JP2013510860A - スピロ−オキシインドールｍｄｍ２アンタゴニスト - Google Patents

スピロ−オキシインドールｍｄｍ２アンタゴニスト Download PDF

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JP2013510860A
JP2013510860A JP2012538940A JP2012538940A JP2013510860A JP 2013510860 A JP2013510860 A JP 2013510860A JP 2012538940 A JP2012538940 A JP 2012538940A JP 2012538940 A JP2012538940 A JP 2012538940A JP 2013510860 A JP2013510860 A JP 2013510860A
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hydrogen
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cycloalkyl
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JP2013510860A5 (enExample
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シャオムオン・ワーン
シャンハイ・ユイ
ウェイ・スゥン
サンジーヴ・クマ
ドゥシン・スゥン
ペン・ゾウ
ユジュイン・ジャオ
ドナ・マキーチャーン
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University of Michigan System
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2012538940A 2009-11-12 2010-11-10 スピロ−オキシインドールｍｄｍ２アンタゴニスト Pending JP2013510860A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US26068509P 2009-11-12 2009-11-12
US61/260,685 2009-11-12
US26366209P 2009-11-23 2009-11-23
US61/263,662 2009-11-23
PCT/US2010/056197 WO2011060049A2 (en) 2009-11-12 2010-11-10 Spiro-oxindole mdm2 antagonists

Publications (2)

Publication Number Publication Date
JP2013510860A true JP2013510860A (ja) 2013-03-28
JP2013510860A5 JP2013510860A5 (enExample) 2013-12-19

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US (3) US8518984B2 (enExample)
EP (1) EP2499145B1 (enExample)
JP (1) JP2013510860A (enExample)
KR (1) KR20120099462A (enExample)
CN (2) CN104876938A (enExample)
AR (1) AR079026A1 (enExample)
AU (1) AU2010319595B2 (enExample)
BR (1) BR112012011317A2 (enExample)
CA (1) CA2780547C (enExample)
CL (1) CL2012001250A1 (enExample)
CO (1) CO6501131A2 (enExample)
CR (1) CR20120313A (enExample)
DO (1) DOP2012000131A (enExample)
EC (1) ECSP12011943A (enExample)
GT (1) GT201200147A (enExample)
IL (1) IL219706A (enExample)
MA (1) MA33815B1 (enExample)
MX (1) MX2012005507A (enExample)
NI (1) NI201200083A (enExample)
NZ (1) NZ600430A (enExample)
PE (1) PE20121282A1 (enExample)
PH (1) PH12012500870A1 (enExample)
RU (1) RU2553269C2 (enExample)
TN (1) TN2012000161A1 (enExample)
TW (1) TWI508967B (enExample)
UA (1) UA107814C2 (enExample)
UY (1) UY33029A (enExample)
WO (1) WO2011060049A2 (enExample)
ZA (1) ZA201203323B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
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JP2014500870A (ja) * 2010-11-12 2014-01-16 ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン スピロ−オキシインドールｍｄｍ２アンタゴニスト
JP2016060729A (ja) * 2014-09-19 2016-04-25 日本テルペン化学株式会社 抗菌活性を持つ化合物、およびその製造方法
JP2016060728A (ja) * 2014-09-19 2016-04-25 日本テルペン化学株式会社 抗菌活性を持つ化合物、およびその製造方法
JP2016106111A (ja) * 2011-05-11 2016-06-16 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン スピロ−オキシインドールｍｄｍ２アンタゴニスト
JP2017525768A (ja) * 2014-08-18 2017-09-07 ハドソン・バイオファーマ・インコーポレイテッド Ｍｄｍ２阻害薬としてのスピロピロリジン

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KR20160061439A (ko) 2007-03-28 2016-05-31 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
CA2780547C (en) 2009-11-12 2015-02-03 The Regents Of The University Of Michigan Spiro-oxindole mdm2 antagonists
US8088815B2 (en) * 2009-12-02 2012-01-03 Hoffman-La Roche Inc. Spiroindolinone pyrrolidines
MX2012011600A (es) * 2010-04-09 2012-11-30 Univ Michigan Biomarcadores para inhibidores de mdm2 para su uso en el tratamiento de enfermedad.
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JP6450191B2 (ja) 2012-02-15 2019-01-09 エイルロン セラピューティクス，インコーポレイテッド ペプチドミメティック大環状化合物
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
MX373639B (es) 2012-12-20 2020-05-04 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de doble minuto 2 humana.
CN103739566B (zh) * 2014-01-24 2016-01-20 中国人民解放军第三军医大学 含有磺酰胺的手性五元并环骨架化合物及制备方法和用途
CN111718354A (zh) 2014-04-17 2020-09-29 密歇根大学董事会 Mdm2抑制剂和使用其的治疗方法
CN103992334A (zh) * 2014-05-29 2014-08-20 中国人民解放军第二军医大学 吲哚酮螺四氢硫代吡喃类抗肿瘤衍生物及其制备方法
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CN107312115B (zh) * 2017-06-22 2020-06-12 北京理工大学 一种双吲哚稀土金属催化剂、制备方法及应用
CN109988070B (zh) * 2017-12-29 2022-07-26 南京富润凯德生物医药有限公司 反式-1-羟基-1-(三氟甲基)-3-氨基环丁烷盐酸盐的中间体及制备方法和应用
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EP3863720A1 (en) 2018-10-08 2021-08-18 The Regents Of The University Of Michigan Small molecule mdm2 protein degraders
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Citations (3)

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