TW201940166A - 作為cdk4及cdk6抑制劑之2h-吲唑衍生物及其治療用途 - Google Patents
作為cdk4及cdk6抑制劑之2h-吲唑衍生物及其治療用途 Download PDFInfo
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- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-M oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC([O-])=O ZQPPMHVWECSIRJ-KTKRTIGZSA-M 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
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- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 235000019477 peppermint oil Nutrition 0.000 description 1
- JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical compound [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- YSWYYGKGAYSAOJ-UHFFFAOYSA-N phosphane Chemical compound P.P YSWYYGKGAYSAOJ-UHFFFAOYSA-N 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
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- 150000004885 piperazines Chemical class 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-M pivalate Chemical compound CC(C)(C)C([O-])=O IUGYQRQAERSCNH-UHFFFAOYSA-M 0.000 description 1
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- 238000005498 polishing Methods 0.000 description 1
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- 239000002861 polymer material Substances 0.000 description 1
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- SCVFZCLFOSHCOH-UHFFFAOYSA-M potassium acetate Chemical compound [K+].CC([O-])=O SCVFZCLFOSHCOH-UHFFFAOYSA-M 0.000 description 1
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- 230000008569 process Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
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- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000011253 protective coating Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- BXEMXLDMNMKWPV-UHFFFAOYSA-N pyridine Chemical compound C1=CC=NC=C1.C1=CC=NC=C1 BXEMXLDMNMKWPV-UHFFFAOYSA-N 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- QJZUKDFHGGYHMC-UHFFFAOYSA-N pyridine-3-carbaldehyde Chemical class O=CC1=CC=CN=C1 QJZUKDFHGGYHMC-UHFFFAOYSA-N 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 1
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- 235000019204 saccharin Nutrition 0.000 description 1
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- 229940113147 shellac Drugs 0.000 description 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 238000007614 solvation Methods 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
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- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
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- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 229940070710 valerate Drugs 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 239000007762 w/o emulsion Substances 0.000 description 1
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- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
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- 229930195724 β-lactose Natural products 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862623516P | 2018-01-29 | 2018-01-29 | |
| US62/623,516 | 2018-01-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201940166A true TW201940166A (zh) | 2019-10-16 |
Family
ID=67394794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108103389A TW201940166A (zh) | 2018-01-29 | 2019-01-29 | 作為cdk4及cdk6抑制劑之2h-吲唑衍生物及其治療用途 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11352341B2 (https=) |
| EP (1) | EP3746072B1 (https=) |
| JP (1) | JP7337395B2 (https=) |
| KR (1) | KR20200115583A (https=) |
| CN (1) | CN111989099A (https=) |
| AU (1) | AU2019211491B2 (https=) |
| BR (1) | BR112020015405A2 (https=) |
| CA (1) | CA3088381A1 (https=) |
| EA (1) | EA202091450A1 (https=) |
| IL (1) | IL275948A (https=) |
| MX (1) | MX2020007959A (https=) |
| PH (1) | PH12020551155A1 (https=) |
| SG (1) | SG11202006748RA (https=) |
| TW (1) | TW201940166A (https=) |
| WO (1) | WO2019148161A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019018584A1 (en) | 2017-07-18 | 2019-01-24 | GiraFpharma LLC | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
| EP3654982A4 (en) | 2017-07-18 | 2021-04-14 | Nuvation Bio Inc. | 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES |
| WO2019161224A1 (en) | 2018-02-15 | 2019-08-22 | GiraFpharma LLC | Heterocyclic compounds as kinase inhibitors |
| PL3806898T3 (pl) * | 2018-06-18 | 2026-02-23 | UCB Biopharma SRL | Antagonista gremlin-1 do zastosowania w leczeniu nowotworu |
| EP3911324A4 (en) | 2019-01-18 | 2022-08-17 | Nuvation Bio Inc. | 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES |
| EP3911323A4 (en) | 2019-01-18 | 2022-11-16 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
| AU2020215684B2 (en) * | 2019-01-29 | 2025-08-21 | Beta Pharma, Inc. | 2h-indazole derivatives as therapeutic agents for brain cancers and brain metastases |
| MX2021013531A (es) | 2019-05-05 | 2022-02-11 | Qilu Regor Therapeutics Inc | Inhibidores de cdk. |
| EP4159728A4 (en) * | 2020-06-22 | 2024-06-26 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | MANUFACTURING PROCESS FOR CDK4/6 INHIBITOR |
| US20230416271A1 (en) * | 2020-11-26 | 2023-12-28 | Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd. | Heteroarylquinazoline compounds as protein kinase inhibitors |
| WO2022113003A1 (en) | 2020-11-27 | 2022-06-02 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2251677T3 (es) | 2002-01-22 | 2006-05-01 | Warner-Lambert Company Llc | 2-(piridin-2-ilamino)-pirido(2,3-d)pirimidin-7-onas. |
| ATE412650T1 (de) | 2003-07-11 | 2008-11-15 | Warner Lambert Co | Isethionat salz eines selektiven cdk4 inhibitors |
| CN1956982A (zh) | 2004-05-21 | 2007-05-02 | 万有制药株式会社 | 具有氨基噻唑骨架的Cdk4、6选择性抑制剂 |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | 諾華公司 | 吡咯并嘧啶化合物及其用途 |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| ES2522346T3 (es) | 2008-08-22 | 2014-11-14 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de CDK |
| JO2885B1 (en) | 2008-12-22 | 2015-03-15 | ايلي ليلي اند كومباني | Protein kinase inhibitors |
| US9796701B2 (en) | 2013-12-31 | 2017-10-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| MY187555A (en) | 2014-07-24 | 2021-09-29 | Beta Pharma Inc | 2-h-indazole derivatives as cyclin-dependent kinase (cdk) inhibitors and therapeutic uses thereof |
| US9969719B2 (en) | 2015-03-11 | 2018-05-15 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Substituted 2-hydrogen-pyrazole derivative serving as anticancer drug |
| CN107286134B (zh) | 2016-04-11 | 2019-04-12 | 上海勋和医药科技有限公司 | 2，4-二取代嘧啶衍生物作为cdk抑制剂及其应用 |
-
2019
- 2019-01-29 CA CA3088381A patent/CA3088381A1/en not_active Abandoned
- 2019-01-29 BR BR112020015405-9A patent/BR112020015405A2/pt not_active Application Discontinuation
- 2019-01-29 EA EA202091450A patent/EA202091450A1/ru unknown
- 2019-01-29 KR KR1020207024587A patent/KR20200115583A/ko not_active Withdrawn
- 2019-01-29 JP JP2020562086A patent/JP7337395B2/ja active Active
- 2019-01-29 CN CN201980010752.7A patent/CN111989099A/zh active Pending
- 2019-01-29 TW TW108103389A patent/TW201940166A/zh unknown
- 2019-01-29 MX MX2020007959A patent/MX2020007959A/es unknown
- 2019-01-29 SG SG11202006748RA patent/SG11202006748RA/en unknown
- 2019-01-29 EP EP19743187.7A patent/EP3746072B1/en active Active
- 2019-01-29 US US16/965,376 patent/US11352341B2/en active Active
- 2019-01-29 WO PCT/US2019/015547 patent/WO2019148161A1/en not_active Ceased
- 2019-01-29 AU AU2019211491A patent/AU2019211491B2/en active Active
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2020
- 2020-07-09 IL IL275948A patent/IL275948A/en unknown
- 2020-07-29 PH PH12020551155A patent/PH12020551155A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3746072B1 (en) | 2023-04-12 |
| US11352341B2 (en) | 2022-06-07 |
| AU2019211491B2 (en) | 2024-03-14 |
| IL275948A (en) | 2020-08-31 |
| US20210139459A1 (en) | 2021-05-13 |
| CA3088381A1 (en) | 2019-08-01 |
| KR20200115583A (ko) | 2020-10-07 |
| EP3746072A1 (en) | 2020-12-09 |
| PH12020551155A1 (en) | 2021-06-07 |
| BR112020015405A2 (pt) | 2020-12-08 |
| CN111989099A (zh) | 2020-11-24 |
| JP2021512161A (ja) | 2021-05-13 |
| MX2020007959A (es) | 2020-09-18 |
| AU2019211491A1 (en) | 2020-07-30 |
| EA202091450A1 (ru) | 2021-01-14 |
| EP3746072A4 (en) | 2021-06-02 |
| WO2019148161A1 (en) | 2019-08-01 |
| JP7337395B2 (ja) | 2023-09-04 |
| SG11202006748RA (en) | 2020-08-28 |
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