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 PDFInfo
- 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
- Authority
- CN
- China
- Prior art keywords
- clomiphene
- trans
- pharmaceutical composition
- metabolite
- metabolites
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
Landscapes
- 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)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Gynecology & Obstetrics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pregnancy & Childbirth (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161515278P | 2011-08-04 | 2011-08-04 | |
| US61/515278 | 2011-08-04 | ||
| US61/515,278 | 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)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (https=) |
| EP (2) | EP3351527A1 (https=) |
| JP (2) | JP6433785B2 (https=) |
| KR (1) | KR20140054110A (https=) |
| CN (1) | CN103702975B (https=) |
| AU (2) | AU2012289964B2 (https=) |
| BR (1) | BR112014000908A2 (https=) |
| CA (1) | CA2841572C (https=) |
| CL (1) | CL2014000268A1 (https=) |
| CO (1) | CO6862154A2 (https=) |
| CR (1) | CR20140124A (https=) |
| EA (1) | EA201490416A1 (https=) |
| IL (1) | IL230287B (https=) |
| MX (1) | MX355316B (https=) |
| MY (2) | MY191802A (https=) |
| NI (1) | NI201400008A (https=) |
| PH (1) | PH12014500144A1 (https=) |
| SG (1) | SG10201606425WA (https=) |
| UA (1) | UA113291C2 (https=) |
| WO (1) | WO2013020017A1 (https=) |
| ZA (1) | ZA201400406B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120284764A1 (en) * | 2011-05-05 | 2012-11-08 | Keith Ball | Method and system for requesting services by a media device |
| UA113291C2 (xx) | 2011-08-04 | 2017-01-10 | Метаболіти транскломіфену і їх застосування | |
| SG11201407397WA (en) | 2012-05-31 | 2014-12-30 | Repros Therapeutics Inc | Formulations and methods for vaginal delivery of antiprogestins |
| ES2688821T3 (es) | 2012-11-02 | 2018-11-07 | Repros Therapeutics Inc. | Métodos y composiciones para tratar afecciones dependientes de la progesterona |
| WO2014070523A1 (en) * | 2012-11-02 | 2014-05-08 | Repros Therapeutics Inc. | Trans-clomiphene for use in cancer therapy |
| WO2017123577A1 (en) * | 2016-01-12 | 2017-07-20 | Repros Therapeutics Inc. | Trans-clomiphene and progesterone receptor antagonist combination therapy for treating hormone-dependent conditions |
| CN108883083A (zh) * | 2016-02-25 | 2018-11-23 | 艾森潘帕克制药股份有限公司 | 两种氯米芬异构体的口服剂型及使用其治疗继发性腺功能减退症的方法 |
| WO2017182097A1 (en) | 2016-04-22 | 2017-10-26 | F.I.S. - Fabbrica Italiana Sintetici S.P.A. | Process for the preparation of enclomiphene citrate having needle shaped crystal habit. |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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| US4061733A (en) | 1976-10-15 | 1977-12-06 | Narayan Vishwanath Gunjikar | Veterinary compositions for inducing estrus in animals and method |
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| DE3660489D1 (en) | 1985-06-08 | 1988-09-15 | Asta Pharma Ag | Derivatives of 1,1,2,2-tetramethyl-1,2-bis(2-fluoro-4-hydroxyphenyl) ethane |
| US4820736A (en) * | 1987-03-20 | 1989-04-11 | Yale University | Use of clomiphene to predict fertility in a human female |
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| UA113291C2 (xx) | 2011-08-04 | 2017-01-10 | Метаболіти транскломіфену і їх застосування | |
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-
2012
- 2012-03-08 UA UAA201402168A patent/UA113291C2/uk unknown
- 2012-08-03 JP JP2014524097A patent/JP6433785B2/ja not_active Expired - Fee Related
- 2012-08-03 AU AU2012289964A patent/AU2012289964B2/en not_active Ceased
- 2012-08-03 MY MYPI2017001676A patent/MY191802A/en unknown
- 2012-08-03 KR KR1020147004588A patent/KR20140054110A/ko not_active Ceased
- 2012-08-03 WO PCT/US2012/049451 patent/WO2013020017A1/en not_active Ceased
- 2012-08-03 PH PH1/2014/500144A patent/PH12014500144A1/en unknown
- 2012-08-03 BR BR112014000908A patent/BR112014000908A2/pt active Search and Examination
- 2012-08-03 EA EA201490416A patent/EA201490416A1/ru unknown
- 2012-08-03 EP EP18161551.9A patent/EP3351527A1/en not_active Withdrawn
- 2012-08-03 SG SG10201606425WA patent/SG10201606425WA/en unknown
- 2012-08-03 CN CN201280038230.6A patent/CN103702975B/zh not_active Expired - Fee Related
- 2012-08-03 EP EP12750508.9A patent/EP2744777A1/en not_active Withdrawn
- 2012-08-03 MY MYPI2014000022A patent/MY170718A/en unknown
- 2012-08-03 US US14/236,868 patent/US9981906B2/en not_active Expired - Fee Related
- 2012-08-03 MX MX2014000825A patent/MX355316B/es active IP Right Grant
- 2012-08-03 CA CA2841572A patent/CA2841572C/en not_active Expired - Fee Related
-
2014
- 2014-01-02 IL IL230287A patent/IL230287B/en active IP Right Grant
- 2014-01-17 ZA ZA2014/00406A patent/ZA201400406B/en unknown
- 2014-01-24 CO CO14014339A patent/CO6862154A2/es unknown
- 2014-01-30 NI NI201400008A patent/NI201400008A/es unknown
- 2014-02-03 CL CL2014000268A patent/CL2014000268A1/es unknown
- 2014-03-13 CR CR20140124A patent/CR20140124A/es unknown
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2017
- 2017-06-20 AU AU2017204171A patent/AU2017204171A1/en not_active Abandoned
-
2018
- 2018-10-01 JP JP2018186696A patent/JP2019023210A/ja active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Non-Patent Citations (3)
| Title |
|---|
| Clomiphene Analogs with Activity In Vitro and InVivo against Human Breast Cancer Cells;R. Jeffrey Baumann等;《Biochemical Pharmacology》;19980301;第55卷;841-851 * |
| Phenolic Metabolites of Clomiphene:[ (E,Z)-2-[4 - ( 1,2-Diphenyl-2-ch loroviny1)ph enoxylet hylldieth ylamine. Preparation, Electrophilicity, and Effects in MCF 7 Breast Cancer Cells;Peter C. Ruenitz等;《J. Med. Chem.》;19890101;第32卷(第1期);192-197 * |
| Quantification of clomiphene metabolite isomers in human plasma by rapid-resolution liquid chromatography–electrospray ionization–tandem mass spectrometry;Boian Ganchev等;《Anal Bioanal Chem》;20110501;第400卷(第10期);3429-3441 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20140163114A1 (en) | 2014-06-12 |
| EP2744777A1 (en) | 2014-06-25 |
| CN103702975A (zh) | 2014-04-02 |
| NI201400008A (es) | 2015-12-10 |
| US9981906B2 (en) | 2018-05-29 |
| EA201490416A1 (ru) | 2014-11-28 |
| AU2012289964A1 (en) | 2014-01-30 |
| UA113291C2 (xx) | 2017-01-10 |
| KR20140054110A (ko) | 2014-05-08 |
| PH12014500144A1 (en) | 2014-02-24 |
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| HK1196349A1 (zh) | 2014-12-12 |
| JP2014529584A (ja) | 2014-11-13 |
| SG10201606425WA (en) | 2016-09-29 |
| JP2019023210A (ja) | 2019-02-14 |
| IL230287B (en) | 2019-07-31 |
| NZ621892A (en) | 2016-03-31 |
| EP3351527A1 (en) | 2018-07-25 |
| BR112014000908A2 (pt) | 2017-02-21 |
| CO6862154A2 (es) | 2014-02-10 |
| CA2841572A1 (en) | 2013-02-07 |
| AU2012289964B2 (en) | 2017-03-23 |
| MX355316B (es) | 2018-04-16 |
| WO2013020017A1 (en) | 2013-02-07 |
| JP6433785B2 (ja) | 2018-12-05 |
| CA2841572C (en) | 2020-10-13 |
| MY191802A (en) | 2022-07-15 |
| ZA201400406B (en) | 2014-11-26 |
| MX2014000825A (es) | 2014-02-27 |
| AU2017204171A1 (en) | 2017-07-13 |
| IL230287A0 (en) | 2014-03-06 |
| CR20140124A (es) | 2014-05-13 |
| MY170718A (en) | 2019-08-27 |
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