IL274037B2 - A pyrimidine compound as a JAK kinase inhibitor - Google Patents

A pyrimidine compound as a JAK kinase inhibitor

Info

Publication number
IL274037B2
IL274037B2 IL274037A IL27403720A IL274037B2 IL 274037 B2 IL274037 B2 IL 274037B2 IL 274037 A IL274037 A IL 274037A IL 27403720 A IL27403720 A IL 27403720A IL 274037 B2 IL274037 B2 IL 274037B2
Authority
IL
Israel
Prior art keywords
compound
crystalline form
formula
acceptable salt
pharmaceutical composition
Prior art date
Application number
IL274037A
Other languages
English (en)
Hebrew (he)
Other versions
IL274037B1 (en
IL274037A (en
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 IL274037A publication Critical patent/IL274037A/en
Publication of IL274037B1 publication Critical patent/IL274037B1/en
Publication of IL274037B2 publication Critical patent/IL274037B2/en

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
IL274037A 2017-10-27 2018-10-26 A pyrimidine compound as a JAK kinase inhibitor IL274037B2 (en)

Applications Claiming Priority (2)

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

Publications (3)

Publication Number Publication Date
IL274037A IL274037A (en) 2020-06-30
IL274037B1 IL274037B1 (en) 2023-07-01
IL274037B2 true IL274037B2 (en) 2023-11-01

Family

ID=64277858

Family Applications (1)

Application Number Title Priority Date Filing Date
IL274037A IL274037B2 (en) 2017-10-27 2018-10-26 A pyrimidine compound as a JAK kinase inhibitor

Country Status (38)

Country Link
US (7) US10308646B2 (https=)
EP (1) EP3672965B1 (https=)
JP (1) JP7218364B2 (https=)
KR (1) KR102613503B1 (https=)
CN (1) CN111247142B (https=)
AR (1) AR113803A1 (https=)
AU (1) AU2018354370B2 (https=)
BR (1) BR112020008015A2 (https=)
CA (1) CA3074034A1 (https=)
CL (1) CL2020001090A1 (https=)
CR (1) CR20200180A (https=)
CU (1) CU24671B1 (https=)
DK (1) DK3672965T3 (https=)
DO (1) DOP2020000083A (https=)
EA (1) EA202091016A1 (https=)
EC (1) ECSP20023795A (https=)
ES (1) ES2932526T3 (https=)
GE (2) GEAP202115340A (https=)
HR (1) HRP20221221T1 (https=)
HU (1) HUE060401T2 (https=)
IL (1) IL274037B2 (https=)
LT (1) LT3672965T (https=)
MA (1) MA49956B1 (https=)
MD (1) MD3672965T2 (https=)
MX (1) MX2020004255A (https=)
NI (1) NI202000032A (https=)
PE (1) PE20201495A1 (https=)
PH (1) PH12020500528A1 (https=)
PL (1) PL3672965T3 (https=)
PT (1) PT3672965T (https=)
RS (1) RS63608B1 (https=)
SG (1) SG11202001706RA (https=)
SI (1) SI3672965T1 (https=)
SM (1) SMT202200409T1 (https=)
TW (1) TWI789446B (https=)
UA (1) UA125130C2 (https=)
WO (1) WO2019084383A1 (https=)
ZA (1) ZA202001641B (https=)

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HRP20221221T1 (hr) 2017-10-27 2022-12-09 Theravance Biopharma R&D Ip, Llc Pirimidinski spoj kao inhibitor jak kinaze
JP2022510980A (ja) * 2018-11-30 2022-01-28 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 ヘテロ芳香族誘導体調節因子、その製造方法及び使用
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
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors
BR112023001283A2 (pt) 2020-07-28 2023-02-14 Arcutis Biotherapeutics Inc Composição farmacêutica tópica; método para tratar uma doença, distúrbio ou afecção inflamatória de pele em um indivíduo que necessita do mesmo; e método para intensificar a penetração em pele em um indivíduo de uma formulação farmacêutica tópica
AU2021333760A1 (en) * 2020-08-26 2023-04-06 Nalo Therapeutics Modulators of Myc family proto-oncogene protein
EP4225438A4 (en) * 2020-10-08 2025-02-19 Icahn School of Medicine at Mount Sinai COMPOSITIONS FOR THE TREATMENT OF 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
JP2024539280A (ja) 2021-10-25 2024-10-28 カイメラ セラピューティクス, インコーポレイテッド Tyk2分解剤およびそれらの使用
KR20240125610A (ko) 2021-12-15 2024-08-19 아큐티스 바이오테라퓨틱스, 인크. Shr0302의 안정된 제형
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

Citations (3)

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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
WO2016191524A1 (en) * 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors

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US4919934A (en) 1989-03-02 1990-04-24 Richardson-Vicks Inc. Cosmetic sticks
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
NZ526472A (en) 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
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
CA2629781A1 (en) 2005-11-16 2007-05-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
JP2009541480A (ja) 2006-06-30 2009-11-26 アストラゼネカ アクチボラグ 癌の治療において有用なピリミジン誘導体
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
BR112014015549A8 (pt) 2011-12-22 2017-07-04 Hoffmann La Roche composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção
JP2017535520A (ja) * 2014-09-30 2017-11-30 ハンミ・ファイン・ケミカル・カンパニー・リミテッドHanmi Fine Chemical Co., Ltd. 高純度の(r)−9−[2−(ホスホノメトキシ)プロピル]アデニンの製造方法
WO2017044434A1 (en) * 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
MX377180B (es) * 2016-04-28 2025-03-07 Theravance Biopharma R&D Ip Llc Compuestos de pirimidina como inhibidores de la quinasa jak.
HRP20221221T1 (hr) * 2017-10-27 2022-12-09 Theravance Biopharma R&D Ip, Llc Pirimidinski spoj kao inhibitor jak kinaze
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors
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

Patent Citations (3)

* 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
WO2016191524A1 (en) * 2015-05-28 2016-12-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors

Also Published As

Publication number Publication date
AU2018354370B2 (en) 2023-04-27
GEAP202115340A (en) 2021-08-10
ES2932526T3 (es) 2023-01-20
MX2020004255A (es) 2020-07-29
EP3672965B1 (en) 2022-09-07
US20220396573A1 (en) 2022-12-15
CU20200053A7 (es) 2021-03-11
CR20200180A (es) 2020-08-12
WO2019084383A1 (en) 2019-05-02
MA49956A (fr) 2020-07-01
US10988470B2 (en) 2021-04-27
US10562894B2 (en) 2020-02-18
PT3672965T (pt) 2022-09-29
US20200369660A1 (en) 2020-11-26
BR112020008015A2 (pt) 2020-10-27
PE20201495A1 (es) 2020-12-29
PL3672965T3 (pl) 2023-01-16
UA125130C2 (uk) 2022-01-12
US20190127364A1 (en) 2019-05-02
EA202091016A1 (ru) 2020-07-17
DK3672965T3 (da) 2022-10-03
MD3672965T2 (ro) 2022-12-31
TW201930304A (zh) 2019-08-01
CU24671B1 (es) 2023-07-12
ECSP20023795A (es) 2020-06-30
SG11202001706RA (en) 2020-03-30
HUE060401T2 (hu) 2023-02-28
US20190241555A1 (en) 2019-08-08
JP7218364B2 (ja) 2023-02-06
CA3074034A1 (en) 2019-05-02
RS63608B1 (sr) 2022-10-31
CN111247142B (zh) 2022-12-02
US11420965B2 (en) 2022-08-23
EP3672965A1 (en) 2020-07-01
HRP20221221T1 (hr) 2022-12-09
SMT202200409T1 (it) 2022-11-18
US10308646B2 (en) 2019-06-04
IL274037B1 (en) 2023-07-01
US12172994B2 (en) 2024-12-24
US10774080B2 (en) 2020-09-15
AR113803A1 (es) 2020-06-10
TWI789446B (zh) 2023-01-11
US11814377B2 (en) 2023-11-14
MA49956B1 (fr) 2022-11-30
IL274037A (en) 2020-06-30
JP2021501151A (ja) 2021-01-14
ZA202001641B (en) 2021-04-28
DOP2020000083A (es) 2020-08-15
PH12020500528A1 (en) 2021-06-07
SI3672965T1 (sl) 2022-11-30
KR102613503B1 (ko) 2023-12-13
US20210214349A1 (en) 2021-07-15
CN111247142A (zh) 2020-06-05
US20240158389A1 (en) 2024-05-16
CL2020001090A1 (es) 2020-08-21
LT3672965T (lt) 2022-10-10
NI202000032A (es) 2020-10-09
US20200140430A1 (en) 2020-05-07
KR20200078517A (ko) 2020-07-01
GEP20227344B (en) 2022-01-25
AU2018354370A1 (en) 2020-04-09

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