JP6893520B2 - ホスファチジルイノシトール3−キナーゼガンマの新規の阻害剤 - Google Patents
ホスファチジルイノシトール3−キナーゼガンマの新規の阻害剤 Download PDFInfo
- Publication number
- JP6893520B2 JP6893520B2 JP2018547461A JP2018547461A JP6893520B2 JP 6893520 B2 JP6893520 B2 JP 6893520B2 JP 2018547461 A JP2018547461 A JP 2018547461A JP 2018547461 A JP2018547461 A JP 2018547461A JP 6893520 B2 JP6893520 B2 JP 6893520B2
- Authority
- JP
- Japan
- Prior art keywords
- dihydro
- isoindole
- oxo
- acetamide
- thiazole
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 Cc1c(*)nc(*)[s]1 Chemical compound Cc1c(*)nc(*)[s]1 0.000 description 6
- OJMAGGNZTSZMGZ-UHFFFAOYSA-N CC(Nc1nc(C)c(-c(cc2CN3C(C4CC4)=C=[IH])cc(N[S-](=O)=O)c2C3=O)[s]1)=O Chemical compound CC(Nc1nc(C)c(-c(cc2CN3C(C4CC4)=C=[IH])cc(N[S-](=O)=O)c2C3=O)[s]1)=O OJMAGGNZTSZMGZ-UHFFFAOYSA-N 0.000 description 1
- FTIVXZGHNYMURD-UHFFFAOYSA-N CCOC(c([nH]1)cc2c1[o]cc2C)=O Chemical compound CCOC(c([nH]1)cc2c1[o]cc2C)=O FTIVXZGHNYMURD-UHFFFAOYSA-N 0.000 description 1
- LZSXKOQVSYULPZ-UHFFFAOYSA-N Cc([nH]1)nc2c1ncc(C)c2 Chemical compound Cc([nH]1)nc2c1ncc(C)c2 LZSXKOQVSYULPZ-UHFFFAOYSA-N 0.000 description 1
- ORUIZIXJCCIGAI-UHFFFAOYSA-N Cc([nH]1)nc2c1ncnc2N Chemical compound Cc([nH]1)nc2c1ncnc2N ORUIZIXJCCIGAI-UHFFFAOYSA-N 0.000 description 1
- DWLVOLHIRQSGOK-UHFFFAOYSA-N Cc1c(N)ncc2c1cccc2 Chemical compound Cc1c(N)ncc2c1cccc2 DWLVOLHIRQSGOK-UHFFFAOYSA-N 0.000 description 1
- DYDNCXUOHQQBBO-UHFFFAOYSA-N Cc1c2nccc[n]2nc1N Chemical compound Cc1c2nccc[n]2nc1N DYDNCXUOHQQBBO-UHFFFAOYSA-N 0.000 description 1
- WZAWVDBIHPIESK-UHFFFAOYSA-N Cc1c[n](ccnc2N)c2n1 Chemical compound Cc1c[n](ccnc2N)c2n1 WZAWVDBIHPIESK-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical 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)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662306328P | 2016-03-10 | 2016-03-10 | |
| US62/306,328 | 2016-03-10 | ||
| PCT/EP2017/055552 WO2017153527A1 (en) | 2016-03-10 | 2017-03-09 | Novel inhibitors of phosphatidylinositol 3-kinase gamma |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019507788A JP2019507788A (ja) | 2019-03-22 |
| JP2019507788A5 JP2019507788A5 (https=) | 2020-03-05 |
| JP6893520B2 true JP6893520B2 (ja) | 2021-06-23 |
Family
ID=58264542
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018547461A Expired - Fee Related JP6893520B2 (ja) | 2016-03-10 | 2017-03-09 | ホスファチジルイノシトール3−キナーゼガンマの新規の阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10858355B2 (https=) |
| EP (1) | EP3426652B1 (https=) |
| JP (1) | JP6893520B2 (https=) |
| KR (1) | KR20180117693A (https=) |
| CN (1) | CN108779110B (https=) |
| AR (1) | AR107840A1 (https=) |
| AU (1) | AU2017229445B2 (https=) |
| BR (1) | BR112018068075A2 (https=) |
| CA (1) | CA3015893C (https=) |
| EA (1) | EA036388B1 (https=) |
| MX (1) | MX387125B (https=) |
| TW (1) | TWI746525B (https=) |
| WO (1) | WO2017153527A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11161838B2 (en) | 2018-11-13 | 2021-11-02 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
| US11078204B2 (en) | 2018-11-13 | 2021-08-03 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| EP3952870B1 (en) * | 2019-04-10 | 2025-09-24 | Nanjing Zenshine Pharmaceuticals Co., Ltd. | Phosphatidylinositol 3-kinase inhibitors |
| KR20220047247A (ko) * | 2019-06-04 | 2022-04-15 | 아르커스 바이오사이언시즈 인코포레이티드 | 2,3,5-삼치환 피라졸로[1,5-a]피리미딘 화합물 |
| WO2022017371A1 (zh) * | 2020-07-21 | 2022-01-27 | 中国医药研究开发中心有限公司 | 具有磷脂酰肌醇3-激酶δ和γ的双重抑制剂活性的杂环化合物及其医药用途 |
| CN115611883B (zh) * | 2021-07-13 | 2025-03-28 | 生物岛实验室 | 一种双环结构的PI3Kα抑制剂及其制备方法和用途 |
| WO2024046454A1 (zh) * | 2022-09-01 | 2024-03-07 | 上海海雁医药科技有限公司 | 杂芳基取代的吡啶并吡咯酮衍生物、其药物组合物及应用 |
| CN117683036A (zh) * | 2022-09-09 | 2024-03-12 | 上海璎黎药业有限公司 | 一种含氮杂环化合物、其药物组合物及应用 |
| CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
| CN121816181A (zh) | 2023-06-30 | 2026-04-07 | 柏林合作研究学会 | 噻唑并四氢喹啉化合物作为ii类磷酸肌醇3-激酶抑制剂 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200613272A (en) * | 2004-08-13 | 2006-05-01 | Astrazeneca Ab | Isoindolone compounds and their use as metabotropic glutamate receptor potentiators |
| WO2006089106A2 (en) * | 2005-02-17 | 2006-08-24 | Icos Corporation | Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation |
| MY149143A (en) * | 2006-01-18 | 2013-07-15 | Amgen Inc | Thiazole compounds as protien kinase b (pkb) inhibitors |
| EP2016075A1 (en) * | 2006-05-03 | 2009-01-21 | AstraZeneca AB | Thiazole derivatives and their use as anti-tumour agents |
| EP1894931A1 (en) * | 2006-08-30 | 2008-03-05 | Cellzome Ag | Triazole derivatives as kinase inhibitors |
| WO2010024258A1 (ja) * | 2008-08-29 | 2010-03-04 | 塩野義製薬株式会社 | Pi3k阻害活性を有する縮環アゾール誘導体 |
| CA2752596A1 (en) * | 2009-02-17 | 2010-08-26 | Vertex Pharmaceuticals Incorporated | Tetrahydrothiazolopyridine inhibitors of phosphatidylinositol 3-kinase |
| AU2010341573B2 (en) * | 2009-12-22 | 2016-10-13 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| CN104379573A (zh) * | 2012-04-20 | 2015-02-25 | 艾伯维公司 | 异吲哚酮衍生物 |
| SG10201802061TA (en) * | 2013-09-25 | 2018-05-30 | Vertex Pharma | A selective inhibitor of phosphatidylinositol 3-kinase-gamma |
| KR20160145780A (ko) | 2014-04-24 | 2016-12-20 | 노파르티스 아게 | 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피리딘 유도체 |
| EP3134397A1 (en) | 2014-04-24 | 2017-03-01 | Novartis AG | Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
| KR20160141856A (ko) | 2014-04-24 | 2016-12-09 | 노파르티스 아게 | 포스파티딜이노시톨 3-키나제 억제제로서의 피라진 유도체 |
-
2017
- 2017-03-09 AR ARP170100589A patent/AR107840A1/es unknown
- 2017-03-09 CN CN201780014898.XA patent/CN108779110B/zh not_active Expired - Fee Related
- 2017-03-09 US US16/082,880 patent/US10858355B2/en not_active Expired - Fee Related
- 2017-03-09 AU AU2017229445A patent/AU2017229445B2/en not_active Ceased
- 2017-03-09 WO PCT/EP2017/055552 patent/WO2017153527A1/en not_active Ceased
- 2017-03-09 BR BR112018068075A patent/BR112018068075A2/pt not_active IP Right Cessation
- 2017-03-09 MX MX2018010894A patent/MX387125B/es unknown
- 2017-03-09 CA CA3015893A patent/CA3015893C/en active Active
- 2017-03-09 EP EP17709681.5A patent/EP3426652B1/en active Active
- 2017-03-09 JP JP2018547461A patent/JP6893520B2/ja not_active Expired - Fee Related
- 2017-03-09 TW TW106107711A patent/TWI746525B/zh not_active IP Right Cessation
- 2017-03-09 EA EA201891931A patent/EA036388B1/ru not_active IP Right Cessation
- 2017-03-09 KR KR1020187028625A patent/KR20180117693A/ko not_active Abandoned
-
2020
- 2020-11-04 US US17/088,689 patent/US20210047312A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN108779110B (zh) | 2021-10-29 |
| MX387125B (es) | 2025-03-18 |
| US20210047312A1 (en) | 2021-02-18 |
| CA3015893C (en) | 2021-11-09 |
| EP3426652A1 (en) | 2019-01-16 |
| AU2017229445B2 (en) | 2019-07-11 |
| EA201891931A1 (ru) | 2019-04-30 |
| AR107840A1 (es) | 2018-06-13 |
| US20200299289A1 (en) | 2020-09-24 |
| WO2017153527A1 (en) | 2017-09-14 |
| TW201808945A (zh) | 2018-03-16 |
| EA036388B1 (ru) | 2020-11-03 |
| JP2019507788A (ja) | 2019-03-22 |
| US10858355B2 (en) | 2020-12-08 |
| CA3015893A1 (en) | 2017-09-14 |
| AU2017229445A1 (en) | 2018-10-25 |
| BR112018068075A2 (pt) | 2019-01-08 |
| MX2018010894A (es) | 2018-11-09 |
| CN108779110A (zh) | 2018-11-09 |
| KR20180117693A (ko) | 2018-10-29 |
| EP3426652B1 (en) | 2021-12-01 |
| TWI746525B (zh) | 2021-11-21 |
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