JP2013535491A5 - - Google Patents
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- Publication number
- JP2013535491A5 JP2013535491A5 JP2013523468A JP2013523468A JP2013535491A5 JP 2013535491 A5 JP2013535491 A5 JP 2013535491A5 JP 2013523468 A JP2013523468 A JP 2013523468A JP 2013523468 A JP2013523468 A JP 2013523468A JP 2013535491 A5 JP2013535491 A5 JP 2013535491A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- group
- heterocyclyl
- alkyl
- aryl
- 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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- 150000001875 compounds Chemical class 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 239000012661 PARP inhibitor Substances 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 229940009456 adriamycin Drugs 0.000 claims 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229960003901 dacarbazine Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000003301 hydrolyzing effect Effects 0.000 claims 1
- 230000005865 ionizing radiation Effects 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 210000004881 tumor cell Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102483075A CN102372716A (zh) | 2010-08-09 | 2010-08-09 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
| CN201010248307.5 | 2010-08-09 | ||
| PCT/CN2011/001223 WO2012019427A1 (zh) | 2010-08-09 | 2011-07-26 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013535491A JP2013535491A (ja) | 2013-09-12 |
| JP2013535491A5 true JP2013535491A5 (https=) | 2014-07-24 |
| JP5808408B2 JP5808408B2 (ja) | 2015-11-10 |
Family
ID=45567315
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013523468A Active JP5808408B2 (ja) | 2010-08-09 | 2011-07-26 | フタラジノンケトン誘導体、その製造法および医薬用途 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9273052B2 (https=) |
| EP (1) | EP2604610B1 (https=) |
| JP (1) | JP5808408B2 (https=) |
| KR (1) | KR101829940B1 (https=) |
| CN (2) | CN102372716A (https=) |
| AU (1) | AU2011288876B2 (https=) |
| BR (1) | BR112013002220B1 (https=) |
| CA (1) | CA2806324C (https=) |
| ES (1) | ES2582315T3 (https=) |
| HU (1) | HUE029275T2 (https=) |
| PL (1) | PL2604610T3 (https=) |
| PT (1) | PT2604610T (https=) |
| RU (1) | RU2564527C2 (https=) |
| UA (1) | UA111161C2 (https=) |
| WO (1) | WO2012019427A1 (https=) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102898377B (zh) * | 2012-02-14 | 2016-01-20 | 南京圣和药业股份有限公司 | 一类酞嗪酮衍生物及其用途 |
| CN102702108A (zh) * | 2012-06-27 | 2012-10-03 | 上海大学 | 1,2-二氢酞嗪类化合物及其合成方法 |
| CN103570725B (zh) * | 2012-08-01 | 2017-03-22 | 中国科学院上海药物研究所 | 哌嗪并三唑类化合物及其制备方法和用途 |
| CN102863393A (zh) * | 2012-09-26 | 2013-01-09 | 上海大学 | 1,2-二氢酞嗪类化合物及其合成方法 |
| HUE030613T2 (en) | 2012-12-31 | 2017-05-29 | Cadila Healthcare Ltd | Substituted phthalazin-1 (2H) -one derivatives as selective inhibitors of poly (ADP-ribose) polymerase-1 |
| KR101670126B1 (ko) | 2013-09-13 | 2016-10-27 | 일동제약(주) | 신규 프탈라지논 유도체 및 그 제조방법 |
| TW201605859A (zh) | 2013-11-14 | 2016-02-16 | 必治妥美雅史谷比公司 | 作為酪蛋白激酶１δ／ε抑制劑之新穎經取代之吡唑并－哌 |
| AU2016296905B2 (en) | 2015-07-23 | 2018-07-05 | Centre National De La Recherche Scientifique | Use of a combination of Dbait molecule and parp inhibitors to treat cancer |
| CN108473495B (zh) | 2015-11-20 | 2022-04-12 | 福马治疗有限公司 | 作为泛素-特异性蛋白酶1抑制剂的嘌呤酮 |
| CN106749261A (zh) * | 2015-11-23 | 2017-05-31 | 中国科学院上海药物研究所 | 一类取代三唑并哌嗪类parp抑制剂及其制备方法和用途 |
| WO2017101796A1 (zh) * | 2015-12-16 | 2017-06-22 | 四川科伦博泰生物医药股份有限公司 | 酞嗪酮衍生物、其制备方法及用途 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2018099423A1 (zh) | 2016-12-01 | 2018-06-07 | 江苏恒瑞医药股份有限公司 | 一种vegfr抑制剂与parp抑制剂联合在制备治疗胃癌的药物中的用途 |
| WO2018162439A1 (en) | 2017-03-08 | 2018-09-13 | Onxeo | New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule |
| LT3483164T (lt) | 2017-03-20 | 2020-05-11 | Forma Therapeutics, Inc. | Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai |
| WO2018191389A1 (en) * | 2017-04-12 | 2018-10-18 | Roche Sequencing Solutions, Inc. | A method for sequencing reaction with tagged nucleoside obtained via pictet spengler reaction |
| TWI765086B (zh) * | 2017-08-24 | 2022-05-21 | 大陸商江蘇恒瑞醫藥股份有限公司 | Parp-1抑制劑的晶型及其製備方法 |
| MX2020005659A (es) | 2017-12-06 | 2020-08-20 | Jiangsu Hengrui Medicine Co | Uso de un inhibidor de parp en el tratamiento del cancer de ovario o cancer de mama resistente a la quimioterapia. |
| JP2021509906A (ja) | 2018-01-09 | 2021-04-08 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Ｊｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．， Ｌｔｄ． | Ｐａｒｐ阻害剤の製造方法およびその中間体 |
| AU2019212093B2 (en) * | 2018-01-26 | 2024-05-30 | Recordati Industria Chimica E Farmaceutica S.P.A | Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mGlu5 receptors |
| EP3758695A4 (en) * | 2018-02-28 | 2021-10-06 | The Trustees Of The University Of Pennsylvania | POLY (AD-RIBOSE) -POLYMERASE 1 DEPENDENT CYTOTOXIC AGENTS WITH LOW AFFINITY |
| CA3092779A1 (en) | 2018-03-13 | 2019-09-19 | Onxeo | A dbait molecule against acquired resistance in the treatment of cancer |
| RU2020131507A (ru) * | 2018-03-29 | 2022-05-04 | Боард Оф Реджентс, Де Юниверсити Оф Техас Систем | Имидазопиперазиновые ингибиторы белков-активаторов транскрипции |
| EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
| EP3853206B1 (en) | 2018-09-19 | 2024-04-10 | Novo Nordisk Health Care AG | Treating sickle cell disease with a pyruvate kinase r activating compound |
| TW202029961A (zh) * | 2018-10-22 | 2020-08-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | Ar拮抗劑聯合parp抑制劑在製備治療前列腺癌的藥物中的用途 |
| TWI715291B (zh) * | 2018-11-16 | 2021-01-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | 包含parp抑制劑的藥物組合物 |
| TW202110448A (zh) * | 2019-05-28 | 2021-03-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | Ｐａｒｐ抑制劑聯合ｖｅｇｆｒ抑制劑用於治療卵巢癌或乳腺癌的用途 |
| HRP20251148T1 (hr) | 2019-09-19 | 2025-11-21 | Novo Nordisk Health Care Ag | Pripravci koji aktiviraju piruvat-kinazu r (pkr) |
| CN112870365A (zh) * | 2019-11-29 | 2021-06-01 | 江苏恒瑞医药股份有限公司 | Ezh2抑制剂和/或parp抑制剂与化疗药物联合在制备治疗肿瘤药物中的用途 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2020444056A1 (en) | 2020-04-21 | 2022-11-17 | Idience Co., Ltd. | Crystalline forms of phthalazinone compound |
| JP7626783B2 (ja) | 2020-04-21 | 2025-02-07 | アイディーエンス カンパニー リミテッド | フタラジノン誘導体及びその中間体を調製するプロセス |
| CN111732594B (zh) * | 2020-08-18 | 2022-03-04 | 苏州富士莱医药股份有限公司 | 一种氟唑帕利的制备方法 |
| CA3193745A1 (en) | 2020-10-02 | 2022-04-07 | Kang Le | Imidazopiperazine inhibitors of transcription activating proteins |
| EP4221708A4 (en) | 2020-10-02 | 2024-11-06 | Board of Regents, The University of Texas System | IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION-ACTIVATING PROTEINS |
| US12059419B2 (en) | 2020-10-16 | 2024-08-13 | Idience Co., Ltd. | Pharmaceutical composition comprising phthalazinone derivatives |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| BR112023022496A2 (pt) * | 2021-05-24 | 2024-01-16 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Composto heterocíclico contendo nitrogênio, método de preparação do mesmo, e aplicação do mesmo em medicamentos |
| US20240317762A1 (en) * | 2021-07-16 | 2024-09-26 | Oregon Health & Science University | Phthalazinone-based parp-1 inhibitors |
| JP2024528021A (ja) * | 2021-07-29 | 2024-07-26 | 上海齊魯制藥研究中心有限公司 | 新規なｐａｒｐ７阻害剤及びその使用 |
| CN115650988B (zh) * | 2022-10-27 | 2024-09-13 | 江苏恒瑞医药股份有限公司 | 一种parp抑制剂的制备方法 |
| CN120035596A (zh) * | 2022-11-23 | 2025-05-23 | 江苏恒瑞医药股份有限公司 | 一种含氮杂环类化合物的可药用盐、晶型及制备方法 |
| TW202502341A (zh) * | 2023-03-13 | 2025-01-16 | 大陸商江蘇豪森藥業集團有限公司 | 哌啶烯類化合物在製備治療癌症的藥物中的應用 |
| CN121398822A (zh) | 2023-06-21 | 2026-01-23 | 四方生物科学有限公司 | 用于在治疗hr功能正常的癌症的方法中的用途的包含脱氧胞苷衍生物和parp抑制剂的组合 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU228960B1 (hu) | 2000-10-30 | 2013-07-29 | Kudos Pharm Ltd | Ftalazinon-származékok |
| AU2003211381B9 (en) * | 2002-02-19 | 2009-07-30 | Ono Pharmaceutical Co., Ltd. | Fused pyridazine derivative compounds and drugs containing the compounds as the active ingredient |
| AR043443A1 (es) | 2003-03-07 | 2005-07-27 | Merck & Co Inc | Procedimiento de preparacion de tetrahidrotriazolopirazinas y productos intermedios |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| PL1633724T3 (pl) * | 2003-03-12 | 2011-10-31 | Kudos Pharm Ltd | Pochodne ftalazynonu |
| JP2008510783A (ja) | 2004-08-26 | 2008-04-10 | クドス ファーマシューティカルズ リミテッド | ４−ヘテロアリールメチル置換フタラジノン誘導体 |
| GB0610680D0 (en) * | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
| ES2548353T3 (es) | 2006-12-28 | 2015-10-15 | Abbvie Inc. | Inhibidores de poli(ADP-ribosa)polimerasa |
| US20090023727A1 (en) * | 2007-07-05 | 2009-01-22 | Muhammad Hashim Javaid | Phthalazinone derivatives |
| US8653059B2 (en) | 2007-08-21 | 2014-02-18 | Merck Sharp & Dohme Corp. | Heterocyclic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| CN101468988A (zh) | 2007-12-26 | 2009-07-01 | 上海恒瑞医药有限公司 | 哌嗪类衍生物,其制备方法及其在医药上的应用 |
| WO2009090055A1 (en) | 2008-01-17 | 2009-07-23 | Grünenthal GmbH | Substituted sulfonamide derivatives |
-
2010
- 2010-08-09 CN CN2010102483075A patent/CN102372716A/zh active Pending
-
2011
- 2011-07-26 RU RU2013106754/04A patent/RU2564527C2/ru active
- 2011-07-26 US US13/811,957 patent/US9273052B2/en active Active
- 2011-07-26 AU AU2011288876A patent/AU2011288876B2/en active Active
- 2011-07-26 CA CA2806324A patent/CA2806324C/en active Active
- 2011-07-26 BR BR112013002220-5A patent/BR112013002220B1/pt active IP Right Grant
- 2011-07-26 EP EP11815986.2A patent/EP2604610B1/en active Active
- 2011-07-26 JP JP2013523468A patent/JP5808408B2/ja active Active
- 2011-07-26 ES ES11815986.2T patent/ES2582315T3/es active Active
- 2011-07-26 HU HUE11815986A patent/HUE029275T2/en unknown
- 2011-07-26 KR KR1020137003185A patent/KR101829940B1/ko active Active
- 2011-07-26 CN CN201180003990.9A patent/CN102686591B/zh active Active
- 2011-07-26 UA UAA201301524A patent/UA111161C2/uk unknown
- 2011-07-26 WO PCT/CN2011/001223 patent/WO2012019427A1/zh not_active Ceased
- 2011-07-26 PL PL11815986.2T patent/PL2604610T3/pl unknown
- 2011-07-26 PT PT118159862T patent/PT2604610T/pt unknown
-
2016
- 2016-02-05 US US15/016,986 patent/US9566277B2/en active Active
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