RU2017119219A - 2-карбоксамид циклоамино производные мочевины в комбинации с ингибиторами hsp90 для лечения пролиферативных заболеваний - Google Patents
2-карбоксамид циклоамино производные мочевины в комбинации с ингибиторами hsp90 для лечения пролиферативных заболеваний Download PDFInfo
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- RU2017119219A RU2017119219A RU2017119219A RU2017119219A RU2017119219A RU 2017119219 A RU2017119219 A RU 2017119219A RU 2017119219 A RU2017119219 A RU 2017119219A RU 2017119219 A RU2017119219 A RU 2017119219A RU 2017119219 A RU2017119219 A RU 2017119219A
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- Russia
- Prior art keywords
- pharmaceutically acceptable
- proliferative disease
- alkyl
- substituted
- acceptable salt
- Prior art date
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- 201000010099 disease Diseases 0.000 title claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 12
- 230000002062 proliferating effect Effects 0.000 title claims 12
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 title claims 8
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 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 8
- 150000001875 compounds Chemical class 0.000 claims 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 210000000244 kidney pelvis Anatomy 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 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 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 229950007866 tanespimycin Drugs 0.000 claims 4
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims 3
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 3
- 206010048832 Colon adenoma Diseases 0.000 claims 3
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 210000000481 breast Anatomy 0.000 claims 3
- 210000000621 bronchi Anatomy 0.000 claims 3
- 210000003679 cervix uteri Anatomy 0.000 claims 3
- 210000001072 colon Anatomy 0.000 claims 3
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims 3
- 210000000867 larynx Anatomy 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 208000003747 lymphoid leukemia Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 210000000214 mouth Anatomy 0.000 claims 3
- 208000025113 myeloid leukemia Diseases 0.000 claims 3
- 210000001672 ovary Anatomy 0.000 claims 3
- 210000000496 pancreas Anatomy 0.000 claims 3
- 210000003800 pharynx Anatomy 0.000 claims 3
- 210000002307 prostate Anatomy 0.000 claims 3
- 210000000664 rectum Anatomy 0.000 claims 3
- 210000000813 small intestine Anatomy 0.000 claims 3
- 210000001685 thyroid gland Anatomy 0.000 claims 3
- 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 2
- IHGVAVLSTPCCJP-UHFFFAOYSA-N 4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-amine Chemical compound N1=C(N)SC(C=2C=C(N=CC=2)C(C)(C)C(F)(F)F)=C1C IHGVAVLSTPCCJP-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 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 2
- 208000017897 Carcinoma of esophagus Diseases 0.000 claims 2
- 229940126062 Compound A Drugs 0.000 claims 2
- 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 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 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 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 201000005619 esophageal carcinoma Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 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 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 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 2
- 229950005069 luminespib Drugs 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 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 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 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 2
- 229930192524 radicicol Natural products 0.000 claims 2
- 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 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- PJZQLRJVFCSZHH-UHFFFAOYSA-N 5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-amine Chemical compound N1=C(N)SC(C=2N=C(N=CC=2)C(C)(C)C)=C1C PJZQLRJVFCSZHH-UHFFFAOYSA-N 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- -1 cyano, aminocarbonyl Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 230000007717 exclusion Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 201000000498 stomach carcinoma Diseases 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
Classifications
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- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
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- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US201161547308P | 2011-10-14 | 2011-10-14 | |
| US61/547,308 | 2011-10-14 |
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| RU2014119339A Division RU2624493C2 (ru) | 2011-10-14 | 2012-10-11 | 2-КАРБОКСАМИД ЦИКЛОАМИНО ПРОИЗВОДНЫЕ МОЧЕВИНЫ В КОМБИНАЦИИ С ИНГИБИТОРАМИ Hsp90 ДЛЯ ЛЕЧЕНИЯ ПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ |
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| RU2017119219A RU2017119219A (ru) | 2011-10-14 | 2012-10-11 | 2-карбоксамид циклоамино производные мочевины в комбинации с ингибиторами hsp90 для лечения пролиферативных заболеваний |
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| RU2014119339A RU2624493C2 (ru) | 2011-10-14 | 2012-10-11 | 2-КАРБОКСАМИД ЦИКЛОАМИНО ПРОИЗВОДНЫЕ МОЧЕВИНЫ В КОМБИНАЦИИ С ИНГИБИТОРАМИ Hsp90 ДЛЯ ЛЕЧЕНИЯ ПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ |
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| JP (2) | JP6180420B2 (enExample) |
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| WO (1) | WO2013053833A1 (enExample) |
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| RU2014122198A (ru) * | 2011-11-02 | 2015-12-10 | Новартис Аг | Производные 2-карбоксамид циклоамино мочевины для применения в лечении vegf-зависимых заболеваний |
| WO2018151836A1 (en) | 2017-02-17 | 2018-08-23 | Fred Hutchinson Cancer Research Center | Combination therapies for treatment of bcma-related cancers and autoimmune disorders |
| 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 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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| US4261989A (en) | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| SI1611112T1 (sl) | 2003-02-11 | 2012-12-31 | Vernalis (R&D) Limited | Izoksazolne spojine kot inhibitorji vroäśinskih ĺ ok proteinov |
| 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 |
| PT2182948E (pt) * | 2007-07-24 | 2013-04-30 | Novartis Ag | Utilização de imidazoquinolinas para o tratamento de doenças dependentes do egfr ou doenças que adquiriram resistência a agentes que têm como alvo membros da família 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 |
| CN102227220A (zh) * | 2008-11-28 | 2011-10-26 | 诺瓦提斯公司 | 用于治疗性治疗的Hsp90抑制剂 |
| DE102009012631B4 (de) | 2009-03-11 | 2011-07-28 | Bayer Schering Pharma Aktiengesellschaft, 13353 | Filter für einen Computertomographen sowie Computertomograph |
| CN105412105A (zh) * | 2010-11-08 | 2016-03-23 | 诺华有限公司 | 2-甲酰胺环氨基尿素衍生物在治疗egfr依赖性疾病或对靶向egfr家族成员的药剂有获得性耐受性的疾病中的应用 |
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2012
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- 2012-10-11 CN CN201280050535.9A patent/CN103857392A/zh active Pending
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- 2012-10-11 RU RU2014119339A patent/RU2624493C2/ru not_active IP Right Cessation
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- 2012-10-11 RU RU2017119219A patent/RU2017119219A/ru unknown
- 2012-10-11 AU AU2012322976A patent/AU2012322976B2/en not_active Ceased
- 2012-10-11 US US14/350,577 patent/US20140275089A1/en not_active Abandoned
- 2012-10-11 CA CA2851383A patent/CA2851383A1/en not_active Abandoned
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2016
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2017
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Also Published As
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| MX2014004559A (es) | 2014-08-01 |
| CN106474127A (zh) | 2017-03-08 |
| BR112014008400A2 (pt) | 2017-04-04 |
| CA2851383A1 (en) | 2013-04-18 |
| AU2012322976A1 (en) | 2014-05-01 |
| JP6180420B2 (ja) | 2017-08-16 |
| JP2014528464A (ja) | 2014-10-27 |
| RU2017119219A3 (enExample) | 2018-11-02 |
| US20160199365A1 (en) | 2016-07-14 |
| RU2014119339A (ru) | 2015-11-20 |
| AU2012322976B2 (en) | 2016-05-12 |
| KR20140078656A (ko) | 2014-06-25 |
| RU2624493C2 (ru) | 2017-07-04 |
| CN103857392A (zh) | 2014-06-11 |
| US20140275089A1 (en) | 2014-09-18 |
| EP2766015A1 (en) | 2014-08-20 |
| JP2017214387A (ja) | 2017-12-07 |
| WO2013053833A1 (en) | 2013-04-18 |
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