AU2017258186B2 - Pyrimidine compounds as JAK kinase inhibitors - Google Patents

Pyrimidine compounds as JAK kinase inhibitors Download PDF

Info

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
Other languages
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
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 Theravance Biopharma R&D IP LLC filed Critical Theravance Biopharma R&D IP LLC
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

Links

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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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
EP3303348B1 (en) 2015-05-28 2019-08-07 Theravance Biopharma R&D IP, LLC Naphthyridine compounds as jak kinase inhibitors
WO2017077283A1 (en) 2015-11-03 2017-05-11 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
ES2840650T3 (es) 2015-11-03 2021-07-07 Topivert Pharma Ltd Derivados de 4,5,6,7-tetrahidro-1h-imidazo[4,5-c]piridina y 1,4,5,6,7,8-hexahidroimidazo[4,5-d]azepina como inhibidores de la quinasa janus
CA3020506A1 (en) * 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors
SMT202200409T1 (it) 2017-10-27 2022-11-18 Theravance Biopharma R&D Ip Llc Composto di pirimidina come inibitore di chinasi 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
CA3121408A1 (en) * 2018-11-30 2020-06-04 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Heteroaromatic derivatives for use as regulator, preparation method therefor and use thereof
TW202106681A (zh) 2019-04-24 2021-02-16 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療皮膚疾病之嘧啶jak抑制劑
WO2020219639A1 (en) 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as jak kinase inhibitors
EP4149462A4 (en) * 2020-05-14 2024-04-24 Theravance Biopharma R&D IP, LLC Administration of gut-selective jak3 inhibitor
CN116368134A (zh) * 2020-10-09 2023-06-30 施万生物制药研发Ip有限责任公司 制备泛jak抑制剂的方法和相关中间体化合物
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
WO2025059417A1 (en) * 2023-09-15 2025-03-20 Morphic Therapeutic, Inc. INHIBITING HUMAN INTEGRIN α4β7

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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
NZ526468A (en) 2000-12-21 2004-03-26 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
DE602006021776D1 (de) 2005-11-16 2011-06-16 Vertex Pharma Als kinaseinhibitoren geeignete aminopyrimidine
EP2044063A1 (en) 2006-06-30 2009-04-08 Astra Zeneca AB Pyrimidine derivatives useful in the treatment of cancer
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR and ABL kinase modulators
KR20140103972A (ko) 2011-12-22 2014-08-27 에프. 호프만-라 로슈 아게 세린/트레오닌 키나아제 억제제로서의 2,4-다이아민-피리미딘 유도체
EP3303348B1 (en) 2015-05-28 2019-08-07 Theravance Biopharma R&D IP, LLC Naphthyridine compounds as jak kinase inhibitors
CA3020506A1 (en) 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors

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

Similar Documents

Publication Publication Date Title
AU2017258186B2 (en) Pyrimidine compounds as JAK kinase inhibitors
US11780852B2 (en) Methods for treating Crohn&#39;s disease using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile
WO2019027960A1 (en) BICYCLIC PYRAZOLO AND TRIAZOLO COMPOUNDS AS JAK KINASE INHIBITORS
CA3125039A1 (en) Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
HK40003022B (en) Pyrimidine compounds as jak kinase inhibitors
HK40003022A (en) Pyrimidine compounds as jak kinase inhibitors
HK40014855A (en) Process and intermediates for the preparation of naphthyridine compounds as jak kinase inhibitors
HK1245771B (en) Naphthyridine compounds as jak kinase inhibitors

Legal Events

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