JP6871903B2 - プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 - Google Patents
プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 Download PDFInfo
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- JP6871903B2 JP6871903B2 JP2018500297A JP2018500297A JP6871903B2 JP 6871903 B2 JP6871903 B2 JP 6871903B2 JP 2018500297 A JP2018500297 A JP 2018500297A JP 2018500297 A JP2018500297 A JP 2018500297A JP 6871903 B2 JP6871903 B2 JP 6871903B2
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
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- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
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| US201562188043P | 2015-07-02 | 2015-07-02 | |
| US62/188,043 | 2015-07-02 | ||
| US201662353728P | 2016-06-23 | 2016-06-23 | |
| US62/353,728 | 2016-06-23 | ||
| PCT/US2016/040329 WO2017004342A1 (en) | 2015-07-02 | 2016-06-30 | Chiral diaryl macrocycles as modulators of protein kinases |
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| JP2018519343A JP2018519343A (ja) | 2018-07-19 |
| JP2018519343A5 JP2018519343A5 (enExample) | 2019-07-25 |
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| EP (1) | EP3317285B1 (enExample) |
| JP (1) | JP6871903B2 (enExample) |
| KR (1) | KR102599788B1 (enExample) |
| CN (1) | CN107735399B (enExample) |
| AU (2) | AU2016287568B2 (enExample) |
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| ES (1) | ES2864839T3 (enExample) |
| IL (1) | IL256377A (enExample) |
| MX (1) | MX2017017097A (enExample) |
| RU (1) | RU2732405C2 (enExample) |
| TW (1) | TW201716415A (enExample) |
| WO (1) | WO2017004342A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180026480A (ko) * | 2015-07-06 | 2018-03-12 | 티피 테라퓨틱스, 인크. | 디아릴 매크로사이클 다형체 |
| JP2019527230A (ja) * | 2016-07-28 | 2019-09-26 | ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 大環状キナーゼ阻害剤 |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS53350B (sr) | 2008-09-22 | 2014-10-31 | Array Biopharma, Inc. | Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze |
| EP2350071B1 (en) | 2008-10-22 | 2014-01-08 | Array Biopharma, Inc. | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| PL3205654T3 (pl) | 2010-05-20 | 2019-08-30 | Array Biopharma, Inc. | Związki makrocykliczne jako inhibitory kinazy TRK |
| SG10202000191YA (en) | 2014-01-24 | 2020-03-30 | Turning Point Therapeutics Inc | Diaryl macrocycles as modulators of protein kinases |
| CN107428760B (zh) | 2014-11-16 | 2021-04-27 | 阵列生物制药公司 | (s)-n-(5-((r)-2-(2,5-二氟苯基)-吡咯烷-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羟基吡咯烷-1-甲酰胺硫酸氢盐的晶型 |
| JP6871903B2 (ja) | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
| LT3733187T (lt) | 2015-07-21 | 2024-12-10 | Turning Point Therapeutics, Inc. | Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui |
| BR112018008357A2 (en) | 2015-10-26 | 2018-11-27 | Loxo Oncology, Inc. | dot mutations in trk inhibitor resistant cancer and related methods |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| HRP20201984T1 (hr) | 2016-05-18 | 2021-04-16 | Loxo Oncology, Inc. | Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| WO2018009417A1 (en) * | 2016-07-05 | 2018-01-11 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| SG10201912574WA (en) | 2016-09-28 | 2020-02-27 | Blade Therapeutics Inc | Calpain modulators and therapeutic uses thereof |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JOP20190213A1 (ar) * | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技（苏州）有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
| SMT202400343T1 (it) | 2017-07-28 | 2024-11-15 | Turning Point Therapeutics Inc | Composti macrociclici e loro usi |
| MX2020001979A (es) * | 2017-08-23 | 2020-03-24 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Macrociclo que contiene aminopirazol y pirimidina y composicion farmaceutica y uso de la misma. |
| CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
| JP6986789B2 (ja) * | 2017-11-10 | 2021-12-22 | エンジェクス ファーマシューティカル インコーポレイテッド | 化合物、その薬学的に許容される塩、化合物の使用および医薬組成物 |
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| KR20180026480A (ko) * | 2015-07-06 | 2018-03-12 | 티피 테라퓨틱스, 인크. | 디아릴 매크로사이클 다형체 |
| JP2021119151A (ja) * | 2015-07-06 | 2021-08-12 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics, Inc. | ジアリール大環状多形 |
| JP7212713B2 (ja) | 2015-07-06 | 2023-01-25 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | ジアリール大環状多形 |
| US12187739B2 (en) | 2015-07-06 | 2025-01-07 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
| JP2019527230A (ja) * | 2016-07-28 | 2019-09-26 | ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 大環状キナーゼ阻害剤 |
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| TW201716415A (zh) | 2017-05-16 |
| RU2732405C2 (ru) | 2020-09-16 |
| MX2017017097A (es) | 2018-05-23 |
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