TWI703147B - 用於治療胃腸發炎性疾病之jak抑制劑化合物之前藥 - Google Patents

用於治療胃腸發炎性疾病之jak抑制劑化合物之前藥 Download PDF

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TWI703147B
TWI703147B TW105138180A TW105138180A TWI703147B TW I703147 B TWI703147 B TW I703147B TW 105138180 A TW105138180 A TW 105138180A TW 105138180 A TW105138180 A TW 105138180A TW I703147 B TWI703147 B TW I703147B
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compound
methyl
pharmaceutically acceptable
acceptable salt
formula
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TW105138180A
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TW201720827A (zh
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雷恩 修森
丹尼爾 D 羅恩
唐娜Ａ Ａ 威爾頓
曼蒂 羅伊
派翠克Ｊ 布萊瑟爾
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美商施萬生物製藥研發Ｉｐ有限責任公司
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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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW105138180A 2015-11-24 2016-11-22 用於治療胃腸發炎性疾病之jak抑制劑化合物之前藥 TWI703147B (zh)

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US201562259273P 2015-11-24 2015-11-24
US62/259,273 2015-11-24

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TW201720827A TW201720827A (zh) 2017-06-16
TWI703147B true TWI703147B (zh) 2020-09-01

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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3712152T3 (da) 2015-11-03 2021-03-22 Topivert Pharma Ltd 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridin og 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepinderivater som janus kinase-inhibitorer
EP3371185B1 (en) 2015-11-03 2020-09-30 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
EA035816B1 (ru) 2015-11-24 2020-08-14 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта
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
JP2020520955A (ja) 2017-05-23 2020-07-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ヤヌスキナーゼ阻害剤のグルクロニドプロドラッグ
WO2018217699A1 (en) * 2017-05-23 2018-11-29 Theravance Biopharma R&D Ip, Llc Thiocarbamate prodrugs of tofacitinib
SG11201910198UA (en) * 2017-06-05 2019-11-28 Flagship Pioneering Innovations V Inc Multibiotic agents and methods of using the same
PE20211305A1 (es) 2018-01-05 2021-07-20 Cybrexa 1 Inc Compuestos, composiciones y metodos para tratar enfermedades que involucren tejidos con enfermedades acidas o hipoxicas
WO2019182322A1 (ko) * 2018-03-20 2019-09-26 삼진제약주식회사 신규 염, 이의 제조 방법 및 이를 포함하는 약학 조성물
US12171764B2 (en) 2018-06-20 2024-12-24 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a JAK or other kinase inhibitor
CN111094314B (zh) * 2018-08-15 2022-08-12 江苏豪森药业集团有限公司 含有葡糖苷酸衍生物jak抑制剂的前药及其制备方法和应用
CN119751336A (zh) * 2018-09-06 2025-04-04 艾尼纳制药公司 可用于治疗自身免疫性病症和炎性病症的化合物
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
CA3119294A1 (en) * 2018-11-15 2020-05-22 Janssen Biotech, Inc. Methods and compositions for prediction of response to a therapy of inflammatory bowel disease
CN113692278A (zh) 2018-12-19 2021-11-23 因赛特公司 用于治疗胃肠道疾病的jak1途径抑制剂
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
CR20220057A (es) 2019-07-10 2022-07-19 Cybrexa 3 Inc Conjugados peptídicos de agentes dirigidos a microtúbulos como terapéuticos
CR20220058A (es) 2019-07-10 2022-07-19 Cybrexa 2 Inc Conjugados peptídicos de citotoxinas como terapéuticos
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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
EP4149462A4 (en) 2020-05-14 2024-04-24 Theravance Biopharma R&D IP, LLC Administration of gut-selective jak3 inhibitor
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
WO2022087313A1 (en) * 2020-10-22 2022-04-28 Progenity, Inc. Methods of treating and predicting non-response to anti-tnf treatment in subjects with gastrointestinal tract diseases
EP4351584A4 (en) * 2021-06-07 2025-04-23 The Regents of the University of California COMPOSITIONS AND METHODS FOR TREATING CELIAC DISEASE
IL309840A (en) * 2021-07-20 2024-02-01 Coval Biopharma Shanghai Co Ltd An external antidialectic coupling compound drug, and a method of preparation therefor and use thereof
JP2025516712A (ja) * 2022-05-14 2025-05-30 株式会社スリー・ディー・マトリックス 消化管への治療剤の経口投与のための新規な製剤
CN115073543B (zh) * 2022-07-20 2022-11-15 北京普祺医药科技股份有限公司 一种jak抑制剂的化合物前药及其制备与应用
CN117567460A (zh) * 2022-08-08 2024-02-20 明慧医药（杭州）有限公司 一种前药化合物及其制备方法和用途
KR20250107797A (ko) 2022-08-17 2025-07-14 트랜센드 테라퓨틱스 인코퍼레이티드 페네틸아민 및 카티논 전구체

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140357557A1 (en) * 2013-05-31 2014-12-04 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993022334A1 (en) 1992-05-04 1993-11-11 Sri International Pharmaceutical compositions and methods for colonic delivery of corticosteroids
US5811388A (en) 1995-06-07 1998-09-22 Cibus Pharmaceutical, Inc. Delivery of drugs to the lower GI tract
AU777911B2 (en) 1999-12-10 2004-11-04 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
CA2777114C (en) 2009-10-09 2018-10-23 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
EP2515913A2 (en) 2009-12-23 2012-10-31 Glycomyr Inc. Use of vitamin d glycosides and sulfates for treatment of disease
CN102724967A (zh) 2009-12-31 2012-10-10 安龙制药公司 包括可释放的脲连接体的含芳香胺化合物的聚合缀合物
CN102822177A (zh) * 2010-02-05 2012-12-12 美国辉瑞有限公司 吡咯并[2,3-d]嘧啶脲化合物
US20130109720A1 (en) 2011-11-01 2013-05-02 Hoffmann-La Roche Inc. Indole inhibitors of crac
EP3169348B1 (en) * 2014-06-24 2019-07-31 Institut National de la Sante et de la Recherche Medicale (INSERM) Pharmaceutical compositions comprising agonists of orexin-1 receptor ox1r for the treatment of inflammatory bowel diseases
EA035816B1 (ru) 2015-11-24 2020-08-14 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта
WO2017106957A1 (en) 2015-12-23 2017-06-29 The University Of British Columbia Lipid-linked prodrugs
CN106496233B (zh) 2016-09-26 2018-05-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140357557A1 (en) * 2013-05-31 2014-12-04 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Bouvier E,et al."First enzymatically activated Taxotere prodrugs designed for ADEPT and PMT.", Bioorg Med Chem. 2004 Mar 1;12(5):969-977. *
Clark JD,et al." Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.", J Med Chem. 2014 Jun 26;57(12):5023-5038. *

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EP3380486B1 (en) 2020-02-19
JP6778747B2 (ja) 2020-11-04
NZ742574A (en) 2018-11-30
SI3380486T1 (sl) 2020-07-31
JP2020196742A (ja) 2020-12-10
PT3380486T (pt) 2020-05-22
LT3380486T (lt) 2020-05-11
KR20180080330A (ko) 2018-07-11
SMT202000242T1 (it) 2020-07-08
ME03757B (me) 2021-04-20
MY189979A (en) 2022-03-22
HRP20200561T1 (hr) 2020-06-26
JP2019501133A (ja) 2019-01-17
ZA201802967B (en) 2019-04-24
AU2016359494B2 (en) 2021-01-07
HUE049775T2 (hu) 2020-10-28
US11608354B2 (en) 2023-03-21
WO2017091544A1 (en) 2017-06-01
CA3003283A1 (en) 2017-06-01
CL2018001345A1 (es) 2018-06-22
CN108290918A (zh) 2018-07-17
CY1122918T1 (el) 2021-10-29
US10435428B2 (en) 2019-10-08
UA121270C2 (uk) 2020-04-27
TW201720827A (zh) 2017-06-16
RS60237B1 (sr) 2020-06-30
IL259076A (en) 2018-06-28
IL259076B (en) 2021-05-31
PL3380486T3 (pl) 2020-07-27
US20210179655A1 (en) 2021-06-17
US20190389895A1 (en) 2019-12-26
MX2018006282A (es) 2019-01-21
US20170145044A1 (en) 2017-05-25
EA035816B1 (ru) 2020-08-14
EP3380486A1 (en) 2018-10-03
US10961267B2 (en) 2021-03-30
ES2784523T3 (es) 2020-09-28
EA201891248A1 (ru) 2018-10-31
CN108290918B (zh) 2021-06-08
BR112018010650A8 (pt) 2019-02-26
BR112018010650A2 (pt) 2018-11-13
MX383107B (es) 2025-03-13
CO2018005327A2 (es) 2018-05-31
AU2016359494A1 (en) 2018-06-14
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PH12018501037A1 (en) 2019-01-28
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