JP7218364B2 - Jakキナーゼ阻害剤としてのピリミジン化合物 - Google Patents

Jakキナーゼ阻害剤としてのピリミジン化合物 Download PDF

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JP7218364B2
JP7218364B2 JP2020523324A JP2020523324A JP7218364B2 JP 7218364 B2 JP7218364 B2 JP 7218364B2 JP 2020523324 A JP2020523324 A JP 2020523324A JP 2020523324 A JP2020523324 A JP 2020523324A JP 7218364 B2 JP7218364 B2 JP 7218364B2
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compound
pharmaceutically acceptable
pharmaceutical composition
acceptable salt
inflammatory
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JP2021501151A (ja
JP2021501151A5 (OSRAM
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ジェニファー コザック,
ライアン ハドソン,
ゲイリー イー.エル. ブラント,
ロバート マレー マッキネル,
マータ ダブロス,
ジェリー ゼレム,
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セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Dental Preparations (AREA)
JP2020523324A 2017-10-27 2018-10-26 Jakキナーゼ阻害剤としてのピリミジン化合物 Active JP7218364B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762577852P 2017-10-27 2017-10-27
US62/577,852 2017-10-27
PCT/US2018/057682 WO2019084383A1 (en) 2017-10-27 2018-10-26 PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS

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JP2021501151A JP2021501151A (ja) 2021-01-14
JP2021501151A5 JP2021501151A5 (OSRAM) 2021-09-30
JP7218364B2 true JP7218364B2 (ja) 2023-02-06

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EP (1) EP3672965B1 (OSRAM)
JP (1) JP7218364B2 (OSRAM)
KR (1) KR102613503B1 (OSRAM)
CN (1) CN111247142B (OSRAM)
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SG11202001706RA (en) * 2017-10-27 2020-03-30 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
US20230043863A1 (en) * 2018-11-30 2023-02-09 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Heteroaromatic derivatives for use as regulator, preparation method therefor and use thereof
CA3135383A1 (en) * 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as jak kinase inhibitors
EP3959213B1 (en) * 2019-04-24 2024-06-05 Theravance Biopharma R&D IP, LLC Pyrimidine jak inhibitors for the treatment of skin diseases
IL300006A (en) 2020-07-28 2023-03-01 Arcutis Biotherapeutics Inc A formulation for external use containing a JAK inhibitor and Orat-4
US20230322722A1 (en) * 2020-08-26 2023-10-12 Nalo Therapeutics Modulators of myc family proto-oncogene protein
US20230374124A1 (en) * 2020-10-08 2023-11-23 Icahn School Of Medicine At Mount Sinai Compositions for treatment alopecia areata, biomarkers for treatment success and, methods of use thereof
TW202311256A (zh) * 2021-06-18 2023-03-16 美商基利科學股份有限公司 用於治療fxr誘發之搔癢之il-31調節劑
AU2022378463A1 (en) 2021-10-25 2024-05-09 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
EP4447930A1 (en) 2021-12-15 2024-10-23 Arcutis Biotherapeutics, Inc. Stable formulations of shr0302
CN114246938A (zh) * 2022-01-25 2022-03-29 中山大学中山眼科中心 Il-4在制备用于治疗视网膜变性疾病药物中的应用
CN115487301B (zh) * 2022-11-08 2023-07-07 四川大学华西医院 Il-13抑制剂在制备延缓或治疗视网膜色素变性的药物中的用途

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JP2008525422A (ja) 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
WO2015094803A1 (en) 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
WO2016191524A1 (en) 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
WO2017044434A1 (en) 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
JP2017524022A (ja) 2014-08-21 2017-08-24 ファイザー・インク Jak阻害剤としてのアミノピリミジニル化合物
WO2017189822A1 (en) 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors

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SG11202001706RA (en) 2017-10-27 2020-03-30 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
EP3959213B1 (en) 2019-04-24 2024-06-05 Theravance Biopharma R&D IP, LLC Pyrimidine jak inhibitors for the treatment of skin diseases
CA3135383A1 (en) 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as jak kinase inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008525422A (ja) 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
WO2015094803A1 (en) 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
JP2017524022A (ja) 2014-08-21 2017-08-24 ファイザー・インク Jak阻害剤としてのアミノピリミジニル化合物
WO2016191524A1 (en) 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
WO2017044434A1 (en) 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
WO2017189822A1 (en) 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors

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PE20201495A1 (es) 2020-12-29
EA202091016A1 (ru) 2020-07-17
US20240158389A1 (en) 2024-05-16
US10562894B2 (en) 2020-02-18
MD3672965T2 (ro) 2022-12-31
ECSP20023795A (es) 2020-06-30
JP2021501151A (ja) 2021-01-14
US10774080B2 (en) 2020-09-15
IL274037B2 (en) 2023-11-01
IL274037A (en) 2020-06-30
MX2020004255A (es) 2020-07-29
HUE060401T2 (hu) 2023-02-28
AU2018354370A1 (en) 2020-04-09
CL2020001090A1 (es) 2020-08-21
TW201930304A (zh) 2019-08-01
ZA202001641B (en) 2021-04-28
DK3672965T3 (da) 2022-10-03
US20190241555A1 (en) 2019-08-08
US20200369660A1 (en) 2020-11-26
NI202000032A (es) 2020-10-09
EP3672965B1 (en) 2022-09-07
CA3074034A1 (en) 2019-05-02
TWI789446B (zh) 2023-01-11
KR102613503B1 (ko) 2023-12-13
WO2019084383A1 (en) 2019-05-02
EP3672965A1 (en) 2020-07-01
US11420965B2 (en) 2022-08-23
CU20200053A7 (es) 2021-03-11
SG11202001706RA (en) 2020-03-30
PH12020500528A1 (en) 2021-06-07
GEP20227344B (en) 2022-01-25
US11814377B2 (en) 2023-11-14
AR113803A1 (es) 2020-06-10
IL274037B1 (en) 2023-07-01
US12172994B2 (en) 2024-12-24
SMT202200409T1 (it) 2022-11-18
US10308646B2 (en) 2019-06-04
CN111247142A (zh) 2020-06-05
US20220396573A1 (en) 2022-12-15
ES2932526T3 (es) 2023-01-20
LT3672965T (lt) 2022-10-10
US20190127364A1 (en) 2019-05-02
US10988470B2 (en) 2021-04-27
MA49956A (fr) 2020-07-01
PT3672965T (pt) 2022-09-29
UA125130C2 (uk) 2022-01-12
PL3672965T3 (pl) 2023-01-16
CR20200180A (es) 2020-08-12
DOP2020000083A (es) 2020-08-15
HRP20221221T1 (hr) 2022-12-09
BR112020008015A2 (pt) 2020-10-27
SI3672965T1 (sl) 2022-11-30
CU24671B1 (es) 2023-07-12
US20210214349A1 (en) 2021-07-15
MA49956B1 (fr) 2022-11-30
KR20200078517A (ko) 2020-07-01
US20200140430A1 (en) 2020-05-07
RS63608B1 (sr) 2022-10-31
AU2018354370B2 (en) 2023-04-27
CN111247142B (zh) 2022-12-02

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