CN1954807A - 富含反式克罗米酚的克罗米酚组合物 - Google Patents
富含反式克罗米酚的克罗米酚组合物 Download PDFInfo
- Publication number
- CN1954807A CN1954807A CNA2006101356235A CN200610135623A CN1954807A CN 1954807 A CN1954807 A CN 1954807A CN A2006101356235 A CNA2006101356235 A CN A2006101356235A CN 200610135623 A CN200610135623 A CN 200610135623A CN 1954807 A CN1954807 A CN 1954807A
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- Prior art keywords
- chloramiphene
- testosterone
- trans
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- enclomifene
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Classifications
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| US30431301P | 2001-07-09 | 2001-07-09 | |
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| CNB028174410A Division CN1289075C (zh) | 2001-07-09 | 2002-07-09 | 富含反式克罗米酚的克罗米酚组合物的用途 |
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| CN1954807A true CN1954807A (zh) | 2007-05-02 |
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| CNA2006101356235A Pending CN1954807A (zh) | 2001-07-09 | 2002-07-09 | 富含反式克罗米酚的克罗米酚组合物 |
| CNB028174410A Expired - Lifetime CN1289075C (zh) | 2001-07-09 | 2002-07-09 | 富含反式克罗米酚的克罗米酚组合物的用途 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB028174410A Expired - Lifetime CN1289075C (zh) | 2001-07-09 | 2002-07-09 | 富含反式克罗米酚的克罗米酚组合物的用途 |
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Cited By (1)
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| CN104582686A (zh) * | 2012-08-21 | 2015-04-29 | 利普生物药剂公司 | 反式克罗米酚(trans-clomiphene)调配物和其用途 |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7173064B2 (en) | 2001-07-09 | 2007-02-06 | Repros Therapeutics Inc. | Methods and compositions with trans-clomiphene for treating wasting and lipodystrophy |
| CA2453337C (en) | 2001-07-09 | 2012-08-28 | Zonagen, Inc. | Methods and materials for the treatment of testosterone deficiency in men |
| US7737185B2 (en) * | 2001-07-09 | 2010-06-15 | Repros Therapeutics Inc. | Methods and compositions with trans-clomiphene |
| MX2007000050A (es) * | 2004-07-14 | 2007-07-10 | Repros Therapeutics Inc | Trans-clomifeno para el tratamiento de hipertrofia de prostata benigna, cancer de prostata, hipogonadismo, trigliceridos elevados y colesterol elevado. |
| KR20070100811A (ko) * | 2005-02-04 | 2007-10-11 | 레프로스 쎄라피우틱스 아이엔씨. | 남성불임의 치료를 위한 트랜스―클로미펜을 이용한 물질과치료방법 |
| NZ560551A (en) * | 2005-03-22 | 2010-02-26 | Repros Therapeutics Inc | Dosing regimes for trans-clomiphene |
| WO2008157335A2 (en) * | 2007-06-13 | 2008-12-24 | Quatrx Pharmaceuticals Company | Methods for the treatment of erectile dysfunction using fispemifene |
| US20110118355A1 (en) * | 2007-09-21 | 2011-05-19 | Harry Fisch | Treatment of migraine headaches using antiestrogens |
| ES2718912T3 (es) * | 2007-10-16 | 2019-07-05 | Repros Therapeutics Inc | Trans-clomifeno para el tratamiento de la diabetes en hombres hipogonadales |
| WO2009052377A1 (en) * | 2007-10-18 | 2009-04-23 | Harry Fisch | Treatment of migraine headaches using antiestrogens |
| US20090215733A1 (en) * | 2008-02-26 | 2009-08-27 | Michael Charles Scally | Therapy for the prophylaxis or treatment of adverse body composition changes and/or decreased muscle strength after androgen or gnrh analogue intake |
| TWI477276B (zh) | 2008-04-28 | 2015-03-21 | Repros Therapeutics Inc | 抗黃體素給藥方案 |
| RU2474424C2 (ru) * | 2010-09-24 | 2013-02-10 | Государственное образовательное учреждение высшего профессионального образования "Ивановская государственная медицинская академия Федерального агентства по здравоохранению и социальному развитию" | Способ коррекции гиперэстрадиолемии и нормогонадотропного гипогонадизма у мужчин |
| UA113291C2 (xx) | 2011-08-04 | 2017-01-10 | Метаболіти транскломіфену і їх застосування | |
| CA2881604C (en) * | 2011-08-09 | 2021-09-14 | Kenneth W. Adams | Use of aromatase inhibitor or estrogen blocker for increasing spermatogenesis or testosterone levels in males |
| SG10201704858PA (en) | 2012-05-31 | 2017-07-28 | Repros Therapeutics Inc | Formulations and methods for vaginal delivery of antiprogestins |
| EP2914268B1 (en) | 2012-11-02 | 2018-07-04 | Repros Therapeutics Inc. | Methods and compositions for treating progesterone-dependent conditions |
| CN104994877A (zh) | 2012-11-02 | 2015-10-21 | 利普生物药剂公司 | 用于癌症治疗的反式-克罗米芬 |
| US9814687B2 (en) * | 2014-08-20 | 2017-11-14 | Professional Compounding Centers Of America | Transdermal pharmaceutical compositions including C-SERMs for low testosterone levels in men |
| RU2586305C1 (ru) * | 2015-02-02 | 2016-06-10 | Государственное бюджетное образовательное учреждение высшего профессионального образования "Ивановская государственная медицинская академия" Министерства здравоохранения Российской Федерации | Способ лечения обструктивной азооспермии и криптозооспермии у пациентов с хроническим простатитом |
| 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 (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2914563A (en) * | 1957-08-06 | 1959-11-24 | Wm S Merrell Co | Therapeutic composition |
| IT951631B (it) | 1971-03-18 | 1973-07-10 | Richardson Merrell Spa | Composti utili per la separazione di isomeri ottici geometrici e strutturali e relativo procedimen to di sintesi |
| US4061733A (en) * | 1976-10-15 | 1977-12-06 | Narayan Vishwanath Gunjikar | Veterinary compositions for inducing estrus in animals and method |
| US4729999A (en) * | 1984-10-12 | 1988-03-08 | Bcm Technologies | Antiestrogen therapy for symptoms of estrogen deficiency |
| EP0206021B1 (de) | 1985-06-08 | 1988-08-10 | ASTA Pharma AG | Neue Derivate des 1,1,2,2-Tetramethyl-1,2-bis-(2-fluor-4-hydroxyphenyl)-ethans |
| US4820736A (en) * | 1987-03-20 | 1989-04-11 | Yale University | Use of clomiphene to predict fertility in a human female |
| GB8926171D0 (en) * | 1989-11-20 | 1990-01-10 | Applied Research Systems | Treatment of infertility |
| JPH04312522A (ja) | 1991-04-08 | 1992-11-04 | Yoshiaki Kawashima | 徐放性錠剤の製造方法 |
| US5681585A (en) * | 1991-12-24 | 1997-10-28 | Euro-Celtique, S.A. | Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer |
| US5580578A (en) * | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| US5776923A (en) * | 1993-01-19 | 1998-07-07 | Endorecherche, Inc. | Method of treating or preventing osteoporosis by adminstering dehydropiandrosterone |
| GB9405304D0 (en) * | 1994-03-16 | 1994-04-27 | Scherer Ltd R P | Delivery systems for hydrophobic drugs |
| US5650425A (en) * | 1994-04-04 | 1997-07-22 | Pharmos Corporation | Permanently ionic derivatives of steroid hormones and their antagonists |
| JPH10501814A (ja) | 1994-06-17 | 1998-02-17 | ユニバーシティ・オブ・ネブラスカ・ボード・オブ・リージェンツ | 生物的作用物質用のイン・シツゲル形成デリバリービヒクルおよびその使用方法 |
| RU2089188C1 (ru) * | 1994-07-13 | 1997-09-10 | Владимир Александрович Божедомов | Способ лечения мужского секреторного бесплодия |
| DE4435368A1 (de) * | 1994-09-22 | 1996-03-28 | Schering Ag | Verwendung von Aromatasehemmern zur Herstellung eines Arzneimittels zur Behandlung eines relativen Androgenmangels beim Mann |
| AU6824996A (en) * | 1995-08-17 | 1997-03-12 | Dyer, Alison Margaret | Controlled release products |
| US5773031A (en) * | 1996-02-27 | 1998-06-30 | L. Perrigo Company | Acetaminophen sustained-release formulation |
| IL120262A (en) * | 1996-02-28 | 2001-01-28 | Pfizer | Droloxifene and derivatives thereof for use in increasing serum testosterone levels |
| ES2565163T3 (es) * | 1996-10-28 | 2016-03-31 | General Mills, Inc. | Imbibición y encapsulación de partículas de liberación controlada y producto encapsulado |
| IL132120A0 (en) * | 1997-04-03 | 2001-03-19 | Guilford Pharm Inc | Biodegradable terephthalate polyester-poly (phosphate) polymers compositions articles and methods for making and using the same |
| US6653297B1 (en) * | 1997-07-03 | 2003-11-25 | Medical College Of Hampton Roads | Control of selective estrogen receptor modulators |
| US6342250B1 (en) * | 1997-09-25 | 2002-01-29 | Gel-Del Technologies, Inc. | Drug delivery devices comprising biodegradable protein for the controlled release of pharmacologically active agents and method of making the drug delivery devices |
| US6413533B1 (en) | 1998-05-07 | 2002-07-02 | The University Of Tennessee Research Corporation | Method for chemoprevention of prostate cancer |
| DE69935335T2 (de) * | 1998-08-07 | 2007-11-22 | Novartis Vaccines and Diagnostics, Inc., Emeryville | Pyrazole als modulatoren des östrogenrezeptors |
| US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| CO5180583A1 (es) * | 1999-06-11 | 2002-07-30 | Watson Pharmaceuticals Inc | Administracion de esteroides androgenicos no orales a las mujeres |
| AU6132700A (en) * | 1999-09-30 | 2001-04-05 | Chienna B.V. | Polymers loaded with bioactive agents |
| US6258802B1 (en) | 1999-10-06 | 2001-07-10 | Medical College Of Hampton Roads | Corticoid therapy |
| WO2001052823A2 (en) * | 2000-01-20 | 2001-07-26 | Noven Pharmaceuticals, Inc. | Compositions to effect the release profile in the transdermal administration of drugs |
| US7067557B2 (en) | 2000-05-26 | 2006-06-27 | Harry Fisch | Methods of treating androgen deficiency in men using selective antiestrogens |
| WO2001091744A1 (en) | 2000-05-26 | 2001-12-06 | Harry Fisch | Methods of treating androgen deficiency in men using selective antiestrogens |
| CN100448487C (zh) * | 2000-08-11 | 2009-01-07 | 惠氏公司 | 治疗雌激素受体阳性癌的方法 |
| US6503894B1 (en) * | 2000-08-30 | 2003-01-07 | Unimed Pharmaceuticals, Inc. | Pharmaceutical composition and method for treating hypogonadism |
| CA2462081A1 (en) | 2000-10-11 | 2002-04-18 | Laura Kragie | Composition and method of alleviating adverse side effects and/or enhancing efficacy of agents that inhibit aromatase |
| US6743448B2 (en) * | 2000-12-11 | 2004-06-01 | Abraham H. Kryger | Topical testosterone formulations and associated methods |
| CA2453337C (en) | 2001-07-09 | 2012-08-28 | Zonagen, Inc. | Methods and materials for the treatment of testosterone deficiency in men |
| US7173064B2 (en) * | 2001-07-09 | 2007-02-06 | Repros Therapeutics Inc. | Methods and compositions with trans-clomiphene for treating wasting and lipodystrophy |
| US6645974B2 (en) * | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
| EP1429779A2 (en) | 2001-09-21 | 2004-06-23 | Merck & Co., Inc. | Androstanes as androgen receptor modulators |
| US6600110B1 (en) * | 2001-10-01 | 2003-07-29 | Gram Precision | Portable digital readout scale |
| US20060269611A1 (en) * | 2001-11-29 | 2006-11-30 | Steiner Mitchell S | Prevention and treatment of androgen-deprivation induced osteoporosis |
| US7105679B2 (en) * | 2001-12-19 | 2006-09-12 | Kanojia Ramesh M | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
| JP4312522B2 (ja) | 2003-06-30 | 2009-08-12 | 株式会社リコー | 現像剤補給方法、現像剤補給装置、及び、画像形成装置 |
| MX2007000050A (es) | 2004-07-14 | 2007-07-10 | Repros Therapeutics Inc | Trans-clomifeno para el tratamiento de hipertrofia de prostata benigna, cancer de prostata, hipogonadismo, trigliceridos elevados y colesterol elevado. |
| KR20070100811A (ko) | 2005-02-04 | 2007-10-11 | 레프로스 쎄라피우틱스 아이엔씨. | 남성불임의 치료를 위한 트랜스―클로미펜을 이용한 물질과치료방법 |
| EP1853298A2 (en) * | 2005-02-11 | 2007-11-14 | Regeneron Pharmaceuticals, Inc. | Therapeutic combination of a vegf antagonist (vegf trap) and an anti-hypertensive agent |
| NZ560551A (en) | 2005-03-22 | 2010-02-26 | Repros Therapeutics Inc | Dosing regimes for trans-clomiphene |
| CN101309702A (zh) | 2005-08-05 | 2008-11-19 | 雷普罗斯治疗公司 | 使用克罗米酚治疗女性不育症的方法及其组合物 |
| EP1829534A1 (en) | 2006-03-02 | 2007-09-05 | Laboratorios Del Dr. Esteve, S.A. | Use of compounds binding to the sigma receptor for the treatment of metabolic syndrome |
| ES2718912T3 (es) * | 2007-10-16 | 2019-07-05 | Repros Therapeutics Inc | Trans-clomifeno para el tratamiento de la diabetes en hombres hipogonadales |
| US20100111901A1 (en) * | 2008-11-03 | 2010-05-06 | Auspex Pharmaceuticals, Inc. | Triazole inhibitors of aromatase |
| 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 |
| US20100144687A1 (en) * | 2008-12-05 | 2010-06-10 | Glaser Rebecca L | Pharmaceutical compositions containing testosterone and an aromatase inhibitor |
| CA2881604C (en) | 2011-08-09 | 2021-09-14 | Kenneth W. Adams | Use of aromatase inhibitor or estrogen blocker for increasing spermatogenesis or testosterone levels in males |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104582686A (zh) * | 2012-08-21 | 2015-04-29 | 利普生物药剂公司 | 反式克罗米酚(trans-clomiphene)调配物和其用途 |
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