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
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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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    • 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)
  • Chemical & Material Sciences (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)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)

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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 (14)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
US11021482B2 (en) 2018-08-10 2021-06-01 Adaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
KR20210109522A (ko) 2018-10-31 2021-09-06 인사이트 코포레이션 혈액 질환의 치료를 위한 병용 요법
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제
IL285999B1 (en) 2019-03-05 2025-09-01 Incyte Corp JAK1 inhibitor pathway for the treatment of chronic lung allograft dysfunction
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
EP4041204A1 (en) 2019-10-10 2022-08-17 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)
US20240307396A1 (en) * 2021-06-07 2024-09-19 The Regents Of The University Of California Compositions and methods for treating celiac disease
WO2024102778A1 (en) * 2022-11-08 2024-05-16 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

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01013458A (es) 1999-06-25 2002-07-30 Genentech Inc Anticuerpos humanizados anti-erbb2 y tratamiento con anticuerpos anti-erbb2.
ES2225624T3 (es) 2000-06-28 2005-03-16 Smithkline Beecham Plc Procedimiento de molienda por via humeda.
US20040132101A1 (en) 2002-09-27 2004-07-08 Xencor Optimized Fc variants and methods for their generation
EP2263691B1 (en) 2002-07-15 2012-08-29 F.Hoffmann-La Roche Ag Treatment of cancer with the recombinant humanized monoclonal anti-erbb2 antibody 2C4 (rhuMAb 2C4)
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX354212B (es) * 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
BR112015009942A2 (pt) 2012-11-01 2017-07-11 Incyte Corp derivados de tiofeno fundidos tricíclicos como inibidores de jak
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備ｊａｋ抑制劑之方法及中間物
WO2014186706A1 (en) 2013-05-17 2014-11-20 Incyte Corporation Bipyrazole derivatives as jak inhibitors
MX394928B (es) 2013-08-07 2025-03-24 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
HUE049775T2 (hu) * 2015-11-24 2020-10-28 Theravance Biopharma R&D Ip Llc Gasztrointesztinális gyulladásos betegség kezelésére szolgáló JAK inhibitor vegyület elõgyógyszerei
CN110072519A (zh) 2016-12-14 2019-07-30 普罗根尼蒂公司 使用jak抑制剂治疗胃肠道疾病及装置
WO2018111327A1 (en) * 2016-12-14 2018-06-21 Progenity Inc. Methods and ingestible devices for the regio-specific release of jak inhibitors at the site of gastrointestinal tract disease
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제

Also Published As

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

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