 장애의 치료를 위한 sGC 자극제의 용도 |
| TWI830835B (zh) | 2018-12-17 | 2024-02-01 | 德商亞德維瑞醫藥有限公司 | 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物 |
| US20230067593A1 (en) * | 2020-02-03 | 2023-03-02 | Adverio Pharma Gmbh | Nanoformulations of methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3 -yl]pyrimidin-5-yl} carbamate |
| CN111689961A (zh) * | 2020-06-01 | 2020-09-22 | 江苏华阳制药有限公司 | 一种利奧西呱的新晶型及其制备方法 |
| EP3925953A1 (en) * | 2020-06-16 | 2021-12-22 | Adverio Pharma GmbH | Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate |
| CN112316968B (zh) * | 2020-11-13 | 2022-03-01 | 中国石油大学(北京) | 一种粗对苯二甲酸加氢精制催化剂及其制备方法和应用 |
| CN112316932B (zh) * | 2020-11-13 | 2022-03-01 | 中国石油大学(北京) | 一种粗对苯二甲酸加氢精制催化剂及其制备方法和应用 |
| CN117229282A (zh) * | 2023-09-11 | 2023-12-15 | 安徽美诺华药物化学有限公司 | 一种利奥西呱的合成工艺 |
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