JP2005506366A5 - - Google Patents
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- Publication number
- JP2005506366A5 JP2005506366A5 JP2003537614A JP2003537614A JP2005506366A5 JP 2005506366 A5 JP2005506366 A5 JP 2005506366A5 JP 2003537614 A JP2003537614 A JP 2003537614A JP 2003537614 A JP2003537614 A JP 2003537614A JP 2005506366 A5 JP2005506366 A5 JP 2005506366A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- fluorine
- inhibitor
- methyl
- combination
- 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.)
- Pending
Links
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 25
- 229910052731 fluorine Inorganic materials 0.000 claims description 25
- 239000011737 fluorine Substances 0.000 claims description 25
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 19
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 15
- 229910052801 chlorine Inorganic materials 0.000 claims description 15
- 239000000460 chlorine Substances 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 102000029749 Microtubule Human genes 0.000 claims description 13
- 108091022875 Microtubule Proteins 0.000 claims description 13
- 210000004688 microtubule Anatomy 0.000 claims description 13
- 239000000556 agonist Substances 0.000 claims description 12
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 11
- 229940093444 Cyclooxygenase 2 inhibitor Drugs 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 229940111134 coxibs Drugs 0.000 claims description 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 241000124008 Mammalia Species 0.000 claims description 9
- 150000001875 compounds Chemical class 0.000 claims description 8
- 206010009944 Colon cancer Diseases 0.000 claims description 7
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims description 7
- 210000001072 colon Anatomy 0.000 claims description 7
- 208000029742 colonic neoplasm Diseases 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 150000002148 esters Chemical class 0.000 claims description 7
- 230000003902 lesion Effects 0.000 claims description 7
- -1 methoxy, ethoxy Chemical group 0.000 claims description 7
- 230000002265 prevention Effects 0.000 claims description 7
- 229940002612 prodrug Drugs 0.000 claims description 7
- 239000000651 prodrug Substances 0.000 claims description 7
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 7
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims description 7
- 239000002525 vasculotropin inhibitor Substances 0.000 claims description 7
- 108091008605 VEGF receptors Proteins 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 230000002062 proliferating effect Effects 0.000 claims description 6
- 229940124676 vascular endothelial growth factor receptor Drugs 0.000 claims description 6
- 102000001301 EGF receptor Human genes 0.000 claims description 5
- 108060006698 EGF receptor Proteins 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 5
- 229940121647 egfr inhibitor Drugs 0.000 claims description 5
- 150000002431 hydrogen Chemical class 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- 230000003211 malignant effect Effects 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 239000003112 inhibitor Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 11
- KHPKQFYUPIUARC-UHFFFAOYSA-N lumiracoxib Chemical compound OC(=O)CC1=CC(C)=CC=C1NC1=C(F)C=CC=C1Cl KHPKQFYUPIUARC-UHFFFAOYSA-N 0.000 claims 6
- 239000002552 dosage form Substances 0.000 claims 5
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims 4
- QXRSDHAAWVKZLJ-OXZHEXMSSA-N Epothilone B Natural products O=C1[C@H](C)[C@H](O)[C@@H](C)CCC[C@@]2(C)O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C QXRSDHAAWVKZLJ-OXZHEXMSSA-N 0.000 claims 3
- 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 3
- 229930012538 Paclitaxel Natural products 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 229960003668 docetaxel Drugs 0.000 claims 3
- HESCAJZNRMSMJG-HGYUPSKWSA-N epothilone A Natural products O=C1[C@H](C)[C@H](O)[C@H](C)CCC[C@H]2O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C HESCAJZNRMSMJG-HGYUPSKWSA-N 0.000 claims 3
- QXRSDHAAWVKZLJ-PVYNADRNSA-N epothilone B Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 QXRSDHAAWVKZLJ-PVYNADRNSA-N 0.000 claims 3
- 229960001592 paclitaxel Drugs 0.000 claims 3
- 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 3
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical group C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 claims 3
- AADVCYNFEREWOS-UHFFFAOYSA-N (+)-DDM Natural products C=CC=CC(C)C(OC(N)=O)C(C)C(O)C(C)CC(C)=CC(C)C(O)C(C)C=CC(O)CC1OC(=O)C(C)C(O)C1C AADVCYNFEREWOS-UHFFFAOYSA-N 0.000 claims 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 2
- 229940123237 Taxane Drugs 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 229940122803 Vinca alkaloid Drugs 0.000 claims 2
- 229960001338 colchicine Drugs 0.000 claims 2
- YJGVMLPVUAXIQN-UHFFFAOYSA-N epipodophyllotoxin Natural products COC1=C(OC)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YJGVMLPVUAXIQN-UHFFFAOYSA-N 0.000 claims 2
- 229930013356 epothilone Natural products 0.000 claims 2
- 150000003883 epothilone derivatives Chemical class 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- YJGVMLPVUAXIQN-XVVDYKMHSA-N podophyllotoxin Chemical compound COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-XVVDYKMHSA-N 0.000 claims 2
- 229960001237 podophyllotoxin Drugs 0.000 claims 2
- YVCVYCSAAZQOJI-UHFFFAOYSA-N podophyllotoxin Natural products COC1=C(O)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YVCVYCSAAZQOJI-UHFFFAOYSA-N 0.000 claims 2
- 239000003909 protein kinase inhibitor Substances 0.000 claims 2
- 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 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 229940122255 Microtubule inhibitor Drugs 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 102100038280 Prostaglandin G/H synthase 2 Human genes 0.000 claims 1
- 108050003267 Prostaglandin G/H synthase 2 Proteins 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer 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
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 231100000782 microtubule inhibitor Toxicity 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 102000009465 Growth Factor Receptors Human genes 0.000 description 3
- 108010009202 Growth Factor Receptors Proteins 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 2
- 230000008472 epithelial growth Effects 0.000 description 2
- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 description 1
- 102100031706 Fibroblast growth factor 1 Human genes 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34473501P | 2001-10-25 | 2001-10-25 | |
| US34473401P | 2001-10-25 | 2001-10-25 | |
| US33603301P | 2001-11-15 | 2001-11-15 | |
| PCT/EP2002/011924 WO2003035047A2 (en) | 2001-10-25 | 2002-10-24 | Combinations comprising a selective cyclooxygenase-2 inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005506366A JP2005506366A (ja) | 2005-03-03 |
| JP2005506366A5 true JP2005506366A5 (enExample) | 2006-01-05 |
Family
ID=27407094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003537614A Pending JP2005506366A (ja) | 2001-10-25 | 2002-10-24 | 選択的シクロオキシゲナーゼ−２阻害剤を含む組合せ剤 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US20050043409A1 (enExample) |
| EP (1) | EP1441714B1 (enExample) |
| JP (1) | JP2005506366A (enExample) |
| KR (1) | KR100954625B1 (enExample) |
| CN (1) | CN100506224C (enExample) |
| AT (1) | ATE381930T1 (enExample) |
| AU (2) | AU2006252156A1 (enExample) |
| BR (1) | BR0213486A (enExample) |
| CA (1) | CA2464309C (enExample) |
| CY (1) | CY1108045T1 (enExample) |
| DE (1) | DE60224299T2 (enExample) |
| DK (1) | DK1441714T3 (enExample) |
| ES (1) | ES2295428T3 (enExample) |
| HU (1) | HUP0600235A3 (enExample) |
| IL (1) | IL161462A0 (enExample) |
| MX (1) | MXPA04003878A (enExample) |
| NZ (2) | NZ532418A (enExample) |
| PL (1) | PL369305A1 (enExample) |
| PT (1) | PT1441714E (enExample) |
| RU (1) | RU2333754C2 (enExample) |
| SI (1) | SI1441714T1 (enExample) |
| WO (1) | WO2003035047A2 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0223341D0 (en) * | 2002-10-08 | 2002-11-13 | Groningen Acad Ziekenhuis | Organic compounds |
| WO2005021554A1 (en) | 2003-08-29 | 2005-03-10 | Pfizer Inc. | Thienopyridine-phenylacet amides and their derivatives useful as new anti-angiogenic agents |
| MXPA06003164A (es) * | 2003-09-23 | 2006-06-05 | Novartis Ag | Combinaciones de un inhibidor del receptor de vegf con otros agentes terapeuticos. |
| JP2007505938A (ja) * | 2003-09-23 | 2007-03-15 | ノバルティス アクチエンゲゼルシャフト | Ｖｅｇｆ受容体阻害剤と化学療法剤の組み合わせ |
| CA2551508C (en) | 2003-12-23 | 2011-08-09 | Pfizer Inc. | Novel quinoline derivatives |
| JO2596B1 (en) * | 2004-11-30 | 2011-02-27 | نوفارتيس ايه جي | Compositions include epothelones and tyrosine protein kinase inhibitors and their pharmaceutical uses |
| EP1982718A4 (en) * | 2006-02-09 | 2010-05-12 | Daiichi Sankyo Co Ltd | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OF CANCER |
| EP2065054A1 (en) | 2007-11-29 | 2009-06-03 | Bayer Schering Pharma Aktiengesellschaft | Combinations comprising a prostaglandin and uses thereof |
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| CN103917236A (zh) | 2011-11-11 | 2014-07-09 | 诺华股份有限公司 | 治疗增生性疾病的方法 |
| MD565Z (ro) * | 2012-05-23 | 2013-07-31 | Институт Генетики, Физиологии И Защиты Растений Академии Наук Молдовы | Procedeu de tratare a seminţelor de sfeclă de zahăr |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100558356C (zh) * | 1996-10-15 | 2009-11-11 | G.D.瑟尔公司 | 应用环加氧酶-2抑制剂治疗和预防肿瘤形成的方法 |
| US6380394B1 (en) * | 1996-12-13 | 2002-04-30 | The Scripps Research Institute | Epothilone analogs |
| CO4950519A1 (es) * | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| US6034256A (en) * | 1997-04-21 | 2000-03-07 | G.D. Searle & Co. | Substituted benzopyran derivatives for the treatment of inflammation |
| CO4960662A1 (es) * | 1997-08-28 | 2000-09-25 | Novartis Ag | Ciertos acidos 5-alquil-2-arilaminofenilaceticos y sus derivados |
| US6025353A (en) * | 1997-11-19 | 2000-02-15 | G.D. Searle & Co. | Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents |
| US6887893B1 (en) * | 1997-12-24 | 2005-05-03 | Sankyo Company, Limited | Methods and compositions for treatment and prevention of tumors, tumor-related disorders and cachexia |
| CA2356462A1 (en) * | 1998-12-23 | 2000-07-06 | G.D. Searle & Co. | Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia |
| IL147913A0 (en) * | 1999-08-12 | 2002-08-14 | American Cyanamid Co | Nsaid and efgr kinase inhibitor containing composition for the treatment or inhibition of colonic polyps and colorectal cancer |
| CA2392931A1 (en) * | 1999-12-03 | 2001-06-07 | Pfizer Products Inc. | Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents |
| ITMI992711A1 (it) * | 1999-12-27 | 2001-06-27 | Novartis Ag | Composti organici |
| WO2001060365A1 (en) * | 2000-02-17 | 2001-08-23 | Merck & Co., Inc. | Treatment or prevention of prostate cancer with a cox-2 selective inhibiting drug |
| EP1259236A4 (en) * | 2000-02-25 | 2004-11-03 | Merck & Co Inc | Tyrosine kinase inhibitors |
| WO2001064669A1 (en) * | 2000-03-03 | 2001-09-07 | Pfizer Products Inc. | Pyrazole ether derivatives as anti-inflammatory/analgesic agents |
| TWI310684B (en) * | 2000-03-27 | 2009-06-11 | Bristol Myers Squibb Co | Synergistic pharmaceutical kits for treating cancer |
-
2002
- 2002-10-24 DE DE60224299T patent/DE60224299T2/de not_active Expired - Lifetime
- 2002-10-24 JP JP2003537614A patent/JP2005506366A/ja active Pending
- 2002-10-24 AT AT02787507T patent/ATE381930T1/de active
- 2002-10-24 EP EP02787507A patent/EP1441714B1/en not_active Expired - Lifetime
- 2002-10-24 PT PT02787507T patent/PT1441714E/pt unknown
- 2002-10-24 RU RU2004116069/15A patent/RU2333754C2/ru not_active IP Right Cessation
- 2002-10-24 KR KR1020047006101A patent/KR100954625B1/ko not_active Expired - Fee Related
- 2002-10-24 CA CA2464309A patent/CA2464309C/en not_active Expired - Fee Related
- 2002-10-24 NZ NZ532418A patent/NZ532418A/en not_active IP Right Cessation
- 2002-10-24 SI SI200230672T patent/SI1441714T1/sl unknown
- 2002-10-24 ES ES02787507T patent/ES2295428T3/es not_active Expired - Lifetime
- 2002-10-24 CN CNB028211375A patent/CN100506224C/zh not_active Expired - Fee Related
- 2002-10-24 HU HU0600235A patent/HUP0600235A3/hu unknown
- 2002-10-24 IL IL16146202A patent/IL161462A0/xx unknown
- 2002-10-24 NZ NZ552335A patent/NZ552335A/en not_active IP Right Cessation
- 2002-10-24 BR BR0213486-1A patent/BR0213486A/pt active Search and Examination
- 2002-10-24 PL PL02369305A patent/PL369305A1/xx not_active Application Discontinuation
- 2002-10-24 MX MXPA04003878A patent/MXPA04003878A/es active IP Right Grant
- 2002-10-24 WO PCT/EP2002/011924 patent/WO2003035047A2/en not_active Ceased
- 2002-10-24 DK DK02787507T patent/DK1441714T3/da active
- 2002-10-24 US US10/493,297 patent/US20050043409A1/en not_active Abandoned
-
2006
- 2006-12-20 AU AU2006252156A patent/AU2006252156A1/en not_active Abandoned
-
2008
- 2008-02-18 CY CY20081100197T patent/CY1108045T1/el unknown
-
2010
- 2010-02-08 AU AU2010200433A patent/AU2010200433A1/en not_active Abandoned
- 2010-11-03 US US12/938,868 patent/US20110046190A1/en not_active Abandoned
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