JP2014512362A5 - - Google Patents
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- Publication number
- JP2014512362A5 JP2014512362A5 JP2014504036A JP2014504036A JP2014512362A5 JP 2014512362 A5 JP2014512362 A5 JP 2014512362A5 JP 2014504036 A JP2014504036 A JP 2014504036A JP 2014504036 A JP2014504036 A JP 2014504036A JP 2014512362 A5 JP2014512362 A5 JP 2014512362A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- inhibitor
- aryl
- group
- optionally substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 42
- 125000003118 aryl group Chemical group 0.000 claims 31
- 239000003112 inhibitor Substances 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 13
- 239000003795 chemical substances by application Substances 0.000 claims 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- -1 anthracycline Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 239000000556 agonist Substances 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 101710183280 Topoisomerase Proteins 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 229940100198 alkylating agent Drugs 0.000 claims 4
- 239000002168 alkylating agent Substances 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 4
- 230000000340 anti-metabolite Effects 0.000 claims 4
- 239000002256 antimetabolite Substances 0.000 claims 4
- 229940100197 antimetabolite Drugs 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000005556 hormone Substances 0.000 claims 4
- 229940088597 hormone Drugs 0.000 claims 4
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 238000002648 combination therapy Methods 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- 229940126638 Akt inhibitor Drugs 0.000 claims 2
- 229940123413 Angiotensin II antagonist Drugs 0.000 claims 2
- 229940122815 Aromatase inhibitor Drugs 0.000 claims 2
- 102400000967 Bradykinin Human genes 0.000 claims 2
- 101800004538 Bradykinin Proteins 0.000 claims 2
- 101150013553 CD40 gene Proteins 0.000 claims 2
- 101150065749 Churc1 gene Proteins 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 2
- 102000004127 Cytokines Human genes 0.000 claims 2
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims 2
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims 2
- 102100028043 Fibroblast growth factor 3 Human genes 0.000 claims 2
- 102400000932 Gonadoliberin-1 Human genes 0.000 claims 2
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 2
- 101001060280 Homo sapiens Fibroblast growth factor 3 Proteins 0.000 claims 2
- 101500026183 Homo sapiens Gonadoliberin-1 Proteins 0.000 claims 2
- 239000003458 I kappa b kinase inhibitor Substances 0.000 claims 2
- 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims 2
- 102000004218 Insulin-Like Growth Factor I Human genes 0.000 claims 2
- 229940126560 MAPK inhibitor Drugs 0.000 claims 2
- 102000029749 Microtubule Human genes 0.000 claims 2
- 108091022875 Microtubule Proteins 0.000 claims 2
- 102100038239 Protein Churchill Human genes 0.000 claims 2
- 102000001708 Protein Isoforms Human genes 0.000 claims 2
- 108010029485 Protein Isoforms Proteins 0.000 claims 2
- 229940123237 Taxane Drugs 0.000 claims 2
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 2
- 229940122149 Thymidylate synthase inhibitor Drugs 0.000 claims 2
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims 2
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims 2
- 102100040245 Tumor necrosis factor receptor superfamily member 5 Human genes 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 2
- 230000002280 anti-androgenic effect Effects 0.000 claims 2
- 230000009949 anti-apoptotic pathway Effects 0.000 claims 2
- 229940046836 anti-estrogen Drugs 0.000 claims 2
- 230000001833 anti-estrogenic effect Effects 0.000 claims 2
- 239000000051 antiandrogen Substances 0.000 claims 2
- 229940034982 antineoplastic agent Drugs 0.000 claims 2
- 230000005775 apoptotic pathway Effects 0.000 claims 2
- 239000003886 aromatase inhibitor Substances 0.000 claims 2
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 2
- 230000024245 cell differentiation Effects 0.000 claims 2
- 239000003246 corticosteroid Substances 0.000 claims 2
- 229940111134 coxibs Drugs 0.000 claims 2
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 2
- 239000000824 cytostatic agent Substances 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims 2
- 229940121647 egfr inhibitor Drugs 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 239000000328 estrogen antagonist Substances 0.000 claims 2
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 claims 2
- 229960001442 gonadorelin Drugs 0.000 claims 2
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- 239000003475 metalloproteinase inhibitor Substances 0.000 claims 2
- 210000004688 microtubule Anatomy 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 2
- 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 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 claims 2
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 claims 2
- 239000003197 protein kinase B inhibitor Substances 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 2
- 229940075439 smac mimetic Drugs 0.000 claims 2
- 239000003277 telomerase inhibitor Substances 0.000 claims 2
- 229960004964 temozolomide Drugs 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 239000003734 thymidylate synthase inhibitor Substances 0.000 claims 2
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 229940097396 Aminopeptidase inhibitor Drugs 0.000 claims 1
- 102000004400 Aminopeptidases Human genes 0.000 claims 1
- 108090000915 Aminopeptidases Proteins 0.000 claims 1
- 102000014654 Aromatase Human genes 0.000 claims 1
- 108010078554 Aromatase Proteins 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 229940122204 Cyclooxygenase inhibitor Drugs 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 229940122588 Heparanase inhibitor Drugs 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 229940126033 PPAR agonist Drugs 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 229940123582 Telomerase inhibitor Drugs 0.000 claims 1
- 102000004243 Tubulin Human genes 0.000 claims 1
- 108090000704 Tubulin Proteins 0.000 claims 1
- 230000010721 Tubulin Interactions Effects 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 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
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 claims 1
- 229960002949 fluorouracil Drugs 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
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000002307 peroxisome proliferator activated receptor agonist Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 1
- 229940063683 taxotere Drugs 0.000 claims 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161472968P | 2011-04-07 | 2011-04-07 | |
| US61/472,968 | 2011-04-07 | ||
| PCT/US2012/032568 WO2013106029A1 (en) | 2011-04-07 | 2012-04-06 | Taxane and abeo-taxane analogs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014512362A JP2014512362A (ja) | 2014-05-22 |
| JP2014512362A5 true JP2014512362A5 (OSRAM) | 2015-05-21 |
| JP5970536B2 JP5970536B2 (ja) | 2016-08-17 |
Family
ID=48781786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014504036A Expired - Fee Related JP5970536B2 (ja) | 2011-04-07 | 2012-04-06 | タキサンおよびアベオ−タキサン類似体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8912229B2 (OSRAM) |
| EP (1) | EP2694055A4 (OSRAM) |
| JP (1) | JP5970536B2 (OSRAM) |
| KR (1) | KR20140048113A (OSRAM) |
| CN (1) | CN103764138A (OSRAM) |
| AU (1) | AU2012364858A1 (OSRAM) |
| CA (1) | CA2832596A1 (OSRAM) |
| MX (1) | MX2013011694A (OSRAM) |
| SG (2) | SG10201602309VA (OSRAM) |
| WO (1) | WO2013106029A1 (OSRAM) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX337464B (es) | 2011-06-06 | 2016-03-07 | Arbor Therapeutics Llc | Profarmacos lipofilicos labiles al acido de los agentes quimioterapeuticos contra el cancer. |
| CN104650109B (zh) * | 2013-11-22 | 2019-01-01 | 江苏天士力帝益药业有限公司 | 紫杉烷类化合物 |
| KR20230129388A (ko) | 2020-11-19 | 2023-09-08 | 스펙시스 아게 | 암 치료를 위한 펩타이드 cxcr4 억제제 및 탁산을 포함하는 약제학적 조합물 |
| EP4000613A1 (en) | 2020-11-19 | 2022-05-25 | Polyphor Ag | Pharmaceutical combinations comprising a peptide cxcr4 inhibitor and a taxane for treating cancer |
| EP4223292A1 (en) | 2022-02-07 | 2023-08-09 | Cellestia Biotech AG | Pharmaceutical combinations for treating cancer |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5352806A (en) * | 1992-04-17 | 1994-10-04 | Abbott Laboratories | Taxol derivatives |
| PL1664033T3 (pl) * | 2003-09-25 | 2008-04-30 | Tapestry Pharmaceuticals Inc | Analogi 9,10-alfa, alfa-OH-taksanu i sposoby ich wytwarzania |
| WO2008121476A1 (en) * | 2007-03-28 | 2008-10-09 | Tapestry Pharmaceuticals, Inc. | Biologically active taxane analogs and methods of treatment by oral administration |
| WO2008109360A1 (en) * | 2007-02-28 | 2008-09-12 | Tapestry Pharmaceuticals, Inc | Taxane analogs for the treatment of brain cancer |
| US20080207743A1 (en) * | 2007-02-28 | 2008-08-28 | Rodger Lamb | Biologically Active Taxane Analogs and Methods of Treatment |
| WO2011028571A1 (en) * | 2009-09-01 | 2011-03-10 | Tapestry Pharmaceuticals, Inc. | Taxane analogues, their use, pharmaceutical compositions containing them, and processes for their preparation |
-
2012
- 2012-04-06 SG SG10201602309VA patent/SG10201602309VA/en unknown
- 2012-04-06 JP JP2014504036A patent/JP5970536B2/ja not_active Expired - Fee Related
- 2012-04-06 WO PCT/US2012/032568 patent/WO2013106029A1/en not_active Ceased
- 2012-04-06 AU AU2012364858A patent/AU2012364858A1/en not_active Abandoned
- 2012-04-06 CN CN201280027957.4A patent/CN103764138A/zh active Pending
- 2012-04-06 US US14/110,423 patent/US8912229B2/en not_active Expired - Fee Related
- 2012-04-06 MX MX2013011694A patent/MX2013011694A/es unknown
- 2012-04-06 CA CA2832596A patent/CA2832596A1/en not_active Abandoned
- 2012-04-06 SG SG2013074919A patent/SG194128A1/en unknown
- 2012-04-06 KR KR1020137029373A patent/KR20140048113A/ko not_active Withdrawn
- 2012-04-06 EP EP12864819.3A patent/EP2694055A4/en not_active Withdrawn
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