AR114810A1 - Procesos e intermedios para elaborar un inhibidor de jak - Google Patents

Procesos e intermedios para elaborar un inhibidor de jak

Info

Publication number
AR114810A1
AR114810A1 ARP190100197A ARP190100197A AR114810A1 AR 114810 A1 AR114810 A1 AR 114810A1 AR P190100197 A ARP190100197 A AR P190100197A AR P190100197 A ARP190100197 A AR P190100197A AR 114810 A1 AR114810 A1 AR 114810A1
Authority
AR
Argentina
Prior art keywords
compound
formula
salt
intermediates
processes
Prior art date
Application number
ARP190100197A
Other languages
English (en)
Inventor
Jiacheng Zhou
Yongzhong Wu
Pingli Liu
Dingjin Wang
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of AR114810A1 publication Critical patent/AR114810A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/803Processes of preparation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents

Abstract

Procesos e intermediarios para producir {1-{1-[3-fluoro-2-(trifluorometil)isonicotinioil]piperidin-4-il}-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-]azetidin-3-il}acetonitrilo el cual se utiliza para el tratamiento de enfermedades relacionadas con la actividad de cinasas Janus (JAK) entre las cuales se incluye entre otras a cáncer, trastornos inflamatorios y autoinmunes. Reivindicación 1: Un proceso que comprende hacer reaccionar un compuesto de la fórmula (3), o una sal de este, con 4-hidroxipiperidina para formar un compuesto de la fórmula (4), o una sal de este. Reivindicación 11: El proceso de cualquiera de las reivindicaciones 1 - 10, que comprende, además, hacer reaccionar el compuesto de la fórmula (4), o una sal de este, en condiciones de oxidación para formar un compuesto de fórmula (5), o una sal de este. Reivindicación 25: El proceso de cualquiera de las reivindicaciones 11 - 24, que comprende, además, hacer reaccionar el compuesto de la fórmula (5) con un compuesto de la fórmula (6), o una sal de este; en presencia de un agente de reducción para formar un compuesto de la fórmula (1) o una sal de este; donde Z¹ es H o un grupo protector. Reivindicación 44: Un compuesto de fórmula (3), o una sal de este.
ARP190100197A 2018-01-30 2019-01-29 Procesos e intermedios para elaborar un inhibidor de jak AR114810A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201862623664P 2018-01-30 2018-01-30

Publications (1)

Publication Number Publication Date
AR114810A1 true AR114810A1 (es) 2020-10-21

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190100197A AR114810A1 (es) 2018-01-30 2019-01-29 Procesos e intermedios para elaborar un inhibidor de jak

Country Status (32)

Country Link
US (1) US10899736B2 (es)
EP (2) EP4086245A1 (es)
JP (2) JP7393348B2 (es)
KR (1) KR20200129099A (es)
CN (1) CN112105608B (es)
AR (1) AR114810A1 (es)
AU (1) AU2019213665A1 (es)
BR (1) BR112020015470A2 (es)
CA (1) CA3089832A1 (es)
CL (1) CL2020001983A1 (es)
CO (1) CO2020009994A2 (es)
CR (1) CR20200379A (es)
DK (1) DK3746429T3 (es)
EA (1) EA202091830A1 (es)
ES (1) ES2912469T3 (es)
HR (1) HRP20220510T1 (es)
IL (1) IL276302B2 (es)
LT (1) LT3746429T (es)
MA (1) MA51771B1 (es)
MD (1) MD3746429T2 (es)
MX (1) MX2020007973A (es)
PE (1) PE20211310A1 (es)
PH (1) PH12020551145A1 (es)
PL (1) PL3746429T3 (es)
PT (1) PT3746429T (es)
RS (1) RS63312B1 (es)
SG (1) SG11202007164UA (es)
SI (1) SI3746429T1 (es)
TW (1) TWI797242B (es)
UA (1) UA127488C2 (es)
WO (1) WO2019152374A1 (es)
ZA (1) ZA202004692B (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3746429T3 (pl) 2018-01-30 2022-06-20 Incyte Corporation Procesy do otrzymywania (1-(3-fluoro-2-(trifluorometylo)izonikotynoilo)piperydyn-4-onu)
SG11202007805SA (en) 2018-02-16 2020-09-29 Incyte Corp Jak1 pathway inhibitors for the treatment of cytokine-related disorders
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
MX2020010815A (es) 2018-04-13 2020-12-11 Incyte Corp Biomarcadores para enfermedad de injerto contra hospedero.
US11324749B2 (en) 2018-10-31 2022-05-10 Incyte Corporation Combination therapy for treatment of hematological diseases
KR20210137087A (ko) 2019-03-05 2021-11-17 인사이트 코포레이션 만성 폐 동종이식 기능장애의 치료를 위한 jak1 경로 억제제
CN110683978A (zh) * 2019-10-30 2020-01-14 西安医学院 一种3-腈基亚甲基氮杂环丁烷-1-碳酸叔丁酯的制备方法
CR20230129A (es) 2020-08-18 2023-07-13 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
EP4200278A1 (en) 2020-08-18 2023-06-28 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
KR20230118118A (ko) 2020-12-08 2023-08-10 인사이트 코포레이션 백반증의 치료를 위한 jak1 경로 저해제
CN112625030A (zh) * 2020-12-25 2021-04-09 杭州澳赛诺生物科技有限公司 一种一锅法合成n-保护3-溴代吡唑的合成方法

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