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
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- JP
- Japan
- Prior art keywords
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- pharmaceutically acceptable
- compound
- acceptable salt
- hydrogen
- Prior art date
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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 (cg-RX-API-DMAC10.html) | 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)
Families Citing this family (64)
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|---|---|---|---|---|
| SG176463A1 (en) | 2005-02-22 | 2011-12-29 | Univ Michigan | Small molecule inhibitors of mdm2 and uses thereof |
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| EP3159352B1 (en) | 2007-03-28 | 2023-08-02 | President and Fellows of Harvard College | Stitched polypeptides |
| EP2499145B1 (en) | 2009-11-12 | 2016-01-27 | The Regents Of The University Of Michigan | Spiro-oxindole mdm2 antagonists |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
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| SG11201608667SA (en) | 2014-04-17 | 2016-11-29 | Univ Michigan | Mdm2 inhibitors and therapeutic methods using the same |
| TW201613576A (en) * | 2014-06-26 | 2016-04-16 | Novartis Ag | Intermittent dosing of MDM2 inhibitor |
| 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 |
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| SI3359542T1 (sl) | 2015-10-09 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Spojine in derivati spiro(3H-indol-3,2'-pirolidin)-2(1H)-ona kot MDM2-P53 inhibitorji |
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