CN103702975B - 反式-氯米芬代谢物及其用途 - Google Patents

反式-氯米芬代谢物及其用途 Download PDF

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Publication number
CN103702975B
CN103702975B CN201280038230.6A CN201280038230A CN103702975B CN 103702975 B CN103702975 B CN 103702975B CN 201280038230 A CN201280038230 A CN 201280038230A CN 103702975 B CN103702975 B CN 103702975B
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Prior art keywords
clomiphene
trans
pharmaceutical composition
metabolite
metabolites
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Expired - Fee Related
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CN201280038230.6A
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English (en)
Chinese (zh)
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CN103702975A (zh
Inventor
J.S.波多尔斯基
R.D.维勒
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Repros Therapeutics Inc
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Repros Therapeutics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • 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
    • A61P15/08—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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201280038230.6A 2011-08-04 2012-08-03 反式-氯米芬代谢物及其用途 Expired - Fee Related CN103702975B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161515278P 2011-08-04 2011-08-04
US61/515,278 2011-08-04
US61/515278 2011-08-04
PCT/US2012/049451 WO2013020017A1 (en) 2011-08-04 2012-08-03 Trans-clomiphene metabolites and uses thereof

Publications (2)

Publication Number Publication Date
CN103702975A CN103702975A (zh) 2014-04-02
CN103702975B true CN103702975B (zh) 2016-03-16

Family

ID=46724628

Family Applications (1)

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CN201280038230.6A Expired - Fee Related CN103702975B (zh) 2011-08-04 2012-08-03 反式-氯米芬代谢物及其用途

Country Status (21)

Country Link
US (1) US9981906B2 (enExample)
EP (2) EP2744777A1 (enExample)
JP (2) JP6433785B2 (enExample)
KR (1) KR20140054110A (enExample)
CN (1) CN103702975B (enExample)
AU (2) AU2012289964B2 (enExample)
BR (1) BR112014000908A2 (enExample)
CA (1) CA2841572C (enExample)
CL (1) CL2014000268A1 (enExample)
CO (1) CO6862154A2 (enExample)
CR (1) CR20140124A (enExample)
EA (1) EA201490416A1 (enExample)
IL (1) IL230287B (enExample)
MX (1) MX355316B (enExample)
MY (2) MY170718A (enExample)
NI (1) NI201400008A (enExample)
PH (1) PH12014500144A1 (enExample)
SG (1) SG10201606425WA (enExample)
UA (1) UA113291C2 (enExample)
WO (1) WO2013020017A1 (enExample)
ZA (1) ZA201400406B (enExample)

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US10328022B2 (en) 2012-05-31 2019-06-25 Repros Therapeutics Inc. Formulations and methods for vaginal delivery of antiprogestins
HK1211852A1 (en) 2012-11-02 2016-06-03 Repros Therapeutics Inc. Methods and compositions for treating progesterone-dependent conditions
WO2014070523A1 (en) * 2012-11-02 2014-05-08 Repros Therapeutics Inc. Trans-clomiphene for use in cancer therapy
US20190008804A1 (en) * 2016-01-12 2019-01-10 Repros Therapeutics Inc. Trans-Clomiphene and Progesterone Receptor Antagonist Combination Therapy for Treating Hormone-Dependent Conditions
KR20180112048A (ko) * 2016-02-25 2018-10-11 아스펜 파크 파마슈티컬스 인코포레이티드 클로미펜 이성질체들의 경구 제형 및 이차 생식선 기능저하증 치료를 위하여 이들을 사용하는 방법
EP3368506B1 (en) 2016-04-22 2023-09-06 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Process for the preparation of enclomiphene citrate having needle shaped crystal habit.

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CN101115709A (zh) * 2004-12-13 2008-01-30 小野药品工业株式会社 氨基羧酸衍生物及其医药用途

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Publication number Publication date
BR112014000908A2 (pt) 2017-02-21
NZ621892A (en) 2016-03-31
US20140163114A1 (en) 2014-06-12
JP6433785B2 (ja) 2018-12-05
JP2014529584A (ja) 2014-11-13
KR20140054110A (ko) 2014-05-08
EA201490416A1 (ru) 2014-11-28
CR20140124A (es) 2014-05-13
AU2017204171A1 (en) 2017-07-13
JP2019023210A (ja) 2019-02-14
MY170718A (en) 2019-08-27
AU2012289964A1 (en) 2014-01-30
MY191802A (en) 2022-07-15
CA2841572C (en) 2020-10-13
ZA201400406B (en) 2014-11-26
IL230287A0 (en) 2014-03-06
CL2014000268A1 (es) 2014-11-14
CO6862154A2 (es) 2014-02-10
MX2014000825A (es) 2014-02-27
AU2012289964B2 (en) 2017-03-23
SG10201606425WA (en) 2016-09-29
EP3351527A1 (en) 2018-07-25
MX355316B (es) 2018-04-16
US9981906B2 (en) 2018-05-29
UA113291C2 (xx) 2017-01-10
WO2013020017A1 (en) 2013-02-07
IL230287B (en) 2019-07-31
PH12014500144A1 (en) 2014-02-24
CA2841572A1 (en) 2013-02-07
CN103702975A (zh) 2014-04-02
HK1196349A1 (zh) 2014-12-12
EP2744777A1 (en) 2014-06-25
NI201400008A (es) 2015-12-10

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