JP2015535283A5 - - Google Patents
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- JP2015535283A5 JP2015535283A5 JP2015540702A JP2015540702A JP2015535283A5 JP 2015535283 A5 JP2015535283 A5 JP 2015535283A5 JP 2015540702 A JP2015540702 A JP 2015540702A JP 2015540702 A JP2015540702 A JP 2015540702A JP 2015535283 A5 JP2015535283 A5 JP 2015535283A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- cancer
- clomiphene
- igf
- trans
- 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.)
- Withdrawn
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- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 claims description 27
- 102100037852 Insulin-like growth factor I Human genes 0.000 claims description 27
- GKIRPKYJQBWNGO-QPLCGJKRSA-N zuclomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(/Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-QPLCGJKRSA-N 0.000 claims description 24
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims description 18
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 13
- 239000002246 antineoplastic agent Substances 0.000 claims description 10
- 229940127089 cytotoxic agent Drugs 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 201000011510 cancer Diseases 0.000 claims description 9
- 210000002966 serum Anatomy 0.000 claims description 7
- 101001055320 Myxine glutinosa Insulin-like growth factor Proteins 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 229960003608 clomifene Drugs 0.000 claims description 6
- 206010005003 Bladder cancer Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 4
- 229960004111 buformin Drugs 0.000 claims description 4
- XSEUMFJMFFMCIU-UHFFFAOYSA-N buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 229960003105 metformin Drugs 0.000 claims description 4
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 4
- 201000008968 osteosarcoma Diseases 0.000 claims description 4
- 229960003243 phenformin Drugs 0.000 claims description 4
- ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims description 4
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 4
- 108091034117 Oligonucleotide Proteins 0.000 claims description 3
- 239000000074 antisense oligonucleotide Substances 0.000 claims description 3
- 238000012230 antisense oligonucleotides Methods 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 102000028416 insulin-like growth factor binding Human genes 0.000 claims description 3
- 108091022911 insulin-like growth factor binding Proteins 0.000 claims description 3
- 229940043355 kinase inhibitor Drugs 0.000 claims description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 2
- 206010046766 uterine cancer Diseases 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical class OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 33
- 102000005962 receptors Human genes 0.000 description 7
- 108020003175 receptors Proteins 0.000 description 7
- 239000000328 estrogen antagonist Substances 0.000 description 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 2
- VSNHCAURESNICA-NJFSPNSNSA-N 1-oxidanylurea Chemical compound N[14C](=O)NO VSNHCAURESNICA-NJFSPNSNSA-N 0.000 description 1
- 102100036009 5'-AMP-activated protein kinase catalytic subunit alpha-2 Human genes 0.000 description 1
- 108010006654 Bleomycin Proteins 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical group [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 1
- 101000783681 Homo sapiens 5'-AMP-activated protein kinase catalytic subunit alpha-2 Proteins 0.000 description 1
- 101150097381 Mtor gene Proteins 0.000 description 1
- 229940123237 Taxane Drugs 0.000 description 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 229940046836 anti-estrogen Drugs 0.000 description 1
- 230000001833 anti-estrogenic effect Effects 0.000 description 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 1
- 229960001561 bleomycin Drugs 0.000 description 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 description 1
- 229960004562 carboplatin Drugs 0.000 description 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 1
- 229960004316 cisplatin Drugs 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- 229960004397 cyclophosphamide Drugs 0.000 description 1
- 229960004679 doxorubicin Drugs 0.000 description 1
- 229960002949 fluorouracil Drugs 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229960004768 irinotecan Drugs 0.000 description 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 description 1
- 229960000303 topotecan Drugs 0.000 description 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 229960003048 vinblastine Drugs 0.000 description 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
- 229960004528 vincristine Drugs 0.000 description 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 description 1
- 229960002066 vinorelbine Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261722013P | 2012-11-02 | 2012-11-02 | |
| US61/722,013 | 2012-11-02 | ||
| PCT/US2013/066141 WO2014070523A1 (en) | 2012-11-02 | 2013-10-22 | Trans-clomiphene for use in cancer therapy |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018094685A Division JP2018123168A (ja) | 2012-11-02 | 2018-05-16 | 癌療法における使用のためのトランス−クロミフェン |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015535283A JP2015535283A (ja) | 2015-12-10 |
| JP2015535283A5 true JP2015535283A5 (enExample) | 2016-09-29 |
Family
ID=50627954
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015540702A Withdrawn JP2015535283A (ja) | 2012-11-02 | 2013-10-22 | 癌療法における使用のためのトランス−クロミフェン |
| JP2018094685A Pending JP2018123168A (ja) | 2012-11-02 | 2018-05-16 | 癌療法における使用のためのトランス−クロミフェン |
| JP2020216526A Pending JP2021046448A (ja) | 2012-11-02 | 2020-12-25 | 癌療法における使用のためのトランス−クロミフェン |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018094685A Pending JP2018123168A (ja) | 2012-11-02 | 2018-05-16 | 癌療法における使用のためのトランス−クロミフェン |
| JP2020216526A Pending JP2021046448A (ja) | 2012-11-02 | 2020-12-25 | 癌療法における使用のためのトランス−クロミフェン |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9687458B2 (enExample) |
| EP (1) | EP2914294A1 (enExample) |
| JP (3) | JP2015535283A (enExample) |
| CN (1) | CN104994877A (enExample) |
| AU (1) | AU2013338311A1 (enExample) |
| CA (1) | CA2889770A1 (enExample) |
| HK (1) | HK1216502A1 (enExample) |
| IL (1) | IL238453A0 (enExample) |
| MX (1) | MX2015005160A (enExample) |
| WO (1) | WO2014070523A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170217914A1 (en) * | 2014-08-05 | 2017-08-03 | The Penn State Research Foundation | Novel Triarylethylene Compounds and Methods Using Same |
| US11633382B2 (en) | 2015-11-10 | 2023-04-25 | Paracrine Therapeutics Ab | Treatment of ER-negative breast cancer with an PDGF-CC inhibitor and anti-estrogen |
| JP2018002619A (ja) * | 2016-06-29 | 2018-01-11 | 国立大学法人 東京大学 | オートファジー阻害剤 |
| US20200030259A1 (en) * | 2016-09-26 | 2020-01-30 | Repros Therapeutics Inc. | Antiestrogens and/or Aromatase Inhibitors for Use in Treating Obesity and Related Symptoms |
| CN108420806A (zh) * | 2017-02-15 | 2018-08-21 | 武汉华杰世纪生物医药有限公司 | 具有靶向性的抗肿瘤药物 |
| WO2019236209A2 (en) * | 2018-04-27 | 2019-12-12 | Jin Byung Ju | Methods for high-content drug screening |
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| NZ591955A (en) | 2007-10-16 | 2011-10-28 | Repros Therapeutics Inc | Trans-clomiphene for diabetes mellitus type 2 |
| US20100111901A1 (en) | 2008-11-03 | 2010-05-06 | Auspex Pharmaceuticals, Inc. | Triazole inhibitors of aromatase |
| TWI458478B (zh) * | 2008-11-07 | 2014-11-01 | Repros Therapeutics Inc | 用於代謝症候群與第２型糖尿病的反式氯米芬 |
| US20100144687A1 (en) | 2008-12-05 | 2010-06-10 | Glaser Rebecca L | Pharmaceutical compositions containing testosterone and an aromatase inhibitor |
| UA113291C2 (xx) | 2011-08-04 | 2017-01-10 | Метаболіти транскломіфену і їх застосування | |
| WO2013020215A1 (en) | 2011-08-09 | 2013-02-14 | Adams Kenneth W | Use of aromatase inhibitor or estrogen blocker for increasing spermatogenesis or testosterone levels in males |
| EP2819676B1 (en) | 2012-02-29 | 2018-05-30 | Repros Therapeutics Inc. | Combination therapy for treating androgen deficiency |
| CA2880388A1 (en) | 2012-08-21 | 2014-02-27 | Repros Therapeutics Inc. | Trans-clomiphene formulations and uses thereof |
| CN103351304B (zh) | 2013-07-01 | 2015-12-09 | 暨明医药科技（苏州）有限公司 | 一种克罗米芬的合成方法 |
-
2013
- 2013-10-22 WO PCT/US2013/066141 patent/WO2014070523A1/en not_active Ceased
- 2013-10-22 EP EP13786580.4A patent/EP2914294A1/en not_active Withdrawn
- 2013-10-22 JP JP2015540702A patent/JP2015535283A/ja not_active Withdrawn
- 2013-10-22 CA CA2889770A patent/CA2889770A1/en not_active Abandoned
- 2013-10-22 MX MX2015005160A patent/MX2015005160A/es unknown
- 2013-10-22 US US14/440,007 patent/US9687458B2/en not_active Expired - Fee Related
- 2013-10-22 HK HK16104449.1A patent/HK1216502A1/zh unknown
- 2013-10-22 AU AU2013338311A patent/AU2013338311A1/en not_active Abandoned
- 2013-10-22 CN CN201380057363.2A patent/CN104994877A/zh active Pending
-
2015
- 2015-04-26 IL IL238453A patent/IL238453A0/en unknown
-
2018
- 2018-05-16 JP JP2018094685A patent/JP2018123168A/ja active Pending
-
2020
- 2020-12-25 JP JP2020216526A patent/JP2021046448A/ja active Pending
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