JP2014524934A5 - - Google Patents
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- Publication number
- JP2014524934A5 JP2014524934A5 JP2014523048A JP2014523048A JP2014524934A5 JP 2014524934 A5 JP2014524934 A5 JP 2014524934A5 JP 2014523048 A JP2014523048 A JP 2014523048A JP 2014523048 A JP2014523048 A JP 2014523048A JP 2014524934 A5 JP2014524934 A5 JP 2014524934A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heterocyclic
- alkynyl
- alkenyl
- 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 description 81
- 206010006187 Breast cancer Diseases 0.000 claims description 67
- 208000026310 Breast neoplasm Diseases 0.000 claims description 67
- 150000003839 salts Chemical class 0.000 claims description 40
- 210000004027 cell Anatomy 0.000 claims description 31
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 27
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 27
- 238000009261 endocrine therapy Methods 0.000 claims description 25
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 claims description 25
- 102000015694 estrogen receptors Human genes 0.000 claims description 19
- 108010038795 estrogen receptors Proteins 0.000 claims description 19
- 102100032187 Androgen receptor Human genes 0.000 claims description 11
- 108010080146 androgen receptors Proteins 0.000 claims description 11
- WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 claims description 6
- 229960004671 enzalutamide Drugs 0.000 claims description 6
- 230000004957 immunoregulator effect Effects 0.000 claims description 6
- 229940122815 Aromatase inhibitor Drugs 0.000 claims description 3
- 102000036365 BRCA1 Human genes 0.000 claims description 3
- 108700020463 BRCA1 Proteins 0.000 claims description 3
- 101150072950 BRCA1 gene Proteins 0.000 claims description 3
- 239000003886 aromatase inhibitor Substances 0.000 claims description 3
- 239000002834 estrogen receptor modulator Substances 0.000 claims description 3
- 210000002901 mesenchymal stem cell Anatomy 0.000 claims description 3
- 230000035772 mutation Effects 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 description 282
- 125000000623 heterocyclic group Chemical group 0.000 description 215
- 125000003118 aryl group Chemical group 0.000 description 162
- 229910052739 hydrogen Inorganic materials 0.000 description 155
- 125000000547 substituted alkyl group Chemical group 0.000 description 114
- 229910052799 carbon Inorganic materials 0.000 description 113
- 125000003342 alkenyl group Chemical group 0.000 description 84
- -1 haloacetoxy Chemical group 0.000 description 84
- 239000001257 hydrogen Substances 0.000 description 84
- 125000000304 alkynyl group Chemical group 0.000 description 78
- 150000002431 hydrogen Chemical group 0.000 description 78
- 125000003107 substituted aryl group Chemical group 0.000 description 66
- 125000006615 aromatic heterocyclic group Chemical group 0.000 description 63
- 125000005017 substituted alkenyl group Chemical group 0.000 description 60
- 125000004426 substituted alkynyl group Chemical group 0.000 description 60
- 125000000753 cycloalkyl group Chemical group 0.000 description 58
- 229910052757 nitrogen Chemical group 0.000 description 54
- 229910052760 oxygen Inorganic materials 0.000 description 54
- 125000001072 heteroaryl group Chemical group 0.000 description 52
- 229910052736 halogen Inorganic materials 0.000 description 48
- 150000002367 halogens Chemical group 0.000 description 48
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 48
- 229910052717 sulfur Inorganic materials 0.000 description 48
- 238000000034 method Methods 0.000 description 43
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 42
- 125000005018 aryl alkenyl group Chemical group 0.000 description 42
- 125000003710 aryl alkyl group Chemical group 0.000 description 42
- 125000005015 aryl alkynyl group Chemical group 0.000 description 42
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 36
- 125000004453 alkoxycarbonyl group Chemical class 0.000 description 24
- 125000004457 alkyl amino carbonyl group Chemical class 0.000 description 24
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 description 24
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 description 24
- 125000004849 alkoxymethyl group Chemical group 0.000 description 18
- 125000004475 heteroaralkyl group Chemical group 0.000 description 18
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 18
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical group CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 description 12
- 125000005090 alkenylcarbonyl group Chemical group 0.000 description 12
- 125000004685 alkoxythiocarbonyl group Chemical group 0.000 description 12
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 12
- 125000004691 alkyl thio carbonyl group Chemical group 0.000 description 12
- 125000005087 alkynylcarbonyl group Chemical group 0.000 description 12
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 description 12
- 125000005129 aryl carbonyl group Chemical group 0.000 description 12
- 239000003814 drug Substances 0.000 description 12
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 12
- 125000001188 haloalkyl group Chemical group 0.000 description 12
- 125000004997 halocarbonyl group Chemical group 0.000 description 12
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 12
- 238000004519 manufacturing process Methods 0.000 description 12
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 12
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 6
- NPDLYUOYAGBHFB-WDSKDSINSA-N Asn-Arg Chemical compound NC(=O)C[C@H](N)C(=O)N[C@H](C(O)=O)CCCN=C(N)N NPDLYUOYAGBHFB-WDSKDSINSA-N 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 6
- UCOHKZKRNWNULS-UHFFFAOYSA-N aminocyanamide Chemical compound NNC#N UCOHKZKRNWNULS-UHFFFAOYSA-N 0.000 description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 6
- 125000004432 carbon atom Chemical group C* 0.000 description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 6
- 125000004093 cyano group Chemical group *C#N 0.000 description 6
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 description 6
- 125000004468 heterocyclylthio group Chemical group 0.000 description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 6
- 125000002346 iodo group Chemical group I* 0.000 description 6
- RIFHJAODNHLCBH-UHFFFAOYSA-N methanethione Chemical group S=[CH] RIFHJAODNHLCBH-UHFFFAOYSA-N 0.000 description 6
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 description 6
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 6
- 239000001301 oxygen Substances 0.000 description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
- 125000004193 piperazinyl group Chemical group 0.000 description 6
- 239000011593 sulfur Substances 0.000 description 6
- 230000001225 therapeutic effect Effects 0.000 description 2
- 230000010261 cell growth Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161513361P | 2011-07-29 | 2011-07-29 | |
| US61/513,361 | 2011-07-29 | ||
| PCT/US2012/048471 WO2013066440A1 (en) | 2011-07-29 | 2012-07-27 | Treatment of breast cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017072819A Division JP2017141269A (ja) | 2011-07-29 | 2017-03-31 | 乳がんの処置 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014524934A JP2014524934A (ja) | 2014-09-25 |
| JP2014524934A5 true JP2014524934A5 (OSRAM) | 2015-08-27 |
| JP6158180B2 JP6158180B2 (ja) | 2017-07-05 |
Family
ID=48192564
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014523048A Active JP6158180B2 (ja) | 2011-07-29 | 2012-07-27 | 乳がんの処置 |
| JP2017072819A Pending JP2017141269A (ja) | 2011-07-29 | 2017-03-31 | 乳がんの処置 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017072819A Pending JP2017141269A (ja) | 2011-07-29 | 2017-03-31 | 乳がんの処置 |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US9517229B2 (OSRAM) |
| EP (4) | EP3791724A1 (OSRAM) |
| JP (2) | JP6158180B2 (OSRAM) |
| KR (1) | KR101923250B1 (OSRAM) |
| CN (1) | CN103997894B (OSRAM) |
| BR (1) | BR112014002200A2 (OSRAM) |
| CA (1) | CA2843417C (OSRAM) |
| CY (1) | CY1121038T1 (OSRAM) |
| DK (1) | DK2739153T3 (OSRAM) |
| EA (1) | EA028452B1 (OSRAM) |
| ES (1) | ES2696074T3 (OSRAM) |
| HU (1) | HUE040524T2 (OSRAM) |
| MX (1) | MX359664B (OSRAM) |
| PH (1) | PH12014500248B1 (OSRAM) |
| PL (1) | PL2739153T3 (OSRAM) |
| PT (1) | PT2739153T (OSRAM) |
| SI (1) | SI2739153T1 (OSRAM) |
| WO (1) | WO2013066440A1 (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2739153T3 (en) * | 2011-07-29 | 2018-12-03 | Medivation Prostate Therapeutics Llc | TREATMENT OF BREAST CANCER |
| GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
| UA117663C2 (uk) | 2012-09-26 | 2018-09-10 | Арагон Фармасьютікалз, Інк. | Антиандроген для лікування неметастатичного кастраційно-резистентного раку передміхурової залози |
| JOP20200097A1 (ar) | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | معدل مستقبل أندروجين واستخداماته |
| NZ629469A (en) * | 2013-04-17 | 2017-05-26 | Signal Pharm Llc | Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy |
| JP6945587B2 (ja) * | 2013-11-07 | 2021-10-06 | デシフェラ ファーマシューティカルズ，エルエルシー | ガンの処置に有用なｔｉｅ２キナーゼの阻害方法 |
| WO2015069266A1 (en) * | 2013-11-07 | 2015-05-14 | Flynn Daniel L | Methods for inhibiting tie2 kinase useful in the treatment of cancer |
| WO2015184145A1 (en) * | 2014-05-28 | 2015-12-03 | Eisai R&D Management Co., Ltd. | Use of eribulin and poly (adp ribose) polymerase (parp) inhibitors as combination therapy for the treatment of cancer |
| AU2015360767A1 (en) * | 2014-12-12 | 2017-06-08 | Medivation Prostate Therapeutics Llc | Method for predicting response to breast cancer therapeutic agents and method of treatment of breast cancer |
| WO2016141167A1 (en) | 2015-03-03 | 2016-09-09 | Cureport, Inc. | Combination liposomal pharmaceutical formulations |
| EP3265063A4 (en) | 2015-03-03 | 2018-11-07 | Cureport, Inc. | Dual loaded liposomal pharmaceutical formulations |
| CN104857517B (zh) * | 2015-05-14 | 2018-04-27 | 南京海纳医药科技股份有限公司 | 一种恩杂鲁胺软胶囊及其制备方法 |
| US9963433B2 (en) * | 2016-01-29 | 2018-05-08 | Wayne State University | Anticancer drugs including the chemical structures of an androgen receptor ligand and a histone deacetylase inhibitor |
| MY198676A (en) | 2017-06-22 | 2023-09-15 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| US10702508B2 (en) | 2017-10-16 | 2020-07-07 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer |
| CN107987055A (zh) * | 2017-12-19 | 2018-05-04 | 刘秀云 | 硫代咪唑二酮类雄激素受体拮抗剂及其用途 |
| AU2019216351B2 (en) | 2018-01-31 | 2024-07-25 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of mastocytosis |
| CN111818915B (zh) | 2018-01-31 | 2024-05-24 | 德西费拉制药有限责任公司 | 治疗胃肠道间质瘤的组合疗法 |
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CA3121199A1 (en) * | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Diarylhydantoin compounds and methods of use thereof |
| NZ784949A (en) | 2019-08-12 | 2025-09-26 | Deciphera Pharmaceuticals Llc | Ripretinib for treating gastrointestinal stromal tumors |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| KR20250057151A (ko) | 2019-12-30 | 2025-04-28 | 데시페라 파마슈티칼스, 엘엘씨 | 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의조성물 |
| AU2020419197B2 (en) | 2019-12-30 | 2023-08-31 | Deciphera Pharmaceuticals, Llc | Amorphous kinase inhibitor formulations and methods of use thereof |
| US20230296584A1 (en) * | 2020-08-03 | 2023-09-21 | Oncocyte Corporation | Classifying tumors and predicting responsiveness |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
Family Cites Families (26)
| 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 |
| US7709517B2 (en) | 2005-05-13 | 2010-05-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| RS53967B1 (sr) | 2005-05-13 | 2015-08-31 | The Regents Of The University Of California | Diaril hidantoin jedinjenja kao antagonisti receptora androgena za lečenje raka |
| EP1954708A4 (en) | 2005-11-23 | 2009-05-13 | Univ Utah Res Found | Methods and compositions involving intrinsic genes |
| LT2656841T (lt) * | 2006-03-27 | 2016-09-26 | The Regents Of The University Of California | Androgeno receptoriaus moduliatorius, skirtas prostatos vėžio ir su androgeno receptoriumi susijusių ligų gydymui |
| MX2008012492A (es) | 2006-03-29 | 2008-12-12 | Univ California | Compuestos de diariltiohidantoina. |
| US8680291B2 (en) * | 2007-10-26 | 2014-03-25 | The Regents Of The University Of California | Diarylhydantoin compounds |
| US8450290B2 (en) | 2007-11-26 | 2013-05-28 | Enzon Pharmaceuticals, Inc. | Methods for treating androgen receptor dependent disorders including cancers |
| WO2009114534A1 (en) | 2008-03-14 | 2009-09-17 | The Regents Of The University Of California | Multi-gene classifiers and prognostic indicators for cancers |
| PT2297359E (pt) | 2008-05-30 | 2014-03-19 | Univ North Carolina | Perfis de expressão de genes para prognosticar resultados relativos ao cancro da mama |
| BRPI1007990A2 (pt) | 2009-02-24 | 2015-09-01 | Medivation Prostate Therapeutics Inc | Compostos específicos de diaril-hidantoína e diariltioidantoína. |
| EP2416657A4 (en) | 2009-04-09 | 2012-09-05 | Medivation Prostate Therapeutics Inc | COMPOUNDS COMPRISING SUBSTITUTED DI-ARYLHYDANTOIDS AND DI-ARYLTHIOHYDANTOINES AND METHODS OF USE THEREOF |
| 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 |
| WO2011044327A1 (en) | 2009-10-07 | 2011-04-14 | Medivation Prostate Therapeutics, Inc. | Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea compounds |
| US9066963B2 (en) | 2011-03-15 | 2015-06-30 | The University Of North Carolina At Chapel Hill | Methods of treating breast cancer with anthracycline therapy |
| DK2739153T3 (en) * | 2011-07-29 | 2018-12-03 | Medivation Prostate Therapeutics Llc | TREATMENT OF BREAST CANCER |
| AU2012345789B2 (en) | 2011-11-30 | 2018-02-15 | British Columbia Cancer Agency Branch | Methods of treating breast cancer with taxane therapy |
| AU2013306380A1 (en) | 2012-08-23 | 2015-03-05 | 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 |
| WO2014075067A1 (en) | 2012-11-12 | 2014-05-15 | 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 |
| AU2015360767A1 (en) | 2014-12-12 | 2017-06-08 | Medivation Prostate Therapeutics Llc | Method for predicting response to breast cancer therapeutic agents and method of treatment of breast cancer |
-
2012
- 2012-07-27 DK DK12846720.6T patent/DK2739153T3/en active
- 2012-07-27 WO PCT/US2012/048471 patent/WO2013066440A1/en not_active Ceased
- 2012-07-27 CA CA2843417A patent/CA2843417C/en active Active
- 2012-07-27 KR KR1020147005617A patent/KR101923250B1/ko active Active
- 2012-07-27 PH PH1/2014/500248A patent/PH12014500248B1/en unknown
- 2012-07-27 EA EA201400178A patent/EA028452B1/ru not_active IP Right Cessation
- 2012-07-27 PT PT12846720T patent/PT2739153T/pt unknown
- 2012-07-27 CN CN201280048192.2A patent/CN103997894B/zh active Active
- 2012-07-27 ES ES12846720T patent/ES2696074T3/es active Active
- 2012-07-27 SI SI201231453T patent/SI2739153T1/sl unknown
- 2012-07-27 EP EP20191500.6A patent/EP3791724A1/en not_active Withdrawn
- 2012-07-27 EP EP12846720.6A patent/EP2739153B1/en active Active
- 2012-07-27 EP EP18190012.7A patent/EP3430907A1/en not_active Withdrawn
- 2012-07-27 PL PL12846720T patent/PL2739153T3/pl unknown
- 2012-07-27 MX MX2014001218A patent/MX359664B/es active IP Right Grant
- 2012-07-27 BR BR112014002200A patent/BR112014002200A2/pt not_active Application Discontinuation
- 2012-07-27 US US14/236,036 patent/US9517229B2/en active Active
- 2012-07-27 JP JP2014523048A patent/JP6158180B2/ja active Active
- 2012-07-27 HU HUE12846720A patent/HUE040524T2/hu unknown
- 2012-07-27 EP EP19187649.9A patent/EP3610731A1/en not_active Withdrawn
-
2016
- 2016-12-09 US US15/373,914 patent/US10111861B2/en active Active
-
2017
- 2017-03-31 JP JP2017072819A patent/JP2017141269A/ja active Pending
-
2018
- 2018-10-24 US US16/168,896 patent/US20190262315A1/en not_active Abandoned
- 2018-11-08 CY CY181101174T patent/CY1121038T1/el unknown
-
2020
- 2020-01-22 US US16/749,133 patent/US20210069154A1/en not_active Abandoned
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