EA201891248A1 - Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта - Google Patents

Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта

Info

Publication number
EA201891248A1
EA201891248A1 EA201891248A EA201891248A EA201891248A1 EA 201891248 A1 EA201891248 A1 EA 201891248A1 EA 201891248 A EA201891248 A EA 201891248A EA 201891248 A EA201891248 A EA 201891248A EA 201891248 A1 EA201891248 A1 EA 201891248A1
Authority
EA
Eurasian Patent Office
Prior art keywords
gastrointestinal tract
jak
compounds
inhibitive
connections
Prior art date
Application number
EA201891248A
Other languages
English (en)
Other versions
EA035816B1 (ru
Inventor
Райан Хадсон
Дэниэл Д. Лонг
Донна А.А. Уилтон
Менди Лу
Патрик Дж. Брэссил
Original Assignee
ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи filed Critical ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи
Publication of EA201891248A1 publication Critical patent/EA201891248A1/ru
Publication of EA035816B1 publication Critical patent/EA035816B1/ru

Links

Classifications

    • 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

Landscapes

  • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Изобретение предлагает соединения, которые являются пролекарствами JAK-ингибитора, для направленной доставки JAK-ингибитора к желудочно-кишечному тракту млекопитающего. Изобретение также предлагает фармацевтические композиции, содержащие такие соединения, способы применения таких соединений для лечения воспалительных заболеваний желудочно-кишечного тракта, а также способы и промежуточные соединения, приемлемые для получения соединений.
EA201891248A 2015-11-24 2016-11-22 Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта EA035816B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562259273P 2015-11-24 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 (2)

Publication Number Publication Date
EA201891248A1 true EA201891248A1 (ru) 2018-10-31
EA035816B1 EA035816B1 (ru) 2020-08-14

Family

ID=57518004

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891248A EA035816B1 (ru) 2015-11-24 2016-11-22 Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта

Country Status (32)

Country Link
US (3) US10435428B2 (ru)
EP (1) EP3380486B1 (ru)
JP (2) JP6778747B2 (ru)
KR (1) KR20180080330A (ru)
CN (1) CN108290918B (ru)
AU (1) AU2016359494B2 (ru)
BR (1) BR112018010650A8 (ru)
CA (1) CA3003283A1 (ru)
CL (1) CL2018001345A1 (ru)
CO (1) CO2018005327A2 (ru)
CY (1) CY1122918T1 (ru)
DK (1) DK3380486T3 (ru)
EA (1) EA035816B1 (ru)
ES (1) ES2784523T3 (ru)
HR (1) HRP20200561T1 (ru)
HU (1) HUE049775T2 (ru)
IL (1) IL259076B (ru)
LT (1) LT3380486T (ru)
ME (1) ME03757B (ru)
MX (1) MX2018006282A (ru)
MY (1) MY189979A (ru)
NZ (1) NZ742574A (ru)
PH (1) PH12018501037A1 (ru)
PL (1) PL3380486T3 (ru)
PT (1) PT3380486T (ru)
RS (1) RS60237B1 (ru)
SG (1) SG11201803686UA (ru)
SI (1) SI3380486T1 (ru)
TW (1) TWI703147B (ru)
UA (1) UA121270C2 (ru)
WO (1) WO2017091544A1 (ru)
ZA (1) ZA201802967B (ru)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10851097B2 (en) 2015-11-03 2020-12-01 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
US10556901B2 (en) 2015-11-03 2020-02-11 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
WO2017091544A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
FR3060567B1 (fr) * 2016-12-19 2019-05-24 Ecole Normale Superieure De Lyon Substrat de glycosidase fluorogene et procede de detection associe
EP3592755A1 (en) * 2017-03-08 2020-01-15 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
BR112019024509A2 (pt) 2017-05-23 2020-06-23 Theravance Biopharma R&D Ip, Llc Glicuronídeo de pró-fármacos dos inibidores da janus quinase
CA3062067A1 (en) * 2017-06-05 2018-12-13 Flagship Pioneering Innovations V, Inc. Multibiotic agents and methods of using the same
EP3735297A1 (en) 2018-01-05 2020-11-11 Cybrexa 1, Inc. Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues
WO2019182322A1 (ko) * 2018-03-20 2019-09-26 삼진제약주식회사 신규 염, 이의 제조 방법 및 이를 포함하는 약학 조성물
WO2019246273A1 (en) 2018-06-20 2019-12-26 Progenity, 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
EP3847158A1 (en) * 2018-09-06 2021-07-14 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
WO2020102519A1 (en) * 2018-11-15 2020-05-22 Janssen Biotech, Inc. Methods and compositions for prediction of response to a therapy of an inflammatory bowel disease
WO2020132210A1 (en) * 2018-12-19 2020-06-25 Incyte Corporation Jak1 pathway inhibitors for the treatment of gastrointestinal disease
MX2021009863A (es) 2019-03-21 2021-11-12 Onxeo Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer.
JP2022541747A (ja) 2019-07-10 2022-09-27 サイブレクサ ３，インコーポレイテッド 治療薬としての微小管標的化剤のペプチドコンジュゲート
PE20220563A1 (es) 2019-07-10 2022-04-13 Cybrexa 2 Inc Conjugados peptidicos de citotoxinas como terapeuticos
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
US20210139857A1 (en) * 2019-11-13 2021-05-13 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
CN115867272A (zh) 2020-05-14 2023-03-28 施万生物制药研发Ip有限责任公司 肠道选择性jak3抑制剂的给药
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
EP4232146A1 (en) * 2020-10-22 2023-08-30 Biora Therapeutics, Inc. Methods of treating and predicting non-response to anti-tnf treatment in subjects with gastrointestinal tract diseases
EP4351584A1 (en) * 2021-06-07 2024-04-17 The Regents of the University of California Compositions and methods for treating celiac disease
WO2023225463A2 (en) * 2022-05-14 2023-11-23 3-D Matrix, Ltd. Novel formulations for oral administration of therapeutic agents to the gastrointestinal tract
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

Family Cites Families (13)

* 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
PT1235830E (pt) 1999-12-10 2004-04-30 Pfizer Prod Inc Compostos de pirrolo¬2,3-d|pirimidina como inibidores das proteina cinases
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
EP2515913A2 (en) 2009-12-23 2012-10-31 Glycomyr Inc. Use of vitamin d glycosides and sulfates for treatment of disease
WO2011082368A2 (en) 2009-12-31 2011-07-07 Enzon Pharmaceuticals, Inc Polymeric conjugates of aromatic amine containing compounds including releasable urea linker
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
JP2016528174A (ja) * 2013-05-31 2016-09-15 セルリアン・ファーマ・インコーポレイテッド 治療的送達用のシクロデキストリンベースのポリマー
ES2742179T3 (es) * 2014-06-24 2020-02-13 Inst Nat Sante Rech Med Composiciones farmacéuticas que comprenden agonistas del receptor de orexina-1 OX1R para el tratamiento de enfermedades inflamatorias del intestino
WO2017091544A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
AU2016379454B2 (en) 2015-12-23 2021-01-28 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

Also Published As

Publication number Publication date
EP3380486B1 (en) 2020-02-19
UA121270C2 (uk) 2020-04-27
CN108290918B (zh) 2021-06-08
HUE049775T2 (hu) 2020-10-28
WO2017091544A1 (en) 2017-06-01
RS60237B1 (sr) 2020-06-30
AU2016359494A1 (en) 2018-06-14
PL3380486T3 (pl) 2020-07-27
SI3380486T1 (sl) 2020-07-31
AU2016359494B2 (en) 2021-01-07
NZ742574A (en) 2018-11-30
EP3380486A1 (en) 2018-10-03
KR20180080330A (ko) 2018-07-11
JP2020196742A (ja) 2020-12-10
IL259076A (en) 2018-06-28
US10961267B2 (en) 2021-03-30
PH12018501037A1 (en) 2019-01-28
US20190389895A1 (en) 2019-12-26
US11608354B2 (en) 2023-03-21
TWI703147B (zh) 2020-09-01
CN108290918A (zh) 2018-07-17
CA3003283A1 (en) 2017-06-01
TW201720827A (zh) 2017-06-16
PT3380486T (pt) 2020-05-22
CY1122918T1 (el) 2021-10-29
DK3380486T3 (da) 2020-05-18
US20210179655A1 (en) 2021-06-17
BR112018010650A2 (pt) 2018-11-13
MY189979A (en) 2022-03-22
US10435428B2 (en) 2019-10-08
CL2018001345A1 (es) 2018-06-22
JP6778747B2 (ja) 2020-11-04
US20170145044A1 (en) 2017-05-25
IL259076B (en) 2021-05-31
ZA201802967B (en) 2019-04-24
ME03757B (me) 2021-04-20
MX2018006282A (es) 2019-01-21
ES2784523T3 (es) 2020-09-28
CO2018005327A2 (es) 2018-05-31
HRP20200561T1 (hr) 2020-06-26
EA035816B1 (ru) 2020-08-14
BR112018010650A8 (pt) 2019-02-26
JP2019501133A (ja) 2019-01-17
SG11201803686UA (en) 2018-06-28
LT3380486T (lt) 2020-05-11

Similar Documents

Publication Publication Date Title
EA201891248A1 (ru) Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта
EA201691940A1 (ru) Новые соединения
EA201790078A1 (ru) Ингибиторы mnk и связанные с ними способы
EA201891091A1 (ru) Соединения ингибитора jak киназы для лечения респираторного заболевания
EA201790764A1 (ru) Новые соединения карбоновых кислот, подходящие для ингибирования микросомальной простагландин-e2-синтазы 1
EA201691857A1 (ru) Соединения, применимые в качестве иммуномодуляторов
EA201891103A1 (ru) Композиции для лечения спинальной мышечной атрофии
EA202090486A3 (ru) Соединения для лечения спинальной мышечной атрофии
EA201892740A3 (ru) Полифторзамещенное соединение в качестве ингибитора тирозинкиназы брутона (btk)
EA201792028A1 (ru) Альфа-цинамидные соединения и композиции как ингибиторы hdac8
EA201500926A1 (ru) Фумараты как пролекарства и их применение при лечении различных заболеваний
EA201790273A1 (ru) Флагеллиновые композиции и их применение
EA201890767A1 (ru) C4-модифицированные производные олеаноловой кислоты для ингибирования il-17 и других применений
EA201591166A1 (ru) Ингибиторы аутотаксина
EA201790781A2 (ru) Противовирусные соединения
MY197440A (en) Heteroamatic compounds as btk inhibitors
EA202090098A1 (ru) Фармацевтические композиции терапевтически активных соединений
MX2018004043A (es) Prevencion, tratamiento y reversion de enfermedad usando cantidades terapeuticamente efectivas de acidos grasos activados.
EA201692091A1 (ru) Хиноксалиновые соединения и их применение
EA201790519A1 (ru) Терапевтические соединения в качестве ингибиторов рецептора орексина-1
EA201792571A1 (ru) Терапевтическое применение l-4-хлорокинуренина
EA201790773A1 (ru) Композиции и способы для ингибирования биологической активности растворимых биомолекул
EA201490516A1 (ru) Бифенилкарбоксиамиды в качестве ингибиторов rock-киназ
EA202191478A1 (ru) Гетероароматические соединения в качестве ингибиторов ванина
EA202190588A1 (ru) Гетероароматические соединения в качестве ингибиторов ванина