JP2014528464A5 - - Google Patents
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- Publication number
- JP2014528464A5 JP2014528464A5 JP2014535077A JP2014535077A JP2014528464A5 JP 2014528464 A5 JP2014528464 A5 JP 2014528464A5 JP 2014535077 A JP2014535077 A JP 2014535077A JP 2014535077 A JP2014535077 A JP 2014535077A JP 2014528464 A5 JP2014528464 A5 JP 2014528464A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- fluoro
- alkyl
- deuterium
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 18
- 125000001424 substituent group Chemical group 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 230000002062 proliferating effect Effects 0.000 claims description 17
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 16
- 229910052805 deuterium Inorganic materials 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 16
- AYUNIORJHRXIBJ-TXHRRWQRSA-N tanespimycin Chemical compound N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(NCC=C)C(=O)C=C1C2=O AYUNIORJHRXIBJ-TXHRRWQRSA-N 0.000 claims description 16
- 125000001153 fluoro group Chemical group F* 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 13
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 13
- 210000000244 kidney pelvis Anatomy 0.000 claims description 10
- -1 substituted Chemical class 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 8
- 229950007866 tanespimycin Drugs 0.000 claims description 8
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 5
- 208000003200 Adenoma Diseases 0.000 claims description 5
- 206010001233 Adenoma benign Diseases 0.000 claims description 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 5
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 5
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims description 5
- 208000034578 Multiple myelomas Diseases 0.000 claims description 5
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 5
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 5
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 5
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 5
- 210000000481 breast Anatomy 0.000 claims description 5
- 210000000621 bronchi Anatomy 0.000 claims description 5
- 210000003679 cervix uteri Anatomy 0.000 claims description 5
- 210000001072 colon Anatomy 0.000 claims description 5
- 210000003238 esophagus Anatomy 0.000 claims description 5
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims description 5
- 210000000867 larynx Anatomy 0.000 claims description 5
- 210000004185 liver Anatomy 0.000 claims description 5
- 210000004072 lung Anatomy 0.000 claims description 5
- 208000003747 lymphoid leukemia Diseases 0.000 claims description 5
- 201000001441 melanoma Diseases 0.000 claims description 5
- 208000025113 myeloid leukemia Diseases 0.000 claims description 5
- 210000001672 ovary Anatomy 0.000 claims description 5
- 210000000496 pancreas Anatomy 0.000 claims description 5
- 210000003800 pharynx Anatomy 0.000 claims description 5
- 210000002307 prostate Anatomy 0.000 claims description 5
- 210000000664 rectum Anatomy 0.000 claims description 5
- 210000000813 small intestine Anatomy 0.000 claims description 5
- 210000002784 stomach Anatomy 0.000 claims description 5
- 210000001685 thyroid gland Anatomy 0.000 claims description 5
- 210000003932 urinary bladder Anatomy 0.000 claims description 5
- SWDZPNJZKUGIIH-QQTULTPQSA-N (5z)-n-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2h-1,2-oxazole-3-carboxamide Chemical compound O1NC(C(=O)NCC)=C(C=2C=CC(CN3CCOCC3)=CC=2)\C1=C1/C=C(C(C)C)C(O)=CC1=O SWDZPNJZKUGIIH-QQTULTPQSA-N 0.000 claims description 4
- WSMQUUGTQYPVPD-OAHLLOKOSA-N (7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6h-pyrido[4,3-d]pyrimidin-5-one Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(=O)C3=C(C)N=C(N)N=C3C2)=N1 WSMQUUGTQYPVPD-OAHLLOKOSA-N 0.000 claims description 4
- QQYUAUPJJLOCHU-UHFFFAOYSA-N 6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]purin-2-amine;methanesulfonic acid Chemical compound CS(O)(=O)=O.COC1=C(C)C=NC(CN2C3=NC(N)=NC(Cl)=C3N=C2)=C1C QQYUAUPJJLOCHU-UHFFFAOYSA-N 0.000 claims description 4
- QULDDKSCVCJTPV-UHFFFAOYSA-N BIIB021 Chemical compound COC1=C(C)C=NC(CN2C3=NC(N)=NC(Cl)=C3N=C2)=C1C QULDDKSCVCJTPV-UHFFFAOYSA-N 0.000 claims description 4
- 229940126062 Compound A Drugs 0.000 claims description 4
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims description 4
- AVDSOVJPJZVBTC-UHFFFAOYSA-N [4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate Chemical compound O=C1CC(C)(C)CC2=C1C(C(F)(F)F)=NN2C(C=1)=CC=C(C(N)=O)C=1NC1CCC(OC(=O)CN)CC1 AVDSOVJPJZVBTC-UHFFFAOYSA-N 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 210000004556 brain Anatomy 0.000 claims description 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- QTQAWLPCGQOSGP-GBTDJJJQSA-N geldanamycin Chemical class N1C(=O)\C(C)=C/C=C\[C@@H](OC)[C@H](OC(N)=O)\C(C)=C/[C@@H](C)[C@@H](O)[C@H](OC)C[C@@H](C)CC2=C(OC)C(=O)C=C1C2=O QTQAWLPCGQOSGP-GBTDJJJQSA-N 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- NDAZATDQFDPQBD-UHFFFAOYSA-N luminespib Chemical compound CCNC(=O)C1=NOC(C=2C(=CC(O)=C(C(C)C)C=2)O)=C1C(C=C1)=CC=C1CN1CCOCC1 NDAZATDQFDPQBD-UHFFFAOYSA-N 0.000 claims description 4
- 229950005069 luminespib Drugs 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- VYGYNVZNSSTDLJ-HKCOAVLJSA-N monorden Natural products CC1CC2OC2C=C/C=C/C(=O)CC3C(C(=CC(=C3Cl)O)O)C(=O)O1 VYGYNVZNSSTDLJ-HKCOAVLJSA-N 0.000 claims description 4
- 210000000214 mouth Anatomy 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- AECPBJMOGBFQDN-YMYQVXQQSA-N radicicol Chemical compound C1CCCC(=O)C[C@H]2[C@H](Cl)C(=O)CC(=O)[C@H]2C(=O)O[C@H](C)C[C@H]2O[C@@H]21 AECPBJMOGBFQDN-YMYQVXQQSA-N 0.000 claims description 4
- 229930192524 radicicol Natural products 0.000 claims description 4
- OIRUWDYJGMHDHJ-AFXVCOSJSA-N retaspimycin hydrochloride Chemical compound Cl.N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(O)C1=CC(O)=C2NCC=C OIRUWDYJGMHDHJ-AFXVCOSJSA-N 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 150000001412 amines Chemical class 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000005443 oral cavity cancer Diseases 0.000 claims 1
- 201000008006 pharynx cancer Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 5
- 208000031648 Body Weight Changes Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 230000004579 body weight change Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547308P | 2011-10-14 | 2011-10-14 | |
| US61/547,308 | 2011-10-14 | ||
| PCT/EP2012/070171 WO2013053833A1 (en) | 2011-10-14 | 2012-10-11 | 2 - carboxamide cycloamino urea derivatives in combination with hsp90 inhibitors for the treatment of proliferative diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017114659A Division JP2017214387A (ja) | 2011-10-14 | 2017-06-09 | 増殖性疾患の治療のためのｈｓｐ９０阻害剤と組み合わせた２−カルボキサミドシクロアミノウレア誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014528464A JP2014528464A (ja) | 2014-10-27 |
| JP2014528464A5 true JP2014528464A5 (enExample) | 2015-11-26 |
| JP6180420B2 JP6180420B2 (ja) | 2017-08-16 |
Family
ID=47018207
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014535077A Expired - Fee Related JP6180420B2 (ja) | 2011-10-14 | 2012-10-11 | 増殖性疾患の治療のためのｈｓｐ９０阻害剤と組み合わせた２−カルボキサミドシクロアミノウレア誘導体 |
| JP2017114659A Pending JP2017214387A (ja) | 2011-10-14 | 2017-06-09 | 増殖性疾患の治療のためのｈｓｐ９０阻害剤と組み合わせた２−カルボキサミドシクロアミノウレア誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017114659A Pending JP2017214387A (ja) | 2011-10-14 | 2017-06-09 | 増殖性疾患の治療のためのｈｓｐ９０阻害剤と組み合わせた２−カルボキサミドシクロアミノウレア誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20140275089A1 (enExample) |
| EP (1) | EP2766015A1 (enExample) |
| JP (2) | JP6180420B2 (enExample) |
| KR (1) | KR20140078656A (enExample) |
| CN (2) | CN106474127A (enExample) |
| AU (1) | AU2012322976B2 (enExample) |
| BR (1) | BR112014008400A2 (enExample) |
| CA (1) | CA2851383A1 (enExample) |
| MX (1) | MX2014004559A (enExample) |
| RU (2) | RU2017119219A (enExample) |
| WO (1) | WO2013053833A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2776026A1 (en) * | 2011-11-02 | 2014-09-17 | Novartis AG | 2-carboxamide cycloamino urea derivatives for use in treating vegf - dependent diseases |
| KR20190116420A (ko) | 2017-02-17 | 2019-10-14 | 프레드 헛친슨 켄서 리서치 센터 | Bcma 관련 암 및 자가면역 장애의 치료를 위한 조합 요법 |
| CN111214473B (zh) * | 2020-02-14 | 2022-02-01 | 中国人民解放军陆军军医大学 | Hsp990在制备抗轮状病毒药物中的应用 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4261989A (en) | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| EP1611112B1 (en) | 2003-02-11 | 2012-08-22 | Vernalis (Cambridge) Limited | Isoxazole compounds as inhibitors of heat shock proteins |
| JO2783B1 (en) | 2005-09-30 | 2014-03-15 | نوفارتيس ايه جي | Compounds 2-Amino-7, 8-dihydro-6H-Bayredo (3,4-D) Pyrimidine-5-Ones |
| PL2182948T3 (pl) * | 2007-07-24 | 2013-07-31 | Novartis Ag | Zastosowanie imidazochinolin do leczenia chorób EGFR-zależnych albo chorób wykazujących nabytą oporność wobec środków ukierunkowanych na członków rodziny EGFR |
| TW200922595A (en) * | 2007-10-12 | 2009-06-01 | Novartis Ag | Organic compounds |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| JP2012510444A (ja) * | 2008-11-28 | 2012-05-10 | ノバルティス アーゲー | 治療的処置のためのＨｓｐ９０阻害剤 |
| DE102009012631B4 (de) | 2009-03-11 | 2011-07-28 | Bayer Schering Pharma Aktiengesellschaft, 13353 | Filter für einen Computertomographen sowie Computertomograph |
| CA2815492C (en) * | 2010-11-08 | 2019-04-09 | Novartis Ag | Use of 2-carboxamide cycloamino urea derivatives in the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members |
-
2012
- 2012-10-11 CN CN201610906456.3A patent/CN106474127A/zh active Pending
- 2012-10-11 BR BR112014008400A patent/BR112014008400A2/pt not_active IP Right Cessation
- 2012-10-11 MX MX2014004559A patent/MX2014004559A/es unknown
- 2012-10-11 EP EP12772316.1A patent/EP2766015A1/en not_active Withdrawn
- 2012-10-11 KR KR1020147009376A patent/KR20140078656A/ko not_active Ceased
- 2012-10-11 CA CA2851383A patent/CA2851383A1/en not_active Abandoned
- 2012-10-11 RU RU2017119219A patent/RU2017119219A/ru unknown
- 2012-10-11 US US14/350,577 patent/US20140275089A1/en not_active Abandoned
- 2012-10-11 WO PCT/EP2012/070171 patent/WO2013053833A1/en not_active Ceased
- 2012-10-11 RU RU2014119339A patent/RU2624493C2/ru not_active IP Right Cessation
- 2012-10-11 JP JP2014535077A patent/JP6180420B2/ja not_active Expired - Fee Related
- 2012-10-11 AU AU2012322976A patent/AU2012322976B2/en not_active Ceased
- 2012-10-11 CN CN201280050535.9A patent/CN103857392A/zh active Pending
-
2016
- 2016-03-03 US US15/059,395 patent/US20160199365A1/en not_active Abandoned
-
2017
- 2017-06-09 JP JP2017114659A patent/JP2017214387A/ja active Pending