JP2014500870A5 - - Google Patents
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- JP2014500870A5 JP2014500870A5 JP2013538923A JP2013538923A JP2014500870A5 JP 2014500870 A5 JP2014500870 A5 JP 2014500870A5 JP 2013538923 A JP2013538923 A JP 2013538923A JP 2013538923 A JP2013538923 A JP 2013538923A JP 2014500870 A5 JP2014500870 A5 JP 2014500870A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- pharmaceutically acceptable
- compound
- acceptable salt
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 238000000034 method Methods 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 238000006317 isomerization reaction Methods 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000006332 Choriocarcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 201000000582 Retinoblastoma Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000005350 hydroxycycloalkyl group Chemical group 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- LRJBXXRILYOKRP-RTXPCENHSA-N CC(C)(C)C[C@@H]([C@@](C1Cc2ccccc2)(c(ccc(Cl)c2)c2N2)C2=O)N[C@H]1C(N[C@H](CC1)CC[C@@H]1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@](C1Cc2ccccc2)(c(ccc(Cl)c2)c2N2)C2=O)N[C@H]1C(N[C@H](CC1)CC[C@@H]1O)=O LRJBXXRILYOKRP-RTXPCENHSA-N 0.000 description 1
- NQMLXUVTDJNBIP-OLSAQFFOSA-N CC(C)(C)C[C@@H]([C@@]([C@H]1C(C2)C=CC=C2Cl)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N[C@H](CC1)CC[C@@H]1O)=O Chemical compound CC(C)(C)C[C@@H]([C@@]([C@H]1C(C2)C=CC=C2Cl)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N[C@H](CC1)CC[C@@H]1O)=O NQMLXUVTDJNBIP-OLSAQFFOSA-N 0.000 description 1
- DYTUNXFWZMTYRO-HNOBZUPDSA-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(C1)CC1(C)O)=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(C1)CC1(C)O)=O DYTUNXFWZMTYRO-HNOBZUPDSA-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
- MQWCXKGKQLNYQG-UHFFFAOYSA-N CC(CC1)CCC1O Chemical compound CC(CC1)CCC1O MQWCXKGKQLNYQG-UHFFFAOYSA-N 0.000 description 1
- POOPNLXAGUARSE-SRZAULEESA-N CCN([C@@H](CC(C)(C)C)[C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)[C@H]1C(N[C@H](C1)C[C@@]1(C)O)=O Chemical compound CCN([C@@H](CC(C)(C)C)[C@@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)[C@H]1C(N[C@H](C1)C[C@@]1(C)O)=O POOPNLXAGUARSE-SRZAULEESA-N 0.000 description 1
- YFFXIRDLSYBFRD-CKZFGEAVSA-N C[C@@H]([C@@]([C@H]1Cc2ccccc2)(c(c(N2)c3)ccc3Cl)/C2=[O]\c2ccccc2)N[C@H]1C(NC1CCCCC1)=O Chemical compound C[C@@H]([C@@]([C@H]1Cc2ccccc2)(c(c(N2)c3)ccc3Cl)/C2=[O]\c2ccccc2)N[C@H]1C(NC1CCCCC1)=O YFFXIRDLSYBFRD-CKZFGEAVSA-N 0.000 description 1
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 JP2014500870A (ja) | 2014-01-16 |
| JP2014500870A5 true 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) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ561215A (en) | 2005-02-22 | 2010-12-24 | Univ Michigan | Small molecule inhibitors of MDM2 and uses thereof |
| PL2118123T3 (pl) | 2007-01-31 | 2016-06-30 | Dana Farber Cancer Inst Inc | Stabilizowane peptydy p53 i ich zastosowania |
| JP5631201B2 (ja) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ステッチングされたポリペプチド |
| 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 |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| DK2684880T3 (en) | 2011-03-10 | 2018-05-22 | Daiichi Sankyo Co Ltd | DISPIROPYRROLIDINE DERIVATIVES |
| ES2624808T3 (es) | 2011-05-11 | 2017-07-17 | The Regents Of The University Of Michigan | Antagonistas de MDM2 espirooxindólicos |
| EP2768518A4 (en) | 2011-10-18 | 2015-05-27 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| RU2642299C2 (ru) | 2012-02-15 | 2018-01-24 | Эйлерон Терапьютикс, Инк. | P53 пептидомиметические макроциклы |
| US8993614B2 (en) | 2012-03-15 | 2015-03-31 | F. Hoffmann-La Roche Ag | Substituted pyrrolidine-2-carboxamides |
| JP6171003B2 (ja) | 2012-05-24 | 2017-07-26 | ノバルティス アーゲー | ピロロピロリジノン化合物 |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| EP2935263B1 (en) | 2012-12-20 | 2018-12-05 | 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 |
| US9556180B2 (en) | 2013-01-22 | 2017-01-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction |
| US9403827B2 (en) | 2013-01-22 | 2016-08-02 | Novartis Ag | Substituted purinone compounds |
| CA2913697A1 (en) | 2013-05-27 | 2014-12-04 | Novartis Ag | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| 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 |
| CA2912991A1 (en) | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease |
| MX2016006667A (es) | 2013-11-21 | 2016-07-26 | Novartis Ag | Derivados de pirrolo-pirrolona y su uso como inhibidores. |
| SG11201606239UA (en) | 2014-01-28 | 2016-08-30 | Buck Inst For Res On Aging | Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders |
| EP3131544B1 (en) | 2014-04-17 | 2018-12-12 | 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 |
| JP6503386B2 (ja) | 2014-07-03 | 2019-04-17 | 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阻害剤としての新しいスピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン化合物および誘導体 |
| ES2959097T3 (es) | 2014-08-18 | 2024-02-20 | Hudson Biopharma Inc | Espiropirrolidinas como inhibidores de MDM2 |
| ES2739697T3 (es) | 2014-08-21 | 2020-02-03 | Boehringer Ingelheim Int | Nuevos compuestos y derivados de espiro[3H-indol-3,2-pirrolidin]-2(1H)-ona como inhibidores de MDM2-p53 |
| EP3197478A4 (en) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CN107106642B (zh) | 2014-09-24 | 2021-02-26 | 艾瑞朗医疗公司 | 拟肽大环化合物及其制剂 |
| JP2018516844A (ja) | 2015-03-20 | 2018-06-28 | 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 |
| EP3347372A4 (en) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1 |
| HRP20210960T1 (hr) | 2015-10-09 | 2021-09-03 | Boehringer Ingelheim International Gmbh | Spojevi i derivati spiro[3h-indol-3,2’-pirolidin]-2(1h)-ona kao inhibitori mdm2-p53 |
| 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 |
| JP7037500B2 (ja) * | 2016-04-06 | 2022-03-16 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｍｄｍ２タンパク質分解剤 |
| AU2017246453A1 (en) | 2016-04-06 | 2018-11-08 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| 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 |
| EP3498712B1 (en) | 2016-08-08 | 2024-01-03 | Jiangsu Yayo Biotechnology Co. Ltd | Spirocyclic indolone polyethylene glycol carbonate compound, composition, preparation method and use thereof |
| RU2762573C2 (ru) * | 2016-11-15 | 2021-12-21 | Новартис Аг | Доза и режим введения для ингибиторов взаимодействия hdm2 с p53 |
| US9822128B1 (en) | 2017-06-01 | 2017-11-21 | King Saud University | Substituted spirooxindoles |
| BR112020013069A2 (pt) * | 2017-12-29 | 2020-12-01 | Gan & Lee Pharmaceuticals | compostos capazes de serem usados como inibidor de tumor, método de preparação dos mesmos e aplicação dos mesmos |
| 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 |
| MX2021003999A (es) | 2018-10-08 | 2021-06-23 | Univ Michigan Regents | Moleculas de bajo peso molecular degradadoras de la proteina mdm2. |
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| 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 |
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-
2011
- 2011-11-11 CA CA2817585A patent/CA2817585A1/en not_active Abandoned
- 2011-11-11 EP EP11840490.4A patent/EP2638046A4/en not_active Withdrawn
- 2011-11-11 US US13/294,315 patent/US8680132B2/en not_active Expired - Fee Related
- 2011-11-11 MX MX2013005238A patent/MX2013005238A/es active IP Right Grant
- 2011-11-11 TW TW100141225A patent/TWI535723B/zh not_active IP Right Cessation
- 2011-11-11 SG SG2013035894A patent/SG190230A1/en unknown
- 2011-11-11 UY UY0001033725A patent/UY33725A/es not_active Application Discontinuation
- 2011-11-11 UA UAA201307447A patent/UA109464C2/uk unknown
- 2011-11-11 KR KR1020137015168A patent/KR101929188B1/ko not_active Expired - Fee Related
- 2011-11-11 PE PE2013001063A patent/PE20140408A1/es not_active Application Discontinuation
- 2011-11-11 PH PH1/2013/500955A patent/PH12013500955A1/en unknown
- 2011-11-11 AU AU2011326395A patent/AU2011326395B2/en not_active Ceased
- 2011-11-11 WO PCT/US2011/060300 patent/WO2012065022A2/en not_active Ceased
- 2011-11-11 NZ NZ61186611A patent/NZ611866A/en not_active IP Right Cessation
- 2011-11-11 AR ARP110104223A patent/AR083849A1/es unknown
- 2011-11-11 EA EA201390682A patent/EA201390682A1/ru unknown
- 2011-11-11 CN CN201180064853.6A patent/CN103298818B/zh not_active Expired - Fee Related
- 2011-11-11 JP JP2013538923A patent/JP2014500870A/ja not_active Ceased
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2013
- 2013-05-09 IL IL226275A patent/IL226275A0/en unknown
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- 2013-05-09 GT GT201300118A patent/GT201300118A/es unknown
- 2013-05-10 DO DO2013000104A patent/DOP2013000104A/es unknown
- 2013-06-02 EC ECSP13012678 patent/ECSP13012678A/es unknown
- 2013-06-03 ZA ZA2013/04042A patent/ZA201304042B/en unknown
- 2013-06-07 CR CR20130271A patent/CR20130271A/es unknown
- 2013-06-10 MA MA36005A patent/MA34732B1/fr unknown
- 2013-06-12 CO CO13140762A patent/CO6721010A2/es unknown
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- 2014-01-31 US US14/170,101 patent/US9302120B2/en not_active Expired - Fee Related
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