CU24671B1 - Compuesto de pirimidina inhibidor de las janocinasas, composición, forma cristalina y proceso de preparación - Google Patents

Compuesto de pirimidina inhibidor de las janocinasas, composición, forma cristalina y proceso de preparación

Info

Publication number
CU24671B1
CU24671B1 CU2020000053A CU20200053A CU24671B1 CU 24671 B1 CU24671 B1 CU 24671B1 CU 2020000053 A CU2020000053 A CU 2020000053A CU 20200053 A CU20200053 A CU 20200053A CU 24671 B1 CU24671 B1 CU 24671B1
Authority
CU
Cuba
Prior art keywords
janokinase
inhibitor
crystalline form
composition
preparation process
Prior art date
Application number
CU2020000053A
Other languages
English (en)
Other versions
CU20200053A7 (es
Inventor
Gary E L Brandt
Marta Dabros
Ryan Hudson
Jennifer Kozak
Robert Murray Mckinnell
Jerry Nzerem
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 CU20200053A7 publication Critical patent/CU20200053A7/es
Publication of CU24671B1 publication Critical patent/CU24671B1/es

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
    • C07D451/14—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Dental Preparations (AREA)

Abstract

<p>La invención proporciona un compuesto de Ia fórmula (I):</p> <p>ESPACIO PARA FÓRMULA</p> <p>o una sal farmacéuticamente aceptable de este, que es un inhibidor de las janocinasas (JAK), composiciones farmaceúticas que comprenden dicho compuesto y una forma cristalina, útiles para tratar enfermedades inflamatorias de Ia piel y otras enfermedades. La invención también proporciona procesos y productos intermedios útiles para preparar dicho compuesto.</p>
CU2020000053A 2017-10-27 2018-10-26 Compuesto de pirimidina inhibidor de las janocinasas, composición, forma cristalina y proceso de preparación CU24671B1 (es)

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 (2)

Publication Number Publication Date
CU20200053A7 CU20200053A7 (es) 2021-03-11
CU24671B1 true CU24671B1 (es) 2023-07-12

Family

ID=64277858

Family Applications (1)

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CU2020000053A CU24671B1 (es) 2017-10-27 2018-10-26 Compuesto de pirimidina inhibidor de las janocinasas, composición, forma cristalina y proceso de preparación

Country Status (37)

Country Link
US (7) US10308646B2 (es)
EP (1) EP3672965B1 (es)
JP (1) JP7218364B2 (es)
KR (1) KR102613503B1 (es)
CN (1) CN111247142B (es)
AR (1) AR113803A1 (es)
AU (1) AU2018354370B2 (es)
BR (1) BR112020008015A2 (es)
CA (1) CA3074034A1 (es)
CL (1) CL2020001090A1 (es)
CR (1) CR20200180A (es)
CU (1) CU24671B1 (es)
DK (1) DK3672965T3 (es)
DO (1) DOP2020000083A (es)
EA (1) EA202091016A1 (es)
EC (1) ECSP20023795A (es)
ES (1) ES2932526T3 (es)
GE (1) GEP20227344B (es)
HR (1) HRP20221221T1 (es)
HU (1) HUE060401T2 (es)
IL (1) IL274037B2 (es)
LT (1) LT3672965T (es)
MA (1) MA49956B1 (es)
MD (1) MD3672965T2 (es)
MX (1) MX2020004255A (es)
NI (1) NI202000032A (es)
PE (1) PE20201495A1 (es)
PH (1) PH12020500528A1 (es)
PL (1) PL3672965T3 (es)
PT (1) PT3672965T (es)
RS (1) RS63608B1 (es)
SG (1) SG11202001706RA (es)
SI (1) SI3672965T1 (es)
TW (1) TWI789446B (es)
UA (1) UA125130C2 (es)
WO (1) WO2019084383A1 (es)
ZA (1) ZA202001641B (es)

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BR112020008015A2 (pt) 2017-10-27 2020-10-27 Theravance Biopharma R&D Ip, Llc composto derivado da pirimidina como inibidor da quinase jak
KR20210099611A (ko) * 2018-11-30 2021-08-12 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 헤테로 방향족 유도체 조절제, 이의 제조방법 및 용도
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
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors
IL300006A (en) * 2020-07-28 2023-03-01 Arcutis Biotherapeutics Inc A formulation for external use containing a JAK inhibitor and Orat-4
WO2022046861A1 (en) * 2020-08-26 2022-03-03 Nalo Therapeutics Modulators of myc family proto-oncogene protein
EP4225438A1 (en) * 2020-10-08 2023-08-16 Icahn School of Medicine at Mount Sinai Compositions for treatment alopecia areata, biomarkers for treatment success, and methods of use thereof
AU2022378463A1 (en) 2021-10-25 2024-05-09 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
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

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JP4105948B2 (ja) 2000-09-15 2008-06-25 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
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EP1831216A2 (en) * 2004-12-23 2007-09-12 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
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BR112020008015A2 (pt) * 2017-10-27 2020-10-27 Theravance Biopharma R&D Ip, Llc composto derivado da pirimidina como inibidor da quinase jak
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
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors

Also Published As

Publication number Publication date
MX2020004255A (es) 2020-07-29
UA125130C2 (uk) 2022-01-12
EA202091016A1 (ru) 2020-07-17
AU2018354370B2 (en) 2023-04-27
US10308646B2 (en) 2019-06-04
WO2019084383A1 (en) 2019-05-02
HUE060401T2 (hu) 2023-02-28
CL2020001090A1 (es) 2020-08-21
IL274037B2 (en) 2023-11-01
DOP2020000083A (es) 2020-08-15
US20240158389A1 (en) 2024-05-16
MD3672965T2 (ro) 2022-12-31
DK3672965T3 (da) 2022-10-03
KR20200078517A (ko) 2020-07-01
US10562894B2 (en) 2020-02-18
US20210214349A1 (en) 2021-07-15
KR102613503B1 (ko) 2023-12-13
US20190127364A1 (en) 2019-05-02
CA3074034A1 (en) 2019-05-02
PE20201495A1 (es) 2020-12-29
US20190241555A1 (en) 2019-08-08
US11420965B2 (en) 2022-08-23
US20200369660A1 (en) 2020-11-26
CU20200053A7 (es) 2021-03-11
US20220396573A1 (en) 2022-12-15
AU2018354370A1 (en) 2020-04-09
BR112020008015A2 (pt) 2020-10-27
JP7218364B2 (ja) 2023-02-06
PT3672965T (pt) 2022-09-29
ZA202001641B (en) 2021-04-28
AR113803A1 (es) 2020-06-10
IL274037A (en) 2020-06-30
MA49956A (fr) 2020-07-01
LT3672965T (lt) 2022-10-10
RS63608B1 (sr) 2022-10-31
GEP20227344B (en) 2022-01-25
CN111247142A (zh) 2020-06-05
JP2021501151A (ja) 2021-01-14
US10774080B2 (en) 2020-09-15
ECSP20023795A (es) 2020-06-30
US20200140430A1 (en) 2020-05-07
PH12020500528A1 (en) 2021-06-07
CR20200180A (es) 2020-08-12
EP3672965B1 (en) 2022-09-07
TW201930304A (zh) 2019-08-01
US11814377B2 (en) 2023-11-14
ES2932526T3 (es) 2023-01-20
US10988470B2 (en) 2021-04-27
CN111247142B (zh) 2022-12-02
PL3672965T3 (pl) 2023-01-16
HRP20221221T1 (hr) 2022-12-09
TWI789446B (zh) 2023-01-11
IL274037B1 (en) 2023-07-01
SI3672965T1 (sl) 2022-11-30
NI202000032A (es) 2020-10-09
SG11202001706RA (en) 2020-03-30
MA49956B1 (fr) 2022-11-30
EP3672965A1 (en) 2020-07-01

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