JP6437559B2 - Ｗｅｅ−１キナーゼ阻害剤として有用なピリミドピリミジノン - Google Patents
Ｗｅｅ−１キナーゼ阻害剤として有用なピリミドピリミジノン Download PDFInfo
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- JP6437559B2 JP6437559B2 JP2016541294A JP2016541294A JP6437559B2 JP 6437559 B2 JP6437559 B2 JP 6437559B2 JP 2016541294 A JP2016541294 A JP 2016541294A JP 2016541294 A JP2016541294 A JP 2016541294A JP 6437559 B2 JP6437559 B2 JP 6437559B2
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- methyl
- amino
- group
- dichlorophenyl
- phenyl
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- VLOJEWGCECYEAM-UHFFFAOYSA-N CC1(C=CC(Nc(nc2)nc(N(C)CN3c(c(Cl)ccc4)c4Cl)c2C3=O)=CC1)N1C(C2)CNC2C1 Chemical compound CC1(C=CC(Nc(nc2)nc(N(C)CN3c(c(Cl)ccc4)c4Cl)c2C3=O)=CC1)N1C(C2)CNC2C1 VLOJEWGCECYEAM-UHFFFAOYSA-N 0.000 description 1
- YUPAEYHVCOZVOK-MDYZWHIJSA-N CC1(C=CC(Nc(nc2N(C)CN3c(c(Cl)ccc4)c4Cl)ncc2C3=O)=CC1)N1[C@H](CO)CN(C)CC1 Chemical compound CC1(C=CC(Nc(nc2N(C)CN3c(c(Cl)ccc4)c4Cl)ncc2C3=O)=CC1)N1[C@H](CO)CN(C)CC1 YUPAEYHVCOZVOK-MDYZWHIJSA-N 0.000 description 1
- 0 CN(C(*)(*)N1c(c(Cl)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N2CCNCC2)nc2)c2C1=O Chemical compound CN(C(*)(*)N1c(c(Cl)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N2CCNCC2)nc2)c2C1=O 0.000 description 1
- TYNDDJWXWHJULJ-UHFFFAOYSA-N CN(CC1)CCC1Oc(cc1)ccc1Nc(nc1)nc(N(C)CN2c(c(Cl)ccc3)c3Cl)c1C2=O Chemical compound CN(CC1)CCC1Oc(cc1)ccc1Nc(nc1)nc(N(C)CN2c(c(Cl)ccc3)c3Cl)c1C2=O TYNDDJWXWHJULJ-UHFFFAOYSA-N 0.000 description 1
- HKRAKIIDROVHCU-UHFFFAOYSA-N CN(CN1c(c(Cl)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N(CC2)CCS2(=O)=O)nc2)c2C1=O Chemical compound CN(CN1c(c(Cl)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N(CC2)CCS2(=O)=O)nc2)c2C1=O HKRAKIIDROVHCU-UHFFFAOYSA-N 0.000 description 1
- PIUTZCHAHKDSNS-UHFFFAOYSA-N CN(CN1c(c(Cl)ccc2)c2Cl)c2nc(Nc(cc3)cc(CNCC(F)(F)F)c3N3CCNCC3)ncc2C1=O Chemical compound CN(CN1c(c(Cl)ccc2)c2Cl)c2nc(Nc(cc3)cc(CNCC(F)(F)F)c3N3CCNCC3)ncc2C1=O PIUTZCHAHKDSNS-UHFFFAOYSA-N 0.000 description 1
- ZDMVUMOTHMZRQP-UHFFFAOYSA-N CN(CN1c(c(Cl)ccc2)c2Cl)c2nc(Nc(cc3)ccc3N3CCN(CC(O)=O)CC3)ncc2C1=O Chemical compound CN(CN1c(c(Cl)ccc2)c2Cl)c2nc(Nc(cc3)ccc3N3CCN(CC(O)=O)CC3)ncc2C1=O ZDMVUMOTHMZRQP-UHFFFAOYSA-N 0.000 description 1
- LTHCLGLQFVDPSF-UHFFFAOYSA-N CN(CN1c(c(F)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N2CC(COC)NCC2)nc2)c2C1=O Chemical compound CN(CN1c(c(F)ccc2)c2Cl)c(nc(Nc(cc2)ccc2N2CC(COC)NCC2)nc2)c2C1=O LTHCLGLQFVDPSF-UHFFFAOYSA-N 0.000 description 1
- SZLLSOCIXPGJLW-WMZOPIPTSA-N CN(CN1c(cccc2)c2Cl)c(nc(Nc(cc2)ccc2N2[C@@H](C3)CN[C@@H]3C2)nc2)c2C1=O Chemical compound CN(CN1c(cccc2)c2Cl)c(nc(Nc(cc2)ccc2N2[C@@H](C3)CN[C@@H]3C2)nc2)c2C1=O SZLLSOCIXPGJLW-WMZOPIPTSA-N 0.000 description 1
- QZJJZINNSZRIHM-UHFFFAOYSA-N CN1CCN(Cc(cc2)ccc2Nc(nc2)nc(N(C)CN3c(c(Cl)ccc4)c4Cl)c2C3=O)CC1 Chemical compound CN1CCN(Cc(cc2)ccc2Nc(nc2)nc(N(C)CN3c(c(Cl)ccc4)c4Cl)c2C3=O)CC1 QZJJZINNSZRIHM-UHFFFAOYSA-N 0.000 description 1
- KORCVBOCKBZMRD-MRXNPFEDSA-N C[C@H](C1)N(C)CCN1c(cc1)ccc1Nc(nc1)nc(N(C)CN2c(c(Cl)ccc3)c3Cl)c1C2=O Chemical compound C[C@H](C1)N(C)CCN1c(cc1)ccc1Nc(nc1)nc(N(C)CN2c(c(Cl)ccc3)c3Cl)c1C2=O KORCVBOCKBZMRD-MRXNPFEDSA-N 0.000 description 1
- KVQJFGGAQBGGCB-MRXNPFEDSA-N C[C@H](C1)NCCN1c(c(COC)c1)ccc1Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O Chemical compound C[C@H](C1)NCCN1c(c(COC)c1)ccc1Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O KVQJFGGAQBGGCB-MRXNPFEDSA-N 0.000 description 1
- SAVKMENYJBWNHC-CQSZACIVSA-N C[C@H](C1)NCCN1c(cc1F)ccc1Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O Chemical compound C[C@H](C1)NCCN1c(cc1F)ccc1Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O SAVKMENYJBWNHC-CQSZACIVSA-N 0.000 description 1
- ZOKGXCGRFOEAGH-CQSZACIVSA-N C[C@H](C1)NCCN1c(ccc(Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O)c1)c1F Chemical compound C[C@H](C1)NCCN1c(ccc(Nc(nc1N(C)CN2c(c(Cl)ccc3)c3Cl)ncc1C2=O)c1)c1F ZOKGXCGRFOEAGH-CQSZACIVSA-N 0.000 description 1
- ZSQBZADJUMJJAA-UHFFFAOYSA-N O=C(c1c(N2C3CCC2)nc(Nc(cc2)ccc2N2CCNCC2)nc1)N3c(c(Cl)ccc1)c1Cl Chemical compound O=C(c1c(N2C3CCC2)nc(Nc(cc2)ccc2N2CCNCC2)nc1)N3c(c(Cl)ccc1)c1Cl ZSQBZADJUMJJAA-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1322602.2 | 2013-12-19 | ||
| GBGB1322602.2A GB201322602D0 (en) | 2013-12-19 | 2013-12-19 | Pharmaceutical compounds |
| PCT/GB2014/053793 WO2015092431A1 (en) | 2013-12-19 | 2014-12-19 | Pyrimidopyrimidinones useful as wee-1 kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017500335A JP2017500335A (ja) | 2017-01-05 |
| JP6437559B2 true JP6437559B2 (ja) | 2018-12-12 |
Family
ID=50071157
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016541294A Active JP6437559B2 (ja) | 2013-12-19 | 2014-12-19 | Ｗｅｅ−１キナーゼ阻害剤として有用なピリミドピリミジノン |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9850247B2 (https=) |
| EP (1) | EP3083625B1 (https=) |
| JP (1) | JP6437559B2 (https=) |
| KR (1) | KR102405462B1 (https=) |
| CN (1) | CN105829315B (https=) |
| AU (1) | AU2014369457B2 (https=) |
| BR (1) | BR112016014151B1 (https=) |
| CA (1) | CA2933755C (https=) |
| CY (1) | CY1120035T1 (https=) |
| DK (1) | DK3083625T3 (https=) |
| ES (1) | ES2650013T3 (https=) |
| GB (1) | GB201322602D0 (https=) |
| HR (1) | HRP20180080T1 (https=) |
| HU (1) | HUE037908T2 (https=) |
| IL (1) | IL245672B (https=) |
| LT (1) | LT3083625T (https=) |
| MX (1) | MX371108B (https=) |
| NO (1) | NO3083625T3 (https=) |
| NZ (1) | NZ720178A (https=) |
| PL (1) | PL3083625T3 (https=) |
| PT (1) | PT3083625T (https=) |
| RS (1) | RS56731B1 (https=) |
| RU (1) | RU2691105C1 (https=) |
| SG (1) | SG11201603814TA (https=) |
| SI (1) | SI3083625T1 (https=) |
| SM (1) | SMT201800020T1 (https=) |
| WO (1) | WO2015092431A1 (https=) |
| ZA (1) | ZA201603337B (https=) |
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|---|---|---|---|---|
| CN108137593B (zh) * | 2015-04-21 | 2021-01-05 | 上海交通大学医学院附属瑞金医院 | 蛋白激酶抑制剂的制备和用途 |
| JP6692423B2 (ja) * | 2015-11-01 | 2020-05-13 | ザ リージェンツ オブ ザ ユニヴァーシティ オブ コロラド，ア ボディ コーポレイト | Ｗｅｅ１キナーゼ阻害剤、並びにそれを作製及び使用する方法 |
| US10703759B2 (en) | 2016-11-16 | 2020-07-07 | Impact Therapeutics, Inc | 8,9-dihydroimidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-ones |
| WO2018124001A1 (ja) | 2016-12-27 | 2018-07-05 | 国立研究開発法人理化学研究所 | Ｂｍｐシグナル阻害化合物 |
| JP6717457B2 (ja) | 2017-01-23 | 2020-07-01 | シージャーズォアン サガシティ ニュー ドラッグ デベロップメント カンパニー リミテッド | Ｗｅｅ１阻害剤としての１，２−ジヒドロ−３Ｈ−ピラゾロ［３，４−ｄ］ピリミジン−３−オン誘導体 |
| GB201703881D0 (en) * | 2017-03-10 | 2017-04-26 | Almac Discovery Ltd | Pharmaceutical compounds |
| CN110678169A (zh) | 2017-03-31 | 2020-01-10 | 西雅图遗传学公司 | Chk1-抑制剂与weel-抑制剂的组合 |
| CN110914277B (zh) * | 2017-07-10 | 2022-08-09 | 上海瑛派药业有限公司 | 咪唑并[1,2-b]嘧啶并[4,5-d]哒嗪-5(6H)-酮类化合物及其应用 |
| CN109422754A (zh) * | 2017-08-24 | 2019-03-05 | 上海迪诺医药科技有限公司 | 吡唑并[3,4-d]嘧啶-3-酮衍生物、其药物组合物及应用 |
| EP3694861A4 (en) | 2017-10-09 | 2021-05-19 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| AU2018347307A1 (en) | 2017-10-09 | 2020-04-23 | Nuvation Bio Inc. | Heterocyclic compounds and uses thereof |
| SG11202003974XA (en) | 2017-11-01 | 2020-05-28 | Shijiazhuang Sagacity New Drug Development Co Ltd | Macrocyclic compound serving as weel inhibitor and applications thereof |
| US12220415B2 (en) | 2018-02-28 | 2025-02-11 | The Regents Of The University Of Colorado, A Body Corporate | WEE1 kinase inhibitors and methods of treating cancer using the same |
| KR20210066839A (ko) * | 2018-09-27 | 2021-06-07 | 베타 파머수티컬 컴퍼니 리미티드 | Fgfr4 저해제 및 그것의 용도 |
| US12180184B2 (en) | 2018-10-26 | 2024-12-31 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Pyrimidopyrazolone derivative as Wee1 inhibitor and use thereof |
| WO2020140054A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| KR102697799B1 (ko) | 2019-03-22 | 2024-08-23 | 쇼우야오 홀딩스 (베이징) 코., 엘티디. | Wee1 억제제 및 이의 제조 및 용도 |
| WO2020210377A1 (en) * | 2019-04-09 | 2020-10-15 | Nuvation Bio Inc. | Heterocyclic compounds and uses thereof |
| JP2022526831A (ja) | 2019-04-09 | 2022-05-26 | ニューベイション・バイオ・インコーポレイテッド | ヘテロ環式化合物およびその使用 |
| EP3952878A4 (en) * | 2019-04-09 | 2023-01-04 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AND THEIR USES |
| SI3964510T1 (sl) | 2019-04-30 | 2024-10-30 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Kristalna oblika WEE1 inhibitorske spojine in njena uporaba |
| CN112142763B (zh) * | 2019-06-28 | 2024-01-26 | 上海医药集团股份有限公司 | 一种吡唑酮并嘧啶类化合物、其制备方法及应用 |
| CA3180664A1 (en) | 2020-06-17 | 2021-12-23 | Yuli Xie | Pyrazolo[3,4-d]pyrimidine-3-one derivative as wee-1 inhibitor |
| EP4221710A4 (en) * | 2020-10-01 | 2024-09-18 | University of Washington | DRUG-LIKE MOLECULES AND METHODS FOR THERAPEUTIC TARGETING OF MICRORNA-21 |
| US12551584B1 (en) | 2020-12-07 | 2026-02-17 | Actinium Pharmaceuticals, Inc. | Lewis Y radioimmunotherapy for the treatment of cancer |
| CN116601153B (zh) * | 2020-12-18 | 2025-10-28 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为nav1.8抑制剂的含氮2,3-二氢喹唑啉酮化合物 |
| EP4262978A1 (en) * | 2020-12-18 | 2023-10-25 | GlaxoSmithKline Intellectual Property Development Limited | Chemical compounds useful for inhibiting nav1.8 voltage-gated sodium channels and treating nav1.8 mediated diseases |
| KR20240004539A (ko) | 2021-04-30 | 2024-01-11 | 위겐 바이오메더슨 테크널러지 (상하이) 컴퍼니 리미티드 | Wee-1 억제제로서의 축합 고리 화합물, 그를 위한 제조 방법 및 그의 용도 |
| BR112023025403A2 (pt) | 2021-06-25 | 2024-02-20 | Korea Res Inst Chemical Tech | Composto heterocíclico bifuncional tendo função de degradação de btk por meio da via ubiquitina proteassoma e uso do mesmo |
| CN116462687B (zh) | 2022-01-18 | 2025-01-07 | 江苏天士力帝益药业有限公司 | Wee1抑制剂及其制备和用途 |
| CN116836184B (zh) * | 2022-03-25 | 2025-07-25 | 药雅科技(上海)有限公司 | Wee1激酶抑制剂的制备及其应用 |
| WO2023217201A2 (zh) * | 2022-05-10 | 2023-11-16 | 杭州德睿智药科技有限公司 | 作为Wee1抑制剂的新型嘧啶并杂环类新化合物及其应用 |
| CN117402162A (zh) | 2022-07-13 | 2024-01-16 | 江苏天士力帝益药业有限公司 | Wee1抑制剂及其制备和用途 |
| TW202519226A (zh) | 2023-11-08 | 2025-05-16 | 美商艾克塞里克斯公司 | 使用抑制ｐｋｍｙｔ１之化合物治療癌症之方法 |
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| JP5129812B2 (ja) | 2007-06-15 | 2013-01-30 | Ｍｓｄ株式会社 | ビシクロアニリン誘導体 |
| WO2009054332A1 (ja) * | 2007-10-23 | 2009-04-30 | Banyu Pharmaceutical Co., Ltd. | ピリドン置換ジヒドロピラゾロピリミジノン誘導体 |
| AU2009325400A1 (en) * | 2008-12-12 | 2010-06-17 | Msd K.K. | Dihydropyrimidopyrimidine derivatives |
| AU2009325398A1 (en) | 2008-12-12 | 2010-06-17 | Msd K.K. | Dihydropyrimidopyrimidine derivative |
| KR101861883B1 (ko) * | 2010-12-06 | 2018-05-28 | 글락소 그룹 리미티드 | Lp-PLA₂에 의해 매개되는 질환 또는 상태의 치료에 사용하기 위한 피리미디논 화합물 |
| AR084515A1 (es) * | 2010-12-22 | 2013-05-22 | Merz Pharma Gmbh & Co Kgaa | Derivados heterociclicos nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades asociadas al sistema nervioso central tales como parkinson y alzheimer, entre otras |
| TWI532742B (zh) | 2011-02-28 | 2016-05-11 | 艾伯維有限公司 | 激酶之三環抑制劑 |
| WO2013012681A1 (en) | 2011-07-15 | 2013-01-24 | Abbott Laboratories | Tricyclic inhibitors of kinases useful for the treatment of proliferative diseases |
| US8796289B2 (en) * | 2011-07-19 | 2014-08-05 | Abbvie Inc. | Pyridazino[4,5-D]pyrimidin-5(6H)-one inhibitors of kinases |
| US9181239B2 (en) | 2011-10-20 | 2015-11-10 | Abbvie Inc. | Pyridopyrimidinone inhibitors of kinases |
| MX2014010176A (es) | 2012-02-23 | 2014-11-10 | Abbvie Inc | Inhibidores de cinasas de piridopirimidinona. |
| CN102816164A (zh) * | 2012-08-31 | 2012-12-12 | 北京理工大学 | 一种合成7-氨基-2,3-二氢嘧啶[4,5-d]嘧啶-4(1H)-酮的方法 |
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