JP2010523536A5 - - Google Patents
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- Publication number
- JP2010523536A5 JP2010523536A5 JP2010501589A JP2010501589A JP2010523536A5 JP 2010523536 A5 JP2010523536 A5 JP 2010523536A5 JP 2010501589 A JP2010501589 A JP 2010501589A JP 2010501589 A JP2010501589 A JP 2010501589A JP 2010523536 A5 JP2010523536 A5 JP 2010523536A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- purin
- ylamino
- isopropyl
- pentan
- 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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- 239000003112 inhibitor Substances 0.000 claims 21
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims 15
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims 14
- JYVLIDXNZAXMDK-UHFFFAOYSA-N pentan-2-ol Chemical compound CCCC(C)O JYVLIDXNZAXMDK-UHFFFAOYSA-N 0.000 claims 12
- 239000000825 pharmaceutical preparation Substances 0.000 claims 11
- 229940127557 pharmaceutical product Drugs 0.000 claims 11
- -1 pyridin-3-ylmethyl Chemical group 0.000 claims 8
- QSUPQMGDXOHVLK-FFXKMJQXSA-N 4-n-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-n-[(4r)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine;4-methylbenzenesulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.CC1=CC=C(S(O)(=O)=O)C=C1.C[C@@H]1COC(NC=2C=C3C(NC=4C=C(Cl)C(OCC=5SC=CN=5)=CC=4)=NC=NC3=CC=2)=N1 QSUPQMGDXOHVLK-FFXKMJQXSA-N 0.000 claims 6
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 6
- 229960004891 lapatinib Drugs 0.000 claims 6
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 6
- 229950008835 neratinib Drugs 0.000 claims 6
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims 6
- WVUNYSQLFKLYNI-AATRIKPKSA-N pelitinib Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC1=CC=C(F)C(Cl)=C1 WVUNYSQLFKLYNI-AATRIKPKSA-N 0.000 claims 6
- BTIHMVBBUGXLCJ-OAHLLOKOSA-N seliciclib Chemical compound C=12N=CN(C(C)C)C2=NC(N[C@@H](CO)CC)=NC=1NCC1=CC=CC=C1 BTIHMVBBUGXLCJ-OAHLLOKOSA-N 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- SQUNXPPTEPGMQR-OAHLLOKOSA-N (3r)-2-methyl-3-[[9-propan-2-yl-6-(pyridin-3-ylmethylamino)purin-2-yl]amino]pentan-2-ol Chemical group C=12N=CN(C(C)C)C2=NC(N[C@H](CC)C(C)(C)O)=NC=1NCC1=CC=CN=C1 SQUNXPPTEPGMQR-OAHLLOKOSA-N 0.000 claims 3
- SQUNXPPTEPGMQR-HNNXBMFYSA-N (3s)-2-methyl-3-[[9-propan-2-yl-6-(pyridin-3-ylmethylamino)purin-2-yl]amino]pentan-2-ol Chemical group C=12N=CN(C(C)C)C2=NC(N[C@@H](CC)C(C)(C)O)=NC=1NCC1=CC=CN=C1 SQUNXPPTEPGMQR-HNNXBMFYSA-N 0.000 claims 3
- SCACHXWSWJBIHG-UHFFFAOYSA-N 3-[[9-propan-2-yl-6-(pyridin-3-ylmethylamino)purin-2-yl]amino]pentan-2-ol Chemical compound C=12N=CN(C(C)C)C2=NC(NC(CC)C(C)O)=NC=1NCC1=CC=CN=C1 SCACHXWSWJBIHG-UHFFFAOYSA-N 0.000 claims 3
- OONFNUWBHFSNBT-HXUWFJFHSA-N AEE788 Chemical compound C1CN(CC)CCN1CC1=CC=C(C=2NC3=NC=NC(N[C@H](C)C=4C=CC=CC=4)=C3C=2)C=C1 OONFNUWBHFSNBT-HXUWFJFHSA-N 0.000 claims 3
- ULXXDDBFHOBEHA-ONEGZZNKSA-N Afatinib Chemical compound N1=CN=C2C=C(OC3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-ONEGZZNKSA-N 0.000 claims 3
- 101150029707 ERBB2 gene Proteins 0.000 claims 3
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 3
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 3
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims 3
- 229960005395 cetuximab Drugs 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 229940121647 egfr inhibitor Drugs 0.000 claims 3
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 3
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 3
- 229960001433 erlotinib Drugs 0.000 claims 3
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 3
- 229960002584 gefitinib Drugs 0.000 claims 3
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 3
- 229950008001 matuzumab Drugs 0.000 claims 3
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 3
- 229950010203 nimotuzumab Drugs 0.000 claims 3
- 229960001972 panitumumab Drugs 0.000 claims 3
- 229960002087 pertuzumab Drugs 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- HVXKQKFEHMGHSL-QKDCVEJESA-N tesevatinib Chemical compound N1=CN=C2C=C(OC[C@@H]3C[C@@H]4CN(C)C[C@@H]4C3)C(OC)=CC2=C1NC1=CC=C(Cl)C(Cl)=C1F HVXKQKFEHMGHSL-QKDCVEJESA-N 0.000 claims 3
- 229960000575 trastuzumab Drugs 0.000 claims 3
- 229960000241 vandetanib Drugs 0.000 claims 3
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims 3
- SCACHXWSWJBIHG-HIFRSBDPSA-N (2r,3s)-3-[[9-propan-2-yl-6-(pyridin-3-ylmethylamino)purin-2-yl]amino]pentan-2-ol Chemical group C=12N=CN(C(C)C)C2=NC(N[C@@H](CC)[C@@H](C)O)=NC=1NCC1=CC=CN=C1 SCACHXWSWJBIHG-HIFRSBDPSA-N 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- SQUNXPPTEPGMQR-UHFFFAOYSA-N 2-methyl-3-[[9-propan-2-yl-6-(pyridin-3-ylmethylamino)purin-2-yl]amino]pentan-2-ol Chemical compound C=12N=CN(C(C)C)C2=NC(NC(CC)C(C)(C)O)=NC=1NCC1=CC=CN=C1 SQUNXPPTEPGMQR-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 239000005461 Canertinib Substances 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- LUJZZYWHBDHDQX-QFIPXVFZSA-N [(3s)-morpholin-3-yl]methyl n-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate Chemical compound C=1N2N=CN=C(NC=3C=C4C=NN(CC=5C=C(F)C=CC=5)C4=CC=3)C2=C(C)C=1NC(=O)OC[C@@H]1COCCN1 LUJZZYWHBDHDQX-QFIPXVFZSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229950002826 canertinib Drugs 0.000 claims 1
- OMZCMEYTWSXEPZ-UHFFFAOYSA-N canertinib Chemical compound C1=C(Cl)C(F)=CC=C1NC1=NC=NC2=CC(OCCCN3CCOCC3)=C(NC(=O)C=C)C=C12 OMZCMEYTWSXEPZ-UHFFFAOYSA-N 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000026037 malignant tumor of neck Diseases 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92169907P | 2007-04-04 | 2007-04-04 | |
| GBGB0706633.5A GB0706633D0 (en) | 2007-04-04 | 2007-04-04 | Combination |
| US60/921,699 | 2007-04-04 | ||
| GB0706633.5 | 2007-04-04 | ||
| PCT/GB2008/001189 WO2008122779A1 (en) | 2007-04-04 | 2008-04-02 | Combination of a purine-based cdk inhibitor with a tyrosine kinase inhibitor and use thereof in the treatment of proliferative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010523536A JP2010523536A (ja) | 2010-07-15 |
| JP2010523536A5 true JP2010523536A5 (enExample) | 2011-04-21 |
| JP5514099B2 JP5514099B2 (ja) | 2014-06-04 |
Family
ID=38090894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010501589A Expired - Fee Related JP5514099B2 (ja) | 2007-04-04 | 2008-04-02 | プリンに基づくｃｄｋ阻害剤とチロシンキナーゼ阻害剤の組合せ、及び増殖性障害の治療におけるその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9173938B2 (enExample) |
| EP (1) | EP2139486A1 (enExample) |
| JP (1) | JP5514099B2 (enExample) |
| CN (1) | CN101678029B (enExample) |
| GB (1) | GB0706633D0 (enExample) |
| WO (1) | WO2008122779A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1848414T1 (sl) | 2005-02-03 | 2011-08-31 | Gen Hospital Corp | Postopek za zdravljenje raka, odpornega na gefitinib |
| RU2451524C2 (ru) | 2005-11-04 | 2012-05-27 | Вайет | Противоопухолевые комбинации с ингибиторами mtor, герцептином и/или hki-272 |
| GB0706632D0 (en) * | 2007-04-04 | 2007-05-16 | Cyclacel Ltd | New purine derivatives |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| NZ590009A (en) | 2008-06-17 | 2012-08-31 | Wyeth Llc | Antineoplastic combinations containing hki-272 and vinorelbine |
| KR101434009B1 (ko) | 2008-08-04 | 2014-08-25 | 와이어쓰 엘엘씨 | 4-아닐리노-3-사이아노퀴놀린과 카페시타빈의 항신생물성 조합물 |
| CA2754917A1 (en) * | 2009-03-11 | 2010-09-16 | Research Development Foundation | Low molecular weight cyclin e (lmw-e) as a biomarker for personalization of cancer therapies |
| CN103989681A (zh) | 2009-04-06 | 2014-08-20 | 惠氏有限责任公司 | 用于乳腺癌的利用奈拉替尼的治疗方案 |
| FR2945747A1 (fr) * | 2009-05-25 | 2010-11-26 | Centre Nat Rech Scient | Composition pharmaceutique antitumorale comprenant un inhibiteur de cdks et un inhibiteur de la croissance cellulaire |
| PL2719708T3 (pl) * | 2009-11-13 | 2018-04-30 | Daiichi Sankyo Europe Gmbh | Materiał i sposoby leczenia lub zapobiegania chorobom związanym z HER-3 |
| ES2517367T3 (es) * | 2009-12-11 | 2014-11-03 | Niiki Pharma Inc. | Procedimiento de tratamiento de cáncer pancreático |
| GB201001075D0 (en) * | 2010-01-22 | 2010-03-10 | Cyclacel Ltd | Crystalline forms |
| EA025451B1 (ru) * | 2010-08-26 | 2016-12-30 | Симфони Эволюшн, Инк. | Модулятор киназы рецепторного типа и способы лечения поликистозной болезни почек |
| TW201300105A (zh) | 2011-05-31 | 2013-01-01 | Piramal Life Sciences Ltd | 治療頭頸鱗狀細胞癌之相乘藥物組合物 |
| JP6286421B2 (ja) | 2012-05-15 | 2018-02-28 | サイクラセル リミテッド | サパシタビン及びセリシクリブの投与レジメン |
| TWI839690B (zh) | 2013-07-12 | 2024-04-21 | 印度商皮拉馬爾企業有限公司 | 治療黑色素瘤的藥物組合的用途 |
| EP3611506B1 (en) | 2015-04-20 | 2021-11-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Predicting response to alvocidib by mitochondrial profiling |
| ES2921350T3 (es) | 2015-05-18 | 2022-08-24 | Sumitomo Pharma Oncology Inc | Profármacos de alvocidib que tienen biodisponibilidad aumentada |
| BR112018002427A8 (pt) * | 2015-08-03 | 2022-10-18 | Tolero Pharmaceuticals Inc | Uso de alvocidib e de azacitidina ou decitabina para tratar câncer e kit e composição farmacêutica contendo as ditas substâncias |
| CN108135901A (zh) * | 2015-09-04 | 2018-06-08 | 亚狮康私人有限公司 | 胆管癌的治疗 |
| WO2017160568A1 (en) | 2016-03-16 | 2017-09-21 | Eli Lilly And Company | Combination therapy comprising the cdk4/6 inhibitor necitumumab and the egfr inhibitor abemaciclib for use in treating cancer |
| WO2018094275A1 (en) | 2016-11-18 | 2018-05-24 | Tolero Pharmaceuticals, Inc. | Alvocidib prodrugs and their use as protein kinase inhibitors |
| JP6619519B2 (ja) | 2016-12-19 | 2019-12-11 | トレロ ファーマシューティカルズ， インコーポレイテッド | プロファイリングペプチドおよび感受性プロファイリングのための方法 |
| CN115844877B (zh) * | 2017-01-10 | 2024-07-23 | 浙江嘉驰医药开发有限公司 | 拉索昔芬调节膜结合雌激素信号的应用及治疗癌症的方法 |
| AU2018314234B2 (en) * | 2017-08-11 | 2024-10-24 | Board Of Regents, The University Of Texas System | Targeting kinases for the treatment of cancer metastasis |
| JP7196160B2 (ja) | 2017-09-12 | 2022-12-26 | スミトモ ファーマ オンコロジー， インコーポレイテッド | Ｍｃｌ－１阻害剤アルボシジブを用いた、ｂｃｌ－２阻害剤に対して非感受性である癌の治療レジメン |
| US20210015819A1 (en) * | 2018-03-13 | 2021-01-21 | Board Of Regents, The University Of Texas System | Methods for treatment of cancers with egfr activating mutations |
| CN111818925B (zh) * | 2018-05-23 | 2023-12-12 | 江苏恒瑞医药股份有限公司 | Cdk4/6抑制剂与egfr抑制剂联合在制备治疗肿瘤疾病的药物中的用途 |
| JP2022511029A (ja) | 2018-12-04 | 2022-01-28 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | がんの処置のための薬剤としての使用のためのｃｄｋ９インヒビターおよびその多形 |
| US11793802B2 (en) | 2019-03-20 | 2023-10-24 | Sumitomo Pharma Oncology, Inc. | Treatment of acute myeloid leukemia (AML) with venetoclax failure |
| GB202000901D0 (en) * | 2020-01-22 | 2020-03-04 | Cyclacel Ltd | Process |
| CN116813621A (zh) * | 2023-06-08 | 2023-09-29 | 江南大学 | 9h嘌呤类化合物及其药物组合物和用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2741881B1 (fr) * | 1995-12-01 | 1999-07-30 | Centre Nat Rech Scient | Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques |
| GB0219054D0 (en) | 2002-08-15 | 2002-09-25 | Cyclacel Ltd | New purine derivatives |
| CA2502979A1 (en) | 2002-11-06 | 2004-05-21 | Cyclacel Limited | Pharmaceutical composition comprising a cdk inhibitor and gemcitabine |
| CA2569277A1 (en) * | 2004-06-04 | 2005-12-15 | Pfizer Products Inc. | Method for treating abnormal cell growth |
| GB0523040D0 (en) * | 2005-11-11 | 2005-12-21 | Cyclacel Ltd | Combination |
| EA200802058A1 (ru) * | 2006-05-09 | 2009-06-30 | Пфайзер Продактс Инк. | Производные циклоалкиламинокислот и их фармацевтические композиции |
-
2007
- 2007-04-04 GB GBGB0706633.5A patent/GB0706633D0/en not_active Ceased
-
2008
- 2008-04-02 JP JP2010501589A patent/JP5514099B2/ja not_active Expired - Fee Related
- 2008-04-02 WO PCT/GB2008/001189 patent/WO2008122779A1/en not_active Ceased
- 2008-04-02 CN CN2008800188649A patent/CN101678029B/zh not_active Expired - Fee Related
- 2008-04-02 EP EP08718990A patent/EP2139486A1/en not_active Withdrawn
-
2009
- 2009-10-05 US US12/573,358 patent/US9173938B2/en not_active Expired - Fee Related
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