CN104582686A - 反式克罗米酚(trans-clomiphene)调配物和其用途 - Google Patents

反式克罗米酚(trans-clomiphene)调配物和其用途 Download PDF

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Publication number
CN104582686A
CN104582686A CN201380044056.0A CN201380044056A CN104582686A CN 104582686 A CN104582686 A CN 104582686A CN 201380044056 A CN201380044056 A CN 201380044056A CN 104582686 A CN104582686 A CN 104582686A
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CN
China
Prior art keywords
trans
clomiphene
pharmaceutical formulation
particle size
compound
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Pending
Application number
CN201380044056.0A
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English (en)
Chinese (zh)
Inventor
J.S.波多尔斯基
K.苏
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Repros Therapeutics Inc
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Repros Therapeutics Inc
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Application filed by Repros Therapeutics Inc filed Critical Repros Therapeutics Inc
Publication of CN104582686A publication Critical patent/CN104582686A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00—Stock material or miscellaneous articles
    • Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982—Particulate matter [e.g., sphere, flake, etc.]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Dispersion Chemistry (AREA)
  • Neurology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201380044056.0A 2012-08-21 2013-03-15 反式克罗米酚(trans-clomiphene)调配物和其用途 Pending CN104582686A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261691722P 2012-08-21 2012-08-21
US61/691722 2012-08-21
PCT/US2013/032659 WO2014031177A1 (en) 2012-08-21 2013-03-15 Trans-clomiphene formulations and uses thereof

Publications (1)

Publication Number Publication Date
CN104582686A true CN104582686A (zh) 2015-04-29

Family

ID=48014380

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380044056.0A Pending CN104582686A (zh) 2012-08-21 2013-03-15 反式克罗米酚(trans-clomiphene)调配物和其用途

Country Status (22)

Country Link
US (1) US20150202167A1 (https=)
EP (1) EP2887922A1 (https=)
JP (2) JP2015527360A (https=)
KR (1) KR20150041793A (https=)
CN (1) CN104582686A (https=)
AU (1) AU2013306393A1 (https=)
BR (1) BR112015002288A2 (https=)
CA (1) CA2880388A1 (https=)
CL (1) CL2015000311A1 (https=)
CR (1) CR20150096A (https=)
EA (1) EA201590421A1 (https=)
HK (1) HK1209636A1 (https=)
IL (1) IL236911A0 (https=)
IN (1) IN2015DN01698A (https=)
MX (1) MX2015001912A (https=)
NI (1) NI201500022A (https=)
NZ (1) NZ704679A (https=)
PH (1) PH12015500331A1 (https=)
SG (2) SG11201500641TA (https=)
UA (1) UA113324C2 (https=)
WO (1) WO2014031177A1 (https=)
ZA (1) ZA201501124B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US11737934B2 (en) 2015-10-14 2023-08-29 Qfix Systems, Llc MRI compatible patient trolley

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA113291C2 (xx) 2011-08-04 2017-01-10 Метаболіти транскломіфену і їх застосування
WO2014070523A1 (en) 2012-11-02 2014-05-08 Repros Therapeutics Inc. Trans-clomiphene for use in cancer therapy
EP3015454A1 (en) 2014-10-28 2016-05-04 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Stable solid form of trans-Clomiphene citrate
EP3015453B1 (en) 2014-10-28 2016-10-12 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Process for the preparation of Clomiphene
CA3098725A1 (en) 2019-11-14 2021-05-14 Apotex Inc. Zuclpomiphene salts and crystalline forms thereof
CA3098552A1 (en) 2019-11-14 2021-05-14 Apotex Inc. Processes for the preparation of zuclomiphene and intermediates thereof
CA3105944A1 (en) * 2020-01-22 2021-07-22 Apotex Inc. Crystalline forms of zuclomiphene citrate
EP3907213A1 (en) 2020-05-04 2021-11-10 Pcas Processes for the production of isomerically pure or enriched cis-clomiphene
US11578025B2 (en) 2020-10-19 2023-02-14 Apotex Inc. Processes for the preparation of zuclomiphene intermediates

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1954807A (zh) * 2001-07-09 2007-05-02 佐纳根有限公司 富含反式克罗米酚的克罗米酚组合物
US20070202166A1 (en) * 2006-02-23 2007-08-30 Marvin Heuer Method for increasing the rate and consistency of bioavailability of supplemental dietary ingredients

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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
RU2006138235A (ru) * 2004-03-31 2008-05-10 Трофоджен, Инк. (Us) Суперагонисты человеческих гликопротеиновых гормонов и способы их применения
WO2006019916A1 (en) 2004-07-14 2006-02-23 Repros Therapeutics Inc. Trans-clomiphene for the treatment of benign prostate hypertrophy, prostate cancer, hypogonadism, elevated triglycerides and high cholesterol
SG185311A1 (en) 2007-10-16 2012-11-29 Repros Therapeutics Inc Trans-clomiphene for metabolic syndrome
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1954807A (zh) * 2001-07-09 2007-05-02 佐纳根有限公司 富含反式克罗米酚的克罗米酚组合物
US20070202166A1 (en) * 2006-02-23 2007-08-30 Marvin Heuer Method for increasing the rate and consistency of bioavailability of supplemental dietary ingredients

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11737934B2 (en) 2015-10-14 2023-08-29 Qfix Systems, Llc MRI compatible patient trolley
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

Also Published As

Publication number Publication date
JP2015527360A (ja) 2015-09-17
NZ704679A (en) 2016-02-26
CL2015000311A1 (es) 2015-08-14
IL236911A0 (en) 2015-03-31
KR20150041793A (ko) 2015-04-17
US20150202167A1 (en) 2015-07-23
IN2015DN01698A (https=) 2015-07-03
HK1209636A1 (en) 2016-04-08
JP2017206562A (ja) 2017-11-24
WO2014031177A1 (en) 2014-02-27
AU2013306393A1 (en) 2015-02-19
CR20150096A (es) 2015-05-04
CA2880388A1 (en) 2014-02-27
PH12015500331A1 (en) 2015-04-20
NI201500022A (es) 2016-02-01
SG10201704820SA (en) 2017-07-28
UA113324C2 (xx) 2017-01-10
EA201590421A1 (ru) 2015-06-30
MX2015001912A (es) 2015-06-05
ZA201501124B (en) 2016-04-28
SG11201500641TA (en) 2015-04-29
BR112015002288A2 (pt) 2017-07-04
EP2887922A1 (en) 2015-07-01

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