JP2011508779A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011508779A5 JP2011508779A5 JP2010541518A JP2010541518A JP2011508779A5 JP 2011508779 A5 JP2011508779 A5 JP 2011508779A5 JP 2010541518 A JP2010541518 A JP 2010541518A JP 2010541518 A JP2010541518 A JP 2010541518A JP 2011508779 A5 JP2011508779 A5 JP 2011508779A5
- Authority
- JP
- Japan
- Prior art keywords
- epimer
- compound
- halo
- alkyl
- hydroxy
- 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
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- NIECBBCGLQEPKI-CPTJDMOESA-N 2',3'-Dichlorodihydroenglerin A Chemical compound O([C@H]1[C@@H]2[C@H](C)CC[C@H]2[C@@]2(C)[C@H](OC(=O)CO)C[C@@]1(O2)C(C)C)C(=O)C(Cl)C(Cl)C1=CC=CC=C1 NIECBBCGLQEPKI-CPTJDMOESA-N 0.000 claims 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- GACOFEKSDCOVMV-RRYXBOBMSA-N englerin A Chemical compound O([C@H]1[C@@H]2[C@H](C)CC[C@H]2[C@@]2(C)[C@H](OC(=O)CO)C[C@@]1(O2)C(C)C)C(=O)\C=C\C1=CC=CC=C1 GACOFEKSDCOVMV-RRYXBOBMSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- -1 isopropylidenyl Chemical group 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
Claims (10)
- 式(I):
Arは、C1−C6アルキル、C1−C6ヒドロキシアルキル、C1−C6アルコキシ、ハロ、またはニトロで任意に置換されている、アリール基であり;
Xは、O、NH、またはSであり;
R2およびR3は、独立にC1−C6アルキルであり;
R1は、イソプロピルまたはイソプロピリデニルであり;
「a」は、単結合または二重結合であり;
「a」が二重結合である場合、R4は、水素であり、およびR5は、ハロまたはHであり;
「a」が単結合である場合、R4は、ハロ、ヒドロキシ、またはC1−C6アルコキシからなる群から選ばれ、およびR5は、ハロまたはHであり;
およびR6は、C1−C6アルキルまたはヒドロキシC1−C6アルキルである。]
の化合物またはそのエピマー。 - R6が、ヒドロキシC1−C6アルキルである請求項2に記載の化合物またはエピマー。
- R5が、ハロである請求項2〜4のいずれか一項に記載の化合物またはエピマー。
- Xが、Oである請求項2〜5のいずれか一項に記載の化合物またはエピマー。
- R1が、イソプロピルである請求項2〜6のいずれか一項に記載の化合物またはエピマー。
- 薬学的に許容し得る担体および請求項1〜8のいずれか一項に記載の化合物またはエピマーを含む医薬組成物。
- 有効量の請求項1〜8のいずれか一項に記載の化合物またはエピマーを含有する癌用の医薬。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US1893808P | 2008-01-04 | 2008-01-04 | |
US61/018,938 | 2008-01-04 | ||
US8285008P | 2008-07-23 | 2008-07-23 | |
US61/082,850 | 2008-07-23 | ||
PCT/US2008/088529 WO2009088854A1 (en) | 2008-01-04 | 2008-12-30 | Epoxy-guaiane derivatives and treatment of cancer |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2011508779A JP2011508779A (ja) | 2011-03-17 |
JP2011508779A5 true JP2011508779A5 (ja) | 2012-02-16 |
JP5547653B2 JP5547653B2 (ja) | 2014-07-16 |
Family
ID=40380295
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010541518A Active JP5547653B2 (ja) | 2008-01-04 | 2008-12-30 | エポキシ−グアイアン誘導体および癌の治療 |
Country Status (8)
Country | Link |
---|---|
US (1) | US8410292B2 (ja) |
EP (1) | EP2235021B1 (ja) |
JP (1) | JP5547653B2 (ja) |
AU (1) | AU2008347299C1 (ja) |
CA (1) | CA2711434C (ja) |
DK (1) | DK2235021T3 (ja) |
ES (1) | ES2393877T3 (ja) |
WO (1) | WO2009088854A1 (ja) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2011120886A1 (en) | 2010-03-29 | 2011-10-06 | Institut Català D'investigació Química (Iciq) | A process for the preparation of (-)-englerin a, and analogues and intermediates thereof |
EP2474550A1 (en) * | 2010-12-22 | 2012-07-11 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Derivatives of Englerin for the treatment of cancer |
WO2013106226A2 (en) | 2012-01-09 | 2013-07-18 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methods of treating or preventing insulin resistance and associated diseases and conditions |
JP6255031B2 (ja) * | 2012-11-15 | 2017-12-27 | アメリカ合衆国 | Hiv及びhtlvに感染した患者を治療する方法 |
US9676788B2 (en) * | 2014-02-05 | 2017-06-13 | The United States Of America, As Represented By The Secretary Of Health And Human Services | Aza-epoxy-guaiane derivatives and treatment of cancer |
DK3283489T3 (da) * | 2015-04-13 | 2019-11-18 | Us Health | Epoxyazulenderivater, som kan anvendes til behandling af cancer |
EP3649133B1 (en) * | 2017-07-06 | 2022-02-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Englerin derivatives for treatment of cancer |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
US5019369A (en) | 1984-10-22 | 1991-05-28 | Vestar, Inc. | Method of targeting tumors in humans |
US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
CN1704417A (zh) | 2004-05-26 | 2005-12-07 | 杭州民生药业集团有限公司 | 新化合物莪术醇衍生物 |
-
2008
- 2008-12-30 EP EP08869946A patent/EP2235021B1/en active Active
- 2008-12-30 AU AU2008347299A patent/AU2008347299C1/en active Active
- 2008-12-30 CA CA2711434A patent/CA2711434C/en active Active
- 2008-12-30 US US12/811,245 patent/US8410292B2/en active Active
- 2008-12-30 ES ES08869946T patent/ES2393877T3/es active Active
- 2008-12-30 DK DK08869946.7T patent/DK2235021T3/da active
- 2008-12-30 JP JP2010541518A patent/JP5547653B2/ja active Active
- 2008-12-30 WO PCT/US2008/088529 patent/WO2009088854A1/en active Application Filing
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP2011508779A5 (ja) | ||
JP2009502743A5 (ja) | ||
JP2010529147A5 (ja) | ||
TNSN08408A1 (fr) | PYRIDINE [3,4-b] PYRAZINONES | |
JP2012144574A5 (ja) | ||
JP2013518107A5 (ja) | ||
JP2007302689A5 (ja) | ||
EP2620432A3 (en) | Diarylhydantoin compounds | |
JP2013507423A5 (ja) | ||
JP2009536191A5 (ja) | ||
JP2009500423A5 (ja) | ||
JP2009511508A5 (ja) | ||
DE602006021539D1 (en) | Morpholine als 5ht2c-agonisten | |
JP2009535358A5 (ja) | ||
JP2010504343A5 (ja) | ||
JP2008546770A5 (ja) | ||
JP2014500861A5 (ja) | ||
JP2011519910A5 (ja) | ||
JP2012512863A5 (ja) | ||
NZ734152A (en) | Compounds, compositions and methods useful for cholesterol mobilisation | |
JP2013542261A5 (ja) | ||
NZ603108A (en) | 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9h-carbazole derivatives and their use as prostaglandin d2 receptor modulators | |
JP2013506674A5 (ja) | ||
JP2016512541A5 (ja) | ||
JP2012511558A5 (ja) |