KR102849420B1 - Jak 억제 화합물의 지나포에이트염 - Google Patents

Jak 억제 화합물의 지나포에이트염

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Publication number
KR102849420B1
KR102849420B1 KR1020217001860A KR20217001860A KR102849420B1 KR 102849420 B1 KR102849420 B1 KR 102849420B1 KR 1020217001860 A KR1020217001860 A KR 1020217001860A KR 20217001860 A KR20217001860 A KR 20217001860A KR 102849420 B1 KR102849420 B1 KR 102849420B1
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KR
South Korea
Prior art keywords
fluoro
methylpiperazin
methoxy
delete delete
pyrimidin
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KR1020217001860A
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English (en)
Korean (ko)
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KR20210033474A (ko
Inventor
안나 마틸다 안젤리카 페테르센
제임스 맥케이브
카를-요한 오렐
Original Assignee
아스트라제네카 아베
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Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • 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)
  • 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)
KR1020217001860A 2018-07-18 2019-07-17 Jak 억제 화합물의 지나포에이트염 Active KR102849420B1 (ko)

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

Publications (2)

Publication Number Publication Date
KR20210033474A KR20210033474A (ko) 2021-03-26
KR102849420B1 true KR102849420B1 (ko) 2025-08-25

Family

ID=67396927

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217001860A Active KR102849420B1 (ko) 2018-07-18 2019-07-17 Jak 억제 화합물의 지나포에이트염

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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009031011A2 (en) 2007-09-05 2009-03-12 Pfizer Limited Xinafoate salt of n4-(2, 2-difluoro-4h-benz0 [1,4] 0xazin-3-one) -6-yl] -5-fluoro-n2- [3- (methylaminocar bonylmethyleneoxy) phenyl] 2, 4-pyrimidinediamine
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
PL3189045T3 (pl) 2014-08-11 2022-04-04 Sun Pharmaceutical Industries Limited Nowe sole nilotynibu i jego polimorfy
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
JP7422732B2 (ja) 2024-01-26
JP7644190B2 (ja) 2025-03-11
JP2021530526A (ja) 2021-11-11

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