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
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- 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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2499145B1 (OSRAM) |
| JP (1) | JP2013510860A (OSRAM) |
| KR (1) | KR20120099462A (OSRAM) |
| CN (2) | CN102712650B (OSRAM) |
| AR (1) | AR079026A1 (OSRAM) |
| AU (1) | AU2010319595B2 (OSRAM) |
| BR (1) | BR112012011317A2 (OSRAM) |
| CA (1) | CA2780547C (OSRAM) |
| CL (1) | CL2012001250A1 (OSRAM) |
| CO (1) | CO6501131A2 (OSRAM) |
| CR (1) | CR20120313A (OSRAM) |
| DO (1) | DOP2012000131A (OSRAM) |
| EC (1) | ECSP12011943A (OSRAM) |
| GT (1) | GT201200147A (OSRAM) |
| IL (1) | IL219706A (OSRAM) |
| MA (1) | MA33815B1 (OSRAM) |
| MX (1) | MX2012005507A (OSRAM) |
| NI (1) | NI201200083A (OSRAM) |
| NZ (1) | NZ600430A (OSRAM) |
| PE (1) | PE20121282A1 (OSRAM) |
| PH (1) | PH12012500870A1 (OSRAM) |
| RU (1) | RU2553269C2 (OSRAM) |
| TN (1) | TN2012000161A1 (OSRAM) |
| TW (1) | TWI508967B (OSRAM) |
| UA (1) | UA107814C2 (OSRAM) |
| UY (1) | UY33029A (OSRAM) |
| WO (1) | WO2011060049A2 (OSRAM) |
| ZA (1) | ZA201203323B (OSRAM) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2118123T3 (pl) | 2007-01-31 | 2016-06-30 | Dana Farber Cancer Inst Inc | Stabilizowane peptydy p53 i ich zastosowania |
| KR101525754B1 (ko) | 2007-03-28 | 2015-06-09 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
| 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 |
| US8088815B2 (en) * | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| SG184288A1 (en) * | 2010-04-09 | 2012-11-29 | Univ Michigan | Biomarkers for mdm2 inhibitors for use in treating disease |
| CA2807685C (en) | 2010-08-13 | 2020-10-06 | Aileron Therapeutics, Inc. | P53 derived peptidomimetic macrocycle |
| TWI535723B (zh) * | 2010-11-12 | 2016-06-01 | 密西根大學董事會 | 螺－吲哚酮ｍｄｍ２拮抗劑 |
| RU2612534C2 (ru) | 2011-03-10 | 2017-03-09 | Дайити Санкио Компани, Лимитед | Диспиропирролидиновые производные |
| SG194873A1 (en) | 2011-05-11 | 2013-12-30 | Sanofi Sa | Spiro-oxindole mdm2 antagonists |
| TW201806968A (zh) | 2011-10-18 | 2018-03-01 | 艾利倫治療公司 | 擬肽巨環化合物 |
| EP2788004B1 (en) | 2011-12-07 | 2019-07-03 | Duke University | Methods of identifying and using mdm2 inhibitors |
| BR112014020103A2 (pt) | 2012-02-15 | 2018-10-09 | Aileron Therapeutics, Inc. | macrociclos peptidomiméticos |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| 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 |
| BR112015013611A2 (pt) | 2012-12-20 | 2017-11-14 | Merck Sharp & Dohme | composto, e, composição farmacêutica |
| 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 |
| CA2945527C (en) | 2014-04-17 | 2022-05-17 | 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 |
| US10576064B2 (en) | 2014-07-03 | 2020-03-03 | Boehringer Ingelheim International Gmbh | 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 |
| HRP20191414T1 (hr) | 2014-08-21 | 2019-11-01 | Boehringer Ingelheim Int | Novi spojevi i derivati spiro[3h-indol-3,2'-pirolidin]-2(1h)-ona kao mdm1-p53-inhibitori |
| 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 |
| MX2017003797A (es) | 2014-09-24 | 2017-06-15 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
| SG10201902598VA (en) | 2014-09-24 | 2019-04-29 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and formulations 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 |
| US10253067B2 (en) | 2015-03-20 | 2019-04-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CN108368161A (zh) | 2015-09-10 | 2018-08-03 | 艾瑞朗医疗公司 | 作为mcl-1调节剂的拟肽大环化合物 |
| US9962380B2 (en) | 2015-09-23 | 2018-05-08 | Wisconsin Alumni Research Foundation | Methods for treating cognitive deficits associated with fragile X syndrome |
| GB201517216D0 (en) | 2015-09-29 | 2015-11-11 | Cancer Res Technology Ltd And Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201517217D0 (en) | 2015-09-29 | 2015-11-11 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
| HUE054985T2 (hu) * | 2015-10-09 | 2021-11-29 | Boehringer Ingelheim Int | Spiro[3H-indol-3,2'-pirrolidin]-2(1H)-on vegyületek és számrazékok, mint MDM2-P53 inhibitorok |
| 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 |
| CN109152843A (zh) | 2016-05-20 | 2019-01-04 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| GB201704966D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201704965D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| US9822128B1 (en) | 2017-06-01 | 2017-11-21 | King Saud University | Substituted spirooxindoles |
| 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 |
| KR101857408B1 (ko) | 2018-02-28 | 2018-05-14 | 경북대학교 산학협력단 | 탈모 예방 또는 치료용 조성물 |
| SG11202103282YA (en) | 2018-10-08 | 2021-04-29 | Univ Michigan Regents | Small molecule mdm2 protein degraders |
| GB201919219D0 (en) | 2019-12-23 | 2020-02-05 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| MX2022011602A (es) | 2020-03-19 | 2023-01-04 | Kymera Therapeutics Inc | Degradadores de la proteína de homólogo de ratón de minuto 2 (mdm2) y usos de los mismos. |
| US20230313313A1 (en) | 2020-08-27 | 2023-10-05 | Otsuka Pharmaceutical Co., Ltd. | Biomarkers for cancer therapy using mdm2 antagonists |
| EP4247387A1 (en) | 2020-11-23 | 2023-09-27 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| GB202103080D0 (en) | 2021-03-04 | 2021-04-21 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| CN117337327A (zh) * | 2021-04-24 | 2024-01-02 | 通用测序技术公司 | 用于单分子检测的纳米火车 |
| WO2022235605A1 (en) | 2021-05-04 | 2022-11-10 | Enanta Pharmaceuticals, Inc. | Novel macrocyclic antiviral agents |
| US12398147B2 (en) | 2021-05-11 | 2025-08-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic spiropyrrolidine derived antiviral agents |
| US12479854B2 (en) | 2021-07-29 | 2025-11-25 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| WO2023086352A1 (en) | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| WO2023086350A1 (en) | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Alkyne-containing antiviral agents |
| WO2023086400A1 (en) | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| WO2023107419A1 (en) | 2021-12-08 | 2023-06-15 | Enanta Pharmaceuticals, Inc. | Saturated spirocyclics as antiviral agents |
| EP4493561A1 (en) * | 2022-03-18 | 2025-01-22 | Enanta Pharmaceuticals, Inc. | Processes for the preparation of substituted spirooxindole derivatives |
| US12145942B2 (en) | 2022-04-05 | 2024-11-19 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| US11944604B1 (en) | 2023-03-10 | 2024-04-02 | King Saud University | Nanoformulation of spriooxindole and methods for treating hepatocellular carcinoma |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Family Cites Families (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3219661A (en) * | 1962-12-14 | 1965-11-23 | Warner Lambert Pharmaceutical | Spirooxindole and spirodehydroindole alkaloids and process therefor |
| GB1056537A (en) | 1963-07-16 | 1967-01-25 | Smith Kline French Lab | Improvements in or relating to crystalline alkaloids of mitragyna citiata and compositions thereof |
| JPS444986Y1 (OSRAM) | 1966-10-20 | 1969-02-24 | ||
| US3989816A (en) | 1975-06-19 | 1976-11-02 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacycloheptan-2-ones |
| US4444762A (en) | 1980-04-04 | 1984-04-24 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacyclopentan-2-ones |
| JPH044986A (ja) | 1990-04-20 | 1992-01-09 | Nippon Stainless Steel Co Ltd | ニッケル・ステンレス鋼クラッド材の製造方法 |
| US6605712B1 (en) | 1990-12-20 | 2003-08-12 | Arch Development Corporation | Gene transcription and ionizing radiation: methods and compositions |
| RU2084449C1 (ru) | 1994-03-02 | 1997-07-20 | Всероссийский научный центр по безопасности биологически активных веществ | 1-бензил-2-оксотриптамин гидрохлорид и его производные, обладающие гепатозащитной активностью |
| US5773455A (en) | 1996-06-28 | 1998-06-30 | Biomeasure, Incorporated | Inhibitors of prenyl transferases |
| US7083983B2 (en) | 1996-07-05 | 2006-08-01 | Cancer Research Campaign Technology Limited | Inhibitors of the interaction between P53 and MDM2 |
| ATE467418T1 (de) * | 1997-01-20 | 2010-05-15 | Immodal Pharmaka Gmbh | Verfahren und stoffe zur freisetzung eines wachstumsfaktors aus endothelzellen, und nach dem verfahren freigesetzter wachstumsfaktor sowie seine verwendung |
| AU9307098A (en) | 1997-09-08 | 1999-03-29 | Arqule, Inc. | Spiro{pyrrolidine-2,3'-oxindole} compounds and methods of use |
| US7125659B1 (en) | 1998-08-20 | 2006-10-24 | Chugai Seiyaku Kabushiki Kaisha | Method and screening candidate compounds for drug against tumor |
| US7205404B1 (en) | 1999-03-05 | 2007-04-17 | Metabasis Therapeutics, Inc. | Phosphorus-containing prodrugs |
| US6831155B2 (en) | 1999-12-08 | 2004-12-14 | President And Fellows Of Harvard College | Inhibition of p53 degradation |
| CN1182083C (zh) | 2001-10-08 | 2004-12-29 | 廖宜芳 | 一种杀虫灭菌的配位肥及其制造方法 |
| RU2305095C2 (ru) | 2001-12-18 | 2007-08-27 | Ф.Хоффманн-Ля Рош Аг | Цис-2,4,5-трифенилимидазолины и фармацевтическая композиция на их основе |
| JP4361798B2 (ja) | 2001-12-18 | 2009-11-11 | エフ．ホフマン−ラ ロシュ アーゲー | Ｍｄｍ２インヒビターとしてのシス−イミダゾリン |
| JP4023184B2 (ja) | 2002-03-11 | 2007-12-19 | 昭和電工株式会社 | 発光体粒子及びその製造方法並びにその用途 |
| WO2003106384A2 (en) | 2002-06-01 | 2003-12-24 | Johns Hopkins University | Novel boronic chalcone derivatives and uses thereof |
| WO2004043371A2 (en) | 2002-11-08 | 2004-05-27 | Irm Llc | Methods and compositions for modulating p53 transcription factor |
| US20050227932A1 (en) | 2002-11-13 | 2005-10-13 | Tianbao Lu | Combinational therapy involving a small molecule inhibitor of the MDM2: p53 interaction |
| EP1633749A4 (en) | 2003-02-13 | 2011-03-02 | Us Gov Health & Human Serv | Deazaflavin compounds and methods of use thereof |
| US6916833B2 (en) | 2003-03-13 | 2005-07-12 | Hoffmann-La Roche Inc. | Substituted piperidines |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| US7589233B2 (en) | 2003-07-29 | 2009-09-15 | Signature R&D Holdings, Llc | L-Threonine derivatives of high therapeutic index |
| US8173840B2 (en) | 2003-07-29 | 2012-05-08 | Signature R&D Holdings, Llc | Compounds with high therapeutic index |
| CA2534342C (en) | 2003-07-29 | 2016-05-10 | V. Ravi Chandran | Amino acid prodrugs |
| US7829742B2 (en) | 2003-12-22 | 2010-11-09 | Johns Hopkins University | Boronic acid aryl analogs |
| US8598127B2 (en) | 2004-04-06 | 2013-12-03 | Korea Research Institute Of Bioscience & Biotechnology | Peptides for inhibiting MDM2 function |
| TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
| CN1953965B (zh) | 2004-05-18 | 2012-07-04 | 霍夫曼-拉罗奇有限公司 | 新型顺式咪唑啉类化合物 |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| DK1809622T3 (da) | 2004-09-22 | 2010-11-08 | Janssen Pharmaceutica Nv | Inhibitorer af interaktionen mellem MDM2 og P53 |
| SG176463A1 (en) | 2005-02-22 | 2011-12-29 | Univ Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| KR100944301B1 (ko) * | 2005-02-22 | 2010-02-24 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Ｍｄｍ２의 소분자 억제제 및 이의 용도 |
| ZA200709819B (en) | 2005-05-24 | 2009-09-30 | Serono Lab | Tricyclic spiro derivatives as CRTH2 modulators |
| US7576082B2 (en) * | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| US7495007B2 (en) * | 2006-03-13 | 2009-02-24 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| CN101400680B (zh) * | 2006-03-13 | 2012-04-25 | 霍夫曼-拉罗奇有限公司 | 螺吲哚满酮衍生物 |
| EP2001868B1 (en) | 2006-03-22 | 2013-07-17 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between mdm2 and p53 |
| US8222288B2 (en) | 2006-08-30 | 2012-07-17 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| CA2661354C (en) * | 2006-08-30 | 2012-12-18 | The Regents Of The University Of Michigan | New small molecule inhibitors of mdm2 and the uses thereof |
| US7737174B2 (en) * | 2006-08-30 | 2010-06-15 | The Regents Of The University Of Michigan | Indole inhibitors of MDM2 and the uses thereof |
| US8002528B2 (en) * | 2006-09-18 | 2011-08-23 | Emerson Climate Technologies, Inc. | Compressor assembly having vibration attenuating structure |
| JP2010504298A (ja) * | 2006-09-21 | 2010-02-12 | エフ．ホフマン−ラ ロシュ アーゲー | オキシンドール誘導体 |
| US7638548B2 (en) * | 2006-11-09 | 2009-12-29 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| JPWO2008072655A1 (ja) | 2006-12-14 | 2010-04-02 | 第一三共株式会社 | イミダゾチアゾール誘導体 |
| WO2008106507A2 (en) | 2007-02-27 | 2008-09-04 | University Of South Florida | Mdm2/mdmx inhibitor peptide |
| AR065860A1 (es) | 2007-03-29 | 2009-07-08 | Novartis Ag | 3-imidazolil-indoles para el tratamiento de enfermedades proliferativas |
| US7625895B2 (en) | 2007-04-12 | 2009-12-01 | Hoffmann-Le Roche Inc. | Diphenyl-dihydro-imidazopyridinones |
| WO2008130614A2 (en) | 2007-04-20 | 2008-10-30 | University Of Pittsburg-Of The Commonwealth System Of Higher Education | Selective and dual-action p53/mdm2/mdm4 antagonists |
| US7553833B2 (en) * | 2007-05-17 | 2009-06-30 | Hoffmann-La Roche Inc. | 3,3-spiroindolinone derivatives |
| US7834179B2 (en) * | 2007-05-23 | 2010-11-16 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| AU2008300483B2 (en) | 2007-09-21 | 2013-01-10 | Janssen Pharmaceutica Nv | Inhibitors of the interaction between MDM2 and p53 |
| RU2360914C1 (ru) * | 2007-10-31 | 2009-07-10 | Государственное образовательное учреждение высшего профессионального образования "Пермский государственный университет" | Анальгетическое средство |
| CZ301561B6 (cs) | 2007-12-04 | 2010-04-14 | Výzkumný ústav živocišné výroby, v. v. i. | Prostredek pro prevenci a potlacování kokcidióz |
| US8134001B2 (en) * | 2007-12-14 | 2012-03-13 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| US7776875B2 (en) * | 2007-12-19 | 2010-08-17 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| US7723372B2 (en) * | 2008-03-19 | 2010-05-25 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| WO2009151069A1 (ja) | 2008-06-12 | 2009-12-17 | 第一三共株式会社 | ４，７－ジアザスピロ［２．５］オクタン環構造を有するイミダゾチアゾール誘導体 |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| US7928233B2 (en) * | 2009-02-10 | 2011-04-19 | Hoffmann-La Roche Inc. | Spiroindolinone pyridine derivatives |
| US8076482B2 (en) * | 2009-04-23 | 2011-12-13 | Hoffmann-La Roche Inc. | 3,3′-spiroindolinone derivatives |
| 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 |
| US8088815B2 (en) | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| US8288431B2 (en) | 2010-02-17 | 2012-10-16 | Hoffmann-La Roche Inc. | Substituted spiroindolinones |
| WO2011106650A2 (en) | 2010-02-27 | 2011-09-01 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Novel p53-mdm2/p53-mdm4 antagonists to treat proliferative disease |
| SG184288A1 (en) * | 2010-04-09 | 2012-11-29 | Univ Michigan | Biomarkers for mdm2 inhibitors for use in treating disease |
| US8217044B2 (en) * | 2010-04-28 | 2012-07-10 | Hoffmann-La Roche Inc. | Spiroindolinone pyrrolidines |
| US20120046306A1 (en) | 2010-08-18 | 2012-02-23 | David Joseph Bartkovitz | Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists |
| US20120071499A1 (en) | 2010-09-20 | 2012-03-22 | Xin-Jie Chu | Substituted Spiro[3H-Indole-3,6'(5'H)-[1H]Pyrrolo[1,2c]Imidazole-1',2(1H,2'H)-diones |
| TWI535723B (zh) * | 2010-11-12 | 2016-06-01 | 密西根大學董事會 | 螺－吲哚酮ｍｄｍ２拮抗劑 |
| SG194873A1 (en) | 2011-05-11 | 2013-12-30 | Sanofi Sa | Spiro-oxindole mdm2 antagonists |
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- 2010-11-10 AU AU2010319595A patent/AU2010319595B2/en not_active Ceased
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