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 PDF

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Publication number
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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fluoro
xinafoate
methylpiperazin
methoxy
added
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Japanese (ja)
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JPWO2020016302A5 (https=
JP2021530526A5 (https=
JP2021530526A (ja
Inventor
アンナ・マティルダ・アンニェリカ・ペッテルセン
ジェイムズ・マッケイブ
カール-ヨハン・アウレル
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AstraZeneca AB
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AstraZeneca AB
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • C07C51/412Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255Tartaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds 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
    • C07C65/01Compounds 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
    • C07C65/105Compounds 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
    • C07C65/11Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/14Heterocyclic 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
    • C07D295/145Heterocyclic 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
    • C07D295/15Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • 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)
JP2021502626A 2018-07-18 2019-07-17 Jak阻害化合物のキシナホ酸塩 Active JP7422732B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023171327A JP7644190B2 (ja) 2018-07-18 2023-10-02 Jak阻害化合物のキシナホ酸塩

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862699955P 2018-07-18 2018-07-18
US62/699,955 2018-07-18
US201962866013P 2019-06-25 2019-06-25
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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2023171327A Division JP7644190B2 (ja) 2018-07-18 2023-10-02 Jak阻害化合物のキシナホ酸塩

Publications (4)

Publication Number Publication Date
JP2021530526A JP2021530526A (ja) 2021-11-11
JPWO2020016302A5 JPWO2020016302A5 (https=) 2022-07-19
JP2021530526A5 JP2021530526A5 (https=) 2022-07-19
JP7422732B2 true JP7422732B2 (ja) 2024-01-26

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JP2021502626A Active JP7422732B2 (ja) 2018-07-18 2019-07-17 Jak阻害化合物のキシナホ酸塩
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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JP2023171327A Active JP7644190B2 (ja) 2018-07-18 2023-10-02 Jak阻害化合物のキシナホ酸塩

Country Status (14)

Country Link
US (1) US11149029B2 (https=)
EP (1) EP3823964A1 (https=)
JP (2) JP7422732B2 (https=)
KR (1) KR102849420B1 (https=)
CN (2) CN118580223A (https=)
AU (1) AU2019304014B2 (https=)
BR (1) BR112021000467A2 (https=)
CA (1) CA3105585A1 (https=)
IL (1) IL280025B2 (https=)
MA (1) MA53162A (https=)
MX (1) MX2021000611A (https=)
MY (1) MY209356A (https=)
SG (1) SG11202100240RA (https=)
WO (1) WO2020016302A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
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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