IL284266B2 - History of (pyridin-2-yl)amine as an inhibitor of TGF-β in the cell R1 (ALK5) for cancer treatment - Google Patents

History of (pyridin-2-yl)amine as an inhibitor of TGF-β in the cell R1 (ALK5) for cancer treatment

Info

Publication number
IL284266B2
IL284266B2 IL284266A IL28426621A IL284266B2 IL 284266 B2 IL284266 B2 IL 284266B2 IL 284266 A IL284266 A IL 284266A IL 28426621 A IL28426621 A IL 28426621A IL 284266 B2 IL284266 B2 IL 284266B2
Authority
IL
Israel
Prior art keywords
compound
mixture
ring
pharmaceutically acceptable
alkyl
Prior art date
Application number
IL284266A
Other languages
English (en)
Hebrew (he)
Other versions
IL284266A (en
IL284266B1 (en
Original Assignee
Nexys Therapeutics Inc
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 Nexys Therapeutics Inc filed Critical Nexys Therapeutics Inc
Publication of IL284266A publication Critical patent/IL284266A/en
Publication of IL284266B1 publication Critical patent/IL284266B1/en
Publication of IL284266B2 publication Critical patent/IL284266B2/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
IL284266A 2018-12-27 2019-12-17 History of (pyridin-2-yl)amine as an inhibitor of TGF-β in the cell R1 (ALK5) for cancer treatment IL284266B2 (en)

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 (3)

Publication Number Publication Date
IL284266A IL284266A (en) 2021-08-31
IL284266B1 IL284266B1 (en) 2024-02-01
IL284266B2 true IL284266B2 (en) 2024-06-01

Family

ID=69185691

Family Applications (1)

Application Number Title Priority Date Filing Date
IL284266A IL284266B2 (en) 2018-12-27 2019-12-17 History of (pyridin-2-yl)amine as an inhibitor of TGF-β in the cell R1 (ALK5) for cancer treatment

Country Status (16)

Country Link
US (2) US12102626B2 (https=)
EP (1) EP3902796B1 (https=)
JP (2) JP7515049B2 (https=)
KR (1) KR102832376B1 (https=)
CN (1) CN113348167B (https=)
AR (1) AR117539A1 (https=)
AU (1) AU2019417418B2 (https=)
BR (1) BR112021007006A2 (https=)
CA (1) CA3117838A1 (https=)
EA (1) EA202191619A1 (https=)
ES (1) ES2972516T3 (https=)
IL (1) IL284266B2 (https=)
MX (1) MX2021007738A (https=)
SG (1) SG11202103457PA (https=)
TW (1) TWI884934B (https=)
WO (1) WO2020139636A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021259419A1 (en) 2020-04-21 2022-11-10 Lexicon Pharmaceuticals, Inc. AAK1 inhibitors for use in treating viral infections
US11666575B2 (en) 2020-04-21 2023-06-06 Lexicon Pharmaceuticals, Inc. Pyrazolo[1,5]pyrimidine-based compounds and methods of their use to treat viral 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
US12263576B2 (en) 2021-08-19 2025-04-01 Hyundai Mobis Co., Ltd. Robot system for automated assembly of modular component
MX2024008704A (es) * 2022-01-14 2024-07-22 Shanghai Hansoh Biomedical Co Ltd Derivado policiclico que contiene piridina, y metodo de preparacion de este y uso de este.
CN121554469B (zh) * 2026-01-23 2026-04-17 四川大学华西医院 一种alk5 protac化合物及其应用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1397364B1 (en) 2001-05-24 2007-07-25 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
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
US8080568B1 (en) 2010-06-29 2011-12-20 Ewha University - Industry Collaboration Foundation 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
US20140296248A1 (en) 2011-04-04 2014-10-02 Stichting het Nederlands Kanker Instiuut-Antoni van Leeuwenhoek ziekenhuis Methods and compositions for predicting resistance to anticancer treatment
BR112013028430A2 (pt) * 2011-05-04 2017-08-01 Merck Sharp & Dohme composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto
EP2900665B1 (en) * 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
EP2934525B1 (en) * 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014155300A2 (en) * 2013-03-28 2014-10-02 Aurigene Discovery Technologies Limited Substitued pyrimidine amine derivatives as tak-1 inhibitors
HRP20201384T1 (hr) 2014-01-01 2020-11-27 Medivation Technologies Llc Spojevi i postupci njihove upotrebe
CN106536507B (zh) 2014-04-08 2020-04-07 里格尔药品股份有限公司 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法
JO3336B1 (ar) 2014-10-07 2019-03-13 Lilly Co Eli مركبات أمينو بيريديلوكسي بيرازول
US10702527B2 (en) * 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
KR20180032611A (ko) 2015-07-23 2018-03-30 브리스톨-마이어스 스큅 컴퍼니 Tgf 베타 수용체 길항제
WO2020103817A1 (zh) 2018-11-20 2020-05-28 南京圣和药业股份有限公司 TGF-βR1抑制剂及其应用
EP3990445A4 (en) 2019-06-25 2023-07-05 InventisBio Co., Ltd. HETEROCYCLIC COMPOUNDS, METHODS FOR THEIR PREPARATION AND THEIR METHODS OF USE
CN112707902B (zh) 2020-03-23 2022-04-15 杭州阿诺生物医药科技有限公司 TGF-β受体抑制剂

Also Published As

Publication number Publication date
US20220054465A1 (en) 2022-02-24
EP3902796B1 (en) 2024-02-07
EP3902796C0 (en) 2024-02-07
KR20210110316A (ko) 2021-09-07
JP7515049B2 (ja) 2024-07-12
WO2020139636A1 (en) 2020-07-02
CN113348167B (zh) 2026-01-09
SG11202103457PA (en) 2021-05-28
US20240398776A1 (en) 2024-12-05
AR117539A1 (es) 2021-08-11
MX2021007738A (es) 2021-08-05
EP3902796A1 (en) 2021-11-03
AU2019417418A1 (en) 2021-04-15
CA3117838A1 (en) 2020-07-02
CN113348167A (zh) 2021-09-03
AU2019417418B2 (en) 2025-02-27
TWI884934B (zh) 2025-06-01
JP2023052437A (ja) 2023-04-11
JP2022517730A (ja) 2022-03-10
NZ775362A (en) 2025-02-28
TW202039436A (zh) 2020-11-01
BR112021007006A2 (pt) 2021-08-10
ES2972516T3 (es) 2024-06-13
KR102832376B1 (ko) 2025-07-09
EA202191619A1 (ru) 2021-09-28
US12102626B2 (en) 2024-10-01
IL284266A (en) 2021-08-31
IL284266B1 (en) 2024-02-01

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