EA202191619A1 - Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований - Google Patents

Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований

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Publication number
EA202191619A1
EA202191619A1 EA202191619A EA202191619A EA202191619A1 EA 202191619 A1 EA202191619 A1 EA 202191619A1 EA 202191619 A EA202191619 A EA 202191619A EA 202191619 A EA202191619 A EA 202191619A EA 202191619 A1 EA202191619 A1 EA 202191619A1
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EA
Eurasian Patent Office
Prior art keywords
treatment
alk5
tgf
pyridin
inhibitors
Prior art date
Application number
EA202191619A
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English (en)
Inventor
Том Яо-Хсианг У
Цихой Цзинь
Original Assignee
Нексис Терапьютикс, Инк.
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Application filed by Нексис Терапьютикс, Инк. filed Critical Нексис Терапьютикс, Инк.
Publication of EA202191619A1 publication Critical patent/EA202191619A1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к фармацевтическим соединениям, композициям и способам, в частности, относящимся к композициям и способам для лечения и/или профилактики нарушения пролиферации, ассоциированного с активностью TGFR1, такого как злокачественное новообразование или фиброз. Изобретение относится к соединениям формулы (I) и формулы (II), как представлено в настоящем описании, содержащим кислый остаток, повышающий тканевую специфичность в отношении целевых тканей и органов.Настоящее изобретение включает фармацевтические композиции, фармацевтические комбинации и способы применения этих соединений для лечения состояний, включающих злокачественное новообразование или фиброз.
EA202191619A 2018-12-27 2019-12-17 Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований EA202191619A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862785616P 2018-12-27 2018-12-27
PCT/US2019/066993 WO2020139636A1 (en) 2018-12-27 2019-12-17 (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer

Publications (1)

Publication Number Publication Date
EA202191619A1 true EA202191619A1 (ru) 2021-09-28

Family

ID=69185691

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202191619A EA202191619A1 (ru) 2018-12-27 2019-12-17 Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований

Country Status (16)

Country Link
US (1) US12102626B2 (ru)
EP (1) EP3902796B1 (ru)
JP (2) JP7515049B2 (ru)
KR (1) KR20210110316A (ru)
CN (1) CN113348167A (ru)
AR (1) AR117539A1 (ru)
AU (1) AU2019417418A1 (ru)
BR (1) BR112021007006A2 (ru)
CA (1) CA3117838A1 (ru)
EA (1) EA202191619A1 (ru)
ES (1) ES2972516T3 (ru)
IL (1) IL284266B2 (ru)
MX (1) MX2021007738A (ru)
SG (1) SG11202103457PA (ru)
TW (1) TW202039436A (ru)
WO (1) WO2020139636A1 (ru)

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JP2023522688A (ja) 2020-04-21 2023-05-31 レクシコン ファーマシューティカルズ インコーポレイテッド ウイルス感染症の治療に使用されるaak1阻害剤
EP4138844A1 (en) 2020-04-21 2023-03-01 Lexicon Pharmaceuticals, Inc. 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections
CN113214111A (zh) * 2021-04-30 2021-08-06 上海立科化学科技有限公司 3-(2-氰基苯基)丙酸及4-氰基-1-茚满酮的制备方法
US20230054602A1 (en) 2021-08-19 2023-02-23 Hyundai Mobis Co., Ltd. Robot system for automated assembly of modular component

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DE60221392T2 (de) 2001-05-24 2008-04-17 Eli Lilly And Co., Indianapolis Neue pyrrolderivate als pharmazeutische mittel
UA80571C2 (en) 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
WO2005080377A1 (ja) 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
WO2009022171A1 (en) 2007-08-13 2009-02-19 Astrazeneca Ab Pyridinyiioxy pyridines as alk5 inhibitors
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EP2694677A2 (en) 2011-04-04 2014-02-12 Netherland Cancer Institute Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors
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EP2900665B1 (en) * 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
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WO2014155300A2 (en) * 2013-03-28 2014-10-02 Aurigene Discovery Technologies Limited Substitued pyrimidine amine derivatives as tak-1 inhibitors
SI3089971T1 (sl) 2014-01-01 2020-11-30 Medivation Technologies Llc Spojine in postopki za uporabo
JP6767875B2 (ja) 2014-04-08 2020-10-14 ライジェル ファーマシューティカルズ, インコーポレイテッド Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法
TWI582083B (zh) 2014-10-07 2017-05-11 美國禮來大藥廠 胺基吡啶基氧基吡唑化合物
WO2016201370A1 (en) * 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
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Also Published As

Publication number Publication date
IL284266A (en) 2021-08-31
SG11202103457PA (en) 2021-05-28
EP3902796B1 (en) 2024-02-07
ES2972516T3 (es) 2024-06-13
AU2019417418A1 (en) 2021-04-15
IL284266B2 (en) 2024-06-01
AR117539A1 (es) 2021-08-11
JP7515049B2 (ja) 2024-07-12
JP2022517730A (ja) 2022-03-10
CN113348167A (zh) 2021-09-03
US20220054465A1 (en) 2022-02-24
IL284266B1 (en) 2024-02-01
KR20210110316A (ko) 2021-09-07
EP3902796A1 (en) 2021-11-03
US12102626B2 (en) 2024-10-01
EP3902796C0 (en) 2024-02-07
JP2023052437A (ja) 2023-04-11
WO2020139636A1 (en) 2020-07-02
MX2021007738A (es) 2021-08-05
CA3117838A1 (en) 2020-07-02
BR112021007006A2 (pt) 2021-08-10
TW202039436A (zh) 2020-11-01

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