RU2016129953A - Фармацевтические комбинации - Google Patents
Фармацевтические комбинации Download PDFInfo
- Publication number
- RU2016129953A RU2016129953A RU2016129953A RU2016129953A RU2016129953A RU 2016129953 A RU2016129953 A RU 2016129953A RU 2016129953 A RU2016129953 A RU 2016129953A RU 2016129953 A RU2016129953 A RU 2016129953A RU 2016129953 A RU2016129953 A RU 2016129953A
- Authority
- RU
- Russia
- Prior art keywords
- pharmaceutical combination
- inhibitor
- pharmaceutically acceptable
- methyl
- acceptable salt
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 claims 45
- 201000011510 cancer Diseases 0.000 claims 45
- 150000003839 salts Chemical class 0.000 claims 29
- 229940118537 p53 inhibitor Drugs 0.000 claims 25
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims 18
- 101710168331 ALK tyrosine kinase receptor Proteins 0.000 claims 18
- 229940122531 Anaplastic lymphoma kinase inhibitor Drugs 0.000 claims 15
- 238000000034 method Methods 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 206010029260 Neuroblastoma Diseases 0.000 claims 7
- 239000013543 active substance Substances 0.000 claims 4
- 229940125431 BRAF inhibitor Drugs 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- -1 5-chloro-1-methyl-2-oxo-1,2-dihydropyridin-3-yl Chemical group 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- VERWOWGGCGHDQE-UHFFFAOYSA-N ceritinib Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCNCC1 VERWOWGGCGHDQE-UHFFFAOYSA-N 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 229940127557 pharmaceutical product Drugs 0.000 claims 2
- AGBSXNCBIWWLHD-FQEVSTJZSA-N siremadlin Chemical compound COC1=NC(OC)=NC=C1C(N1C(C)C)=NC2=C1[C@H](C=1C=CC(Cl)=CC=1)N(C=1C(N(C)C=C(Cl)C=1)=O)C2=O AGBSXNCBIWWLHD-FQEVSTJZSA-N 0.000 claims 2
- CLRSLRWKONPSRQ-CPOWQTMSSA-N (1s)-1-(4-chlorophenyl)-6-methoxy-2-[4-[methyl-[[4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl]methyl]amino]phenyl]-7-propan-2-yloxy-1,4-dihydroisoquinolin-3-one Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=CC(=CC=2)N(C)CC2CCC(CC2)N2CC(=O)N(C)CC2)=CC=C(Cl)C=C1 CLRSLRWKONPSRQ-CPOWQTMSSA-N 0.000 claims 1
- DGLXELIGVRDJBG-PEBXRYMYSA-N (4s)-5-(3-chloro-4-fluorophenyl)-4-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-3-[(2r)-1-methoxypropan-2-yl]-4h-pyrrolo[3,4-d]imidazol-6-one Chemical compound C1([C@@H]2N(C(=O)C=3N=C(N(C2=3)[C@H](C)COC)C=2C(=NC(OC)=NC=2)OC)C=2C=C(Cl)C(F)=CC=2)=CC=C(Cl)C=C1 DGLXELIGVRDJBG-PEBXRYMYSA-N 0.000 claims 1
- CHOHEJZMEHHXSJ-IBGZPJMESA-N (4s)-5-(5-chloro-2-oxo-1h-pyridin-3-yl)-4-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-3-propan-2-yl-4h-pyrrolo[3,4-d]imidazol-6-one Chemical compound COC1=NC(OC)=NC=C1C(N1C(C)C)=NC2=C1[C@H](C=1C=CC(Cl)=CC=1)N(C=1C(NC=C(Cl)C=1)=O)C2=O CHOHEJZMEHHXSJ-IBGZPJMESA-N 0.000 claims 1
- CAAMSDWKXXPUJR-UHFFFAOYSA-N 3,5-dihydro-4H-imidazol-4-one Chemical compound O=C1CNC=N1 CAAMSDWKXXPUJR-UHFFFAOYSA-N 0.000 claims 1
- IQYWWOVGZNKRNH-QFIPXVFZSA-N 4-[(4s)-5-(3-chloro-2-fluorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-6-oxo-3-propan-2-yl-4h-pyrrolo[3,4-d]imidazol-4-yl]benzonitrile Chemical compound COC1=NC(OC)=NC=C1C(N1C(C)C)=NC2=C1[C@H](C=1C=CC(=CC=1)C#N)N(C=1C(=C(Cl)C=CC=1)F)C2=O IQYWWOVGZNKRNH-QFIPXVFZSA-N 0.000 claims 1
- BZZYIHQWCXHSMZ-FMSKOOSDSA-N C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=CC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)NCC2)=CC=C(Cl)C=C1 Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=CC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)NCC2)=CC=C(Cl)C=C1 BZZYIHQWCXHSMZ-FMSKOOSDSA-N 0.000 claims 1
- QHQFWUOURSTSOD-BXKNEMSHSA-N C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=NC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)C2)=CC=C(Cl)C=C1 Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=NC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)C2)=CC=C(Cl)C=C1 QHQFWUOURSTSOD-BXKNEMSHSA-N 0.000 claims 1
- VZDNISKFMYZWGF-YFMCWZQFSA-N C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=NC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)CC2)=CC=C(Cl)C=C1 Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=NC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)CC2)=CC=C(Cl)C=C1 VZDNISKFMYZWGF-YFMCWZQFSA-N 0.000 claims 1
- MTVMVQKGJODTNB-TWCVDLNQSA-N C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2N=CC(=NC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)C2)=CC=C(Cl)C=C1 Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2N=CC(=NC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)C2)=CC=C(Cl)C=C1 MTVMVQKGJODTNB-TWCVDLNQSA-N 0.000 claims 1
- CLRSLRWKONPSRQ-VKGCBGSESA-N C1=2C=C(OC(C)C)C(OC)=CC=2CC(=O)N(C=2C=CC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)CC2)C1C1=CC=C(Cl)C=C1 Chemical compound C1=2C=C(OC(C)C)C(OC)=CC=2CC(=O)N(C=2C=CC(=CC=2)N(C)C[C@@H]2CC[C@H](CC2)N2CC(=O)N(C)CC2)C1C1=CC=C(Cl)C=C1 CLRSLRWKONPSRQ-VKGCBGSESA-N 0.000 claims 1
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims 1
- HEZVBTASMHXWAD-IZQFIVGESA-N ClC1=CC=C(C=C1)[C@@H]1N(CCC2=CC(=C(C=C12)OC(C)C)OC)C1=CC=C(C=C1)N(C[C@@H]1CC[C@H](CC1)N1CC(N(CC1)C)=O)C Chemical group ClC1=CC=C(C=C1)[C@@H]1N(CCC2=CC(=C(C=C12)OC(C)C)OC)C1=CC=C(C=C1)N(C[C@@H]1CC[C@H](CC1)N1CC(N(CC1)C)=O)C HEZVBTASMHXWAD-IZQFIVGESA-N 0.000 claims 1
- 229940083347 Cyclin-dependent kinase 4 inhibitor Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 229940126523 co-drug Drugs 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- RUZLIIJDZBWWSA-INIZCTEOSA-N methyl 2-[[(1s)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoate Chemical group COC(=O)C1=CC=CC=C1N[C@@H](C)C1=CC(C)=CN2C(=O)C=C(N3CCOCC3)N=C12 RUZLIIJDZBWWSA-INIZCTEOSA-N 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- YAAWASYJIRZXSZ-UHFFFAOYSA-N pyrimidine-2,4-diamine Chemical compound NC1=CC=NC(N)=N1 YAAWASYJIRZXSZ-UHFFFAOYSA-N 0.000 claims 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 1
- 229960003862 vemurafenib Drugs 0.000 claims 1
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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
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- Epidemiology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| CA2939778C (en) | 2007-01-31 | 2019-01-29 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| CA2682174C (en) | 2007-03-28 | 2021-04-06 | President And Fellows Of Harvard College | Stitched polypeptides |
| KR20130099938A (ko) | 2010-08-13 | 2013-09-06 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| CN104039342A (zh) | 2011-10-18 | 2014-09-10 | 爱勒让治疗公司 | 拟肽大环化合物 |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| NZ627528A (en) | 2012-02-15 | 2016-05-27 | Aileron Therapeutics Inc | Peptidomimetic macrocycles |
| SG11201503052RA (en) | 2012-11-01 | 2015-05-28 | Aileron Therapeutics Inc | Disubstituted amino acids and methods of preparation and use thereof |
| WO2014138429A2 (en) | 2013-03-06 | 2014-09-12 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and use thereof in regulating hif1alpha |
| MX2017003797A (es) | 2014-09-24 | 2017-06-15 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
| MX389354B (es) | 2014-09-24 | 2025-03-20 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y formulaciones de los mismos. |
| WO2016154058A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| JP2018526430A (ja) | 2015-07-10 | 2018-09-13 | アルヴィナス・インコーポレイテッド | タンパク質分解のｍｄｍ２系修飾因子および関連の使用方法 |
| MX2018001903A (es) * | 2015-08-14 | 2018-06-20 | Novartis Ag | Inhibidores de mdm2 para el tratamiento de melanoma uveal. |
| ES2962460T3 (es) | 2015-08-28 | 2024-03-19 | Novartis Ag | Inhibidores de mdm2 y combinaciones de estos |
| JP6911019B2 (ja) | 2016-05-17 | 2021-07-28 | 公益財団法人がん研究会 | Ｅｇｆｒ−ｔｋｉ耐性を獲得した肺癌の治療薬 |
| US20200268728A1 (en) * | 2016-12-20 | 2020-08-27 | Sumitomo Dainippon Pharma Co., Ltd. | Drug targeting cancer stem cell |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US20190343836A1 (en) * | 2017-01-10 | 2019-11-14 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| EP3600326B1 (en) * | 2017-03-31 | 2023-01-25 | Novartis AG | Dose and regimen for an hdm2-p53 interaction inhibitor in hematological tumors |
| JP7358372B2 (ja) * | 2018-03-12 | 2023-10-10 | 羅欣薬業（上海）有限公司 | イミダゾピロロン化合物及びその使用 |
| WO2019182936A1 (en) * | 2018-03-19 | 2019-09-26 | Ariad Pharmaceuticals, Inc. | Methods of treating cancer in pediatric patients |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| WO2020023502A1 (en) | 2018-07-23 | 2020-01-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| AU2024212035A1 (en) | 2023-01-26 | 2025-08-14 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
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| EP2024353A2 (en) | 2006-03-16 | 2009-02-18 | Pfizer Products Inc. | Pyrazole compounds |
| KR101364277B1 (ko) * | 2006-12-08 | 2014-02-21 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 |
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| KR101353857B1 (ko) * | 2008-08-22 | 2014-01-21 | 노파르티스 아게 | Ｃｄｋ 억제제로서 피롤로피리미딘 화합물 |
| JO3002B1 (ar) * | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
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| AU2012240240A1 (en) * | 2011-04-04 | 2013-05-09 | Netherlands Cancer Institute | Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors |
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| AU2013341271A1 (en) * | 2012-11-07 | 2015-05-14 | Novartis Ag | Combination therapy |
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2014
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- 2014-12-19 KR KR1020167016376A patent/KR20160100975A/ko not_active Withdrawn
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- 2014-12-19 JP JP2016542139A patent/JP6532878B2/ja not_active Expired - Fee Related
- 2014-12-19 CN CN201480070695.9A patent/CN105848682A/zh active Pending
- 2014-12-19 EP EP14821861.3A patent/EP3086810A2/en not_active Withdrawn
- 2014-12-19 AU AU2014372166A patent/AU2014372166B2/en not_active Ceased
- 2014-12-23 TW TW103145083A patent/TW201609100A/zh unknown
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2017
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2018
- 2018-01-25 US US15/879,942 patent/US20180185365A1/en not_active Abandoned
- 2018-11-05 US US16/180,078 patent/US20190134033A1/en not_active Abandoned
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| RU2016129953A3 (enExample) | 2018-09-27 |
| AU2014372166B2 (en) | 2017-10-26 |
| EP3086810A2 (en) | 2016-11-02 |
| US20160339023A1 (en) | 2016-11-24 |
| AU2014372166A1 (en) | 2016-05-19 |
| JP6532878B2 (ja) | 2019-06-19 |
| MX2016008362A (es) | 2016-09-08 |
| CA2934866A1 (en) | 2015-07-02 |
| CN105848682A (zh) | 2016-08-10 |
| BR112016012506A8 (pt) | 2018-01-30 |
| JP2017504611A (ja) | 2017-02-09 |
| WO2015097621A3 (en) | 2015-10-29 |
| TW201609100A (zh) | 2016-03-16 |
| AU2017245295A1 (en) | 2017-11-02 |
| KR20160100975A (ko) | 2016-08-24 |
| BR112016012506A2 (pt) | 2017-08-08 |
| US20180185365A1 (en) | 2018-07-05 |
| WO2015097621A2 (en) | 2015-07-02 |
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