AU2017258186B2 - Pyrimidine compounds as JAK kinase inhibitors - Google Patents

Pyrimidine compounds as JAK kinase inhibitors Download PDF

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Publication number
AU2017258186B2
AU2017258186B2 AU2017258186A AU2017258186A AU2017258186B2 AU 2017258186 B2 AU2017258186 B2 AU 2017258186B2 AU 2017258186 A AU2017258186 A AU 2017258186A AU 2017258186 A AU2017258186 A AU 2017258186A AU 2017258186 B2 AU2017258186 B2 AU 2017258186B2
Authority
AU
Australia
Prior art keywords
amino
azabicyclo
pyrazol
methyl
nonan
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2017258186A
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English (en)
Other versions
AU2017258186A1 (en
Inventor
Anne-Marie Beausoleil
Paul R. Fatheree
Melissa Fleury
Xiaojun Huang
Ryan Hudson
Jennifer KOZAK
Dante D. PODESTO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Theravance Biopharma R&D IP LLC
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Publication date
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Publication of AU2017258186A1 publication Critical patent/AU2017258186A1/en
Application granted granted Critical
Publication of AU2017258186B2 publication Critical patent/AU2017258186B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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

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)
AU2017258186A 2016-04-28 2017-04-27 Pyrimidine compounds as JAK kinase inhibitors Ceased AU2017258186B2 (en)

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 (2)

Publication Number Publication Date
AU2017258186A1 AU2017258186A1 (en) 2018-11-15
AU2017258186B2 true AU2017258186B2 (en) 2020-09-17

Family

ID=58672793

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017258186A Ceased AU2017258186B2 (en) 2016-04-28 2017-04-27 Pyrimidine compounds as JAK kinase inhibitors

Country Status (20)

Country Link
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 (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016191524A1 (en) 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
US10556901B2 (en) 2015-11-03 2020-02-11 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
EP3865481A1 (en) 2015-11-03 2021-08-18 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
TWI726094B (zh) * 2016-04-28 2021-05-01 美商施萬生物製藥研發Ｉｐ有限責任公司 作為jak激酶抑制劑之嘧啶化合物
TWI789446B (zh) 2017-10-27 2023-01-11 美商施萬生物製藥研發 Ip有限責任公司 作為jak激酶抑制劑之嘧啶化合物
WO2019246273A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor
CN111601804B (zh) * 2018-11-27 2024-06-04 江苏豪森药业集团有限公司 含氮杂芳类衍生物调节剂、其制备方法和应用
WO2020108613A1 (zh) * 2018-11-30 2020-06-04 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
HUE067909T2 (hu) * 2019-04-24 2024-11-28 Theravance Biopharma R&D Ip Llc Pirimidin JAK-inhibitorok bõrbetegségek kezelésére
US11155549B2 (en) 2019-04-24 2021-10-26 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as JAK kinase inhibitors
JP2023528239A (ja) * 2020-05-14 2023-07-04 テラバンス バイオファーマ アールアンドディー アイピー リミテッド ライアビリティ カンパニー 腸管選択的ｊａｋ３阻害剤の投与
EP4225754A1 (en) * 2020-10-09 2023-08-16 Theravance Biopharma R&D IP, LLC Processes for preparing a pan-jak inhibitor and related intermediate compounds
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

Citations (2)

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WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US20160052930A1 (en) * 2014-08-21 2016-02-25 Pfizer Inc. Aminopyrimidinyl compounds

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US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7625913B2 (en) 2000-12-21 2009-12-01 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1841760B1 (en) * 2004-12-30 2011-08-10 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
WO2008001070A1 (en) 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
AU2007269540B2 (en) 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
CA2854248A1 (en) 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag 2,4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors
WO2016191524A1 (en) 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
TWI726094B (zh) 2016-04-28 2021-05-01 美商施萬生物製藥研發Ｉｐ有限責任公司 作為jak激酶抑制劑之嘧啶化合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US20160052930A1 (en) * 2014-08-21 2016-02-25 Pfizer Inc. Aminopyrimidinyl compounds

Also Published As

Publication number Publication date
US10485803B2 (en) 2019-11-26
MX2018013191A (es) 2019-02-13
WO2017189822A1 (en) 2017-11-02
EA035226B1 (ru) 2020-05-19
US20180303836A1 (en) 2018-10-25
DK3433253T3 (da) 2020-04-06
BR112018072168A2 (pt) 2019-02-12
IL262386B (en) 2021-08-31
EA201892436A1 (ru) 2019-04-30
ZA201807179B (en) 2019-08-28
JP6881879B2 (ja) 2021-06-02
KR20190002591A (ko) 2019-01-08
CN109071529A (zh) 2018-12-21
AU2017258186A1 (en) 2018-11-15
JP2019514903A (ja) 2019-06-06
MX377180B (es) 2025-03-07
US20200046709A1 (en) 2020-02-13
IL262386A (en) 2018-11-29
US10028960B2 (en) 2018-07-24
SG11201809342YA (en) 2018-11-29
ES2779880T3 (es) 2020-08-20
KR102244257B1 (ko) 2021-04-26
CL2018003060A1 (es) 2018-12-14
TWI726094B (zh) 2021-05-01
CN109071529B (zh) 2021-08-06
PT3433253T (pt) 2020-04-30
US20170312280A1 (en) 2017-11-02
EP3433253A1 (en) 2019-01-30
TW201739747A (zh) 2017-11-16
US11110095B2 (en) 2021-09-07
CO2018011408A2 (es) 2018-11-13
CA3020506A1 (en) 2017-11-02
EP3433253B1 (en) 2020-02-12

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired