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
Links
- 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 |
| GB0706633.5 | 2007-04-04 | ||
| US60/921,699 | 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 (https=) | 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 (https=) |
| EP (1) | EP2139486A1 (https=) |
| JP (1) | JP5514099B2 (https=) |
| CN (1) | CN101678029B (https=) |
| GB (1) | GB0706633D0 (https=) |
| WO (1) | WO2008122779A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2364495T3 (es) | 2005-02-03 | 2011-09-05 | The General Hospital Corporation | Método para tratar cáncer resistente a gefitinib. |
| JP2009514870A (ja) | 2005-11-04 | 2009-04-09 | ワイス | ｍＴＯＲインヒビター、ハーセプチン、および／またはＨＫＩ−２７２の抗悪性腫瘍性組み合わせ |
| 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 |
| ES2692769T3 (es) | 2008-06-17 | 2018-12-05 | Wyeth Llc | Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina |
| CN105147713A (zh) | 2008-08-04 | 2015-12-16 | 惠氏有限责任公司 | 4-苯胺基-3-氰基喹啉和卡培他滨的抗肿瘤组合 |
| 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 |
| SG174382A1 (en) | 2009-04-06 | 2011-11-28 | Wyeth Llc | Treatment regimen utilizing neratinib for breast cancer |
| 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 |
| MX358013B (es) * | 2009-11-13 | 2018-08-01 | Amgen Inc | Materiales y metodos para el tratamiento o prevencion de enfermedades asociadas al her-3. |
| EP2509599B1 (en) * | 2009-12-11 | 2014-08-13 | Niiki Pharma Inc. | Method for treating pancreatic cancer |
| GB201001075D0 (en) * | 2010-01-22 | 2010-03-10 | Cyclacel Ltd | Crystalline forms |
| CN103313713B (zh) | 2010-08-26 | 2014-12-31 | 和谐进化股份有限公司 | 受体型激酶调节剂和多囊性肾病的治疗方法 |
| 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 |
| WO2013171473A1 (en) | 2012-05-15 | 2013-11-21 | Cyclacel Limited | Dosage regimen for sapacitabine and seliciclib |
| CN105530931B (zh) | 2013-07-12 | 2019-11-08 | 皮拉马尔企业有限公司 | 用于治疗黑素瘤的药物组合 |
| US9901574B2 (en) | 2015-04-20 | 2018-02-27 | Tolero Pharmaceuticals, Inc. | Predicting response to alvocidib by mitochondrial profiling |
| ES2739749T3 (es) | 2015-05-18 | 2020-02-03 | Tolero Pharmaceuticals Inc | Profármacos de alvocidib que tienen biodisponibilidad aumentada |
| MX2018001289A (es) | 2015-08-03 | 2018-04-30 | Tolero Pharmaceuticals Inc | Terapias de combinacion para el tratamiento del cancer. |
| WO2017037300A1 (en) * | 2015-09-04 | 2017-03-09 | Aslan Pharmaceuticals Pte Limited | Varlitinib for use in the treatment of resistant or refractory cancer |
| 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 |
| KR20190099260A (ko) | 2016-12-19 | 2019-08-26 | 톨레로 파마수티컬스, 인크. | 프로파일링 펩티드 및 감도 프로파일링을 위한 방법 |
| WO2018129645A1 (en) * | 2017-01-10 | 2018-07-19 | Wang, Wei | Lasofoxifene modulation of membrane-initiated estrogen signals and methods for tumor treatment |
| CA3072087A1 (en) * | 2017-08-11 | 2019-02-14 | Board Of Regents, The University Of Texas System | Targeting kinases for the treatment of cancer metastasis |
| WO2019055579A1 (en) | 2017-09-12 | 2019-03-21 | Tolero Pharmaceuticals, Inc. | TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR |
| WO2019178239A1 (en) * | 2018-03-13 | 2019-09-19 | Board Of Regents, The University Of Texas System | Methods for treatment of cancers with egfr activating mutations |
| TWI762784B (zh) * | 2018-05-23 | 2022-05-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | Cdk4/6抑制劑與egfr抑制劑聯合在製備治療腫瘤疾病的藥物中的用途 |
| US11034710B2 (en) | 2018-12-04 | 2021-06-15 | Sumitomo Dainippon Pharma Oncology, Inc. | CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer |
| 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 |
| BR0316004A (pt) | 2002-11-06 | 2005-09-13 | Cyclacel Ltd | Composição farmacêutica compreendendo um inibidor de cdk e gemcitabina |
| MXPA06014021A (es) * | 2004-06-04 | 2007-02-08 | Pfizer Prod Inc | Procedimiento para tratar crecimiento celular anormal. |
| 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 CN CN2008800188649A patent/CN101678029B/zh not_active Expired - Fee Related
- 2008-04-02 WO PCT/GB2008/001189 patent/WO2008122779A1/en not_active Ceased
- 2008-04-02 EP EP08718990A patent/EP2139486A1/en not_active Withdrawn
- 2008-04-02 JP JP2010501589A patent/JP5514099B2/ja not_active Expired - Fee Related
-
2009
- 2009-10-05 US US12/573,358 patent/US9173938B2/en not_active Expired - Fee Related
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