JP2007501774A5 - - Google Patents
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- Publication number
- JP2007501774A5 JP2007501774A5 JP2006522329A JP2006522329A JP2007501774A5 JP 2007501774 A5 JP2007501774 A5 JP 2007501774A5 JP 2006522329 A JP2006522329 A JP 2006522329A JP 2006522329 A JP2006522329 A JP 2006522329A JP 2007501774 A5 JP2007501774 A5 JP 2007501774A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- methyl
- amino
- heteroaryl
- 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
- -1 hydroxy, amino Chemical group 0.000 claims description 21
- 125000001072 heteroaryl group Chemical group 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 15
- 150000001875 compounds Chemical class 0.000 claims description 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- ZLUZDKXBTNQWOL-MDZDMXLPSA-N (e)-n-hydroxy-3-[4-[[2-(1h-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide Chemical compound C1=CC(/C=C/C(=O)NO)=CC=C1CNCCC1=CNC2=CC=CC=C12 ZLUZDKXBTNQWOL-MDZDMXLPSA-N 0.000 claims description 4
- BWDQBBCUWLSASG-MDZDMXLPSA-N (e)-n-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1h-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide Chemical group C=1NC2=CC=CC=C2C=1CCN(CCO)CC1=CC=C(\C=C\C(=O)NO)C=C1 BWDQBBCUWLSASG-MDZDMXLPSA-N 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- FPOHNWQLNRZRFC-ZHACJKMWSA-N panobinostat Chemical compound CC=1NC2=CC=CC=C2C=1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FPOHNWQLNRZRFC-ZHACJKMWSA-N 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 12
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 12
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000002252 acyl group Chemical group 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 6
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 6
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical group C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 3
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 2
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004532 benzofuran-3-yl group Chemical group O1C=C(C2=C1C=CC=C2)* 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000003367 polycyclic group Chemical group 0.000 claims 1
- 125000004585 polycyclic heterocycle group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004548 quinolin-3-yl group Chemical group N1=CC(=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 description 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 description 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 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49382803P | 2003-08-08 | 2003-08-08 | |
| PCT/EP2004/008848 WO2005014004A1 (en) | 2003-08-08 | 2004-08-06 | Combinations comprising staurosporines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007501774A JP2007501774A (ja) | 2007-02-01 |
| JP2007501774A5 true JP2007501774A5 (https=) | 2007-11-01 |
Family
ID=34135288
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006522329A Pending JP2007501774A (ja) | 2003-08-08 | 2004-08-06 | スタウロスポリンを含む組み合わせ |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20070191338A1 (https=) |
| EP (2) | EP1653973A1 (https=) |
| JP (1) | JP2007501774A (https=) |
| CN (1) | CN100536850C (https=) |
| AU (1) | AU2004262927B2 (https=) |
| BR (1) | BRPI0413439A (https=) |
| CA (1) | CA2533861A1 (https=) |
| MX (1) | MXPA06001524A (https=) |
| WO (1) | WO2005014004A1 (https=) |
Families Citing this family (14)
| 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 |
| GB0419159D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| 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 |
| KR20080046161A (ko) * | 2005-08-09 | 2008-05-26 | 요하네스 구텐베르크-유니버시타트 마인츠 | 비-소세포 폐암의 치료를 위한 스타우로스포린 유도체 |
| WO2007030455A2 (en) * | 2005-09-07 | 2007-03-15 | Novartis Ag | Mutations and polymorphisms of hdac10 |
| GB0522932D0 (en) * | 2005-11-10 | 2005-12-21 | Univ Southampton | PKC412 in treatment of atypical chronic myeloid leukemia |
| GB0612542D0 (en) * | 2006-06-23 | 2006-08-02 | Novartis Ag | Combinations comprising staurosporines |
| GEP20125708B (en) | 2008-03-26 | 2012-12-10 | Novartis Ag | Hydroxamate-based inhibitors of deacetylases b |
| US20110053925A1 (en) * | 2009-08-28 | 2011-03-03 | Novartis Ag | Hydroxamate-Based Inhibitors of Deacetylases |
| CN102101866A (zh) * | 2010-11-04 | 2011-06-22 | 中国海洋大学 | 十字孢碱卤代衍生物及其制备方法和应用 |
| WO2014009609A1 (en) | 2012-07-13 | 2014-01-16 | Turun Yliopisto | Combination therapy iii |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62220196A (ja) | 1986-03-20 | 1987-09-28 | Kyowa Hakko Kogyo Co Ltd | 新規物質ｕｃｎ―０１ |
| IL86632A0 (en) | 1987-06-15 | 1988-11-30 | Ciba Geigy Ag | Derivatives substituted at methyl-amino nitrogen |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| GB8803048D0 (en) | 1988-02-10 | 1988-03-09 | Hoffmann La Roche | Substituted pyrroles |
| NZ227850A (en) | 1988-02-10 | 1991-11-26 | Hoffmann La Roche | Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders |
| MC2096A1 (fr) | 1989-02-23 | 1991-02-15 | Hoffmann La Roche | Pyrroles substitues |
| CA2046801C (en) | 1990-08-07 | 2002-02-26 | Peter D. Davis | Substituted pyrroles |
| WO1993007153A1 (en) | 1991-10-10 | 1993-04-15 | Schering Corporation | 4'-(n-substituted-n-oxide)staurosporine derivatives |
| US5344926A (en) | 1992-06-22 | 1994-09-06 | Kyowa Hakko Kogyo Co., Ltd. | Process for producing staurosporine derivatives |
| US5461146A (en) | 1992-07-24 | 1995-10-24 | Cephalon, Inc. | Selected protein kinase inhibitors for the treatment of neurological disorders |
| PH30300A (en) | 1993-05-07 | 1997-01-20 | Ciba Geigy Ag | Polycyclic compounds and processes for the preparation thereof |
| AU678435B2 (en) | 1993-05-10 | 1997-05-29 | F. Hoffmann-La Roche Ag | Substituted pyrroles |
| PT657458E (pt) | 1993-12-07 | 2002-02-28 | Lilly Co Eli | Inibidores de proteina cinase c |
| GB9325395D0 (en) | 1993-12-11 | 1994-02-16 | Ciba Geigy Ag | Compositions |
| AU2565795A (en) | 1994-06-01 | 1995-12-21 | Ciba-Geigy Ag | Carbazole derivatives as agents against multi-drug resistance |
| EP0763042A1 (en) | 1994-06-01 | 1997-03-19 | Novartis AG | Polycyclic lactam derivatives for sensitizing multidrug-resistant cells to antitumour agents |
| EP0711557A1 (de) | 1994-11-09 | 1996-05-15 | Ciba-Geigy Ag | Pharmazeutische Formulierungsgrundlage |
| EP0733372A3 (de) | 1995-03-21 | 1998-05-20 | Ciba-Geigy Ag | Pharmazeutische Formulierungsgrundlage für Nanosuspensionen |
| NL1003692C2 (nl) | 1996-07-26 | 1998-01-28 | Stork Protecon Langen Bv | Inrichting voor het afscheiden van vleesmassa van van vleesresten voorziene botten. |
| CO4940430A1 (es) | 1997-07-07 | 2000-07-24 | Novartis Ag | Compuestos policiclicos que contienen estaurosporina hidrogenada con propiedades farmacologicas convenientes y un efecto inhibidor sobre el crecimiento de las celulas tumorales |
| DE19744676A1 (de) * | 1997-10-10 | 1999-04-15 | Forschungszentrum Borstel Zent | Kombinationspräparate für die Therapie von Tumoren |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| TWI238824B (en) * | 2001-05-14 | 2005-09-01 | Novartis Ag | 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives |
| DE60213842T2 (de) * | 2001-10-30 | 2007-09-06 | Novartis Ag | Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung |
| US20040152632A1 (en) * | 2002-11-06 | 2004-08-05 | Wyeth | Combination therapy for the treatment of acute leukemia and myelodysplastic syndrome |
| BRPI0409227C1 (pt) * | 2003-04-07 | 2021-05-25 | Axys Pharm Inc | composto, composição farmacêutica, uso de um composto e processo para a preparação de um composto de fórmula (i) |
| MXPA05012464A (es) * | 2003-05-21 | 2006-01-30 | Novartis Ag | Combinacion de inhibidores de deacetilasa de histona con agentes quimioterapeuticos. |
-
2004
- 2004-08-06 EP EP04763879A patent/EP1653973A1/en not_active Withdrawn
- 2004-08-06 US US10/567,897 patent/US20070191338A1/en not_active Abandoned
- 2004-08-06 WO PCT/EP2004/008848 patent/WO2005014004A1/en not_active Ceased
- 2004-08-06 CN CNB2004800227221A patent/CN100536850C/zh not_active Expired - Fee Related
- 2004-08-06 CA CA002533861A patent/CA2533861A1/en not_active Abandoned
- 2004-08-06 EP EP10175357A patent/EP2305265A1/en not_active Withdrawn
- 2004-08-06 JP JP2006522329A patent/JP2007501774A/ja active Pending
- 2004-08-06 AU AU2004262927A patent/AU2004262927B2/en not_active Ceased
- 2004-08-06 BR BRPI0413439-7A patent/BRPI0413439A/pt not_active IP Right Cessation
- 2004-08-06 MX MXPA06001524A patent/MXPA06001524A/es not_active Application Discontinuation
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