JP2017519821A5 - - Google Patents
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- Publication number
- JP2017519821A5 JP2017519821A5 JP2017518397A JP2017518397A JP2017519821A5 JP 2017519821 A5 JP2017519821 A5 JP 2017519821A5 JP 2017518397 A JP2017518397 A JP 2017518397A JP 2017518397 A JP2017518397 A JP 2017518397A JP 2017519821 A5 JP2017519821 A5 JP 2017519821A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- membered
- alkyl group
- formula
- 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.)
- Granted
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- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 8
- 229910052794 bromium Inorganic materials 0.000 claims 7
- 229910052801 chlorine Inorganic materials 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 229910052740 iodine Inorganic materials 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- -1 heterocyclic hydrocarbon Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000005149 cycloalkylsulfinyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000004011 3 membered carbocyclic group Chemical group 0.000 claims 1
- 125000001845 4 membered carbocyclic group Chemical group 0.000 claims 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000005257 alkyl acyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 1
- 125000005144 cycloalkylsulfonyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000004969 haloethyl group Chemical group 0.000 claims 1
- 125000004970 halomethyl group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 125000006216 methylsulfinyl group Chemical group [H]C([H])([H])S(*)=O 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- 0 O=C1N(****2)C2=NC2=C1OCCC2 Chemical compound O=C1N(****2)C2=NC2=C1OCCC2 0.000 description 3
- UVBMZKBIZUWTLV-UHFFFAOYSA-N CCCN(C)CCC Chemical compound CCCN(C)CCC UVBMZKBIZUWTLV-UHFFFAOYSA-N 0.000 description 1
- SECXISVLQFMRJM-UHFFFAOYSA-N CN(CCC1)C1=O Chemical compound CN(CCC1)C1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 1
- KVIZTDNKHOCNAM-UHFFFAOYSA-N CN(CCN1)CC1=O Chemical compound CN(CCN1)CC1=O KVIZTDNKHOCNAM-UHFFFAOYSA-N 0.000 description 1
- FGQBGDBLZZPFCM-UHFFFAOYSA-N CN(CCOC1)C1=O Chemical compound CN(CCOC1)C1=O FGQBGDBLZZPFCM-UHFFFAOYSA-N 0.000 description 1
- MCBFNYVOJAYSCR-UHFFFAOYSA-N CN1C2COCC1CC2 Chemical compound CN1C2COCC1CC2 MCBFNYVOJAYSCR-UHFFFAOYSA-N 0.000 description 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N CN1CCNCC1 Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- UQFQONCQIQEYPJ-UHFFFAOYSA-N C[n]1nccc1 Chemical compound C[n]1nccc1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| 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 | ||
| PCT/CN2015/081518 WO2015192760A1 (zh) | 2014-06-17 | 2015-06-16 | 作为pi3k抑制剂的吡啶并［1，2-a］嘧啶酮类似物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017519821A JP2017519821A (ja) | 2017-07-20 |
| JP2017519821A5 true JP2017519821A5 (enExample) | 2018-06-28 |
| JP6680774B2 JP6680774B2 (ja) | 2020-04-15 |
Family
ID=54934872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017518397A Active JP6680774B2 (ja) | 2014-06-17 | 2015-06-16 | ＰＩ３Ｋ阻害剤としてのピリド［１，２−ａ］ピリミドン類似体 |
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 |
Family Cites Families (11)
| 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 |
| NZ604478A (en) * | 2010-07-02 | 2014-12-24 | 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 |
| 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 |
| TW201443037A (zh) * | 2013-01-09 | 2014-11-16 | Gilead Sciences Inc | 治療用化合物 |
| RU2658912C1 (ru) * | 2014-06-17 | 2018-06-26 | Шанхай Цзя Тань Фарматек Ко. Лтд. | АНАЛОГ ПИРИДИНО[1,2-А]ПИРИМИДОНА, ИСПОЛЬЗУЕМЫЙ В КАЧЕСТВЕ ИНГИБИТОРА mTOR/PI3K |
-
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
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