KR101923250B1 - 유방암의 치료 - Google Patents
유방암의 치료 Download PDFInfo
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- KR101923250B1 KR101923250B1 KR1020147005617A KR20147005617A KR101923250B1 KR 101923250 B1 KR101923250 B1 KR 101923250B1 KR 1020147005617 A KR1020147005617 A KR 1020147005617A KR 20147005617 A KR20147005617 A KR 20147005617A KR 101923250 B1 KR101923250 B1 KR 101923250B1
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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| KR102708177B1 (ko) | 2018-01-31 | 2024-09-23 | 데시페라 파마슈티칼스, 엘엘씨. | 위장관 기질 종양의 치료를 위한 병용 요법 |
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| EP3938363A1 (en) | 2019-03-11 | 2022-01-19 | Teva Pharmaceuticals International GmbH | Solid state forms of ripretinib |
| LT4013412T (lt) | 2019-08-12 | 2026-03-25 | Deciphera Pharmaceuticals, Llc | Ripretinibas, skirtas virškinamojo trakto stromos navikų gydymui |
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070004753A1 (en) | 2005-05-13 | 2007-01-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| WO2010099238A1 (en) | 2009-02-24 | 2010-09-02 | Medivation Prostate Therapeutics, Inc. | Specific diarylhydantoin and diarylthiohydantoin compounds |
| WO2010118354A1 (en) | 2009-04-09 | 2010-10-14 | Medivation Prostate Therapeutics, Inc. | Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods for use thereof |
| US20110003839A1 (en) | 2006-03-27 | 2011-01-06 | The Regents Of The University Of California | Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases |
| WO2011044327A1 (en) | 2009-10-07 | 2011-04-14 | Medivation Prostate Therapeutics, Inc. | Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea compounds |
| US20110130296A1 (en) | 2008-03-14 | 2011-06-02 | The Regents Of The University Of California | Multi-gene classifiers and prognostic indicators for cancers |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4559157A (en) | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
| LU84979A1 (fr) | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
| US4820508A (en) | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
| US4992478A (en) | 1988-04-04 | 1991-02-12 | Warner-Lambert Company | Antiinflammatory skin moisturizing composition and method of preparing same |
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| JP4644737B2 (ja) | 2005-05-13 | 2011-03-02 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | ジアリールヒダントイン化合物 |
| CA2630974A1 (en) | 2005-11-23 | 2007-05-31 | University Of Utah Research Foundation | Methods and compositions involving intrinsic genes |
| KR101456722B1 (ko) * | 2006-03-29 | 2014-10-31 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 디아릴티오히단토인 화합물 |
| TWI469971B (zh) | 2007-10-26 | 2015-01-21 | Univ California | 二芳基乙內醯脲類化合物 |
| US8450290B2 (en) * | 2007-11-26 | 2013-05-28 | Enzon Pharmaceuticals, Inc. | Methods for treating androgen receptor dependent disorders including cancers |
| DK2297359T3 (en) | 2008-05-30 | 2014-02-24 | Univ Utah Res Found | Gene expression profiles to predict the outcome of breast cancer |
| WO2011022316A1 (en) * | 2009-08-20 | 2011-02-24 | The Regents Of The University Of Colorado, A Body Corporate | Mirnas dysregulated in triple-negative breast cancer |
| AU2012229123B2 (en) | 2011-03-15 | 2017-02-02 | British Columbia Cancer Agency Branch | Methods of treating breast cancer with anthracycline therapy |
| KR101923250B1 (ko) * | 2011-07-29 | 2018-11-28 | 메디베이션 프로스테이트 테라퓨틱스 엘엘씨 | 유방암의 치료 |
| AU2012345789B2 (en) | 2011-11-30 | 2018-02-15 | British Columbia Cancer Agency Branch | Methods of treating breast cancer with taxane therapy |
| US10175240B2 (en) | 2012-08-23 | 2019-01-08 | The Regents Of The University Of Colorado, A Body Corporate | Method for determining breast cancer treatment |
| US9175291B2 (en) | 2012-10-11 | 2015-11-03 | Isis Pharmaceuticals Inc. | Modulation of androgen receptor expression |
| US20140154681A1 (en) | 2012-11-12 | 2014-06-05 | Nanostring Technologies, Inc. | Methods to Predict Breast Cancer Outcome |
| US10679730B2 (en) | 2013-05-28 | 2020-06-09 | The University Of Chicago | Prognostic and predictive breast cancer signature |
| SG11201704425TA (en) | 2014-12-12 | 2017-06-29 | Medivation Prostate Therapeutics Inc | Method for predicting response to breast cancer therapeutic agents and method of treatment of breast cancer |
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Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070004753A1 (en) | 2005-05-13 | 2007-01-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| US20110003839A1 (en) | 2006-03-27 | 2011-01-06 | The Regents Of The University Of California | Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases |
| US20110130296A1 (en) | 2008-03-14 | 2011-06-02 | The Regents Of The University Of California | Multi-gene classifiers and prognostic indicators for cancers |
| WO2010099238A1 (en) | 2009-02-24 | 2010-09-02 | Medivation Prostate Therapeutics, Inc. | Specific diarylhydantoin and diarylthiohydantoin compounds |
| WO2010118354A1 (en) | 2009-04-09 | 2010-10-14 | Medivation Prostate Therapeutics, Inc. | Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods for use thereof |
| WO2011044327A1 (en) | 2009-10-07 | 2011-04-14 | Medivation Prostate Therapeutics, Inc. | Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea compounds |
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