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EA201892436A1 - Пиримидиновые соединения в качестве ингибиторов jak киназы - Google Patents

Пиримидиновые соединения в качестве ингибиторов jak киназы

Info

Publication number
EA201892436A1
EA201892436A1 EA201892436A EA201892436A EA201892436A1 EA 201892436 A1 EA201892436 A1 EA 201892436A1 EA 201892436 A EA201892436 A EA 201892436A EA 201892436 A EA201892436 A EA 201892436A EA 201892436 A1 EA201892436 A1 EA 201892436A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
compounds
pyrimidine compounds
jak kinase
methods
Prior art date
Application number
EA201892436A
Other languages
English (en)
Other versions
EA035226B1 (ru
Inventor
Райан Хадсон
Дженнифер Козак
Мелисса Флери
Пол Р. Фазери
Анн-Мари Босолей
Данте Д. Подесто
Сяоцзюнь Хуан
Original Assignee
ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи filed Critical ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи
Publication of EA201892436A1 publication Critical patent/EA201892436A1/ru
Publication of EA035226B1 publication Critical patent/EA035226B1/ru

Links

Classifications

    • 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
    • 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
    • C07D451/14—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

Landscapes

  • 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)

Abstract

В изобретении предложены соединения формулы (I)где переменные имеют значение, определенное в описании изобретения, или фармацевтически приемлемая соль такого соединения, которые являются ингибиторами JAK киназ. Изобретение также обеспечивает фармацевтические композиции, включающие такие соединения, способы применения таких соединений для лечения желудочно-кишечных и других воспалительных заболеваний и способы и промежуточные соединения, полезные для получения таких соединений.
EA201892436A 2016-04-28 2017-04-27 Пиримидиновые соединения в качестве ингибиторов jak киназы EA035226B1 (ru)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
EA201892436A1 true EA201892436A1 (ru) 2019-04-30
EA035226B1 EA035226B1 (ru) 2020-05-19

Family

ID=58672793

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201892436A EA035226B1 (ru) 2016-04-28 2017-04-27 Пиримидиновые соединения в качестве ингибиторов jak киназы

Country Status (20)

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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3303348B1 (en) 2015-05-28 2019-08-07 Theravance Biopharma R&D IP, LLC Naphthyridine compounds as jak kinase inhibitors
PL3712152T3 (pl) 2015-11-03 2021-08-02 Topivert Pharma Limited Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych
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
AU2017258186B2 (en) 2016-04-28 2020-09-17 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors
GEP20227344B (en) 2017-10-27 2022-01-25 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
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
AR118767A1 (es) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc Pirimidinas sustituidas como inhibidores de jak y su uso para el tratamiento de enfermedades inflamatorias o autoinmunes cutáneas
HUE066802T2 (hu) 2019-04-24 2024-09-28 Theravance Biopharma R&D Ip Llc JAK kináz inhibitor észter és karbonát pirimidin vegyületek
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
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
WO2025059417A1 (en) * 2023-09-15 2025-03-20 Morphic Therapeutic, Inc. INHIBITING HUMAN INTEGRIN α4β7

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US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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JP5208516B2 (ja) * 2004-12-30 2013-06-12 エグゼリクシス， インコーポレイテッド キナーゼモジュレーターとしてのピリミジン誘導体および使用方法
JP2009515992A (ja) 2005-11-16 2009-04-16 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用なアミノピリミジン
CA2654852A1 (en) 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
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EP3303348B1 (en) 2015-05-28 2019-08-07 Theravance Biopharma R&D IP, LLC Naphthyridine compounds as jak kinase inhibitors
AU2017258186B2 (en) 2016-04-28 2020-09-17 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors

Also Published As

Publication number Publication date
JP2019514903A (ja) 2019-06-06
ZA201807179B (en) 2019-08-28
EP3433253B1 (en) 2020-02-12
US10485803B2 (en) 2019-11-26
MX377180B (es) 2025-03-07
US20200046709A1 (en) 2020-02-13
CO2018011408A2 (es) 2018-11-13
KR102244257B1 (ko) 2021-04-26
BR112018072168A2 (pt) 2019-02-12
CN109071529A (zh) 2018-12-21
DK3433253T3 (da) 2020-04-06
ES2779880T3 (es) 2020-08-20
AU2017258186A1 (en) 2018-11-15
SG11201809342YA (en) 2018-11-29
US20170312280A1 (en) 2017-11-02
US10028960B2 (en) 2018-07-24
US20180303836A1 (en) 2018-10-25
IL262386B (en) 2021-08-31
TWI726094B (zh) 2021-05-01
JP6881879B2 (ja) 2021-06-02
KR20190002591A (ko) 2019-01-08
CN109071529B (zh) 2021-08-06
AU2017258186B2 (en) 2020-09-17
TW201739747A (zh) 2017-11-16
EP3433253A1 (en) 2019-01-30
WO2017189822A1 (en) 2017-11-02
US11110095B2 (en) 2021-09-07
MX2018013191A (es) 2019-02-13
EA035226B1 (ru) 2020-05-19
PT3433253T (pt) 2020-04-30
CL2018003060A1 (es) 2018-12-14
CA3020506A1 (en) 2017-11-02
IL262386A (en) 2018-11-29

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