JP2014500870A - 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 PDFInfo
- Publication number
- JP2014500870A JP2014500870A JP2013538923A JP2013538923A JP2014500870A JP 2014500870 A JP2014500870 A JP 2014500870A JP 2013538923 A JP2013538923 A JP 2013538923A JP 2013538923 A JP2013538923 A JP 2013538923A JP 2014500870 A JP2014500870 A JP 2014500870A
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- pharmaceutically acceptable
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- 0 *C(*C(C(N(*)*)=O)=C1*)C1(C(*1)=O)c2c1c(*)c(*)c(*)c2* Chemical compound *C(*C(C(N(*)*)=O)=C1*)C1(C(*1)=O)c2c1c(*)c(*)c(*)c2* 0.000 description 7
- MQWCXKGKQLNYQG-UHFFFAOYSA-N CC(CC1)CCC1O Chemical compound CC(CC1)CCC1O MQWCXKGKQLNYQG-UHFFFAOYSA-N 0.000 description 2
- FOSNOMMMKGKRNB-UHFFFAOYSA-N C1CN[IH]CC1 Chemical compound C1CN[IH]CC1 FOSNOMMMKGKRNB-UHFFFAOYSA-N 0.000 description 1
- IDKAKZRYYDCJDU-WALOOIOGSA-N CC(C)(C)C[C@@H]([C@@]([C@@H]1c(cccc2Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@@H]1C(NC(CC1)CCC1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@]([C@@H]1c(cccc2Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@@H]1C(NC(CC1)CCC1O)=O IDKAKZRYYDCJDU-WALOOIOGSA-N 0.000 description 1
- HJUXMSHDBZHSAK-RCNUJAENSA-N CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N(C)[C@H]1C(NC(CC1)CCC1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N(C)[C@H]1C(NC(CC1)CCC1O)=O HJUXMSHDBZHSAK-RCNUJAENSA-N 0.000 description 1
- IDKAKZRYYDCJDU-AEPXTFJPSA-N CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NC(CC1)CCC1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NC(CC1)CCC1O)=O IDKAKZRYYDCJDU-AEPXTFJPSA-N 0.000 description 1
- JTLMNSKNXKBDOI-ZFFYJMMBSA-N CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NCC(CC1)CCC1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NCC(CC1)CCC1O)=O JTLMNSKNXKBDOI-ZFFYJMMBSA-N 0.000 description 1
- HTXXERXORVZZPC-PIZZKARASA-N CC(C)(C)C[C@H]([C@]([C@@H]1c(cccc2Cl)c2F)(c2ccc(C)cc2N2)C2=O)N[C@@H]1C(NC(CC1)CCC1O)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@@H]1c(cccc2Cl)c2F)(c2ccc(C)cc2N2)C2=O)N[C@@H]1C(NC(CC1)CCC1O)=O HTXXERXORVZZPC-PIZZKARASA-N 0.000 description 1
- OYBCSLNXEWAQMA-JXMROGBWSA-N CC(CC1)CCC1/C=N/S(C)(=O)=O Chemical compound CC(CC1)CCC1/C=N/S(C)(=O)=O OYBCSLNXEWAQMA-JXMROGBWSA-N 0.000 description 1
- KVWFRFHLAHUTDH-UHFFFAOYSA-N CC(CC1)CCC1NS(C)(=O)=O Chemical compound CC(CC1)CCC1NS(C)(=O)=O KVWFRFHLAHUTDH-UHFFFAOYSA-N 0.000 description 1
- GLJJKGQEJZOKEQ-IZLXSQMJSA-N C[C@H](C1)C[C@@H]1NS(C)(=O)=O Chemical compound C[C@H](C1)C[C@@H]1NS(C)(=O)=O GLJJKGQEJZOKEQ-IZLXSQMJSA-N 0.000 description 1
- GLJJKGQEJZOKEQ-OLQVQODUSA-N C[C@H](C1)C[C@H]1NS(C)(=O)=O Chemical compound C[C@H](C1)C[C@H]1NS(C)(=O)=O GLJJKGQEJZOKEQ-OLQVQODUSA-N 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
-
- 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
- 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
- A61P17/00—Drugs for dermatological disorders
-
- 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
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Pathology (AREA)
- Radiology & Medical Imaging (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41309410P | 2010-11-12 | 2010-11-12 | |
| US61/413,094 | 2010-11-12 | ||
| US201161451968P | 2011-03-11 | 2011-03-11 | |
| US201161451958P | 2011-03-11 | 2011-03-11 | |
| US61/451,968 | 2011-03-11 | ||
| US61/451,958 | 2011-03-11 | ||
| US201161470992P | 2011-04-01 | 2011-04-01 | |
| US61/470,992 | 2011-04-01 | ||
| PCT/US2011/060300 WO2012065022A2 (en) | 2010-11-12 | 2011-11-11 | Spiro-oxindole mdm2 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014500870A true JP2014500870A (ja) | 2014-01-16 |
| JP2014500870A5 JP2014500870A5 (enExample) | 2014-12-25 |
Family
ID=46048358
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013538923A Ceased JP2014500870A (ja) | 2010-11-12 | 2011-11-11 | スピロ−オキシインドールmdm2アンタゴニスト |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US8680132B2 (enExample) |
| EP (1) | EP2638046A4 (enExample) |
| JP (1) | JP2014500870A (enExample) |
| KR (1) | KR101929188B1 (enExample) |
| CN (1) | CN103298818B (enExample) |
| AR (1) | AR083849A1 (enExample) |
| AU (1) | AU2011326395B2 (enExample) |
| CA (1) | CA2817585A1 (enExample) |
| CO (1) | CO6721010A2 (enExample) |
| CR (1) | CR20130271A (enExample) |
| DO (1) | DOP2013000104A (enExample) |
| EA (1) | EA201390682A1 (enExample) |
| EC (1) | ECSP13012678A (enExample) |
| GT (1) | GT201300118A (enExample) |
| IL (1) | IL226275A0 (enExample) |
| MA (1) | MA34732B1 (enExample) |
| MX (1) | MX2013005238A (enExample) |
| NI (1) | NI201300041A (enExample) |
| NZ (1) | NZ611866A (enExample) |
| PE (1) | PE20140408A1 (enExample) |
| PH (1) | PH12013500955A1 (enExample) |
| SG (1) | SG190230A1 (enExample) |
| TW (1) | TWI535723B (enExample) |
| UA (1) | UA109464C2 (enExample) |
| UY (1) | UY33725A (enExample) |
| WO (1) | WO2012065022A2 (enExample) |
| ZA (1) | ZA201304042B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021508727A (ja) * | 2017-12-29 | 2021-03-11 | 甘李薬業股▲フン▼有限公司Gan&Lee Pharmaceuticals | 腫瘍阻害剤として使用できる化合物およびその調製方法と応用 |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG176463A1 (en) | 2005-02-22 | 2011-12-29 | Univ Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| US8889632B2 (en) | 2007-01-31 | 2014-11-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| EP2508531B1 (en) | 2007-03-28 | 2016-10-19 | President and Fellows of Harvard College | Stitched polypeptides |
| NZ600430A (en) | 2009-11-12 | 2014-06-27 | Univ Michigan | Spiro-oxindole mdm2 antagonists |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| RU2016111360A (ru) | 2010-08-13 | 2018-11-27 | Эйлерон Терапьютикс, Инк. | Пептидомиметические макроциклы |
| SI2684880T1 (en) | 2011-03-10 | 2018-08-31 | Daiichi Sankyo Company, Limited | DERIVAT DISPIROPYROLIDINE |
| JP2014513699A (ja) | 2011-05-11 | 2014-06-05 | 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 |
| CN108929375A (zh) | 2011-10-18 | 2018-12-04 | 爱勒让治疗公司 | 拟肽大环化合物 |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| RU2017145921A (ru) | 2012-02-15 | 2019-02-21 | Эйлерон Терапьютикс, Инк. | Пептидомиметические макроциклы |
| US8993614B2 (en) | 2012-03-15 | 2015-03-31 | F. Hoffmann-La Roche Ag | Substituted pyrrolidine-2-carboxamides |
| CN104321325B (zh) | 2012-05-24 | 2016-11-16 | 诺华股份有限公司 | 吡咯并吡咯烷酮化合物 |
| CN104812384B (zh) | 2012-11-01 | 2020-09-18 | 爱勒让治疗公司 | 二取代的氨基酸及其制备和使用方法 |
| CA2895504A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| EP2752191A1 (en) | 2013-01-07 | 2014-07-09 | Sanofi | Compositions and methods using hdm2 antagonist and mek inhibitor |
| WO2014115077A1 (en) | 2013-01-22 | 2014-07-31 | Novartis Ag | Substituted purinone compounds |
| US9556180B2 (en) | 2013-01-22 | 2017-01-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction |
| EA029312B1 (ru) | 2013-05-27 | 2018-03-30 | Новартис Аг | Производные имидазопирролидинона и их применение при лечении заболеваний |
| CN105246896B (zh) | 2013-05-28 | 2017-09-08 | 诺华股份有限公司 | 吡唑并吡咯烷‑4‑酮衍生物及其在治疗疾病中的用途 |
| CA2912986A1 (en) | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
| AU2014351413B2 (en) | 2013-11-21 | 2017-06-01 | Novartis Ag | Pyrrolopyrrolone derivatives and their use as BET inhibitors |
| EP3669881B1 (en) | 2014-01-28 | 2022-03-30 | Buck Institute for Research on Aging | Compositions for use in the treatment of senescence-assiocated eye disease and disorders |
| US9745314B2 (en) | 2014-04-17 | 2017-08-29 | The Regents Of The University Of Michigan | MDM2 inhibitors and therapeutic methods using the same |
| TW201613576A (en) * | 2014-06-26 | 2016-04-16 | Novartis Ag | Intermittent dosing of MDM2 inhibitor |
| EP3164401B1 (en) | 2014-07-03 | 2018-12-26 | Boehringer Ingelheim International GmbH | New spiro[3h-indole-3,2´-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors |
| WO2016028391A2 (en) | 2014-08-18 | 2016-02-25 | Hudson Biopharma Inc. | Spiropyrrolidines as mdm2 inhibitors |
| CN107001385B (zh) | 2014-08-21 | 2020-03-13 | 勃林格殷格翰国际有限公司 | 作为mdm2-p53抑制剂的螺-[3h-吲哚-3,2’-吡咯烷]-2(1h)-酮化合物及其衍生物 |
| JP2017533889A (ja) | 2014-09-24 | 2017-11-16 | 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使用 |
| MX389354B (es) | 2014-09-24 | 2025-03-20 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y formulaciones de los mismos. |
| US10253067B2 (en) | 2015-03-20 | 2019-04-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| US10023613B2 (en) | 2015-09-10 | 2018-07-17 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles as modulators of MCL-1 |
| JP6602470B2 (ja) | 2015-10-09 | 2019-11-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Mdm2−p53阻害薬としてのスピロ[3h−インドール−3,2‘−ピロリジン]−2(1h)−オン化合物及び誘導体 |
| CN105693738A (zh) * | 2016-01-14 | 2016-06-22 | 绍兴文理学院 | 3’-苯基螺[吲哚啉-3,2’-吡咯烷]-2-酮类衍生物及其制备方法和应用 |
| CN109311900A (zh) | 2016-04-06 | 2019-02-05 | 密执安大学评议会 | 用于配体依赖性靶蛋白质降解的单官能中间体 |
| CN109415336B (zh) | 2016-04-06 | 2023-08-29 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| WO2017201449A1 (en) | 2016-05-20 | 2017-11-23 | Genentech, Inc. | Protac antibody conjugates and methods of use |
| CN107652296B (zh) * | 2016-07-26 | 2020-08-04 | 南开大学 | 螺环氧化吲哚酰腙衍生物及其制备方法和在防治植物病毒、杀菌、杀虫方面的应用 |
| WO2018027477A1 (zh) | 2016-08-08 | 2018-02-15 | 肖飞 | 螺环吲哚酮聚乙二醇碳酸酯类化合物和其组合物、制备方法及用途 |
| JP6890659B2 (ja) | 2016-11-15 | 2021-06-18 | ノバルティス アーゲー | HDM2−p53相互作用阻害剤の用量およびレジメン |
| US9822128B1 (en) | 2017-06-01 | 2017-11-21 | King Saud University | Substituted spirooxindoles |
| 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 |
| EP3511334A1 (en) * | 2018-01-16 | 2019-07-17 | Adamed sp. z o.o. | 1,2,3',5'-tetrahydro-2'h-spiro[indole-3,1'-pyrrolo[3,4-c]pyrrole]-2,3'-dione compounds as therapeutic agents activating tp53 |
| EP3863720A1 (en) | 2018-10-08 | 2021-08-18 | The Regents Of The University Of Michigan | Small molecule mdm2 protein degraders |
| JP2023518423A (ja) | 2020-03-19 | 2023-05-01 | カイメラ セラピューティクス, インコーポレイテッド | Mdm2分解剤およびそれらの使用 |
| US11976084B2 (en) | 2020-11-23 | 2024-05-07 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| WO2022159644A1 (en) * | 2021-01-23 | 2022-07-28 | Newave Pharmaceutical Inc. | Spirocyclic mdm2 modulator and uses thereof |
| CN112876488B (zh) * | 2021-02-18 | 2021-12-21 | 苏州大学 | 螺环吲哚啉衍生物及其制备方法和应用 |
| EP4294513A1 (en) | 2021-02-19 | 2023-12-27 | Mevion Medical Systems, Inc. | Gantry for a particle therapy system |
| CN115215872A (zh) * | 2021-04-15 | 2022-10-21 | 中国科学院上海药物研究所 | 具有取代苯基螺[吲哚啉-3,3′-吡咯烷]结构的小分子化合物 |
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| US12398147B2 (en) | 2021-05-11 | 2025-08-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic spiropyrrolidine derived antiviral agents |
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| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| US11912714B2 (en) | 2021-11-12 | 2024-02-27 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| WO2023086350A1 (en) * | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Alkyne-containing antiviral agents |
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| WO2023107419A1 (en) | 2021-12-08 | 2023-06-15 | Enanta Pharmaceuticals, Inc. | Saturated spirocyclics as antiviral agents |
| US12145941B2 (en) | 2021-12-08 | 2024-11-19 | Enanta Pharmaceuticals, Inc. | Heterocyclic antiviral agents |
| CN116283701B (zh) * | 2021-12-21 | 2025-04-22 | 中国科学院上海药物研究所 | 具有4-(取代氨甲基)-5-新戊基-n-取代基吡咯烷-2-甲酰胺结构的化合物 |
| WO2023196307A1 (en) | 2022-04-05 | 2023-10-12 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| WO2024078370A1 (zh) * | 2022-10-13 | 2024-04-18 | 中国科学院上海药物研究所 | 具有取代苯基螺[吲哚啉-3,3'-吡咯烷]结构的小分子化合物 |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008531504A (ja) * | 2005-02-22 | 2008-08-14 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | Mdm2の小分子阻害剤およびその使用 |
| JP2010502620A (ja) * | 2006-08-30 | 2010-01-28 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | Mdm2の小分子阻害剤およびその使用 |
| JP2013510860A (ja) * | 2009-11-12 | 2013-03-28 | 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 |
Family Cites Families (66)
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