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 | ||
| US201161451958P | 2011-03-11 | 2011-03-11 | |
| US201161451968P | 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 (64)
| 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 |
| EP2952522B1 (en) | 2007-01-31 | 2019-10-30 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| ES2430067T3 (es) | 2007-03-28 | 2013-11-18 | President And Fellows Of Harvard College | Polipéptidos cosidos |
| RU2553269C2 (ru) | 2009-11-12 | 2015-06-10 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Спирооксиндольные антагонисты mdm2 |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| PL2603600T3 (pl) | 2010-08-13 | 2019-06-28 | Aileron Therapeutics, Inc. | Makrocykle peptidomometyczne |
| TR201807311T4 (tr) | 2011-03-10 | 2018-06-21 | Daiichi Sankyo Co Ltd | Dispiropirolidin derivesi. |
| 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 |
| CA2852468A1 (en) | 2011-10-18 | 2013-04-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocyles |
| MX362492B (es) | 2012-02-15 | 2019-01-21 | Aileron Therapeutics Inc | Macrociclos peptidomiméticos. |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| 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 |
| SG11201503052RA (en) | 2012-11-01 | 2015-05-28 | Aileron Therapeutics Inc | Disubstituted amino acids and methods of preparation and use thereof |
| 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 |
| US9403827B2 (en) | 2013-01-22 | 2016-08-02 | Novartis Ag | Substituted purinone compounds |
| EP2948453B1 (en) | 2013-01-22 | 2017-08-02 | Novartis AG | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction |
| EP3004109A1 (en) | 2013-05-27 | 2016-04-13 | Novartis AG | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| EA028035B1 (ru) | 2013-05-28 | 2017-09-29 | Новартис Аг | Производные пиразолопирролидин-4-она и их применение при лечении заболевания |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| WO2015075665A1 (en) | 2013-11-21 | 2015-05-28 | Novartis Ag | Pyrrolopyrrolone derivatives and their use as bet inhibitors |
| IL311537A (en) | 2014-01-28 | 2024-05-01 | Mayo Found Medical Education & Res | Methods and preparations for killing aging cells and for the treatment of diseases and disorders related to aging |
| CN106794171B (zh) | 2014-04-17 | 2020-03-24 | 密歇根大学董事会 | Mdm2抑制剂和使用其的治疗方法 |
| 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 |
| WO2016028391A2 (en) | 2014-08-18 | 2016-02-25 | Hudson Biopharma Inc. | Spiropyrrolidines as mdm2 inhibitors |
| EA038071B1 (ru) | 2014-08-21 | 2021-07-01 | Бёрингер Ингельхайм Интернациональ Гмбх | СОЕДИНЕНИЕ СПИРО[3H-ИНДОЛ-3,2'-ПИРРОЛИДИН]-2(1H)-ОНА И ЕГО ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ MDM2-p53 |
| SG11201702223UA (en) | 2014-09-24 | 2017-04-27 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and uses thereof |
| US10905739B2 (en) | 2014-09-24 | 2021-02-02 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and formulations thereof |
| AU2016235424A1 (en) | 2015-03-20 | 2017-10-05 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| EP3347372A4 (en) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1 |
| MX377009B (es) | 2015-10-09 | 2025-03-07 | Boehringer Ingelheim Int | Nuevos compuestos de espiro[3h-indol-3,2´-pirrolidin]-2(1h)-ona y derivados como inhibidores de 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 |
| JP7001614B2 (ja) | 2016-04-06 | 2022-02-03 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | リガンド依存性の標的タンパク質分解のための単官能性中間体 |
| 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 |
| 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 |
| JP6848047B2 (ja) | 2016-08-08 | 2021-03-24 | フェイ シアオ， | スピロインドロンポリエチレングリコールカーボネート系化合物及びその組成物、調製方法及びその使用 |
| WO2018092020A1 (en) | 2016-11-15 | 2018-05-24 | Novartis Ag | Dose and regimen for hdm2-p53 interaction inhibitors |
| US9822128B1 (en) | 2017-06-01 | 2017-11-21 | King Saud University | Substituted spirooxindoles |
| CA3087110A1 (en) * | 2017-12-29 | 2019-07-04 | Gan & Lee Pharmaceuticals | Compounds capable of being used as tumor inhibitor, preparation method thereof, and application thereof |
| 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 |
| BR112021006647A2 (pt) | 2018-10-08 | 2021-07-13 | The Regents Of The University Of Michigan | degradores de proteína mdm2 de pequenas moléculas |
| 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. |
| CA3202764A1 (en) | 2020-11-23 | 2022-05-27 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| US20250073340A1 (en) * | 2021-01-23 | 2025-03-06 | 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 |
| US11970502B2 (en) | 2021-05-04 | 2024-04-30 | Enanta Pharmaceuticals, Inc. | 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 |
| WO2023086400A1 (en) | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| US11858945B2 (en) | 2021-11-12 | 2024-01-02 | Enanta Pharmaceuticals, Inc. | Alkyne-containing antiviral agents |
| WO2023086352A1 (en) | 2021-11-12 | 2023-05-19 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| US12145941B2 (en) | 2021-12-08 | 2024-11-19 | Enanta Pharmaceuticals, Inc. | Heterocyclic antiviral agents |
| WO2023107419A1 (en) | 2021-12-08 | 2023-06-15 | Enanta Pharmaceuticals, Inc. | Saturated spirocyclics as 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 |
| CN118047784B (zh) * | 2022-10-13 | 2025-09-16 | 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 |
Family Cites Families (69)
| 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 |
| 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 |
| 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 |
| DE59814452D1 (de) | 1997-01-20 | 2010-06-24 | Immodal Pharmaka Gmbh | Verfahren und stoffe zur freisetzung eines wachstumsfaktors aus endothelzellen, und nach dem verfahren freigesetzter wachstumsfaktor sowie seine verwendung |
| WO1999012904A1 (en) | 1997-09-08 | 1999-03-18 | Arqule, Inc. | Spiro[pyrrolidine-2,3'-oxindole] compounds and methods of use |
| EP1109020B1 (en) | 1998-08-20 | 2008-12-24 | Chugai Seiyaku Kabushiki Kaisha | Method for screening candidate compounds for antitumor drug |
| 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 |
| ES2307822T3 (es) | 2001-12-18 | 2008-12-01 | F. Hoffmann-La Roche Ag | Cis-imidazolinas como inhibidores de mdm2. |
| AU2002366278B2 (en) | 2001-12-18 | 2007-07-19 | F. Hoffmann-La Roche Ag | CIS-2,4,5- triphenyl-imidazolines and their use in the treatment of tumors |
| 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 |
| US7514579B2 (en) | 2002-06-13 | 2009-04-07 | Johns Hopkins University | 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 |
| US7498336B2 (en) | 2003-02-13 | 2009-03-03 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Deazaflavin compounds and methods of use thereof |
| US6916833B2 (en) | 2003-03-13 | 2005-07-12 | Hoffmann-La Roche Inc. | Substituted piperidines |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| WO2005046575A2 (en) | 2003-07-29 | 2005-05-26 | Signature R & D Holdings, Lcc | Amino acid prodrugs |
| US8173840B2 (en) | 2003-07-29 | 2012-05-08 | Signature R&D Holdings, Llc | Compounds with high therapeutic index |
| US7589233B2 (en) | 2003-07-29 | 2009-09-15 | Signature R&D Holdings, Llc | L-Threonine derivatives of high therapeutic index |
| WO2005063774A1 (en) | 2003-12-22 | 2005-07-14 | 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 |
| JP4814228B2 (ja) | 2004-05-18 | 2011-11-16 | エフ．ホフマン−ラ ロシュ アーゲー | 新規ｃｉｓ−イミダゾリン |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| NZ553646A (en) | 2004-09-22 | 2010-07-30 | Janssen Pharmaceutica Nv | Inhibitors of the interaction between MDM2 and p53 |
| EP1856123B1 (en) * | 2005-02-22 | 2016-02-17 | The Regents Of The University Of Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| SG176463A1 (en) | 2005-02-22 | 2011-12-29 | Univ Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| UA90145C2 (ru) | 2005-05-24 | 2010-04-12 | Лаборатуар Сероно С.А. | Трициклические спиро-производные как модуляторы crth2 |
| 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 |
| CA2644643C (en) | 2006-03-22 | 2015-05-19 | 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 |
| WO2008036168A2 (en) * | 2006-08-30 | 2008-03-27 | 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 |
| AU2007299130A1 (en) | 2006-09-21 | 2008-03-27 | F. Hoffmann-La Roche Ag | Oxindole derivatives as anticancer agents |
| US7638548B2 (en) | 2006-11-09 | 2009-12-29 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| WO2008072655A1 (ja) | 2006-12-14 | 2008-06-19 | Daiichi Sankyo Company, Limited | 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 |
| BRPI0810082A2 (pt) | 2007-03-29 | 2014-10-21 | Novartis Ag | 3-imidazolil-indóis para o tratamento de doenças 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 |
| JP5438008B2 (ja) | 2007-09-21 | 2014-03-12 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ＭＤＭ２とｐ５３の間の相互作用の阻害剤 |
| 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 |
| RU2553269C2 (ru) * | 2009-11-12 | 2015-06-10 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Спирооксиндольные антагонисты mdm2 |
| 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 |
| RU2012147597A (ru) * | 2010-04-09 | 2014-05-20 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Биомаркеры для ингибиторов mdm2, использующиеся для лечения заболевания |
| 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 |
| 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 |
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