TW202315636A - (r)-n-乙基-5-氟-n-異丙基-2-((5-(2-(6-((2-甲氧基乙基)(甲基)胺基)-2-甲基己-3-基)-2,6-二氮雜螺[3.4]辛-6-基)-1,2,4-三𠯤-6-基)氧基)苯甲醯胺苯磺酸鹽 - Google Patents

(r)-n-乙基-5-氟-n-異丙基-2-((5-(2-(6-((2-甲氧基乙基)(甲基)胺基)-2-甲基己-3-基)-2,6-二氮雜螺[3.4]辛-6-基)-1,2,4-三𠯤-6-基)氧基)苯甲醯胺苯磺酸鹽 Download PDF

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TW202315636A
TW202315636A TW111122342A TW111122342A TW202315636A TW 202315636 A TW202315636 A TW 202315636A TW 111122342 A TW111122342 A TW 111122342A TW 111122342 A TW111122342 A TW 111122342A TW 202315636 A TW202315636 A TW 202315636A
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compound
leukemia
ethyl
fluoro
mixture
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TW111122342A
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Chinese (zh)
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蔡偉
學東 戴
奧利維爾 奎羅
喬內斯 圖靈
艾麗西亞 吳
尼古拉斯 達維爾
羅伯特 格特曼
迪帕利 阿胡佳
劉穎濤
維尼特 潘德
愛德華 克萊特爾
西里爾 本海姆
西蒙 斯莫爾德斯
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比利時商健生藥品公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/02Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/46Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW111122342A 2021-06-17 2022-06-16 (r)-n-乙基-5-氟-n-異丙基-2-((5-(2-(6-((2-甲氧基乙基)(甲基)胺基)-2-甲基己-3-基)-2,6-二氮雜螺[3.4]辛-6-基)-1,2,4-三𠯤-6-基)氧基)苯甲醯胺苯磺酸鹽 TW202315636A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2021100466 2021-06-17
WOPCT/CN2021/100466 2021-06-17
CN2022091677 2022-05-09
WOPCT/CN2022/091677 2022-05-09

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TW202315636A true TW202315636A (zh) 2023-04-16

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TW111122342A TW202315636A (zh) 2021-06-17 2022-06-16 (r)-n-乙基-5-氟-n-異丙基-2-((5-(2-(6-((2-甲氧基乙基)(甲基)胺基)-2-甲基己-3-基)-2,6-二氮雜螺[3.4]辛-6-基)-1,2,4-三𠯤-6-基)氧基)苯甲醯胺苯磺酸鹽

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EP (1) EP4355747A1 (https=)
JP (1) JP2024525145A (https=)
KR (1) KR20240021808A (https=)
CN (2) CN117597348A (https=)
AU (1) AU2022292697A1 (https=)
CA (1) CA3220099A1 (https=)
CL (1) CL2023003731A1 (https=)
CO (1) CO2023018577A2 (https=)
DO (1) DOP2023000260A (https=)
IL (1) IL309359A (https=)
MX (1) MX2023014890A (https=)
PE (1) PE20240923A1 (https=)
PH (1) PH12023553300A1 (https=)
TW (1) TW202315636A (https=)
UY (1) UY39823A (https=)
WO (1) WO2022262796A1 (https=)

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Publication number Priority date Publication date Assignee Title
TW202525813A (zh) 2019-12-19 2025-07-01 比利時商健生藥品公司 經取代之直鏈螺環接衍生物
EP4698182A1 (en) 2023-04-17 2026-02-25 Janssen Pharmaceutica NV Combination of a menin-ll1 inhibitor, a dna intercalating agent and a pyrimidine analogue to treat a hematopoietic disorder
WO2025082444A2 (en) 2023-10-20 2025-04-24 Janssen Pharmaceutica Nv (r) -n-ethyl-5-fluoro-n-isopropyl-2- ( (5- (2- (6- ( (2-methoxyethyl) (methyl) amino) -2-methylhexan-3-yl) -2, 6-diazaspiro [3.4] octan-6-yl) -1, 2, 4-triazin-6-yl) oxy) benzamide, formulations and dosage regimens thereof, for use in treating cancer

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CN102984941B (zh) 2009-09-04 2016-08-17 密执安大学评议会 用于治疗白血病的组合物和方法
WO2014164543A1 (en) 2013-03-13 2014-10-09 The Regents Of The University Of Michigan Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
USRE49687E1 (en) 2014-09-09 2023-10-10 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制menin及mll蛋白之交互作用的方法及組合物
HK1246593A1 (zh) 2015-06-04 2018-09-14 Kura Oncology, Inc. 用於抑制menin蛋白与mll蛋白的相互作用的方法及组合物
AU2016378579A1 (en) 2015-12-22 2018-06-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-MLL interaction
US10869868B2 (en) 2016-01-26 2020-12-22 Memorial Sloan Kettering Cancer Center Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia
PH12018501955B1 (en) 2016-03-16 2024-01-24 Kura Oncology Inc Bridged bicyclic inhibitors of menin-mll and methods of use
PL3429591T3 (pl) 2016-03-16 2023-07-17 Kura Oncology, Inc. Podstawione pochodne tieno[2,3-d]pirymidyny jako inhibitory meniny-mll i metody ich zastosowania
JP6991585B2 (ja) 2016-05-02 2022-01-12 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン メニン阻害剤としてのピペリジン
WO2017207387A1 (en) 2016-05-31 2017-12-07 Bayer Pharma Aktiengesellschaft Spiro condensed azetidine derivatives as inhibitors of the menin-mml1 interaction
WO2017214367A1 (en) * 2016-06-10 2017-12-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-mll interaction
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JP2022503792A (ja) 2018-09-26 2022-01-12 クラ オンコロジー,インク. メニン阻害剤を用いた血液悪性腫瘍の処置
TW202525813A (zh) * 2019-12-19 2025-07-01 比利時商健生藥品公司 經取代之直鏈螺環接衍生物

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DOP2023000260A (es) 2024-05-15
WO2022262796A1 (en) 2022-12-22
CN118852178A (zh) 2024-10-29
CA3220099A1 (en) 2022-12-22
AU2022292697A1 (en) 2024-02-01
PH12023553300A1 (en) 2024-04-08
WO2022262796A8 (en) 2023-03-23
IL309359A (en) 2024-02-01
EP4355747A1 (en) 2024-04-24
CN117597348A (zh) 2024-02-23
PE20240923A1 (es) 2024-04-30
CL2023003731A1 (es) 2024-07-05
UY39823A (es) 2023-01-31
MX2023014890A (es) 2024-04-29
KR20240021808A (ko) 2024-02-19
JP2024525145A (ja) 2024-07-10
CO2023018577A2 (es) 2024-01-15

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