JP6971970B2 - ペプチド模倣大環状分子およびその使用 - Google Patents

ペプチド模倣大環状分子およびその使用 Download PDF

Info

Publication number
JP6971970B2
JP6971970B2 JP2018511684A JP2018511684A JP6971970B2 JP 6971970 B2 JP6971970 B2 JP 6971970B2 JP 2018511684 A JP2018511684 A JP 2018511684A JP 2018511684 A JP2018511684 A JP 2018511684A JP 6971970 B2 JP6971970 B2 JP 6971970B2
Authority
JP
Japan
Prior art keywords
independently
xaa
cancer
peptide
macrocyclic molecule
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2018511684A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018536621A5 (enExample
JP2018536621A (ja
Inventor
マニュエル アイバドー,
ヴァンサン ゲラヴァイス,
カレン オルソン,
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rein Therapeutics Inc
Original Assignee
Aileron 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 Aileron Therapeutics Inc filed Critical Aileron Therapeutics Inc
Publication of JP2018536621A publication Critical patent/JP2018536621A/ja
Publication of JP2018536621A5 publication Critical patent/JP2018536621A5/ja
Application granted granted Critical
Publication of JP6971970B2 publication Critical patent/JP6971970B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/664—Amides of phosphorus acids
    • 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
    • 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
    • A61K31/7068—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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15—Depsipeptides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19—Cytokines; Lymphokines; Interferons
    • A61K38/21—Interferons [IFN]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/50—Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y305/00—Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5)
    • C12Y305/01—Hydrolases acting on carbon-nitrogen bonds, other than peptide bonds (3.5) in linear amides (3.5.1)
    • C12Y305/01001—Asparaginase (3.5.1.1)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • G01N33/5023—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects on expression patterns
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Mycology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
JP2018511684A 2015-09-03 2016-09-02 ペプチド模倣大環状分子およびその使用 Expired - Fee Related JP6971970B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201562214142P 2015-09-03 2015-09-03
US62/214,142 2015-09-03
US201662310254P 2016-03-18 2016-03-18
US62/310,254 2016-03-18
US201662344651P 2016-06-02 2016-06-02
US201662344791P 2016-06-02 2016-06-02
US62/344,651 2016-06-02
US62/344,791 2016-06-02
PCT/US2016/050194 WO2017040990A1 (en) 2015-09-03 2016-09-02 Peptidomimetic macrocycles and uses thereof

Publications (3)

Publication Number Publication Date
JP2018536621A JP2018536621A (ja) 2018-12-13
JP2018536621A5 JP2018536621A5 (enExample) 2019-10-17
JP6971970B2 true JP6971970B2 (ja) 2021-11-24

Family

ID=58188595

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018511684A Expired - Fee Related JP6971970B2 (ja) 2015-09-03 2016-09-02 ペプチド模倣大環状分子およびその使用

Country Status (11)

Country Link
US (2) US20170114098A1 (enExample)
EP (1) EP3344275B8 (enExample)
JP (1) JP6971970B2 (enExample)
KR (1) KR20180043835A (enExample)
CN (1) CN108348571B (enExample)
AU (1) AU2016315878A1 (enExample)
BR (1) BR112018003985A2 (enExample)
CA (1) CA2996685A1 (enExample)
IL (1) IL257706A (enExample)
MX (1) MX2018002723A (enExample)
WO (1) WO2017040990A1 (enExample)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2686827C (en) 2006-12-14 2014-09-16 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
CN109627287A (zh) 2007-02-23 2019-04-16 爱勒让治疗公司 三唑大环系统
EP2508531B1 (en) 2007-03-28 2016-10-19 President and Fellows of Harvard College Stitched polypeptides
EP2376100B1 (en) 2009-01-14 2017-10-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2774973A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
SI2603600T1 (sl) 2010-08-13 2019-04-30 Aileron Therapeutics, Inc. Peptidomimetični makrocikli
TW201806968A (zh) 2011-10-18 2018-03-01 艾利倫治療公司 擬肽巨環化合物
KR102112373B1 (ko) 2012-02-15 2020-05-18 에일러론 테라퓨틱스 인코포레이티드 펩티드모방체 마크로사이클
WO2014071241A1 (en) 2012-11-01 2014-05-08 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
BR112017005598A2 (pt) 2014-09-24 2017-12-12 Aileron Therapeutics Inc macrociclos peptidomiméticos e usos dos mesmos
JP2018503595A (ja) 2014-09-24 2018-02-08 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. ペプチド模倣大環状分子およびその製剤
WO2016154058A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
US20190240210A1 (en) * 2016-10-17 2019-08-08 Daiichi Sankyo Company, Limited Treatment Method by Combined Use of MDM2 Inhibitor and DNA Methyltransferase Inhibitor
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
US11040027B2 (en) 2017-01-17 2021-06-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
EP3621633A2 (en) * 2017-05-11 2020-03-18 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
EP3630840A1 (en) 2017-06-01 2020-04-08 Bristol-Myers Squibb Company Methods of treating a tumor using an anti-pd-1 antibody
WO2018218633A1 (en) 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
JP2021515013A (ja) * 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法
WO2019195959A1 (en) 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
JP2021527666A (ja) 2018-06-21 2021-10-14 アイカーン スクール オブ メディスン アット マウント シナイ Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法
WO2020010204A1 (en) 2018-07-05 2020-01-09 Icahn School Of Medicine At Mount Sinai Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use
US11091522B2 (en) * 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
WO2020036852A1 (en) 2018-08-13 2020-02-20 Beijing Percans Oncology Co. Ltd. Biomarkers for cancer therapy
MY204234A (en) 2018-08-27 2024-08-16 Regeneron Pharma Use of raman spectroscopy in downstream purification
WO2020112868A1 (en) * 2018-11-30 2020-06-04 Aileron Therapeutics, Inc. Combination therapy of peptidomimetic macrocycles
WO2020123656A1 (en) * 2018-12-11 2020-06-18 Kartos Therapeutics Methods and compositions of treating an ophthalmic condition
CN109731104A (zh) * 2018-12-29 2019-05-10 苏州明基医院有限公司 一种多肽-稀土材料递送系统及制备方法和应用
EP3938051A4 (en) * 2019-03-15 2022-12-07 Aileron Therapeutics, Inc. PEPTIDOMIMETIC MACROCYCLES AND USES THEREOF
WO2020198734A1 (en) * 2019-03-28 2020-10-01 The Penn State Research Foundation Methods, compositions relating to treatment of cancer
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
WO2021202961A1 (en) * 2020-04-02 2021-10-07 United States As Represented By Dept Of Veterans Affairs Methods of treating immunotherapy resistant metastatic melanoma
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CA3183081A1 (en) 2020-06-24 2021-12-30 Arnold Levine Combination therapy for treatment of cancer
CN111825621A (zh) * 2020-07-22 2020-10-27 天津理工大学 一种奥拉帕尼与丙二酸的共晶及其制备方法
US11760747B2 (en) 2020-12-21 2023-09-19 Alkermes, Inc. Substituted piperidino compounds and related methods of treatment
JP7833486B2 (ja) 2021-05-26 2026-03-19 アルカーメス,インコーポレイテッド 置換されるカルバメート大環状化合物および関連のある治療方法
CN115137731B (zh) * 2022-05-19 2023-11-21 上海交通大学医学院附属新华医院 Flt3抑制剂及其药学上可接受的盐在制备治疗皮肤t细胞淋巴瘤药物中的应用
WO2024083223A1 (zh) * 2022-10-21 2024-04-25 正大天晴药业集团股份有限公司 大环类化合物及其医药用途
GB202219576D0 (en) * 2022-12-22 2023-02-08 Univ Court Univ Of Glasgow Polypeptides
AU2024361979A1 (en) * 2023-10-20 2026-03-05 Alkermes, Inc. Compound for use in treating narcolepsy
WO2025096608A1 (en) * 2023-10-31 2025-05-08 The Board Of Trustees Of The Leland Stanford Junior University Egfr covalent inhibition with macrocycles

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US5364851A (en) 1991-06-14 1994-11-15 International Synthecon, Llc Conformationally restricted biologically active peptides, methods for their production and uses thereof
US5446128A (en) 1993-06-18 1995-08-29 The Board Of Trustees Of The University Of Illinois Alpha-helix mimetics and methods relating thereto
US5824483A (en) 1994-05-18 1998-10-20 Pence Inc. Conformationally-restricted combinatiorial library composition and method
US5811515A (en) 1995-06-12 1998-09-22 California Institute Of Technology Synthesis of conformationally restricted amino acids, peptides, and peptidomimetics by catalytic ring closing metathesis
US6713280B1 (en) 1999-04-07 2004-03-30 Thomas Jefferson University Enhancement of peptide cellular uptake
US7192713B1 (en) 1999-05-18 2007-03-20 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
ES2367430T3 (es) 2002-12-23 2011-11-03 Wyeth Llc Anticuerpos contra pd-1 y sus usos.
WO2005118620A2 (en) 2004-05-27 2005-12-15 New York University Methods for preparing internally constraied peptides and peptidomimetics
EP3530736A3 (en) 2005-05-09 2019-11-06 ONO Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
KR101704734B1 (ko) 2005-07-01 2017-02-09 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체
US7932397B2 (en) 2006-11-22 2011-04-26 Massachusetts Institute Of Technology Olefin metathesis catalysts and related methods
EP2508531B1 (en) 2007-03-28 2016-10-19 President and Fellows of Harvard College Stitched polypeptides
PT2170959E (pt) 2007-06-18 2014-01-07 Merck Sharp & Dohme Anticorpos para o receptor humano de morte programada pd-1
CA2712503C (en) 2008-01-25 2017-04-18 Massachusetts Institute Of Technology Catalysts for metathesis reactions including enantioselective olefin metathesis, and related methods
WO2010098788A2 (en) 2008-08-25 2010-09-02 Amplimmune, Inc. Pd-i antagonists and methods for treating infectious disease
WO2010060112A1 (en) * 2008-11-24 2010-05-27 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with improved properties
MX356367B (es) 2008-12-09 2018-05-25 Genentech Inc Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t.
EP2504028A4 (en) 2009-11-24 2014-04-09 Amplimmune Inc SIMULTANEOUS INHIBITION OF PD-L1 / PD-L2
US8598400B2 (en) 2010-02-08 2013-12-03 Massachusetts Institute Of Technology Efficient methods for Z- or cis-selective cross-metathesis
SI2603600T1 (sl) * 2010-08-13 2019-04-30 Aileron Therapeutics, Inc. Peptidomimetični makrocikli
BR112014002353B1 (pt) 2011-08-01 2022-09-27 Genentech, Inc Usos de antagonistas de ligação do eixo pd-1 e inibidores de mek, composições farmacêuticas, e kit
KR102112373B1 (ko) * 2012-02-15 2020-05-18 에일러론 테라퓨틱스 인코포레이티드 펩티드모방체 마크로사이클
EP2817023A4 (en) * 2012-02-22 2015-11-25 Univ New York REVERSIBLE NETWORKED SCREW-MOUNTED HYDROGEN BONDING SUPPLY MACROCYCLES
EP3077004B1 (en) * 2013-12-05 2020-02-19 F.Hoffmann-La Roche Ag Novel combination treatment for acute myeloid leukemia (aml)
BR112017005598A2 (pt) * 2014-09-24 2017-12-12 Aileron Therapeutics Inc macrociclos peptidomiméticos e usos dos mesmos
JP2018503595A (ja) * 2014-09-24 2018-02-08 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. ペプチド模倣大環状分子およびその製剤
WO2016154058A1 (en) * 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof

Also Published As

Publication number Publication date
CN108348571B (zh) 2022-03-22
EP3344275A1 (en) 2018-07-11
KR20180043835A (ko) 2018-04-30
BR112018003985A2 (pt) 2018-09-25
AU2016315878A1 (en) 2018-03-29
IL257706A (en) 2018-04-30
CA2996685A1 (en) 2017-03-09
EP3344275B8 (en) 2023-04-12
WO2017040990A1 (en) 2017-03-09
EP3344275A4 (en) 2019-05-01
CN108348571A (zh) 2018-07-31
MX2018002723A (es) 2018-08-15
US20170114098A1 (en) 2017-04-27
US20200369728A1 (en) 2020-11-26
JP2018536621A (ja) 2018-12-13
EP3344275B1 (en) 2023-03-08

Similar Documents

Publication Publication Date Title
CN108348571B (zh) 拟肽大环化合物及其用途
JP2018536621A5 (enExample)
KR20180128022A (ko) 펩티드 모방 거대고리에 대한 동반 진단 도구
US10471120B2 (en) Peptidomimetic macrocycles and uses thereof
JP2018516844A (ja) ペプチド模倣大環状分子およびその使用
US11091522B2 (en) Peptidomimetic macrocycles and uses thereof
JP2020519595A (ja) ペプチド模倣大環状分子およびその使用
RS62630B1 (sr) Modulatori aktivnosti komplementa
JP2022525416A (ja) ペプチド模倣大環状分子およびその使用
WO2020112868A1 (en) Combination therapy of peptidomimetic macrocycles
HK40043424A (en) Peptidomimetic macrocycles and uses thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190902

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190902

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200721

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201021

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210310

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210610

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20211006

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20211102

R150 Certificate of patent or registration of utility model

Ref document number: 6971970

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees