TWI884142B - 用於治療胃腸道疾病之jak1路徑抑制劑 - Google Patents

用於治療胃腸道疾病之jak1路徑抑制劑 Download PDF

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Publication number
TWI884142B
TWI884142B TW108146771A TW108146771A TWI884142B TW I884142 B TWI884142 B TW I884142B TW 108146771 A TW108146771 A TW 108146771A TW 108146771 A TW108146771 A TW 108146771A TW I884142 B TWI884142 B TW I884142B
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Taiwan
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
acetonitrile
pyrimidin
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TW108146771A
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English (en)
Chinese (zh)
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TW202038944A (zh
Inventor
克里施奈斯瓦米 伊勒史汪
保羅 史密斯
喬傑瑞 Ｆ 何李斯
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美商英塞特公司
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Publication of TW202038944A publication Critical patent/TW202038944A/zh
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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW108146771A 2018-12-19 2019-12-19 用於治療胃腸道疾病之jak1路徑抑制劑 TWI884142B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201862781877P 2018-12-19 2018-12-19
US62/781,877 2018-12-19
US201962854801P 2019-05-30 2019-05-30
US62/854,801 2019-05-30
US201962901377P 2019-09-17 2019-09-17
US62/901,377 2019-09-17

Publications (2)

Publication Number Publication Date
TW202038944A TW202038944A (zh) 2020-11-01
TWI884142B true TWI884142B (zh) 2025-05-21

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Family Applications (1)

Application Number Title Priority Date Filing Date
TW108146771A TWI884142B (zh) 2018-12-19 2019-12-19 用於治療胃腸道疾病之jak1路徑抑制劑

Country Status (15)

Country Link
US (2) US11596632B2 (https=)
EP (1) EP3897627A1 (https=)
JP (1) JP7624922B2 (https=)
KR (1) KR20210116487A (https=)
CN (1) CN113692278A (https=)
AU (1) AU2019403304B2 (https=)
CA (1) CA3123596A1 (https=)
IL (1) IL284034A (https=)
MA (1) MA54544A (https=)
MX (1) MX2021007260A (https=)
PH (1) PH12021551455A1 (https=)
SG (1) SG11202106470TA (https=)
TW (1) TWI884142B (https=)
UA (1) UA130221C2 (https=)
WO (1) WO2020132210A1 (https=)

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WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
WO2020033955A1 (en) 2018-08-10 2020-02-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine itk inhibitors
CA3117969A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
CA3123596A1 (en) 2018-12-19 2020-06-25 Incyte Corporation Jak1 pathway inhibitors for the treatment of gastrointestinal disease
MA55201A (fr) 2019-03-05 2022-01-12 Incyte Corp Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
EP4351584A4 (en) * 2021-06-07 2025-04-23 The Regents of the University of California COMPOSITIONS AND METHODS FOR TREATING CELIAC DISEASE
EP4615440A1 (en) * 2022-11-08 2025-09-17 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of itk mediated conditions
WO2025144781A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Crystalline polymorph of an itk inhibitor
CN120699157B (zh) * 2025-07-16 2025-12-16 安康市中心医院 一种治疗溃疡性结肠炎的恢复肠屏障功能抗体及其应用

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JP5775070B2 (ja) 2009-05-22 2015-09-09 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体
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Also Published As

Publication number Publication date
US12150943B2 (en) 2024-11-26
KR20210116487A (ko) 2021-09-27
TW202038944A (zh) 2020-11-01
US20200197399A1 (en) 2020-06-25
AU2019403304A1 (en) 2021-07-08
CN113692278A (zh) 2021-11-23
SG11202106470TA (en) 2021-07-29
US20230172939A1 (en) 2023-06-08
CA3123596A1 (en) 2020-06-25
AU2019403304B2 (en) 2025-09-04
JP7624922B2 (ja) 2025-01-31
PH12021551455A1 (en) 2022-04-18
WO2020132210A1 (en) 2020-06-25
MA54544A (fr) 2021-10-27
EP3897627A1 (en) 2021-10-27
IL284034A (en) 2021-08-31
JP2022514089A (ja) 2022-02-09
UA130221C2 (uk) 2025-12-24
US11596632B2 (en) 2023-03-07
MX2021007260A (es) 2021-09-08

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