SG11202005563YA - Inhibitors of fibroblast activation protein - Google Patents

Inhibitors of fibroblast activation protein

Info

Publication number
SG11202005563YA
SG11202005563YA SG11202005563YA SG11202005563YA SG11202005563YA SG 11202005563Y A SG11202005563Y A SG 11202005563YA SG 11202005563Y A SG11202005563Y A SG 11202005563YA SG 11202005563Y A SG11202005563Y A SG 11202005563YA SG 11202005563Y A SG11202005563Y A SG 11202005563YA
Authority
SG
Singapore
Prior art keywords
inhibitors
activation protein
fibroblast activation
fibroblast
protein
Prior art date
Application number
SG11202005563YA
Inventor
Jennifer Alfaro
Sebastian Belmar
Sebastian Bernales
Brahmam Pujala
Dayanand Panpatil
Bhawana Bhatt
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.)
Filing date
Publication date
Application filed by Praxis Biotech LLC filed Critical Praxis Biotech LLC
Publication of SG11202005563YA publication Critical patent/SG11202005563YA/en

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Classifications

    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (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)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
SG11202005563YA 2017-12-15 2018-12-14 Inhibitors of fibroblast activation protein SG11202005563YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762599630P 2017-12-15 2017-12-15
PCT/US2018/065859 WO2019118932A1 (en) 2017-12-15 2018-12-14 Inhibitors of fibroblast activation protein

Publications (1)

Publication Number Publication Date
SG11202005563YA true SG11202005563YA (en) 2020-07-29

Family

ID=66815562

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202005563YA SG11202005563YA (en) 2017-12-15 2018-12-14 Inhibitors of fibroblast activation protein

Country Status (13)

Country Link
US (1) US11780821B2 (en)
EP (1) EP3723753A4 (en)
JP (1) JP2021506972A (en)
KR (1) KR20200110653A (en)
CN (1) CN112105354A (en)
AU (1) AU2018386298B2 (en)
BR (1) BR112020011862A2 (en)
CA (1) CA3085803A1 (en)
IL (1) IL275333B2 (en)
MX (1) MX2020006128A (en)
RU (1) RU2020122712A (en)
SG (1) SG11202005563YA (en)
WO (1) WO2019118932A1 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2972577T3 (en) 2016-12-14 2024-06-13 Purdue Research Foundation Imaging and therapy targeting fibroblast activation protein (FAP)
AU2018386298B2 (en) 2017-12-15 2023-09-07 Praxis Biotech LLC Inhibitors of fibroblast activation protein
US11504364B2 (en) 2018-12-21 2022-11-22 Praxis Biotech LLC Inhibitors of fibroblast activation protein
CA3124525A1 (en) * 2019-01-04 2020-07-09 Praxis Biotech LLC Inhibitors of fibroblast activation protein
DK3891138T3 (en) 2020-02-12 2022-04-04 Philochem Ag FIBROBLAST ACTIVATION PROTEIN LIGANDS FOR TARGETED ADMINISTRATION USES
IL295571A (en) * 2020-02-12 2022-10-01 Philochem Ag Fibroblast activation protein ligands for targeted delivery applications
EP4146628A1 (en) * 2020-05-06 2023-03-15 Bayer Aktiengesellschaft Pyridine (thio)amides as fungicidal compounds
EP4147053A1 (en) 2020-05-07 2023-03-15 Institut Curie Antxr1 as a biomarker of immunosuppressive fibroblast populations and its use for predicting response to immunotherapy
US20230295138A1 (en) * 2020-06-04 2023-09-21 Bayer Aktiengesellschaft Heterocyclyl pyridines as novel fungicides
CN116745291A (en) 2020-12-17 2023-09-12 阿斯利康(瑞典)有限公司 N- (2- (4-cyanothiazolidin-3-yl) -2-oxoethyl) -quinoline-4-carboxamide
CN114790195B (en) * 2020-12-21 2024-05-17 苏州药明博锐生物科技有限公司 Fibroblast activation protein inhibitor
CN114790194B (en) * 2020-12-21 2024-03-26 苏州药明博锐生物科技有限公司 Fibroblast activation protein inhibitor
MX2023009486A (en) 2021-02-12 2023-10-16 Philochem Ag Bivalent fibroblast activation protein ligands for targeted delivery applications.
EP4043452A1 (en) 2021-02-12 2022-08-17 Philochem AG Bivalent fibroblast activation protein ligands for targeted delivery applications
CN113105432B (en) * 2021-03-30 2022-03-04 上海交通大学医学院附属仁济医院 Carbon-11 (C)11C) Radiopharmaceutical, preparation method and application thereof
TW202320805A (en) * 2021-08-18 2023-06-01 美商杜夫特學院信託管理公司 Radiofluorinated agents for pet imaging selectively targeting fibroblast activation protein
CN117460826A (en) * 2021-09-14 2024-01-26 菲柏生物医学技术(广州)有限公司 siRNA conjugate targeting FAP positive cells, and pharmaceutical composition and application thereof
MX2024004077A (en) 2021-10-04 2024-04-18 Philochem Ag Radiolabelled fibroblast activation protein ligands.
CN113861111B (en) * 2021-11-23 2023-05-26 浙江工业大学 N-aryl-4-sulfur (selenium) ethyl multi-membered ring [ C ] -1-pyridone derivative and synthetic method and application thereof
WO2023144379A1 (en) 2022-01-30 2023-08-03 Philochem Ag High-affinity ligands of fibroblast activation protein for targeted delivery applications
CN115304582B (en) * 2022-07-20 2023-05-12 北京法伯新天医药科技有限公司 FAP-alpha specific tumor diagnostic imaging agent
WO2024052333A1 (en) 2022-09-06 2024-03-14 Philochem Ag Multivalent fibroblast activation protein ligands for targeted delivery applications

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EP2730571A1 (en) 2012-11-12 2014-05-14 Universitat De Barcelona 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives
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WO2017189569A1 (en) * 2016-04-25 2017-11-02 Trustees Of Tufts College Multimediator dpp4 and fap inhibitors, and uses related thereto
ES2972577T3 (en) 2016-12-14 2024-06-13 Purdue Research Foundation Imaging and therapy targeting fibroblast activation protein (FAP)
EP3554587B1 (en) 2016-12-14 2022-03-30 MedImmune, LLC Embedded multiple-part sensor within a plunger rod to capture and transmit injection information
AU2018355222A1 (en) 2017-10-23 2020-04-30 The Johns Hopkins University Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α)
AU2018386298B2 (en) 2017-12-15 2023-09-07 Praxis Biotech LLC Inhibitors of fibroblast activation protein
AU2019219057B2 (en) 2018-02-06 2022-11-24 Universität Heidelberg FAP inhibitor
US11504364B2 (en) 2018-12-21 2022-11-22 Praxis Biotech LLC Inhibitors of fibroblast activation protein
CA3124525A1 (en) 2019-01-04 2020-07-09 Praxis Biotech LLC Inhibitors of fibroblast activation protein
CA3125929A1 (en) 2019-01-11 2020-07-16 Grunenthal Gmbh Substituted pyrrolidine amides iii

Also Published As

Publication number Publication date
US20190185451A1 (en) 2019-06-20
RU2020122712A (en) 2022-01-18
IL275333B2 (en) 2023-09-01
MX2020006128A (en) 2020-09-21
RU2020122712A3 (en) 2022-01-18
KR20200110653A (en) 2020-09-24
JP2021506972A (en) 2021-02-22
AU2018386298B2 (en) 2023-09-07
EP3723753A4 (en) 2022-01-26
BR112020011862A2 (en) 2020-11-24
IL275333A (en) 2020-07-30
EP3723753A1 (en) 2020-10-21
AU2018386298A1 (en) 2020-07-30
IL275333B1 (en) 2023-05-01
CN112105354A (en) 2020-12-18
US11780821B2 (en) 2023-10-10
CA3085803A1 (en) 2019-06-20
WO2019118932A1 (en) 2019-06-20

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