JP2005535608A5 - - Google Patents
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- JP2005535608A5 JP2005535608A5 JP2004510831A JP2004510831A JP2005535608A5 JP 2005535608 A5 JP2005535608 A5 JP 2005535608A5 JP 2004510831 A JP2004510831 A JP 2004510831A JP 2004510831 A JP2004510831 A JP 2004510831A JP 2005535608 A5 JP2005535608 A5 JP 2005535608A5
- Authority
- JP
- Japan
- Prior art keywords
- combination
- administration
- epothilone
- effect
- active ingredient
- 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
- 239000004480 active ingredient Substances 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 230000003902 lesion Effects 0.000 description 5
- 150000003883 epothilone derivatives Chemical class 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 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 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 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 description 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 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 208000037821 progressive disease Diseases 0.000 description 3
- 230000002195 synergetic effect Effects 0.000 description 3
- 206010012735 Diarrhoea Diseases 0.000 description 2
- 230000001142 anti-diarrhea Effects 0.000 description 2
- 229940125714 antidiarrheal agent Drugs 0.000 description 2
- 239000003793 antidiarrheal agent Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 150000003951 lactams Chemical class 0.000 description 2
- RDOIQAHITMMDAJ-UHFFFAOYSA-N loperamide Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 RDOIQAHITMMDAJ-UHFFFAOYSA-N 0.000 description 2
- 229960001571 loperamide Drugs 0.000 description 2
- 229940005483 opioid analgesics Drugs 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 description 1
- LVRVABPNVHYXRT-BQWXUCBYSA-N 52906-92-0 Chemical compound C([C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(O)=O)C(C)C)C1=CC=CC=C1 LVRVABPNVHYXRT-BQWXUCBYSA-N 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 102000002419 Motilin Human genes 0.000 description 1
- 101800002372 Motilin Proteins 0.000 description 1
- 108010016076 Octreotide Proteins 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 208000037844 advanced solid tumor Diseases 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000003908 antipruritic agent Substances 0.000 description 1
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 description 1
- 229940093265 berberine Drugs 0.000 description 1
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- ZREIPSZUJIFJNP-UHFFFAOYSA-K bismuth subsalicylate Chemical compound C1=CC=C2O[Bi](O)OC(=O)C2=C1 ZREIPSZUJIFJNP-UHFFFAOYSA-K 0.000 description 1
- 229960000782 bismuth subsalicylate Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 229960004126 codeine Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- UFIVBRCCIRTJTN-UHFFFAOYSA-N difenoxin Chemical compound C1CC(C(=O)O)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 UFIVBRCCIRTJTN-UHFFFAOYSA-N 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 229960004192 diphenoxylate Drugs 0.000 description 1
- HYPPXZBJBPSRLK-UHFFFAOYSA-N diphenoxylate Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 HYPPXZBJBPSRLK-UHFFFAOYSA-N 0.000 description 1
- 230000008034 disappearance Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229930013356 epothilone Natural products 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 239000000472 muscarinic agonist Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 229960002700 octreotide Drugs 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 229940127240 opiate Drugs 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 229940069533 paregoric Drugs 0.000 description 1
- 239000008414 paregoric Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000001814 pectin Substances 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 238000006722 reduction reaction Methods 0.000 description 1
- 238000005932 reductive alkylation reaction Methods 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38702502P | 2002-06-10 | 2002-06-10 | |
| US40623902P | 2002-08-27 | 2002-08-27 | |
| US40623802P | 2002-08-27 | 2002-08-27 | |
| US43867703P | 2003-01-08 | 2003-01-08 | |
| US43867603P | 2003-01-08 | 2003-01-08 | |
| PCT/EP2003/005988 WO2003103712A1 (en) | 2002-06-01 | 2003-06-06 | Combinations comprising epothilones and pharmaceutical uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005535608A JP2005535608A (ja) | 2005-11-24 |
| JP2005535608A5 true JP2005535608A5 (https=) | 2006-07-20 |
Family
ID=29741146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004510831A Pending JP2005535608A (ja) | 2002-06-10 | 2003-06-06 | エポシロンを含む組み合わせおよびその薬学的使用 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20050271669A1 (https=) |
| EP (2) | EP1515750B1 (https=) |
| JP (1) | JP2005535608A (https=) |
| CN (2) | CN101816792A (https=) |
| AT (1) | ATE476995T1 (https=) |
| AU (1) | AU2003242646A1 (https=) |
| BR (1) | BR0311714A (https=) |
| CA (1) | CA2487147A1 (https=) |
| DE (1) | DE60333754D1 (https=) |
| IL (1) | IL165180A0 (https=) |
| MX (1) | MXPA04012444A (https=) |
| NO (1) | NO20050096L (https=) |
| PL (1) | PL372070A1 (https=) |
| SG (1) | SG162616A1 (https=) |
| WO (1) | WO2003103712A1 (https=) |
| ZA (1) | ZA200409137B (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7381825B2 (en) | 2003-03-17 | 2008-06-03 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| JO2596B1 (en) * | 2004-11-30 | 2011-02-27 | نوفارتيس ايه جي | Compositions include epothelones and tyrosine protein kinase inhibitors and their pharmaceutical uses |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| EP1824831A2 (en) | 2004-12-16 | 2007-08-29 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| EP1896436A2 (en) | 2005-05-11 | 2008-03-12 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| EA200800321A1 (ru) | 2005-07-14 | 2008-06-30 | Такеда Сан Диего, Инк. | Ингибиторы гистондеацетилазы |
| CN101677977A (zh) * | 2006-11-10 | 2010-03-24 | 欣达克斯制药公司 | 用于治疗癌症的ERα+配体和组蛋白脱乙酰化酶抑制剂组合 |
| WO2009015203A1 (en) * | 2007-07-23 | 2009-01-29 | Syndax Pharmaceuticals, Inc. | Novel compounds and methods of using them |
| US20100267779A1 (en) * | 2007-07-23 | 2010-10-21 | Syndax Pharmaceuticals, Inc. | Novel Compounds and Methods of Using Them |
| US20090149511A1 (en) * | 2007-10-30 | 2009-06-11 | Syndax Pharmaceuticals, Inc. | Administration of an Inhibitor of HDAC and an mTOR Inhibitor |
| US20090131367A1 (en) * | 2007-11-19 | 2009-05-21 | The Regents Of The University Of Colorado | Combinations of HDAC Inhibitors and Proteasome Inhibitors |
| CA2725390C (en) * | 2008-04-08 | 2014-09-23 | Syndax Pharmaceuticals, Inc. | Use of a hdac inhibitor and a her-2 inhibitor in the treatment of breast cancer |
| US20110300150A1 (en) | 2010-05-18 | 2011-12-08 | Scott Eliasof | Compositions and methods for treatment of autoimmune and other disease |
| WO2018081556A1 (en) * | 2016-10-28 | 2018-05-03 | Acetylon Pharmaceuticals, Inc. | Pharmaceutical combinations comprising a histone deacetylase inhibitor and epothilone and methods of use thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3040121B2 (ja) * | 1988-01-12 | 2000-05-08 | ジェネンテク，インコーポレイテッド | 増殖因子レセプターの機能を阻害することにより腫瘍細胞を処置する方法 |
| US5516775A (en) * | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| CA2273083C (en) * | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| TR200002299T2 (tr) * | 1998-02-05 | 2000-11-21 | Novartis Ag | Epotilon kompozisyonları. |
| CA2322157C (en) * | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2000000485A1 (de) * | 1998-06-30 | 2000-01-06 | Schering Aktiengesellschaft | Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung |
| HK1044946A1 (zh) * | 1999-02-11 | 2002-11-08 | 舍林股份公司 | 依泊昔酮衍生物、其製備方法及藥物用途 |
| DE19908760A1 (de) * | 1999-02-18 | 2000-08-24 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
| US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
| JP2004500388A (ja) * | 2000-03-01 | 2004-01-08 | スローン−ケッタリング インスティトュート フォア キャンサー リサーチ | エポチロン、その中間体およびその類似体の合成 |
| TWI310684B (en) * | 2000-03-27 | 2009-06-11 | Bristol Myers Squibb Co | Synergistic pharmaceutical kits for treating cancer |
| DE10020517A1 (de) * | 2000-04-19 | 2001-10-25 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
| DE10020899A1 (de) * | 2000-04-20 | 2001-10-25 | Schering Ag | 9-Oxa-Epothilon-Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten |
| PE20020354A1 (es) * | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| IL157443A0 (en) * | 2001-03-14 | 2004-03-28 | Bristol Myers Squibb Co | Pharmaceutical compositions for the treatment of cancer including an epothilone analog and a chemotherapeutic agent |
-
2003
- 2003-06-06 CN CN201010166742A patent/CN101816792A/zh active Pending
- 2003-06-06 MX MXPA04012444A patent/MXPA04012444A/es active IP Right Grant
- 2003-06-06 SG SG200608597-1A patent/SG162616A1/en unknown
- 2003-06-06 WO PCT/EP2003/005988 patent/WO2003103712A1/en not_active Ceased
- 2003-06-06 DE DE60333754T patent/DE60333754D1/de not_active Expired - Lifetime
- 2003-06-06 US US10/517,074 patent/US20050271669A1/en not_active Abandoned
- 2003-06-06 JP JP2004510831A patent/JP2005535608A/ja active Pending
- 2003-06-06 CN CN038134489A patent/CN1658904A/zh active Pending
- 2003-06-06 EP EP03757040A patent/EP1515750B1/en not_active Expired - Lifetime
- 2003-06-06 AU AU2003242646A patent/AU2003242646A1/en not_active Abandoned
- 2003-06-06 CA CA002487147A patent/CA2487147A1/en not_active Abandoned
- 2003-06-06 PL PL03372070A patent/PL372070A1/xx not_active Application Discontinuation
- 2003-06-06 BR BR0311714-6A patent/BR0311714A/pt not_active IP Right Cessation
- 2003-06-06 EP EP20090178302 patent/EP2179745A1/en not_active Withdrawn
- 2003-06-06 AT AT03757040T patent/ATE476995T1/de not_active IP Right Cessation
-
2004
- 2004-11-11 ZA ZA2004/09137A patent/ZA200409137B/en unknown
- 2004-11-11 IL IL16518004A patent/IL165180A0/xx unknown
-
2005
- 2005-01-07 NO NO20050096A patent/NO20050096L/no unknown
-
2010
- 2010-10-20 US US12/908,533 patent/US20110033458A1/en not_active Abandoned
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