JP7422732B2 - Jak阻害化合物のキシナホ酸塩 - Google Patents
Jak阻害化合物のキシナホ酸塩 Download PDFInfo
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- JP7422732B2 JP7422732B2 JP2021502626A JP2021502626A JP7422732B2 JP 7422732 B2 JP7422732 B2 JP 7422732B2 JP 2021502626 A JP2021502626 A JP 2021502626A JP 2021502626 A JP2021502626 A JP 2021502626A JP 7422732 B2 JP7422732 B2 JP 7422732B2
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- Prior art keywords
- fluoro
- xinafoate
- methylpiperazin
- methoxy
- added
- Prior art date
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- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
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- 102000042838 JAK family Human genes 0.000 claims description 43
- 108091082332 JAK family Proteins 0.000 claims description 43
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/255—Tartaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
- C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pulmonology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| JP2023171327A JP7644190B2 (ja) | 2018-07-18 | 2023-10-02 | Jak阻害化合物のキシナホ酸塩 |
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| US62/866,013 | 2019-06-25 | ||
| PCT/EP2019/069252 WO2020016302A1 (en) | 2018-07-18 | 2019-07-17 | A xinafoate salt of a jak inhibiting compound |
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| JP2021530526A JP2021530526A (ja) | 2021-11-11 |
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| JP2023171327A Active JP7644190B2 (ja) | 2018-07-18 | 2023-10-02 | Jak阻害化合物のキシナホ酸塩 |
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| EP (1) | EP3823964A1 (https=) |
| JP (2) | JP7422732B2 (https=) |
| KR (1) | KR102849420B1 (https=) |
| CN (2) | CN118580223A (https=) |
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| CN115260128B (zh) * | 2022-09-21 | 2022-12-09 | 苏州凯瑞医药科技有限公司 | 一种新型jak抑制剂关键中间体的制备方法 |
| GB202316063D0 (en) | 2023-10-20 | 2023-12-06 | Astrazeneca Ab | Dosing regime |
| GB202403369D0 (en) | 2024-03-08 | 2024-04-24 | Astrazeneca Ab | Process and intermediates for the production of a jak1 inhibitor |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009084270A (ja) | 2007-09-05 | 2009-04-23 | Pfizer Ltd | 塩形態 |
| WO2016024289A2 (en) | 2014-08-11 | 2016-02-18 | Sun Pharmaceutical Industries Ltd | Novel salts of nilotinib and polymorphs thereof |
| WO2017050938A1 (en) | 2015-09-25 | 2017-03-30 | Astrazeneca Ab | Compounds and methods for inhibiting jak |
| WO2018134213A1 (en) | 2017-01-17 | 2018-07-26 | Astrazeneca Ab | Jak1 selective inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| MX2013003019A (es) * | 2010-09-15 | 2013-05-28 | Hoffmann La Roche | Compuestos de azabenzotiazol, composiciones y metodos de uso. |
| AU2014342338B2 (en) * | 2013-11-01 | 2016-12-01 | Novartis Ag | Aminoheteroaryl benzamides as kinase inhibitors |
| CN106831538B (zh) * | 2017-01-22 | 2019-06-25 | 苏州楚凯药业有限公司 | 托法替尼中间体的制备方法 |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009084270A (ja) | 2007-09-05 | 2009-04-23 | Pfizer Ltd | 塩形態 |
| WO2016024289A2 (en) | 2014-08-11 | 2016-02-18 | Sun Pharmaceutical Industries Ltd | Novel salts of nilotinib and polymorphs thereof |
| WO2017050938A1 (en) | 2015-09-25 | 2017-03-30 | Astrazeneca Ab | Compounds and methods for inhibiting jak |
| WO2018134213A1 (en) | 2017-01-17 | 2018-07-26 | Astrazeneca Ab | Jak1 selective inhibitors |
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| AU2019304014B2 (en) | 2022-08-18 |
| IL280025B1 (en) | 2024-10-01 |
| KR102849420B1 (ko) | 2025-08-25 |
| WO2020016302A1 (en) | 2020-01-23 |
| BR112021000467A2 (pt) | 2021-04-06 |
| WO2020016302A8 (en) | 2020-11-12 |
| JP2024001109A (ja) | 2024-01-09 |
| MA53162A (fr) | 2021-05-26 |
| CN112424187B (zh) | 2024-06-21 |
| IL280025A (en) | 2021-03-01 |
| AU2019304014A1 (en) | 2021-03-04 |
| SG11202100240RA (en) | 2021-02-25 |
| MY209356A (en) | 2025-07-03 |
| MX2021000611A (es) | 2021-04-13 |
| EP3823964A1 (en) | 2021-05-26 |
| CN112424187A (zh) | 2021-02-26 |
| US11149029B2 (en) | 2021-10-19 |
| KR20210033474A (ko) | 2021-03-26 |
| CA3105585A1 (en) | 2020-01-23 |
| CN118580223A (zh) | 2024-09-03 |
| IL280025B2 (en) | 2025-02-01 |
| US20200062737A1 (en) | 2020-02-27 |
| JP7644190B2 (ja) | 2025-03-11 |
| JP2021530526A (ja) | 2021-11-11 |
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