JP7423010B2 - Ｂｃｌ－２関連死プロモーター（ｂａｄ）のリン酸化の小分子阻害剤 - Google Patents

Ｂｃｌ－２関連死プロモーター（ｂａｄ）のリン酸化の小分子阻害剤 Download PDF

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JP7423010B2
JP7423010B2 JP2020507978A JP2020507978A JP7423010B2 JP 7423010 B2 JP7423010 B2 JP 7423010B2 JP 2020507978 A JP2020507978 A JP 2020507978A JP 2020507978 A JP2020507978 A JP 2020507978A JP 7423010 B2 JP7423010 B2 JP 7423010B2
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methyl
piperazin
dichlorophenyl
aryl
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ピーター エドワード ロビー
ヴィジャイ クマール パンディ
サブゴウダ ランガッパ カンチューガラコッパル
バサッパ サルンディ
ダナンジャヤ モハン チャクラバヴィ
ショビス ランガッパ
シュリニヴァーサ ヴェンカタチャライアー
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National University of Singapore
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/06—Peri-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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)
  • Professional, Industrial, Or Sporting Protective Garments (AREA)
JP2020507978A 2017-04-19 2018-04-18 Ｂｃｌ－２関連死プロモーター（ｂａｄ）のリン酸化の小分子阻害剤 Active JP7423010B2 (ja)

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Application Number Priority Date Filing Date Title
GB1706162.3 2017-04-19
GBGB1706162.3A GB201706162D0 (en) 2017-04-19 2017-04-19 Compounds
PCT/SG2018/050194 WO2018194520A1 (en) 2017-04-19 2018-04-18 Small molecule inhibitors of bcl-2-associated death promoter (bad) phosphorylation

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JP2020517745A JP2020517745A (ja) 2020-06-18
JP2020517745A5 JP2020517745A5 (https=) 2021-06-10
JP7423010B2 true JP7423010B2 (ja) 2024-01-29

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US (1) US11292773B2 (https=)
EP (1) EP3612518A4 (https=)
JP (1) JP7423010B2 (https=)
KR (1) KR102753110B1 (https=)
CN (1) CN110719906B (https=)
AU (1) AU2018256285B2 (https=)
CA (1) CA3060939A1 (https=)
GB (1) GB201706162D0 (https=)
IL (1) IL270078B (https=)
MX (1) MX2024000001A (https=)
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GB201706162D0 (en) * 2017-04-19 2017-05-31 Nat Univ Singapore Compounds
CN112481298A (zh) * 2020-11-11 2021-03-12 清华-伯克利深圳学院筹备办公室 重组质粒及其应用
CN115340527B (zh) * 2021-05-13 2023-09-15 成都先导药物开发股份有限公司 一种bcl-xl抑制剂及其制备方法和用途

Citations (6)

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JP2002518493A (ja) 1998-06-25 2002-06-25 チバ スペシャルティ ケミカルズ ホールディング インコーポレーテッド ３−アリール−ベンゾフラノンの製造方法
JP2003505420A (ja) 1999-07-26 2003-02-12 シェーリング コーポレイション 咳を処置するのに使用するノシセプチンレセプタｏｒｌ−１
JP2007508350A (ja) 2003-10-15 2007-04-05 イーエムテーエム ゲーエムベーハー 異なる細胞に機能的に影響を及ぼし、免疫性疾患、炎症性疾患、神経疾患、およびその他の疾患を治療するための二重のアラニルアミノペプチダーゼおよびジペプチジルペプチダーゼｉｖの阻害剤
WO2010052448A2 (en) 2008-11-05 2010-05-14 Ucb Pharma S.A. Fused pyrazine derivatives as kinase inhibitors
US20130096133A1 (en) 2011-10-14 2013-04-18 The Board of Trustees of the University lllinois Procaspase-activating compounds and compositions
JP2017128541A (ja) 2016-01-21 2017-07-27 学校法人東京女子医科大学 アポトーシス誘導剤

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US8252832B2 (en) * 2007-12-14 2012-08-28 Novartis Ag Kinesin inhibitors as cancer therapeutics
GB201706162D0 (en) * 2017-04-19 2017-05-31 Nat Univ Singapore Compounds

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Publication number Priority date Publication date Assignee Title
JP2002518493A (ja) 1998-06-25 2002-06-25 チバ スペシャルティ ケミカルズ ホールディング インコーポレーテッド ３−アリール−ベンゾフラノンの製造方法
JP2003505420A (ja) 1999-07-26 2003-02-12 シェーリング コーポレイション 咳を処置するのに使用するノシセプチンレセプタｏｒｌ−１
JP2007508350A (ja) 2003-10-15 2007-04-05 イーエムテーエム ゲーエムベーハー 異なる細胞に機能的に影響を及ぼし、免疫性疾患、炎症性疾患、神経疾患、およびその他の疾患を治療するための二重のアラニルアミノペプチダーゼおよびジペプチジルペプチダーゼｉｖの阻害剤
WO2010052448A2 (en) 2008-11-05 2010-05-14 Ucb Pharma S.A. Fused pyrazine derivatives as kinase inhibitors
US20130096133A1 (en) 2011-10-14 2013-04-18 The Board of Trustees of the University lllinois Procaspase-activating compounds and compositions
JP2017128541A (ja) 2016-01-21 2017-07-27 学校法人東京女子医科大学 アポトーシス誘導剤

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Doan, Phuong; 他，Synthesis and biological screening for cytotoxic activity of N-substituted indolines and morpholines，European Journal of Medicinal Chemistry ，2016年，120,，296-303
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He, Xinwei; Tao, Jiajia; Hu, Xiaoqian; Wang, Hui; Shang, Yongjia，FeCl3-Mediated One-Pot Domino Reactions for the Synthesis of 9-Aryl/9-Arylethynyl-2,3,4,9-tetrahydro-1H-xanthen-1-ones from Propargylic Amines/Diaryl Amines and 1,3-Cyclohexanediones，Journal of Organic Chemistry ，2016年，81(5),，2062-2069
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Schlienger, N.; Bryce, M. R.; Hansen, T. K.，The Boronic Mannich Reaction in a Solid-Phase Approach，Tetrahedron，2000年，56(51)，10023-10030
Tabassum, S.; Govindaraju, S.; Pasha, M. A.，Sonochemistry - an innovative opportunity towards a one-pot three-component synthesis of novel pyridylpiperazine derivatives catalysed by meglumine in water，New Journal of Chemistry ，2017年，41(9),，3515-3523
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Tremblay-Morin, Jean-Philipe; Raeppel, Stephane; Gaudette, Frederic，Lewis acid-catalyzed Mannich type reactions with potassium organotrifluoroborates，Tetrahedron Letters，2004年，45(17),，3471-3474
Yadav, J. S.; Reddy, B. V. Subba; Lakshmi, P. Naga，Ionic liquid-accelerated Petasis reaction. A green protocol for the synthesis of alkylaminophenols，Journal of Molecular Catalysis A: Chemical ，2007年，274(1-2)，101-104

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WO2018194520A9 (en) 2019-10-17
IL270078B (en) 2022-09-01
US20200131139A1 (en) 2020-04-30
WO2018194520A1 (en) 2018-10-25
JP2020517745A (ja) 2020-06-18
EP3612518A1 (en) 2020-02-26
GB201706162D0 (en) 2017-05-31
CA3060939A1 (en) 2018-10-25
US11292773B2 (en) 2022-04-05
CN110719906A (zh) 2020-01-21
MX2024000001A (es) 2024-02-20
KR102753110B1 (ko) 2025-01-09
KR20200029384A (ko) 2020-03-18
AU2018256285B2 (en) 2022-08-04
RU2019135562A (ru) 2021-05-19
SG11201909418WA (en) 2019-11-28
AU2018256285A1 (en) 2019-11-07
CN110719906B (zh) 2023-07-28
IL270078A (https=) 2019-12-31
RU2019135562A3 (https=) 2021-07-21
BR112019022015A2 (pt) 2020-05-12
EP3612518A4 (en) 2020-11-25

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