JP2015506988A5 - - Google Patents
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- JP2015506988A5 JP2015506988A5 JP2014556834A JP2014556834A JP2015506988A5 JP 2015506988 A5 JP2015506988 A5 JP 2015506988A5 JP 2014556834 A JP2014556834 A JP 2014556834A JP 2014556834 A JP2014556834 A JP 2014556834A JP 2015506988 A5 JP2015506988 A5 JP 2015506988A5
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- JP
- Japan
- Prior art keywords
- composition
- serm
- administered
- item
- patient
- 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.)
- Pending
Links
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims description 24
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 102000015694 estrogen receptors Human genes 0.000 claims description 6
- 108010038795 estrogen receptors Proteins 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 5
- 230000001404 mediated effect Effects 0.000 claims description 5
- ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 claims description 4
- 206010059594 Secondary hypogonadism Diseases 0.000 claims description 4
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims description 4
- 230000002513 anti-ovulatory effect Effects 0.000 claims description 4
- 229950004203 droloxifene Drugs 0.000 claims description 4
- 201000003368 hypogonadotropic hypogonadism Diseases 0.000 claims description 4
- LUMKNAVTFCDUIE-VHXPQNKSSA-N ospemifene Chemical compound C1=CC(OCCO)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 LUMKNAVTFCDUIE-VHXPQNKSSA-N 0.000 claims description 4
- -1 levormeroxifene Chemical compound 0.000 claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical group [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- 229950005529 arzoxifene Drugs 0.000 claims description 2
- MCGDSOGUHLTADD-UHFFFAOYSA-N arzoxifene Chemical compound C1=CC(OC)=CC=C1C1=C(OC=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 MCGDSOGUHLTADD-UHFFFAOYSA-N 0.000 claims description 2
- 229960000817 bazedoxifene Drugs 0.000 claims description 2
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 claims description 2
- 230000005906 menstruation Effects 0.000 claims description 2
- 229960004622 raloxifene Drugs 0.000 claims description 2
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 2
- 210000002966 serum Anatomy 0.000 claims description 2
- 230000002269 spontaneous effect Effects 0.000 claims description 2
- 229960003604 testosterone Drugs 0.000 claims description 2
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- XZEUAXYWNKYKPL-WDYNHAJCSA-N levormeloxifene Chemical compound C1([C@H]2[C@@H](C3=CC=C(C=C3OC2(C)C)OC)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 XZEUAXYWNKYKPL-WDYNHAJCSA-N 0.000 claims 1
- 229950002728 levormeloxifene Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 description 25
- 206010006187 Breast cancer Diseases 0.000 description 4
- 208000026310 Breast neoplasm Diseases 0.000 description 4
- 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 description 4
- 208000007984 Female Infertility Diseases 0.000 description 3
- 208000035150 Hypercholesterolemia Diseases 0.000 description 3
- 206010021928 Infertility female Diseases 0.000 description 3
- 206010049287 Lipodystrophy acquired Diseases 0.000 description 3
- 208000007466 Male Infertility Diseases 0.000 description 3
- 208000001132 Osteoporosis Diseases 0.000 description 3
- 206010033128 Ovarian cancer Diseases 0.000 description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 description 3
- 206010060862 Prostate cancer Diseases 0.000 description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 description 3
- 208000006575 hypertriglyceridemia Diseases 0.000 description 3
- 208000006132 lipodystrophy Diseases 0.000 description 3
- 206010046766 uterine cancer Diseases 0.000 description 3
- 206010020880 Hypertrophy Diseases 0.000 description 2
- 208000025865 Ulcer Diseases 0.000 description 2
- 210000002307 prostate Anatomy 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 description 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 230000009245 menopause Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261598723P | 2012-02-14 | 2012-02-14 | |
| US61/598,723 | 2012-02-14 | ||
| PCT/US2013/026178 WO2013123218A1 (en) | 2012-02-14 | 2013-02-14 | Selective estrogen receptor modulators with short half-lives and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015506988A JP2015506988A (ja) | 2015-03-05 |
| JP2015506988A5 true JP2015506988A5 (enExample) | 2016-03-24 |
Family
ID=47755046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014556834A Pending JP2015506988A (ja) | 2012-02-14 | 2013-02-14 | 半減期の短い選択的エストロゲン受容体モジュレーターおよびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9161940B2 (enExample) |
| EP (2) | EP3300725A3 (enExample) |
| JP (1) | JP2015506988A (enExample) |
| CN (2) | CN104114162A (enExample) |
| AU (1) | AU2013221478B2 (enExample) |
| CA (1) | CA2864104A1 (enExample) |
| HK (1) | HK1203155A1 (enExample) |
| MX (1) | MX2014009154A (enExample) |
| WO (1) | WO2013123218A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20160038506A1 (en) * | 2012-02-14 | 2016-02-11 | Repros Therapeutics Inc. | Selective Estrogen Receptor Modulators With Short Half-Lives and Uses Thereof |
| US9744177B2 (en) | 2014-03-10 | 2017-08-29 | Endorecherche, Inc. | Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with SERM |
| CN108463453A (zh) | 2016-04-22 | 2018-08-28 | 意大利合成制造有限公司 | 用于制备具有针状晶体习性的柠檬酸恩氯米芬的方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4133814A (en) | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
| DE3046719C2 (de) | 1980-12-11 | 1983-02-17 | Klinge Pharma GmbH, 8000 München | 1,1,2-Triphenyl-but-1-en-Derivate, Verfahren zu ihrer Herstellung und Arzneimittel |
| US4418068A (en) | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| US4447622A (en) | 1981-09-22 | 1984-05-08 | Council Of Scientific And Industrial Research Rafi Marg | Preparation of l- and d-isomers of dl-3,4-trans-2,2-disubstituted-3,4-diarylchromans and derivatives thereof |
| US5596004A (en) * | 1993-12-21 | 1997-01-21 | Eli Lilly And Company | Methods of inhibiting male infertility |
| US5510357A (en) | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| IL120262A (en) * | 1996-02-28 | 2001-01-28 | Pfizer | Droloxifene and derivatives thereof for use in increasing serum testosterone levels |
| US5998402A (en) | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
| US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
| AU2991301A (en) * | 2000-01-28 | 2001-08-07 | Endorecherche Inc. | Selective estrogen receptor modulators in combination with estrogens |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| NZ560551A (en) * | 2005-03-22 | 2010-02-26 | Repros Therapeutics Inc | Dosing regimes for trans-clomiphene |
| TW201500041A (zh) * | 2008-11-07 | 2015-01-01 | Repros Therapeutics Inc | 用於代謝症候群與第２型糖尿病的反式氯米芬 |
-
2013
- 2013-02-14 US US14/378,573 patent/US9161940B2/en not_active Expired - Fee Related
- 2013-02-14 JP JP2014556834A patent/JP2015506988A/ja active Pending
- 2013-02-14 EP EP17201930.9A patent/EP3300725A3/en not_active Withdrawn
- 2013-02-14 WO PCT/US2013/026178 patent/WO2013123218A1/en not_active Ceased
- 2013-02-14 CN CN201380009176.7A patent/CN104114162A/zh active Pending
- 2013-02-14 EP EP13706870.6A patent/EP2814471A1/en not_active Ceased
- 2013-02-14 HK HK15103740.0A patent/HK1203155A1/xx unknown
- 2013-02-14 CA CA2864104A patent/CA2864104A1/en not_active Abandoned
- 2013-02-14 AU AU2013221478A patent/AU2013221478B2/en not_active Ceased
- 2013-02-14 MX MX2014009154A patent/MX2014009154A/es unknown
- 2013-02-14 CN CN201710050063.1A patent/CN106890185A/zh active Pending
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