JP6881879B2 - 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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JP6881879B2
JP6881879B2 JP2018555938A JP2018555938A JP6881879B2 JP 6881879 B2 JP6881879 B2 JP 6881879B2 JP 2018555938 A JP2018555938 A JP 2018555938A JP 2018555938 A JP2018555938 A JP 2018555938A JP 6881879 B2 JP6881879 B2 JP 6881879B2
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amino
azabicyclo
methyl
pyrazole
nonane
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JP2019514903A5 (enExample
JP2019514903A (ja
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ライアン ハドソン，
ライアン ハドソン，
ジェニファー コザック，
ジェニファー コザック，
メリッサ フルーリー，
メリッサ フルーリー，
ポール アール． ファザリー，
ポール アール． ファザリー，
アン−マリー ボーソレイユ，
アン−マリー ボーソレイユ，
ダンテ ディー． ポデスト，
ダンテ ディー． ポデスト，
シャオジュン ファン，
シャオジュン ファン，
Original Assignee
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
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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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2018555938A 2016-04-28 2017-04-27 Ｊａｋキナーゼ阻害剤としてのピリミジン化合物 Active JP6881879B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662328737P 2016-04-28 2016-04-28
US62/328,737 2016-04-28
PCT/US2017/029796 WO2017189822A1 (en) 2016-04-28 2017-04-27 Pyrimidine compounds as jak kinase inhibitors

Publications (3)

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JP2019514903A JP2019514903A (ja) 2019-06-06
JP2019514903A5 JP2019514903A5 (enExample) 2020-04-23
JP6881879B2 true JP6881879B2 (ja) 2021-06-02

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JP2018555938A Active JP6881879B2 (ja) 2016-04-28 2017-04-27 Ｊａｋキナーゼ阻害剤としてのピリミジン化合物

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US (3) US10028960B2 (enExample)
EP (1) EP3433253B1 (enExample)
JP (1) JP6881879B2 (enExample)
KR (1) KR102244257B1 (enExample)
CN (1) CN109071529B (enExample)
AU (1) AU2017258186B2 (enExample)
BR (1) BR112018072168A2 (enExample)
CA (1) CA3020506A1 (enExample)
CL (1) CL2018003060A1 (enExample)
CO (1) CO2018011408A2 (enExample)
DK (1) DK3433253T3 (enExample)
EA (1) EA035226B1 (enExample)
ES (1) ES2779880T3 (enExample)
IL (1) IL262386B (enExample)
MX (1) MX377180B (enExample)
PT (1) PT3433253T (enExample)
SG (1) SG11201809342YA (enExample)
TW (1) TWI726094B (enExample)
WO (1) WO2017189822A1 (enExample)
ZA (1) ZA201807179B (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
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ES2924698T3 (es) 2015-05-28 2022-10-10 Theravance Biopharma R&D Ip Llc Proceso e intermedios para la preparación de compuestos de naftiridina como inhibidores de quinasa JAK
EP3831830A1 (en) 2015-11-03 2021-06-09 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
DK3712152T3 (da) 2015-11-03 2021-03-22 Topivert Pharma Ltd 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridin og 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepinderivater som janus kinase-inhibitorer
WO2017189822A1 (en) * 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors
MA49956B1 (fr) 2017-10-27 2022-11-30 Theravance Biopharma R&D Ip Llc Composés de pyrimidine utilisés en tant qu'inhibiteurs de kinase jak
US12171764B2 (en) 2018-06-20 2024-12-24 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a JAK or other kinase inhibitor
TWI740288B (zh) * 2018-11-27 2021-09-21 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
CN115925705B (zh) * 2018-11-30 2024-12-31 江苏豪森药业集团有限公司 杂芳类衍生物调节剂、其制备方法和应用
JP7482152B2 (ja) * 2019-04-24 2024-05-13 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 皮膚疾患の処置のためのピリミジンｊａｋ阻害剤 発明の背景
JP7470713B2 (ja) * 2019-04-24 2024-04-18 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 Ｊａｋキナーゼ阻害剤としてのエステルおよびカルボナートピリミジン化合物
TW202207918A (zh) * 2020-05-14 2022-03-01 美商施萬生物製藥研發Ｉｐ有限責任公司 腸道選擇性ｊａｋ３抑制劑的投與
TW202233636A (zh) * 2020-10-09 2022-09-01 美商賽若凡斯生物製藥研發智財有限責任公司 製備泛ｊａｋ抑制劑之方法及相關中間化合物
WO2022083687A1 (zh) * 2020-10-21 2022-04-28 南京明德新药研发有限公司 硒杂环类化合物及其应用
WO2023011359A1 (zh) * 2021-08-05 2023-02-09 南京明德新药研发有限公司 桥环类化合物及其应用
CN113883920B (zh) * 2021-10-25 2024-01-23 安徽华铂再生资源科技有限公司 一种降低空分装置空冷塔出口温度的方法
WO2023202706A1 (zh) * 2022-04-21 2023-10-26 南京明德新药研发有限公司 硒杂环类化合物的盐型和晶型及其应用
WO2025040148A1 (zh) * 2023-08-22 2025-02-27 北京普祺医药科技股份有限公司 一种用于jak抑制剂的外用凝胶及其用途
TW202515852A (zh) * 2023-09-15 2025-04-16 美商莫菲克醫療股份有限公司 抑制人類整合素α４β７
US12684500B2 (en) 2024-01-17 2026-07-14 T-Mobile Usa, Inc. Dynamic scheduling request framework for HP UE SAR reduction

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BR0116493A (pt) 2000-12-21 2003-09-30 Vertex Pharma Compostos de pirazol úteis como inibidores de proteìna cinase
US8211929B2 (en) * 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
ATE508126T1 (de) 2005-11-16 2011-05-15 Vertex Pharma Als kinaseinhibitoren geeignete aminopyrimidine
TW200817391A (en) 2006-06-30 2008-04-16 Astrazeneca Ab Novel compounds
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RU2014129740A (ru) 2011-12-22 2016-02-10 Ф.Хоффманн-Ля Рош Аг Производные 2,4-диаминопиримидина в качестве ингибиторов серин/треонин киназы
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
NO2721710T3 (enExample) * 2014-08-21 2018-03-31
ES2924698T3 (es) 2015-05-28 2022-10-10 Theravance Biopharma R&D Ip Llc Proceso e intermedios para la preparación de compuestos de naftiridina como inhibidores de quinasa JAK
WO2017189822A1 (en) * 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors

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Publication number Publication date
MX377180B (es) 2025-03-07
PT3433253T (pt) 2020-04-30
TW201739747A (zh) 2017-11-16
TWI726094B (zh) 2021-05-01
US20200046709A1 (en) 2020-02-13
AU2017258186B2 (en) 2020-09-17
IL262386A (en) 2018-11-29
MX2018013191A (es) 2019-02-13
EA035226B1 (ru) 2020-05-19
WO2017189822A1 (en) 2017-11-02
DK3433253T3 (da) 2020-04-06
CO2018011408A2 (es) 2018-11-13
KR102244257B1 (ko) 2021-04-26
CL2018003060A1 (es) 2018-12-14
AU2017258186A1 (en) 2018-11-15
IL262386B (en) 2021-08-31
US10028960B2 (en) 2018-07-24
US20170312280A1 (en) 2017-11-02
CA3020506A1 (en) 2017-11-02
ES2779880T3 (es) 2020-08-20
CN109071529B (zh) 2021-08-06
US10485803B2 (en) 2019-11-26
JP2019514903A (ja) 2019-06-06
SG11201809342YA (en) 2018-11-29
KR20190002591A (ko) 2019-01-08
EP3433253A1 (en) 2019-01-30
US20180303836A1 (en) 2018-10-25
CN109071529A (zh) 2018-12-21
ZA201807179B (en) 2019-08-28
BR112018072168A2 (pt) 2019-02-12
EA201892436A1 (ru) 2019-04-30
EP3433253B1 (en) 2020-02-12
US11110095B2 (en) 2021-09-07

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