BR112021011861A2 - Inibidores da proteína de ativação de fibroblastos - Google Patents

Inibidores da proteína de ativação de fibroblastos Download PDF

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Publication number
BR112021011861A2
BR112021011861A2 BR112021011861-6A BR112021011861A BR112021011861A2 BR 112021011861 A2 BR112021011861 A2 BR 112021011861A2 BR 112021011861 A BR112021011861 A BR 112021011861A BR 112021011861 A2 BR112021011861 A2 BR 112021011861A2
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BR
Brazil
Prior art keywords
pharmaceutically acceptable
compound
aryl
acceptable salt
cyano
Prior art date
Application number
BR112021011861-6A
Other languages
English (en)
Portuguese (pt)
Inventor
Sebastian Bernales
Brahmam Pujala
Dayanand PANPATIL
Gonzalo Andrés Ureta Díaz
Sebastian BELMAR
Original Assignee
Praxis Biotech LLC
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.)
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Publication date
Application filed by Praxis Biotech LLC filed Critical Praxis Biotech LLC
Publication of BR112021011861A2 publication Critical patent/BR112021011861A2/pt

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    • 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
    • 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
BR112021011861-6A 2019-01-04 2020-01-03 Inibidores da proteína de ativação de fibroblastos BR112021011861A2 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962788722P 2019-01-04 2019-01-04
US62/788,722 2019-01-04
US201962863853P 2019-06-19 2019-06-19
US62/863,853 2019-06-19
PCT/US2020/012260 WO2020142742A1 (en) 2019-01-04 2020-01-03 Inhibitors of fibroblast activation protein

Publications (1)

Publication Number Publication Date
BR112021011861A2 true BR112021011861A2 (pt) 2021-09-08

Family

ID=71404153

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021011861-6A BR112021011861A2 (pt) 2019-01-04 2020-01-03 Inibidores da proteína de ativação de fibroblastos

Country Status (13)

Country Link
US (1) US20200216417A1 (https=)
EP (1) EP3906024A4 (https=)
JP (1) JP2022516555A (https=)
KR (1) KR20210113634A (https=)
CN (1) CN114126597A (https=)
AU (1) AU2020204714A1 (https=)
BR (1) BR112021011861A2 (https=)
CA (1) CA3124525A1 (https=)
CL (1) CL2021001739A1 (https=)
IL (1) IL284434A (https=)
MX (1) MX2021007948A (https=)
SG (1) SG11202106399XA (https=)
WO (1) WO2020142742A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116474108A (zh) 2016-12-14 2023-07-25 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
JP2021506972A (ja) 2017-12-15 2021-02-22 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤
EP3728228A1 (en) 2017-12-22 2020-10-28 Ravenna Pharmaceuticals, Inc. Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
CN113811529A (zh) 2018-12-21 2021-12-17 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
WO2020254559A1 (en) 2019-06-19 2020-12-24 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
WO2021155292A1 (en) * 2020-01-31 2021-08-05 Philip Stewart Low Fibroblast activation protein (fap) - targeted antifibrotic therapy
CN119798158B (zh) * 2022-08-02 2025-10-17 中国科学院上海应用物理研究所 一种含苯并吡啶环类化合物及其制备方法
WO2025159534A1 (ko) * 2024-01-24 2025-07-31 서울대학교산학협력단 3-스티릴피리딘 구조 기반의 섬유아세포 활성화 단백질 표적 물질
CN118978511A (zh) * 2024-08-02 2024-11-19 江苏华益科技有限公司 一种靶向fap化合物及其制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1943257A2 (en) * 2005-05-19 2008-07-16 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
AU2006278039B2 (en) * 2005-08-11 2010-10-21 F. Hoffmann-La Roche Ag Pharmaceutical composition comprising a DPP-lV inhibitor
WO2013107820A1 (en) * 2012-01-17 2013-07-25 Universiteit Antwerpen Novel fap inhibitors
JP2021506972A (ja) * 2017-12-15 2021-02-22 プラクシス バイオテック エルエルシー 線維芽細胞活性化タンパク質の阻害剤
CN113811529A (zh) * 2018-12-21 2021-12-17 普拉西斯生物技术有限责任公司 成纤维细胞激活蛋白抑制剂

Also Published As

Publication number Publication date
AU2020204714A1 (en) 2021-07-08
CA3124525A1 (en) 2020-07-09
EP3906024A1 (en) 2021-11-10
CL2021001739A1 (es) 2022-01-21
IL284434A (en) 2021-08-31
EP3906024A4 (en) 2022-10-26
KR20210113634A (ko) 2021-09-16
JP2022516555A (ja) 2022-02-28
US20200216417A1 (en) 2020-07-09
WO2020142742A1 (en) 2020-07-09
CN114126597A (zh) 2022-03-01
SG11202106399XA (en) 2021-07-29
MX2021007948A (es) 2021-08-11

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B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements