KR20180080330A - 위장관 염증 질환의 치료를 위한 jak 저해제 화합물의 프로드러그 - Google Patents

위장관 염증 질환의 치료를 위한 jak 저해제 화합물의 프로드러그 Download PDF

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Publication number
KR20180080330A
KR20180080330A KR1020187017879A KR20187017879A KR20180080330A KR 20180080330 A KR20180080330 A KR 20180080330A KR 1020187017879 A KR1020187017879 A KR 1020187017879A KR 20187017879 A KR20187017879 A KR 20187017879A KR 20180080330 A KR20180080330 A KR 20180080330A
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South Korea
Prior art keywords
compound
methyl
formula
amino
gastrointestinal inflammatory
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KR1020187017879A
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English (en)
Korean (ko)
Inventor
라이언 허드슨
다니엘 디. 롱
도나 에이.에이. 윌턴
맨디 루
패트릭 제이. 브래실
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세라밴스 바이오파마 알앤디 아이피, 엘엘씨
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Publication of KR20180080330A publication Critical patent/KR20180080330A/ko
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/16—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing two or more hetero rings
    • C12P17/165—Heterorings having nitrogen atoms as the only ring heteroatoms

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020187017879A 2015-11-24 2016-11-22 위장관 염증 질환의 치료를 위한 jak 저해제 화합물의 프로드러그 Withdrawn KR20180080330A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562259273P 2015-11-24 2015-11-24
US62/259,273 2015-11-24
PCT/US2016/063254 WO2017091544A1 (en) 2015-11-24 2016-11-22 Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease

Publications (1)

Publication Number Publication Date
KR20180080330A true KR20180080330A (ko) 2018-07-11

Family

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Family Applications (1)

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KR1020187017879A Withdrawn KR20180080330A (ko) 2015-11-24 2016-11-22 위장관 염증 질환의 치료를 위한 jak 저해제 화합물의 프로드러그

Country Status (33)

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US (3) US10435428B2 (enExample)
EP (1) EP3380486B1 (enExample)
JP (2) JP6778747B2 (enExample)
KR (1) KR20180080330A (enExample)
CN (1) CN108290918B (enExample)
AU (1) AU2016359494B2 (enExample)
BR (1) BR112018010650A8 (enExample)
CA (1) CA3003283A1 (enExample)
CL (1) CL2018001345A1 (enExample)
CO (1) CO2018005327A2 (enExample)
CY (1) CY1122918T1 (enExample)
DK (1) DK3380486T3 (enExample)
EA (1) EA035816B1 (enExample)
ES (1) ES2784523T3 (enExample)
HR (1) HRP20200561T1 (enExample)
HU (1) HUE049775T2 (enExample)
IL (1) IL259076B (enExample)
LT (1) LT3380486T (enExample)
ME (1) ME03757B (enExample)
MX (1) MX383107B (enExample)
MY (1) MY189979A (enExample)
NZ (1) NZ742574A (enExample)
PH (1) PH12018501037A1 (enExample)
PL (1) PL3380486T3 (enExample)
PT (1) PT3380486T (enExample)
RS (1) RS60237B1 (enExample)
SG (1) SG11201803686UA (enExample)
SI (1) SI3380486T1 (enExample)
SM (1) SMT202000242T1 (enExample)
TW (1) TWI703147B (enExample)
UA (1) UA121270C2 (enExample)
WO (1) WO2017091544A1 (enExample)
ZA (1) ZA201802967B (enExample)

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PL3371185T3 (pl) 2015-11-03 2021-04-06 Topivert Pharma Limited Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych
EP3865481A1 (en) 2015-11-03 2021-08-18 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
HUE049775T2 (hu) 2015-11-24 2020-10-28 Theravance Biopharma R&D Ip Llc Gasztrointesztinális gyulladásos betegség kezelésére szolgáló JAK inhibitor vegyület elõgyógyszerei
FR3060567B1 (fr) * 2016-12-19 2019-05-24 Ecole Normale Superieure De Lyon Substrat de glycosidase fluorogene et procede de detection associe
US10472366B2 (en) 2017-03-08 2019-11-12 Theravance Biopharma R&D Ip, Llc Glucuronide prodrugs of tofacitinib
CN110662755A (zh) * 2017-05-23 2020-01-07 施万生物制药研发Ip有限责任公司 托法替尼的硫代氨基甲酸酯前药
US10745405B2 (en) 2017-05-23 2020-08-18 Theravance Biopharma R&D Ip, Llc Glucuronide prodrugs of Janus kinase inhibitors
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KR20200121800A (ko) 2018-01-05 2020-10-26 싸이브렉사 1, 인크. 산성 또는 저산소성 질환에 걸린 조직에 관련된 질환의 치료를 위한 화합물, 조성물 및 방법
KR20190110459A (ko) * 2018-03-20 2019-09-30 삼진제약주식회사 신규 염, 이의 제조 방법 및 이를 포함하는 약학 조성물
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US11555015B2 (en) * 2018-09-06 2023-01-17 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
CN109134564B (zh) * 2018-09-21 2022-03-11 合肥锐思生物医药有限公司 乳果糖糖苷衍生物、其制备方法及其用途
AU2019378008A1 (en) * 2018-11-15 2021-06-03 Janssen Biotech, Inc. Methods and compositions for prediction of response to a therapy of an inflammatory bowel disease
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
CN114341162B (zh) 2019-07-10 2025-10-17 赛博克萨2公司 作为治疗剂的细胞毒素的肽缀合物
US11555019B2 (en) 2019-07-10 2023-01-17 Cybrexa 3, Inc. Peptide conjugates of microtubule-targeting agents as therapeutics
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021097074A1 (en) * 2019-11-13 2021-05-20 New York University Intestinal organoid co-culture systems and methods for treating or preventing a disease or disorder associated with immune response-mediated tissue injury
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US20230107927A1 (en) * 2020-02-28 2023-04-06 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
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CN113943312A (zh) * 2020-07-17 2022-01-18 轶诺(浙江)药业有限公司 一类肠道裂解型共药及其制备和用途
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US20240307396A1 (en) * 2021-06-07 2024-09-19 The Regents Of The University Of California Compositions and methods for treating celiac disease
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EP3380486A1 (en) 2018-10-03
CA3003283A1 (en) 2017-06-01
MY189979A (en) 2022-03-22
ME03757B (me) 2021-04-20
UA121270C2 (uk) 2020-04-27
LT3380486T (lt) 2020-05-11
US20170145044A1 (en) 2017-05-25
MX2018006282A (es) 2019-01-21
SI3380486T1 (sl) 2020-07-31
PT3380486T (pt) 2020-05-22
TW201720827A (zh) 2017-06-16
JP6778747B2 (ja) 2020-11-04
IL259076B (en) 2021-05-31
BR112018010650A2 (pt) 2018-11-13
RS60237B1 (sr) 2020-06-30
US20190389895A1 (en) 2019-12-26
US20210179655A1 (en) 2021-06-17
ES2784523T3 (es) 2020-09-28
HUE049775T2 (hu) 2020-10-28
SMT202000242T1 (it) 2020-07-08
HRP20200561T1 (hr) 2020-06-26
DK3380486T3 (da) 2020-05-18
US10961267B2 (en) 2021-03-30
US10435428B2 (en) 2019-10-08
WO2017091544A1 (en) 2017-06-01
US11608354B2 (en) 2023-03-21
EA201891248A1 (ru) 2018-10-31
JP2019501133A (ja) 2019-01-17
CN108290918A (zh) 2018-07-17
IL259076A (en) 2018-06-28
SG11201803686UA (en) 2018-06-28
MX383107B (es) 2025-03-13
CO2018005327A2 (es) 2018-05-31
PH12018501037A1 (en) 2019-01-28
BR112018010650A8 (pt) 2019-02-26
EP3380486B1 (en) 2020-02-19
AU2016359494A1 (en) 2018-06-14
JP2020196742A (ja) 2020-12-10
EA035816B1 (ru) 2020-08-14
CL2018001345A1 (es) 2018-06-22
NZ742574A (en) 2018-11-30
ZA201802967B (en) 2019-04-24
TWI703147B (zh) 2020-09-01
AU2016359494B2 (en) 2021-01-07
CY1122918T1 (el) 2021-10-29
CN108290918B (zh) 2021-06-08
PL3380486T3 (pl) 2020-07-27

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