TWI709562B - 吡咯并〔２，３-ｄ〕嘧啶化合物的製造方法與中間產物及其用途 - Google Patents

吡咯并〔２，３-ｄ〕嘧啶化合物的製造方法與中間產物及其用途 Download PDF

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TWI709562B
TWI709562B TW108123441A TW108123441A TWI709562B TW I709562 B TWI709562 B TW I709562B TW 108123441 A TW108123441 A TW 108123441A TW 108123441 A TW108123441 A TW 108123441A TW I709562 B TWI709562 B TW I709562B
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compound
pyrrolo
amino
methyl
following structure
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TW108123441A
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TW202017929A (zh
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卡皮爾戴 阿羅拉
雅各 迪佛斯特
安德魯 希爾斯
布萊恩 瓊斯
克里斯 瓊斯
查德 路易斯
阿尼爾 雷恩
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美商輝瑞股份有限公司
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    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
TW108123441A 2018-07-06 2019-07-03 吡咯并〔２，３-ｄ〕嘧啶化合物的製造方法與中間產物及其用途 TWI709562B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201862694698P 2018-07-06 2018-07-06
US62/694,698 2018-07-06
US201862776642P 2018-12-07 2018-12-07
US62/776,642 2018-12-07
US201962855071P 2019-05-31 2019-05-31
US62/855,071 2019-05-31

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TW202017929A TW202017929A (zh) 2020-05-16
TWI709562B true TWI709562B (zh) 2020-11-11

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US (3) US10815240B2 (enExample)
EP (1) EP3817810B1 (enExample)
JP (1) JP7437646B2 (enExample)
KR (1) KR102568464B1 (enExample)
CN (1) CN112384282B (enExample)
AU (1) AU2019299666B2 (enExample)
BR (1) BR112020025701A2 (enExample)
CA (1) CA3105161C (enExample)
ES (1) ES3045115T3 (enExample)
IL (1) IL279926B2 (enExample)
MX (2) MX2020013896A (enExample)
TW (1) TWI709562B (enExample)
WO (1) WO2020008391A1 (enExample)
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WO2020232470A1 (en) 2019-05-13 2020-11-19 Boragen, Inc. Chemical compounds
CN113637018A (zh) 2020-04-27 2021-11-12 苏州晶云药物科技股份有限公司 磺酰胺类化合物的晶型及其制备方法
CN112279785B (zh) * 2020-10-29 2022-08-16 苏利制药科技江阴有限公司 3,3-二氟环丁胺盐酸盐中间体及其合成方法和3,3-二氟环丁胺盐酸盐合成方法
CN113583992B (zh) * 2021-07-15 2023-06-27 华东理工大学 一种还原胺化酶及其在仲胺合成中的应用
US20240383893A1 (en) * 2021-09-10 2024-11-21 Haihe Biopharma Co., Ltd. Hydroxamic Acid Compound Having ENPP1 Inhibitory Activity and Use Thereof
ES2993658B2 (es) 2023-06-27 2025-07-02 Moehs Iberica Sl (3-(metil(7h-pirrolo[2,3-d]pirimidin-4-il)amino)ciclobutilo)carbamato de bencilo o una sal del mismo, procedimiento para su preparacion y su uso en la sintesis de abrocitinib
ES3040374A1 (es) 2024-04-30 2025-10-30 Moehs Iberica Sl Cocristales de N-{cis-3-[metil(7H-pirrolo[2,3-d]pirimidin-4-il)amino]ciclobutil}propano-1-sulfonamida

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Vazquez ML. et al."Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases." J Med Chem. 2018 Feb 8;61(3):1130-1152.
Vazquez ML. et al."Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases." J Med Chem. 2018 Feb 8;61(3):1130-1152. Caira M.R. et al."Crystalline Polymorphism of Organic Compounds." In: Weber E. et al. (eds) Design of Organic Solids. Topics in Current Chemistry.Springer, Berlin, Heidelberg.vol 198:163-208. CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 18 August 2006, REGISTRY no. 902708-70-7 *

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MX2023006842A (es) 2023-06-22
US20220127274A1 (en) 2022-04-28
IL279926A (en) 2021-03-01
TW202017929A (zh) 2020-05-16
CN112384282A (zh) 2021-02-19
EP3817810A1 (en) 2021-05-12
JP7437646B2 (ja) 2024-02-26
WO2020008391A1 (en) 2020-01-09
CN112384282B (zh) 2024-07-02
US10815240B2 (en) 2020-10-27
CA3105161A1 (en) 2020-01-09
US20210009601A1 (en) 2021-01-14
JP2020007308A (ja) 2020-01-16
IL279926B1 (en) 2023-08-01
AU2019299666A1 (en) 2021-01-07
US11254684B2 (en) 2022-02-22
MX2020013896A (es) 2021-03-09
US20200123159A1 (en) 2020-04-23
ES3045115T3 (en) 2025-11-27
EP3817810B1 (en) 2025-09-17
AU2019299666B2 (en) 2024-07-11
US12018031B2 (en) 2024-06-25
ZA202100196B (en) 2022-09-28
CA3105161C (en) 2022-11-15
IL279926B2 (en) 2023-12-01
BR112020025701A2 (pt) 2021-03-16
KR102568464B1 (ko) 2023-08-21
EP3817810C0 (en) 2025-09-17
KR20210029234A (ko) 2021-03-15

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