IL292475A - Combinations for the treatment of neoplasms using quiescent cell targeting and inhibitors of mitosis - Google Patents
Combinations for the treatment of neoplasms using quiescent cell targeting and inhibitors of mitosisInfo
- Publication number
- IL292475A IL292475A IL292475A IL29247522A IL292475A IL 292475 A IL292475 A IL 292475A IL 292475 A IL292475 A IL 292475A IL 29247522 A IL29247522 A IL 29247522A IL 292475 A IL292475 A IL 292475A
- Authority
- IL
- Israel
- Prior art keywords
- cancer
- inhibitor
- mitosis
- subject
- substituted
- Prior art date
Links
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- 206010028980 Neoplasm Diseases 0.000 title claims 39
- 238000011282 treatment Methods 0.000 title claims 2
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- 238000000034 method Methods 0.000 claims 55
- 230000011278 mitosis Effects 0.000 claims 31
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- 125000000217 alkyl group Chemical group 0.000 claims 16
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- LRCZQSDQZJBHAF-PUBGEWHCSA-N dha-paclitaxel Chemical compound N([C@H]([C@@H](OC(=O)CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CC)C(=O)O[C@@H]1C(=C2[C@@H](OC(C)=O)C(=O)[C@]3(C)[C@@H](O)C[C@H]4OC[C@]4([C@H]3[C@H](OC(=O)C=3C=CC=CC=3)[C@](C2(C)C)(O)C1)OC(C)=O)C)C=1C=CC=CC=1)C(=O)C1=CC=CC=C1 LRCZQSDQZJBHAF-PUBGEWHCSA-N 0.000 claims 6
- MYEJOKLXXLVMPR-STNHEDLKSA-N (ne)-n-[(6e)-6-[2-(1-hydroxypyridin-4-ylidene)ethylidene]cyclohexa-2,4-dien-1-ylidene]-4-methoxybenzenesulfonamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)\N=C(/C=CC=C/1)\C\1=C\C=C1C=CN(O)C=C1 MYEJOKLXXLVMPR-STNHEDLKSA-N 0.000 claims 5
- QHLVBNKYJGBCQJ-UHFFFAOYSA-N 1-(2-hydroxyethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide Chemical compound C1CN(C)CCN1C1=CC=C(OC(F)(F)F)C(NC=2N=C3C=4N(CCO)N=C(C=4CCC3=CN=2)C(N)=O)=C1 QHLVBNKYJGBCQJ-UHFFFAOYSA-N 0.000 claims 5
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- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims 5
- DJNZZLZKAXGMMC-UHFFFAOYSA-N 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide Chemical compound COC1=CC(C(=O)NC2CCN(C)CC2)=CC=C1NC(N=C12)=NC=C1N(C)C(=O)C(F)(F)CN2C1CCCC1 DJNZZLZKAXGMMC-UHFFFAOYSA-N 0.000 claims 5
- JSKUWFIZUALZLX-UHFFFAOYSA-N 5-(5,6-dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide Chemical compound C1=2C=C(OC)C(OC)=CC=2N=CN1C(SC=1C(N)=O)=CC=1OCC1=CC=CC=C1C(F)(F)F JSKUWFIZUALZLX-UHFFFAOYSA-N 0.000 claims 5
- ZHJGWYRLJUCMRT-QGZVFWFLSA-N 5-[6-[(4-methyl-1-piperazinyl)methyl]-1-benzimidazolyl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide Chemical compound O([C@H](C)C=1C(=CC=CC=1)C(F)(F)F)C(=C(S1)C(N)=O)C=C1N(C1=C2)C=NC1=CC=C2CN1CCN(C)CC1 ZHJGWYRLJUCMRT-QGZVFWFLSA-N 0.000 claims 5
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- 229940122803 Vinca alkaloid Drugs 0.000 claims 5
- GMJWGJSDPOAZTP-MIDYMNAOSA-N bms-188797 Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](OC(C)=O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)C=4C=CC=CC=4)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)OC)C(=O)C1=CC=CC=C1 GMJWGJSDPOAZTP-MIDYMNAOSA-N 0.000 claims 5
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 claims 5
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Classifications
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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- A—HUMAN NECESSITIES
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
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- Bioinformatics & Cheminformatics (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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| US201662323583P | 2016-04-15 | 2016-04-15 | |
| PCT/US2017/027734 WO2017181087A1 (en) | 2016-04-15 | 2017-04-14 | Combinations for the treatment of neoplasms using quiescent cell targeting and inhibitors of mitosis |
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| IL262325A IL262325B (en) | 2016-04-15 | 2018-10-11 | Combinations for treating tumors using quiescent cell targeting and cell division inhibitors |
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| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
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| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
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| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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| HUE024568T2 (hu) * | 2009-09-11 | 2016-02-29 | Amgen Inc | N-(4-((3-(2-amino-4-pirimidinil)-2-piridinil)oxi)fenil)-4-(4-metil-2-tienil)-1-ftalazinamin antimitotikus szerre rezisztens rák kezelésében történõ alkalmazásra |
| US20120184562A1 (en) | 2011-01-19 | 2012-07-19 | Kin-Chun Luk | 1,6- and 1,8-naphthyridines |
| CN103797002B (zh) * | 2011-08-19 | 2017-02-22 | 迪亚克森海特公司 | Dyrk1抑制剂及其用途 |
| FR2993317B1 (fr) | 2012-07-16 | 2014-08-15 | Snecma | Carter de turbomachine dans un materiau composite et procede de fabrication associe |
| EP2999698A1 (en) * | 2012-10-10 | 2016-03-30 | Felicitex Therapeutics, Inc. | Treatment of cancer by targeting quiescent cancer cells |
| HK1219879A1 (zh) * | 2013-06-11 | 2017-04-21 | Bayer Pharma Aktiengesellschaft | 用於治疗癌症的包含mps-1激酶抑制剂和有丝分裂抑制剂的组合 |
| CA2854542A1 (en) * | 2013-06-18 | 2014-12-18 | 4Sc Discovery Gmbh | Method of inhibiting dyrk1b |
| WO2015116696A1 (en) | 2014-01-28 | 2015-08-06 | Massachusetts Institute Of Technology | Combination therapies and methods of use thereof for treating cancer |
| MX2016012208A (es) | 2014-03-20 | 2017-01-26 | Samumed Llc | Indazol-3-carboxamidas 5-substituidas y preparacion y uso de las mismas. |
| US20170304313A1 (en) | 2014-10-06 | 2017-10-26 | Novartis Ag | Therapeutic Combination For The Treatment Of Cancer |
| CN108135871B (zh) * | 2015-07-23 | 2022-11-04 | 博蔚医药生物科技股份有限公司 | 阻断疾病的泛素化-蛋白酶体系统的胺萘醌化合物及医药组合物 |
| CN109562176A (zh) | 2016-04-15 | 2019-04-02 | 费利克斯疗法公司 | 使用静止细胞靶向和egfr抑制剂的用于治疗肿瘤的组合 |
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| AU2017248807A1 (en) | 2018-10-25 |
| CN109313197A (zh) | 2019-02-05 |
| CA3020978A1 (en) | 2017-10-19 |
| US20190290651A1 (en) | 2019-09-26 |
| IL262325A (en) | 2018-11-29 |
| IL262325B (en) | 2022-06-01 |
| KR102494172B1 (ko) | 2023-02-02 |
| MX2018012508A (es) | 2019-07-08 |
| US20220110941A1 (en) | 2022-04-14 |
| WO2017181087A1 (en) | 2017-10-19 |
| EP3443351A1 (en) | 2019-02-20 |
| US20170296542A1 (en) | 2017-10-19 |
| EP3443351A4 (en) | 2019-12-18 |
| AU2023214240A1 (en) | 2023-08-24 |
| KR20230020560A (ko) | 2023-02-10 |
| US10314843B2 (en) | 2019-06-11 |
| JP7278776B2 (ja) | 2023-05-22 |
| BR112018071023A2 (pt) | 2019-02-05 |
| JP2019511553A (ja) | 2019-04-25 |
| KR20180130575A (ko) | 2018-12-07 |
| MX2022012146A (es) | 2022-10-21 |
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