JP2010523536A5 - - Google Patents

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Publication number: JP2010523536A5
Authority: JP; Japan
Prior art keywords: inhibitor; purin; ylamino; isopropyl; pentan
Prior art date: 2008-04-02
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

Application number

JP2010501589A

Other languages

English (en)

Japanese (ja)

Other versions

JP5514099B2 (ja

JP2010523536A (ja

Filing date

2008-04-02

Publication date

2011-04-21

2007-04-04 Priority claimed from GBGB0706633.5A external-priority patent/GB0706633D0/en

2008-04-02 Application filed filed Critical

2010-07-15 Publication of JP2010523536A publication Critical patent/JP2010523536A/ja

2011-04-21 Publication of JP2010523536A5 publication Critical patent/JP2010523536A5/ja

2014-06-04 Application granted granted Critical

2014-06-04 Publication of JP5514099B2 publication Critical patent/JP5514099B2/ja

Status Expired - Fee Related legal-status Critical Current

2028-04-02 Anticipated expiration legal-status Critical

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

JP2010501589A 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 Expired - Fee Related JP5514099B2 (ja)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US92169907P	2007-04-04	2007-04-04
US60/921,699		2007-04-04
GBGB0706633.5A GB0706633D0 (en)	2007-04-04	2007-04-04	Combination
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 (2)	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 (2)
EP (1)	EP2139486A1 (2)
JP (1)	JP5514099B2 (2)
CN (1)	CN101678029B (2)
GB (1)	GB0706633D0 (2)
WO (1)	WO2008122779A1 (2)

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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
BRPI0914790A2 (pt)	2008-06-17	2015-10-20	Wyeth Llc	uso de um composto de vinorelbina e um composto de hki-272, composição farmacêutica e produto e kit para o tratamento de neoplasma
US8669273B2 (en)	2008-08-04	2014-03-11	Wyeth Llc	Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine
US20120114636A1 (en) *	2009-03-11	2012-05-10	The Board Of Regents Of The University Of Texas System	Low molecular weight cyclin e (lmw-e) as a biomarker for personalization of cancer therapies
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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
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KR101824934B1 (ko) *	2009-12-11	2018-02-02	니키 파머 액퀴지션 코포레이션 2	췌장암의 치료 방법
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JP5931876B2 (ja)	2010-08-26	2016-06-08	シンフォニーエボリューション，インコーポレイテッド	多発性嚢胞腎を処置するためのレセプタータイプキナーゼの調節因子の使用
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HK1251655A1 (zh)	2015-04-20	2019-02-01	Tolero Pharmaceuticals, Inc.	通过线粒体分析预测对阿伏西地的应答
KR102608921B1 (ko)	2015-05-18	2023-12-01	스미토모 파마 온콜로지, 인크.	생체 이용률이 증가된 알보시딥 프로드러그
JP7083497B2 (ja)	2015-08-03	2022-06-13	スミトモ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併用療法
EP3344251B1 (en)	2015-09-04	2021-04-28	Aslan Pharmaceuticals PTE Limited	A combination therapy comprising varlitinib and an anticancer agent
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
AU2017379847B2 (en)	2016-12-19	2022-05-26	Sumitomo Pharma Oncology, Inc.	Profiling peptides and methods for sensitivity profiling
CN115737637A (zh) *	2017-01-10	2023-03-07	王巍	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
CA3072087A1 (en) *	2017-08-11	2019-02-14	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
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
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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 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 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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