TWI628180B - 作為PI3K抑制劑的吡啶并[1,2-a]嘧啶酮類似物 - Google Patents
作為PI3K抑制劑的吡啶并[1,2-a]嘧啶酮類似物 Download PDFInfo
- Publication number
- TWI628180B TWI628180B TW104119646A TW104119646A TWI628180B TW I628180 B TWI628180 B TW I628180B TW 104119646 A TW104119646 A TW 104119646A TW 104119646 A TW104119646 A TW 104119646A TW I628180 B TWI628180 B TW I628180B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- alkyl
- reaction
- acid
- pyrido
- Prior art date
Links
- LVWICFAMYSGSSV-UHFFFAOYSA-N COCCN(CCN1)CC1=O Chemical compound COCCN(CCN1)CC1=O LVWICFAMYSGSSV-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410271282.9 | 2014-06-17 | ||
| CN201410271282.9A CN105461711B (zh) | 2014-06-17 | 2014-06-17 | 作为PI3K抑制剂的吡啶并[1,2-a]嘧啶酮类似物 |
| CN201510324348.0 | 2015-06-12 | ||
| CN201510324348 | 2015-06-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201625612A TW201625612A (zh) | 2016-07-16 |
| TWI628180B true TWI628180B (zh) | 2018-07-01 |
Family
ID=54934872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW104119646A TWI628180B (zh) | 2014-06-17 | 2015-06-17 | 作為PI3K抑制劑的吡啶并[1,2-a]嘧啶酮類似物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9856256B2 (enExample) |
| EP (1) | EP3159341B8 (enExample) |
| JP (1) | JP6680774B2 (enExample) |
| KR (1) | KR102495840B1 (enExample) |
| CN (1) | CN106470992B (enExample) |
| AU (1) | AU2015276699B2 (enExample) |
| CA (1) | CA2951971C (enExample) |
| EA (1) | EA032642B1 (enExample) |
| ES (1) | ES2754264T3 (enExample) |
| TW (1) | TWI628180B (enExample) |
| WO (1) | WO2015192760A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108602815B (zh) * | 2015-12-16 | 2020-07-28 | 正大天晴药业集团股份有限公司 | 吡啶并[1,2-a]嘧啶酮类似物、其晶型、其中间体及其制备方法 |
| CN110386932A (zh) * | 2018-04-20 | 2019-10-29 | 艾科思莱德制药公司 | 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂 |
| KR102740196B1 (ko) * | 2019-01-24 | 2024-12-10 | 지앙수 아오사이캉 파마수티칼 씨오., 엘티디. | TGF-β R1 키나아제 억제제로서의 5-(4-피리딜옥시)피라졸 화합물 |
| KR20220113431A (ko) | 2019-12-02 | 2022-08-12 | 스톰 테라퓨틱스 리미티드 | Mettl3 저해제로서의 폴리헤테로환식 화합물 |
| CA3170021A1 (en) * | 2020-02-10 | 2021-08-19 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Use of pyrido[1,2-a]pyrimidinone compound in treating lymphoma |
| WO2021180111A1 (zh) | 2020-03-10 | 2021-09-16 | 正大天晴药业集团股份有限公司 | 包括吡啶并[1,2-a]嘧啶酮化合物的药物组合 |
| US20230321104A1 (en) * | 2020-09-15 | 2023-10-12 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Use of pyrido[1,2-a]pyrimidinone compound in treating peripheral t cell lymphoma |
| WO2022121929A1 (zh) * | 2020-12-08 | 2022-06-16 | 正大天晴药业集团股份有限公司 | 吡啶并[1,2-a]嘧啶酮化合物的治疗妇科肿瘤的用途 |
| WO2023169488A1 (zh) * | 2022-03-09 | 2023-09-14 | 正大天晴药业集团股份有限公司 | 包括吡啶并[1,2-a]嘧啶酮化合物和EGFR抑制剂的药物组合 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120010192A1 (en) * | 2010-07-02 | 2012-01-12 | Gilead Sciences, Inc. | Fused Heterocyclic Compounds as Ion Channel Modulators |
| WO2012037108A1 (en) * | 2010-09-13 | 2012-03-22 | Glaxosmithkline Llc | Aminoquinoline derivatives as antiviral agents |
| TW201443037A (zh) * | 2013-01-09 | 2014-11-16 | Gilead Sciences Inc | 治療用化合物 |
| TW201602107A (zh) * | 2014-06-17 | 2016-01-16 | 南京明德新藥研發股份有限公司 | 作為mTOR/PI3K抑制劑的吡啶并[1,2-a]嘧啶酮類似物 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0415185A (pt) * | 2003-10-10 | 2006-11-28 | Pfizer Prod Inc | 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3 |
| US8778977B2 (en) * | 2006-06-30 | 2014-07-15 | Sunesis Pharmaceuticals, Inc. | Pyridinonyl PDK1 inhibitors |
| EP2211615A4 (en) * | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| ES2474147T3 (es) * | 2008-05-30 | 2014-07-08 | Amgen, Inc | Inhibidores de PI3 cinasa |
| JP5820080B2 (ja) * | 2011-11-17 | 2015-11-24 | 山▲東▼▲軒▼竹医▲葯▼科技有限公司 | 三環系PI3K及び/又はmTOR抑制剤 |
| CN103539777B (zh) * | 2012-07-13 | 2016-03-02 | 广东东阳光药业有限公司 | Pi3激酶调节剂及其使用方法和用途 |
| WO2014022128A1 (en) * | 2012-07-29 | 2014-02-06 | Calitor Sciences, Llc | Pi3 kinase modulators and methods of use |
-
2015
- 2015-06-16 JP JP2017518397A patent/JP6680774B2/ja active Active
- 2015-06-16 CA CA2951971A patent/CA2951971C/en active Active
- 2015-06-16 AU AU2015276699A patent/AU2015276699B2/en active Active
- 2015-06-16 WO PCT/CN2015/081518 patent/WO2015192760A1/zh not_active Ceased
- 2015-06-16 ES ES15810067T patent/ES2754264T3/es active Active
- 2015-06-16 KR KR1020177000523A patent/KR102495840B1/ko active Active
- 2015-06-16 EP EP15810067.7A patent/EP3159341B8/en active Active
- 2015-06-16 CN CN201580027396.1A patent/CN106470992B/zh active Active
- 2015-06-16 EA EA201790016A patent/EA032642B1/ru not_active IP Right Cessation
- 2015-06-16 US US15/319,726 patent/US9856256B2/en active Active
- 2015-06-17 TW TW104119646A patent/TWI628180B/zh active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120010192A1 (en) * | 2010-07-02 | 2012-01-12 | Gilead Sciences, Inc. | Fused Heterocyclic Compounds as Ion Channel Modulators |
| WO2012037108A1 (en) * | 2010-09-13 | 2012-03-22 | Glaxosmithkline Llc | Aminoquinoline derivatives as antiviral agents |
| TW201443037A (zh) * | 2013-01-09 | 2014-11-16 | Gilead Sciences Inc | 治療用化合物 |
| TW201602107A (zh) * | 2014-06-17 | 2016-01-16 | 南京明德新藥研發股份有限公司 | 作為mTOR/PI3K抑制劑的吡啶并[1,2-a]嘧啶酮類似物 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN106470992A (zh) | 2017-03-01 |
| EP3159341B1 (en) | 2019-08-21 |
| CA2951971C (en) | 2024-09-10 |
| EP3159341B8 (en) | 2020-01-08 |
| JP6680774B2 (ja) | 2020-04-15 |
| EP3159341A4 (en) | 2018-05-16 |
| KR102495840B1 (ko) | 2023-02-03 |
| CA2951971A1 (en) | 2015-12-23 |
| TW201625612A (zh) | 2016-07-16 |
| JP2017519821A (ja) | 2017-07-20 |
| ES2754264T3 (es) | 2020-04-16 |
| KR20170016465A (ko) | 2017-02-13 |
| AU2015276699A1 (en) | 2017-01-19 |
| AU2015276699B2 (en) | 2019-10-10 |
| EA032642B1 (ru) | 2019-06-28 |
| EA201790016A1 (ru) | 2017-06-30 |
| CN106470992B (zh) | 2018-11-06 |
| EP3159341A1 (en) | 2017-04-26 |
| WO2015192760A1 (zh) | 2015-12-23 |
| US9856256B2 (en) | 2018-01-02 |
| US20170137420A1 (en) | 2017-05-18 |
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