JP2013510860A5 - - Google Patents
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- JP2013510860A5 JP2013510860A5 JP2012538940A JP2012538940A JP2013510860A5 JP 2013510860 A5 JP2013510860 A5 JP 2013510860A5 JP 2012538940 A JP2012538940 A JP 2012538940A JP 2012538940 A JP2012538940 A JP 2012538940A JP 2013510860 A5 JP2013510860 A5 JP 2013510860A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- group
- hydrogen
- alkyl
- cycloalkyl
- 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.)
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- 229910052739 hydrogen Inorganic materials 0.000 claims 73
- 239000001257 hydrogen Substances 0.000 claims 73
- 150000002431 hydrogen Chemical class 0.000 claims 37
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 26
- 125000000547 substituted alkyl group Chemical group 0.000 claims 21
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 125000003107 substituted aryl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 239000002246 antineoplastic agent Substances 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 230000003463 hyperproliferative effect Effects 0.000 claims 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001768 cations Chemical class 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- -1 hydroxy, amino Chemical group 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010028116 Mucosal inflammation Diseases 0.000 claims 1
- 201000010927 Mucositis Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 125000005466 alkylenyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010013781 dry mouth Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000003265 stomatitis Diseases 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 0 Cc1c(C(C(C(N*)=O)NC2*)C2(c2cc(*)c(*)cc2N2)C2=O)ccc(*)c1* Chemical compound Cc1c(C(C(C(N*)=O)NC2*)C2(c2cc(*)c(*)cc2N2)C2=O)ccc(*)c1* 0.000 description 4
- SVGIKFXUPVGIJZ-IOUGBZEOSA-N CC(C)(C)C[C@@]1([C@]([C@H]2c3cccc(Cl)c3)(c(c(N3)c4)cc(F)c4Cl)C3=O)N[C@@]12C(N(CC1)CCN1C(CCN(C)C)=O)=O Chemical compound CC(C)(C)C[C@@]1([C@]([C@H]2c3cccc(Cl)c3)(c(c(N3)c4)cc(F)c4Cl)C3=O)N[C@@]12C(N(CC1)CCN1C(CCN(C)C)=O)=O SVGIKFXUPVGIJZ-IOUGBZEOSA-N 0.000 description 1
- LCMFMFGEKQZWKG-RNQFHKKWSA-N CC(C)(C)C[C@H]([C@]([C@H]1C(C=CCC2(C)Cl)=C2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NC1CCN(CCF)CC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1C(C=CCC2(C)Cl)=C2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(NC1CCN(CCF)CC1)=O LCMFMFGEKQZWKG-RNQFHKKWSA-N 0.000 description 1
- SIOMNZQLKLUVPT-PVIBPIFHSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cc(Cl)ccc2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N1CCN(C)CC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1c2cc(Cl)ccc2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N1CCN(C)CC1)=O SIOMNZQLKLUVPT-PVIBPIFHSA-N 0.000 description 1
- BFVJDEREIGXMRB-IDIXZGLXSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cc(Cl)ccc2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N1CCNCC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1c2cc(Cl)ccc2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(N1CCNCC1)=O BFVJDEREIGXMRB-IDIXZGLXSA-N 0.000 description 1
- KZWTUFPOBNDANL-JJJJYPGHSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2)(C(C)(C2)C(N3)=CC(Cl)=C2F)C3=O)N[C@H]1C(NCCCN1CCN(C)CC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2)(C(C)(C2)C(N3)=CC(Cl)=C2F)C3=O)N[C@H]1C(NCCCN1CCN(C)CC1)=O KZWTUFPOBNDANL-JJJJYPGHSA-N 0.000 description 1
- KSUKTXCLPYRKPU-PYOQLBSMSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(NCCN1CCN(C)CC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(NCCN1CCN(C)CC1)=O KSUKTXCLPYRKPU-PYOQLBSMSA-N 0.000 description 1
- VNGHSQDRWDIUMR-OHMLLRHZSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(NCCCCN1CCCC1)=O Chemical compound CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)cc(F)c3Cl)C2=O)N[C@H]1C(NCCCCN1CCCC1)=O VNGHSQDRWDIUMR-OHMLLRHZSA-N 0.000 description 1
- WEIZOSMFIYTLEC-WKUQZLKGSA-N CC(C)(C)C[C@H]([C@]([C@H]1c2cccc(Cl)c2F)(c(c(N2)c3)ccc3Cl)C2=O)N[C@H]1C(N)=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(N)=O WEIZOSMFIYTLEC-WKUQZLKGSA-N 0.000 description 1
- BNBHLTMRRPRNBX-RAMXQINQSA-N CC(C)(C)C[C@H](c(c(NC(C1c2cccc(C)c2F)=O)c2)ccc2Cl)N[C@H]1C(NCC(C)(C)O)=O Chemical compound CC(C)(C)C[C@H](c(c(NC(C1c2cccc(C)c2F)=O)c2)ccc2Cl)N[C@H]1C(NCC(C)(C)O)=O BNBHLTMRRPRNBX-RAMXQINQSA-N 0.000 description 1
- GJVHGFSISMSDBY-SKWHODKYSA-N CC(C)(C)C[C@H](c(c(NC(C1c2cccc(Cl)c2F)=O)c2)ccc2Cl)N[C@H]1C(NCCN(CC1)CCN1S(C)(=O)=O)=O Chemical compound CC(C)(C)C[C@H](c(c(NC(C1c2cccc(Cl)c2F)=O)c2)ccc2Cl)N[C@H]1C(NCCN(CC1)CCN1S(C)(=O)=O)=O GJVHGFSISMSDBY-SKWHODKYSA-N 0.000 description 1
- UAEPNZWRGJTJPN-UHFFFAOYSA-N CC1CCCCC1 Chemical compound CC1CCCCC1 UAEPNZWRGJTJPN-UHFFFAOYSA-N 0.000 description 1
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 JP2013510860A (ja) | 2013-03-28 |
| JP2013510860A5 true JP2013510860A5 (enExample) | 2013-12-19 |
Family
ID=43974649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012538940A Pending JP2013510860A (ja) | 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 |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US8518984B2 (enExample) |
| EP (1) | EP2499145B1 (enExample) |
| JP (1) | JP2013510860A (enExample) |
| KR (1) | KR20120099462A (enExample) |
| CN (2) | CN102712650B (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) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2118123E (pt) | 2007-01-31 | 2016-02-10 | Harvard College | Péptidos de p53 estabilizados e suas utilizações |
| 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 |
| BR112012011317A2 (pt) | 2009-11-12 | 2019-09-24 | Univ Michigan Regents | antagonistas espiro-oxindóis de mdm2 |
| US8088815B2 (en) * | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| CN103153302A (zh) * | 2010-04-09 | 2013-06-12 | 密歇根大学董事会 | 针对用于治疗疾病的mdm2抑制剂的生物标记 |
| MX355543B (es) | 2010-08-13 | 2018-04-20 | Aileron Therapeutics Inc Star | Macrociclos peptidomiméticos. |
| AU2011326395B2 (en) * | 2010-11-12 | 2016-01-07 | Ascenta Licensing Corporation | Spiro-oxindole MDM2 antagonists |
| WO2012121361A1 (ja) | 2011-03-10 | 2012-09-13 | 第一三共株式会社 | ジスピロピロリジン誘導体 |
| 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 |
| TWI643868B (zh) | 2011-10-18 | 2018-12-11 | 艾利倫治療公司 | 擬肽巨環化合物 |
| CA2858565A1 (en) * | 2011-12-07 | 2013-07-04 | Duke University | Methods of identifying and using mdm2 inhibitors |
| SG11201404648PA (en) | 2012-02-15 | 2014-09-26 | Aileron Therapeutics Inc | Peptidomimetic macrocycles |
| EP2819688A4 (en) | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER |
| 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 |
| KR20150082307A (ko) | 2012-11-01 | 2015-07-15 | 에일러론 테라퓨틱스 인코포레이티드 | 이치환 아미노산 및 이의 제조 및 사용 방법 |
| CA2895504A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| 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 |
| US9745314B2 (en) * | 2014-04-17 | 2017-08-29 | The Regents Of The University Of Michigan | MDM2 inhibitors and therapeutic methods using the same |
| 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 |
| WO2016001376A1 (en) | 2014-07-03 | 2016-01-07 | 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 |
| PT3183254T (pt) | 2014-08-21 | 2019-08-29 | Boehringer Ingelheim Int | Novos compostos de espiro[3h-indole-3,2¿-pirrolidin]-2(1h)-ona e derivados como inibidores de mdm2-p53 |
| JP6412753B2 (ja) * | 2014-09-19 | 2018-10-24 | 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 |
| JP6408318B2 (ja) * | 2014-09-19 | 2018-10-17 | 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 |
| EP3197477A4 (en) | 2014-09-24 | 2018-07-04 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and formulations thereof |
| SG11201702223UA (en) | 2014-09-24 | 2017-04-27 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and uses thereof |
| WO2016147205A1 (en) * | 2015-03-13 | 2016-09-22 | Council Of Scientific & Industrial Research | Novel substituted 3-spirophosphoryl pyrazole-2-oxindoles as anti-infectives and process for the synthesis thereof |
| KR20170129879A (ko) | 2015-03-20 | 2017-11-27 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
| JP2018528217A (ja) | 2015-09-10 | 2018-09-27 | 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． | Ｍｃｌ−１のモジュレーターとしてのペプチド模倣大環状分子 |
| US9962380B2 (en) | 2015-09-23 | 2018-05-08 | Wisconsin Alumni Research Foundation | Methods for treating cognitive deficits associated with fragile X syndrome |
| GB201517217D0 (en) | 2015-09-29 | 2015-11-11 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
| GB201517216D0 (en) | 2015-09-29 | 2015-11-11 | Cancer Res Technology Ltd And Astex Therapeutics Ltd | Pharmaceutical compounds |
| TWI737635B (zh) * | 2015-10-09 | 2021-09-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為mdm2－p53抑制劑之新穎螺﹝3h－吲哚－3，2´－吡咯啶﹞－2（1h）－酮化合物及其衍生物 |
| US10759808B2 (en) | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CN113788818A (zh) | 2016-04-06 | 2021-12-14 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| 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 |
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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 |
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| US11046703B2 (en) | 2018-10-08 | 2021-06-29 | The Regents Of The University Of Michigan | Small molecule MDM2 protein degraders |
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