CA2488864A1 - Inhibiteurs rsk et utilisations therapeutiques de ces derniers - Google Patents
Inhibiteurs rsk et utilisations therapeutiques de ces derniers Download PDFInfo
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- CA2488864A1 CA2488864A1 CA002488864A CA2488864A CA2488864A1 CA 2488864 A1 CA2488864 A1 CA 2488864A1 CA 002488864 A CA002488864 A CA 002488864A CA 2488864 A CA2488864 A CA 2488864A CA 2488864 A1 CA2488864 A1 CA 2488864A1
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- Prior art keywords
- rsk
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- hydroxy
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- 125000001298 n-hexoxy group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])O* 0.000 description 1
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- 229960001553 phloroglucinol Drugs 0.000 description 1
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- 108010077182 raf Kinases Proteins 0.000 description 1
- 102000016914 ras Proteins Human genes 0.000 description 1
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- 239000011347 resin Substances 0.000 description 1
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- MHOVAHRLVXNVSD-UHFFFAOYSA-N rhodium atom Chemical compound [Rh] MHOVAHRLVXNVSD-UHFFFAOYSA-N 0.000 description 1
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- 230000007017 scission Effects 0.000 description 1
- HOZOZZFCZRXYEK-HNHWXVNLSA-M scopolamine butylbromide Chemical compound [Br-].C1([C@@H](CO)C(=O)OC2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CCCC)=CC=CC=C1 HOZOZZFCZRXYEK-HNHWXVNLSA-M 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000012679 serum free medium Substances 0.000 description 1
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- 229910002027 silica gel Inorganic materials 0.000 description 1
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- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- UKLNMMHNWFDKNT-UHFFFAOYSA-M sodium chlorite Chemical compound [Na+].[O-]Cl=O UKLNMMHNWFDKNT-UHFFFAOYSA-M 0.000 description 1
- 229960002218 sodium chlorite Drugs 0.000 description 1
- 210000001082 somatic cell Anatomy 0.000 description 1
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- 238000004381 surface treatment Methods 0.000 description 1
- 238000011477 surgical intervention Methods 0.000 description 1
- JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 description 1
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- HPGGPRDJHPYFRM-UHFFFAOYSA-J tin(iv) chloride Chemical compound Cl[Sn](Cl)(Cl)Cl HPGGPRDJHPYFRM-UHFFFAOYSA-J 0.000 description 1
- 238000006257 total synthesis reaction Methods 0.000 description 1
- 230000037317 transdermal delivery Effects 0.000 description 1
- 238000010361 transduction Methods 0.000 description 1
- 230000026683 transduction Effects 0.000 description 1
- 239000012096 transfection reagent Substances 0.000 description 1
- 230000009261 transgenic effect Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 238000013519 translation Methods 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 239000012137 tryptone Substances 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 238000003026 viability measurement method Methods 0.000 description 1
- 201000005102 vulva cancer Diseases 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/06—Benzopyran radicals
- C07H17/065—Benzo[b]pyrans
- C07H17/07—Benzo[b]pyran-4-ones
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne de nouveaux composés et de nouvelles compositions qui présentent une activité inhibitrice spécifiquement dirigée contre Rsk. On a en outre remarqué que l'inhibition de Rsk par les composés selon la présente invention, ont pour effet de stopper la prolifération des lignées cellulaires cancéreuses tout en n'ayant qu'un faible effet sur la vitesse de prolifération des cellules normales. Par conséquent, cette invention permet d'identifier Rsk en tant que cible pour l'intervention thérapeutique dans les états pathologiques dans lesquels la maladie ou les symptômes peuvent être améliorés par l'inhibition de l'activité catalytique Rsk.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38800602P | 2002-06-12 | 2002-06-12 | |
| US60/388,006 | 2002-06-12 | ||
| US44955303P | 2003-02-24 | 2003-02-24 | |
| US60/449,553 | 2003-02-24 | ||
| PCT/US2003/018734 WO2003105766A2 (fr) | 2002-06-12 | 2003-06-12 | Inhibiteurs rsk et utilisations therapeutiques de ces derniers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2488864A1 true CA2488864A1 (fr) | 2003-12-24 |
Family
ID=29739979
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002488864A Abandoned CA2488864A1 (fr) | 2002-06-12 | 2003-06-12 | Inhibiteurs rsk et utilisations therapeutiques de ces derniers |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1539781A4 (fr) |
| AU (1) | AU2003251513A1 (fr) |
| CA (1) | CA2488864A1 (fr) |
| WO (1) | WO2003105766A2 (fr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9920393D0 (en) | 1999-08-27 | 1999-11-03 | Medix Scient Uk Limited | Plant extract mixtures and their uses |
| KR100590818B1 (ko) | 2004-10-11 | 2006-06-19 | 재단법인서울대학교산학협력재단 | 소분자 유기화합물의 직접적 ｐ90 리보솜 Ｓ6 키나제 1(ＲＳＫ1)의 활성증진에 의한 당뇨병, 비만 및대사증후군의 예방 및 치료용도 |
| EP1845778A2 (fr) | 2005-01-10 | 2007-10-24 | University Of Virginia Patent Foundation | Synthese d'inhibiteurs de p90rsk |
| US20100151050A1 (en) * | 2005-06-07 | 2010-06-17 | Shinji Mizuarai | Method for evaluation of compound using RSK1 |
| GB0512206D0 (en) | 2005-06-15 | 2005-07-27 | Biosynth As | Synthesis |
| US7659313B2 (en) * | 2007-09-13 | 2010-02-09 | Gateway Health Alliances, Inc. | Methods and related compositions using specific indanes to reduce weight and inhibit lipase, α-amylase and α-glucosidase activity in mammals |
| GB0718870D0 (en) * | 2007-09-27 | 2007-11-07 | Univ Dundee | Modulation of RSK |
| US9040673B2 (en) | 2009-08-14 | 2015-05-26 | University Of Virginia Patent Foundation | Synthesis and identification of novel RSK-specific inhibitors |
| WO2013181742A1 (fr) * | 2012-06-04 | 2013-12-12 | Phoenix Molecular Diagnostics Ltd. | Procédés d'inhibition de rsk dans le traitement du cancer du sein |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000066721A2 (fr) * | 1999-04-30 | 2000-11-09 | Beth Israel Deaconess Medical Center | Reduction de la masse adipeuse par modification de l'activite du gene rsk2 |
-
2003
- 2003-06-12 AU AU2003251513A patent/AU2003251513A1/en not_active Abandoned
- 2003-06-12 EP EP03760343A patent/EP1539781A4/fr not_active Withdrawn
- 2003-06-12 WO PCT/US2003/018734 patent/WO2003105766A2/fr not_active Application Discontinuation
- 2003-06-12 CA CA002488864A patent/CA2488864A1/fr not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003251513A8 (en) | 2003-12-31 |
| EP1539781A2 (fr) | 2005-06-15 |
| AU2003251513A1 (en) | 2003-12-31 |
| WO2003105766A3 (fr) | 2004-03-11 |
| EP1539781A4 (fr) | 2009-12-02 |
| WO2003105766A2 (fr) | 2003-12-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |