JP2021524835A - Ａｘｌキナーゼ阻害剤およびその使用 - Google Patents

Ａｘｌキナーゼ阻害剤およびその使用 Download PDF

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JP2021524835A
JP2021524835A JP2020523746A JP2020523746A JP2021524835A JP 2021524835 A JP2021524835 A JP 2021524835A JP 2020523746 A JP2020523746 A JP 2020523746A JP 2020523746 A JP2020523746 A JP 2020523746A JP 2021524835 A JP2021524835 A JP 2021524835A
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subject
compound
cancer
tartrate
certain embodiments
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JP2021524835A5 (OSRAM
Inventor
アダム・シディッキ−ジャイン
スティーブン・エル・ワーナー
ポール・フリン
デイビッド・ジェイ・ベアス
ジェイソン・マーク・フォークス
望 富松
望 富松
藤村　健
健 藤村
宏紀 楳原
宏紀 楳原
彰人 野々山
彰人 野々山
祥仁 木口屋
祥仁 木口屋
Original Assignee
スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド
スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド
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Publication of JP2021524835A publication Critical patent/JP2021524835A/ja
Publication of JP2021524835A5 publication Critical patent/JP2021524835A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen 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
    • A61K31/33—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
JP2020523746A 2018-04-05 2019-04-05 Ａｘｌキナーゼ阻害剤およびその使用 Pending JP2021524835A (ja)

Applications Claiming Priority (21)

Application Number Priority Date Filing Date Title
US201862653394P 2018-04-05 2018-04-05
US62/653,394 2018-04-05
US201862663146P 2018-04-26 2018-04-26
US62/663,146 2018-04-26
US201862678980P 2018-05-31 2018-05-31
US62/678,980 2018-05-31
US201862688161P 2018-06-21 2018-06-21
US62/688,161 2018-06-21
US201862695609P 2018-07-09 2018-07-09
US62/695,609 2018-07-09
US201862698638P 2018-07-16 2018-07-16
US62/698,638 2018-07-16
US201862760882P 2018-11-13 2018-11-13
US62/760,882 2018-11-13
US201862767475P 2018-11-14 2018-11-14
US62/767,475 2018-11-14
US201862778856P 2018-12-12 2018-12-12
US62/778,856 2018-12-12
US201962813705P 2019-03-04 2019-03-04
US62/813,705 2019-03-04
PCT/US2019/026094 WO2019195753A1 (en) 2018-04-05 2019-04-05 Axl kinase inhibitors and use of the same

Publications (2)

Publication Number Publication Date
JP2021524835A true JP2021524835A (ja) 2021-09-16
JP2021524835A5 JP2021524835A5 (OSRAM) 2022-04-13

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JP2020523746A Pending JP2021524835A (ja) 2018-04-05 2019-04-05 Ａｘｌキナーゼ阻害剤およびその使用

Country Status (13)

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US (3) US11013741B1 (OSRAM)
EP (1) EP3773591A4 (OSRAM)
JP (1) JP2021524835A (OSRAM)
KR (1) KR20210003780A (OSRAM)
CN (1) CN112533602A (OSRAM)
AU (1) AU2019247498A1 (OSRAM)
BR (1) BR112020020246A8 (OSRAM)
CA (1) CA3096984A1 (OSRAM)
IL (1) IL277600A (OSRAM)
MX (1) MX2020010437A (OSRAM)
PH (1) PH12020551853A1 (OSRAM)
SG (1) SG11202009443RA (OSRAM)
WO (1) WO2019195753A1 (OSRAM)

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US12398176B2 (en) 2018-08-27 2025-08-26 Regeneron Pharmaceuticals, Inc. Use of Raman spectroscopy in downstream purification

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BR112020020246A8 (pt) 2018-04-05 2022-10-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de cinase axl e uso dos mesmos
WO2020023910A1 (en) 2018-07-26 2020-01-30 Tolero Pharmaceuticals, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
WO2021067772A1 (en) * 2019-10-04 2021-04-08 Sumitomo Dainippon Pharma Oncology, Inc. Axl inhibitor formulations
WO2022005881A1 (en) * 2020-06-29 2022-01-06 Bacainn Biotherapeutics, Inc. Probenecid compounds for the treatment of inflammasome-mediated lung disease
US20230277631A1 (en) * 2020-07-19 2023-09-07 Aravive Inc Diagnostic methods for cancer using axl decoy receptors
EP4464699A1 (en) * 2022-01-14 2024-11-20 Lisen Therapeutics, Inc. Pyrimidine-2,4-diamine derivatives as well as preparation method therefor and use thereof
WO2024097229A1 (en) * 2022-11-04 2024-05-10 Bacainn Biotherapeutics, Inc. Probenecid compounds for the treatment of inflammasome-mediated dermatological conditions

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