JP2004527493A5 - - Google Patents
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- Publication number
- JP2004527493A5 JP2004527493A5 JP2002567308A JP2002567308A JP2004527493A5 JP 2004527493 A5 JP2004527493 A5 JP 2004527493A5 JP 2002567308 A JP2002567308 A JP 2002567308A JP 2002567308 A JP2002567308 A JP 2002567308A JP 2004527493 A5 JP2004527493 A5 JP 2004527493A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- formula
- lower alkyl
- pharmaceutically acceptable
- combination according
- 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
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- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 17
- 239000004480 active ingredient Substances 0.000 claims 9
- -1 4-pyrazinyl Chemical group 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 108010055723 PDGF receptor tyrosine kinase Proteins 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 150000003883 epothilone derivatives Chemical class 0.000 claims 6
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 230000002062 proliferating effect Effects 0.000 claims 5
- 150000001721 carbon Chemical group 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 230000007423 decrease Effects 0.000 claims 3
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 claims 3
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 150000004046 2-(N-anilino)pyrimidines Chemical class 0.000 claims 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- XRYJULCDUUATMC-CYBMUJFWSA-N 4-[4-[[(1r)-1-phenylethyl]amino]-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenol Chemical compound N([C@H](C)C=1C=CC=CC=1)C(C=1C=2)=NC=NC=1NC=2C1=CC=C(O)C=C1 XRYJULCDUUATMC-CYBMUJFWSA-N 0.000 claims 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 claims 1
- 101800003838 Epidermal growth factor Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 claims 1
- 125000005277 alkyl imino group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 229940116977 epidermal growth factor Drugs 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical class 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical class 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0104840.4A GB0104840D0 (en) | 2001-02-27 | 2001-02-27 | Use of organic compounds |
| US33904001P | 2001-10-30 | 2001-10-30 | |
| PCT/EP2002/002049 WO2002067941A2 (en) | 2001-02-27 | 2002-02-26 | Combination comprising a signal transduction inhibitor and an epothilone derivative |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004527493A JP2004527493A (ja) | 2004-09-09 |
| JP2004527493A5 true JP2004527493A5 (https=) | 2005-12-22 |
| JP4499359B2 JP4499359B2 (ja) | 2010-07-07 |
Family
ID=26245767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002567308A Expired - Fee Related JP4499359B2 (ja) | 2001-02-27 | 2002-02-26 | シグナル変換阻害剤とエポチロン誘導体とを含有してなる組合せ剤 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US7723339B2 (https=) |
| EP (1) | EP1385522B1 (https=) |
| JP (1) | JP4499359B2 (https=) |
| KR (1) | KR100848197B1 (https=) |
| CN (1) | CN1511036B (https=) |
| AT (1) | ATE434438T1 (https=) |
| AU (1) | AU2002308218B2 (https=) |
| BR (1) | BR0207649A (https=) |
| CA (1) | CA2439268C (https=) |
| CY (1) | CY1109347T1 (https=) |
| DE (1) | DE60232719D1 (https=) |
| DK (1) | DK1385522T3 (https=) |
| ES (1) | ES2326264T3 (https=) |
| IL (2) | IL157466A0 (https=) |
| MX (1) | MXPA03007729A (https=) |
| NO (1) | NO325416B1 (https=) |
| NZ (1) | NZ527764A (https=) |
| PL (1) | PL207197B1 (https=) |
| PT (1) | PT1385522E (https=) |
| RU (1) | RU2313345C2 (https=) |
| SK (1) | SK287489B6 (https=) |
| WO (1) | WO2002067941A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| CA2273083C (en) | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| 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 |
| CA2444867C (en) * | 2001-05-16 | 2010-08-17 | Novartis Ag | Combination comprising n-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent |
| EP1704863A3 (en) * | 2001-05-16 | 2010-11-24 | Novartis AG | Combination comprising N-5-4-(4-Methyl-Piperazino-Methyl-)Benzoyla Mido]-2-Methylphenyl -4-(3-Pyridyl)-2Phyrimidine-amine and a chemotherapeutic agent |
| EP1441736A2 (en) * | 2001-10-29 | 2004-08-04 | Novartis AG | Use of 7h-pyrrolo[2,3-d]pyrimidine derivatives in the treatment of solid tumor diseases |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| EP2186811A1 (en) | 2002-08-23 | 2010-05-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US20050171167A1 (en) * | 2003-11-04 | 2005-08-04 | Haby Thomas A. | Process and formulation containing epothilones and analogs thereof |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| JO2596B1 (en) * | 2004-11-30 | 2011-02-27 | نوفارتيس ايه جي | Compositions include epothelones and tyrosine protein kinase inhibitors and their pharmaceutical uses |
| US7754850B2 (en) | 2005-02-11 | 2010-07-13 | University Of Southern California | Chimeric disintegrin domain |
| EP2029156A4 (en) * | 2006-05-01 | 2010-07-21 | Univ Southern California | COMBINATION THERAPY FOR CANCER TREATMENT |
| US8802394B2 (en) | 2008-11-13 | 2014-08-12 | Radu O. Minea | Method of expressing proteins with disulfide bridges with enhanced yields and activity |
| WO2010108503A1 (en) | 2009-03-24 | 2010-09-30 | Life & Brain Gmbh | Promotion of neuronal integration in neural stem cell grafts |
| US20110300150A1 (en) | 2010-05-18 | 2011-12-08 | Scott Eliasof | Compositions and methods for treatment of autoimmune and other disease |
Family Cites Families (11)
| 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 |
| DE4138042C2 (de) | 1991-11-19 | 1993-10-14 | Biotechnolog Forschung Gmbh | Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel |
| TW225528B (https=) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| US5654307A (en) * | 1994-01-25 | 1997-08-05 | Warner-Lambert Company | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| SI9620103A (sl) * | 1995-07-06 | 1998-10-31 | Novartis Ag | Pirolopirimidini in postopki za njihovo pripravo |
| ES2312695T3 (es) | 1996-11-18 | 2009-03-01 | Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) | Epotilones e y f. |
| CO4940418A1 (es) * | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| US6302838B1 (en) * | 1998-02-25 | 2001-10-16 | Novartis Ag | Cancer treatment with epothilones |
| 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 |
-
2002
- 2002-02-26 RU RU2003127392/15A patent/RU2313345C2/ru not_active IP Right Cessation
- 2002-02-26 EP EP02744903A patent/EP1385522B1/en not_active Expired - Lifetime
- 2002-02-26 AT AT02744903T patent/ATE434438T1/de active
- 2002-02-26 PL PL363288A patent/PL207197B1/pl not_active IP Right Cessation
- 2002-02-26 NZ NZ527764A patent/NZ527764A/en not_active IP Right Cessation
- 2002-02-26 KR KR1020037011205A patent/KR100848197B1/ko not_active Expired - Fee Related
- 2002-02-26 SK SK1071-2003A patent/SK287489B6/sk not_active IP Right Cessation
- 2002-02-26 US US10/469,367 patent/US7723339B2/en not_active Expired - Fee Related
- 2002-02-26 AU AU2002308218A patent/AU2002308218B2/en not_active Ceased
- 2002-02-26 WO PCT/EP2002/002049 patent/WO2002067941A2/en not_active Ceased
- 2002-02-26 ES ES02744903T patent/ES2326264T3/es not_active Expired - Lifetime
- 2002-02-26 DE DE60232719T patent/DE60232719D1/de not_active Expired - Lifetime
- 2002-02-26 CA CA002439268A patent/CA2439268C/en not_active Expired - Fee Related
- 2002-02-26 BR BR0207649-7A patent/BR0207649A/pt not_active Application Discontinuation
- 2002-02-26 JP JP2002567308A patent/JP4499359B2/ja not_active Expired - Fee Related
- 2002-02-26 IL IL15746602A patent/IL157466A0/xx unknown
- 2002-02-26 MX MXPA03007729A patent/MXPA03007729A/es active IP Right Grant
- 2002-02-26 DK DK02744903T patent/DK1385522T3/da active
- 2002-02-26 CN CN028056086A patent/CN1511036B/zh not_active Expired - Fee Related
- 2002-02-26 PT PT02744903T patent/PT1385522E/pt unknown
-
2003
- 2003-08-18 IL IL157466A patent/IL157466A/en not_active IP Right Cessation
- 2003-08-25 NO NO20033769A patent/NO325416B1/no not_active IP Right Cessation
-
2009
- 2009-08-28 CY CY20091100900T patent/CY1109347T1/el unknown
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