BR112021024533A2 - Método de síntese de composto de furoimidazopiridina, forma cristalina de composto de furoimidazopiridina, e forma cristalina de sal do mesmo - Google Patents
Método de síntese de composto de furoimidazopiridina, forma cristalina de composto de furoimidazopiridina, e forma cristalina de sal do mesmoInfo
- Publication number
- BR112021024533A2 BR112021024533A2 BR112021024533A BR112021024533A BR112021024533A2 BR 112021024533 A2 BR112021024533 A2 BR 112021024533A2 BR 112021024533 A BR112021024533 A BR 112021024533A BR 112021024533 A BR112021024533 A BR 112021024533A BR 112021024533 A2 BR112021024533 A2 BR 112021024533A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- crystalline form
- furoimidazopyridine
- salt
- synthesis
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 4
- 150000003839 salts Chemical class 0.000 title abstract 4
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 abstract 3
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 abstract 2
- 230000002194 synthesizing effect Effects 0.000 abstract 2
- AQCQKDBQDZRGAH-UHFFFAOYSA-N 7-chloro-6-nitrofuro[3,2-b]pyridine Chemical compound C1(=C(Cl)C=2OC=CC=2N=C1)N(=O)=O AQCQKDBQDZRGAH-UHFFFAOYSA-N 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 238000003763 carbonization Methods 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 238000009509 drug development Methods 0.000 abstract 1
- 238000009776 industrial production Methods 0.000 abstract 1
- 101150079478 jak1 gene Proteins 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 abstract 1
- 229910052763 palladium Inorganic materials 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000007363 ring formation reaction Methods 0.000 abstract 1
- 239000007858 starting material Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 238000001308 synthesis method Methods 0.000 abstract 1
- 125000004187 tetrahydropyran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C([H])([H])C1([H])[H] 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
-
- 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
- A61K31/4353—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
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
método de síntese de composto de furoimidazopiridina, forma cristalina de composto de furoimidazopiridina, e forma cristalina de sal do mesmo. um método é fornecido para sintetizar um composto 2-[(2r,5s)-5-[2-[(r)-1-hidroxietil]furo[3,2-b]imidazo[4,5-d]piridin-1-il]tetrahidropiran-2-il]acetonitrila como um inibidor de jak1/tyk2 quinase seletivo. o composto é preparado por substituição nucleofílica, redução de paládio em carbono, e reação de ciclização com uso de 7-cloro-6-nitrofuro[3,2-b]piridina como um material de partida. o método de síntese tem condições de reação branda, alto rendimento de produto, e alta pureza, e é adequado para produção industrial. são adicionalmente fornecidos uma forma cristalina do composto, forma cristalina de seus sais, e seus métodos de preparação. a forma cristalina do composto e as formas cristalinas de seus sais têm propriedades físicas e químicas satisfatórias e são adequadas para desenvolvimento de fármaco.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201910490418 | 2019-06-06 | ||
PCT/CN2020/088121 WO2020244348A1 (zh) | 2019-06-06 | 2020-04-30 | 呋喃并咪唑并吡啶类化合物的合成方法、呋喃并咪唑并吡啶类化合物的晶型及其盐的晶型 |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112021024533A2 true BR112021024533A2 (pt) | 2022-01-18 |
Family
ID=73652738
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112021024533A BR112021024533A2 (pt) | 2019-06-06 | 2020-04-30 | Método de síntese de composto de furoimidazopiridina, forma cristalina de composto de furoimidazopiridina, e forma cristalina de sal do mesmo |
Country Status (11)
Country | Link |
---|---|
US (1) | US20220227777A1 (pt) |
EP (3) | EP4248967A3 (pt) |
JP (2) | JP7320628B2 (pt) |
KR (1) | KR20220016955A (pt) |
CN (2) | CN117327083A (pt) |
AU (1) | AU2020289149B2 (pt) |
BR (1) | BR112021024533A2 (pt) |
CA (1) | CA3142625A1 (pt) |
IL (1) | IL288348A (pt) |
MX (1) | MX2021014319A (pt) |
WO (1) | WO2020244348A1 (pt) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2023035913A1 (en) * | 2021-09-13 | 2023-03-16 | Hangzhou Highlightll Pharmaceutical Co., Ltd | Methods of treating cns disorders |
CN114213424B (zh) * | 2021-12-30 | 2023-05-26 | 杭州高光制药有限公司 | 一种呋喃[3,2-b]并吡啶衍生物的合成方法 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG10201703533VA (en) * | 2012-11-01 | 2017-06-29 | Incyte Corp | Tricyclic fused thiophene derivatives as jak inhibitors |
TW201625643A (zh) * | 2014-04-30 | 2016-07-16 | 英塞特公司 | 製備jak1抑制劑之方法及其新形式 |
PT3509591T (pt) * | 2016-10-03 | 2021-12-27 | Highlightll Pharmaceutical Hainan Co Ltd | Novos inibidores seletivos da jak1 e usos dos mesmos |
EP4086256A1 (en) * | 2016-12-16 | 2022-11-09 | Janssen Pharmaceutica NV | Small molecule inhibitors of the jak family of kinases |
-
2020
- 2020-04-30 CA CA3142625A patent/CA3142625A1/en active Pending
- 2020-04-30 JP JP2021572485A patent/JP7320628B2/ja active Active
- 2020-04-30 CN CN202311283291.5A patent/CN117327083A/zh active Pending
- 2020-04-30 AU AU2020289149A patent/AU2020289149B2/en active Active
- 2020-04-30 EP EP23182049.9A patent/EP4248967A3/en active Pending
- 2020-04-30 EP EP20818305.3A patent/EP3981771A4/en active Pending
- 2020-04-30 WO PCT/CN2020/088121 patent/WO2020244348A1/zh active Application Filing
- 2020-04-30 CN CN202080036439.3A patent/CN113906035B/zh active Active
- 2020-04-30 EP EP23182042.4A patent/EP4248966A3/en active Pending
- 2020-04-30 KR KR1020227000069A patent/KR20220016955A/ko not_active Application Discontinuation
- 2020-04-30 US US17/615,313 patent/US20220227777A1/en active Pending
- 2020-04-30 MX MX2021014319A patent/MX2021014319A/es unknown
- 2020-04-30 BR BR112021024533A patent/BR112021024533A2/pt unknown
-
2021
- 2021-11-24 IL IL288348A patent/IL288348A/en unknown
-
2023
- 2023-04-14 JP JP2023066167A patent/JP2023089169A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
EP3981771A1 (en) | 2022-04-13 |
AU2020289149B2 (en) | 2023-05-11 |
CN113906035B (zh) | 2023-11-10 |
JP2022543183A (ja) | 2022-10-11 |
CN113906035A (zh) | 2022-01-07 |
MX2021014319A (es) | 2022-01-26 |
WO2020244348A1 (zh) | 2020-12-10 |
EP3981771A4 (en) | 2023-03-15 |
EP4248966A2 (en) | 2023-09-27 |
CA3142625A1 (en) | 2020-12-10 |
CN117327083A (zh) | 2024-01-02 |
IL288348A (en) | 2022-01-01 |
EP4248967A3 (en) | 2023-10-11 |
JP7320628B2 (ja) | 2023-08-03 |
EP4248966A3 (en) | 2023-10-11 |
EP4248967A2 (en) | 2023-09-27 |
KR20220016955A (ko) | 2022-02-10 |
JP2023089169A (ja) | 2023-06-27 |
AU2020289149A1 (en) | 2022-01-06 |
US20220227777A1 (en) | 2022-07-21 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B25A | Requested transfer of rights approved |
Owner name: HANGZHOU HIGHLIGHTLL PHARMACEUTICAL CO., LTD (CN) |