CN1672685A - 一种新的避孕药物 - Google Patents

一种新的避孕药物 Download PDF

Info

Publication number: CN1672685A
Authority: CN; China
Prior art keywords: estradione; acetylene; preparation; estradiol; corpus luteum
Prior art date: 2004-03-26
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

Application number

CNA2004100296007A

Other languages

English (en)

Chinese (zh)

Inventor

董可文

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

DONG KEJUAN

Original Assignee

DONG KEJUAN

Priority date (The priority date 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 date listed.)

2004-03-26

Filing date

2004-03-26

Publication date

2005-09-28

2004-03-26 Application filed by DONG KEJUAN filed Critical DONG KEJUAN

2004-03-26 Priority to CNA2004100296007A priority Critical patent/CN1672685A/zh

2004-04-14 Priority to PCT/CN2004/000348 priority patent/WO2005092346A1/fr

2005-09-28 Publication of CN1672685A publication Critical patent/CN1672685A/zh

Status Pending legal-status Critical Current

Links

239000003814 drug Substances 0.000 title claims abstract description 61
238000002360 preparation method Methods 0.000 claims abstract description 63
RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims abstract description 60
229940011871 estrogen Drugs 0.000 claims abstract description 40
239000000262 estrogen Substances 0.000 claims abstract description 40
229960003387 progesterone Drugs 0.000 claims abstract description 35
239000000186 progesterone Substances 0.000 claims abstract description 35
238000000034 method Methods 0.000 claims abstract description 22
125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 56
IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 claims description 55
HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 55
210000004246 corpus luteum Anatomy 0.000 claims description 32
229940079593 drug Drugs 0.000 claims description 19
230000001076 estrogenic effect Effects 0.000 claims description 19
239000000126 substance Substances 0.000 claims description 17
230000003203 everyday effect Effects 0.000 claims description 15
VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 13
229960005309 estradiol Drugs 0.000 claims description 11
150000002576 ketones Chemical class 0.000 claims description 11
BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 10
BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 10
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229960002568 ethinylestradiol Drugs 0.000 claims description 10
238000004806 packaging method and process Methods 0.000 claims description 10
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239000000825 pharmaceutical preparation Substances 0.000 claims description 10
229930182833 estradiol Natural products 0.000 claims description 9
WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims description 8
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VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 claims description 7
DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims description 6
RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 6
DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims description 6
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RPLCPCMSCLEKRS-BPIQYHPVSA-N desogestrel Chemical compound C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 RPLCPCMSCLEKRS-BPIQYHPVSA-N 0.000 claims description 6
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IMSSROKUHAOUJS-MJCUULBUSA-N mestranol Chemical compound C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(OC)=CC=C3[C@H]21 IMSSROKUHAOUJS-MJCUULBUSA-N 0.000 claims description 6
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DBPWSSGDRRHUNT-CEGNMAFCSA-N 17α-hydroxyprogesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 DBPWSSGDRRHUNT-CEGNMAFCSA-N 0.000 claims description 3
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UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 claims description 3
VQOAQMIKPYNCMV-FMQUCBEESA-N Diethylstilbestrol dimethyl ether Chemical compound C=1C=C(OC)C=CC=1C(/CC)=C(\CC)C1=CC=C(OC)C=C1 VQOAQMIKPYNCMV-FMQUCBEESA-N 0.000 claims description 3
UOACKFBJUYNSLK-XRKIENNPSA-N Estradiol Cypionate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H](C4=CC=C(O)C=C4CC3)CC[C@@]21C)C(=O)CCC1CCCC1 UOACKFBJUYNSLK-XRKIENNPSA-N 0.000 claims description 3
RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims description 3
BJJXHLWLUDYTGC-ANULTFPQSA-N Gestrinone Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](CC)([C@](CC3)(O)C#C)C=C3)C3=C21 BJJXHLWLUDYTGC-ANULTFPQSA-N 0.000 claims description 3
APTGJECXMIKIET-WOSSHHRXSA-N Norethindrone enanthate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)CCCCCC)[C@@]1(C)CC2 APTGJECXMIKIET-WOSSHHRXSA-N 0.000 claims description 3
QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
WAHQVRCNDCHDIB-QZYSPNBYSA-N [(3s,8r,9s,10r,13s,14s,17r)-17-acetyl-17-acetyloxy-6,10,13-trimethyl-1,2,3,8,9,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-yl] 3-cyclopentylpropanoate Chemical compound O([C@@H]1C=C2C(C)=C[C@H]3[C@@H]4CC[C@]([C@]4(CC[C@@H]3[C@@]2(C)CC1)C)(OC(=O)C)C(C)=O)C(=O)CCC1CCCC1 WAHQVRCNDCHDIB-QZYSPNBYSA-N 0.000 claims description 3
VZMLEMYJUIIHNF-QURGRASLSA-N [4-[(e)-4-(4-propanoyloxyphenyl)hex-3-en-3-yl]phenyl] propanoate Chemical compound C1=CC(OC(=O)CC)=CC=C1C(\CC)=C(/CC)C1=CC=C(OC(=O)CC)C=C1 VZMLEMYJUIIHNF-QURGRASLSA-N 0.000 claims description 3
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 3
KDPAWGWELVVRCH-UHFFFAOYSA-M bromoacetate Chemical compound [O-]C(=O)CBr KDPAWGWELVVRCH-UHFFFAOYSA-M 0.000 claims description 3
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BFPSDSIWYFKGBC-UHFFFAOYSA-N chlorotrianisene Chemical compound C1=CC(OC)=CC=C1C(Cl)=C(C=1C=CC(OC)=CC=1)C1=CC=C(OC)C=C1 BFPSDSIWYFKGBC-UHFFFAOYSA-N 0.000 claims description 3
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Classifications

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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
- 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
- A61P15/18—Feminine contraceptives
- 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
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/34—Gestagens

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Health & Medical Sciences (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
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Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
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CNA2004100296007A 2004-03-26 2004-03-26 一种新的避孕药物 Pending CN1672685A (zh)

Priority Applications (2)

Application Number	Priority Date	Filing Date	Title
CNA2004100296007A CN1672685A (zh)	2004-03-26	2004-03-26	一种新的避孕药物
PCT/CN2004/000348 WO2005092346A1 (fr)	2004-03-26	2004-04-14	Utilisation d'une combinaison d'oestrogene et de progestine a dose ultra-faible pour une contraception orale de longue duree

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
CNA2004100296007A CN1672685A (zh)	2004-03-26	2004-03-26	一种新的避孕药物

Publications (1)

Publication Number	Publication Date
CN1672685A true CN1672685A (zh)	2005-09-28

Family

ID=35045627

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CNA2004100296007A Pending CN1672685A (zh)	2004-03-26	2004-03-26	一种新的避孕药物

Country Status (2)

Country	Link
CN (1)	CN1672685A (fr)
WO (1)	WO2005092346A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN102302779A (zh) *	2011-07-29	2012-01-04	岳中瑾	治疗包茎的乳膏制剂及其应用
CN101848716B (zh) *	2007-11-05	2012-11-28	拜耳先灵医药股份有限公司	与雌激素以及一种或多种药学上可接受的赋形剂/载体组合的助孕剂用于无乳糖口服避孕药的用途
CN101455644B (zh) *	2008-02-05	2013-05-01	北京紫竹药业有限公司	一种长效复方避孕微球及其制备
CN107995864A (zh) *	2015-05-18	2018-05-04	敏捷治疗公司	避孕组合物及提高效能和调节副作用的方法
CN114259498A (zh) *	2021-12-02	2022-04-01	南通联亚药业有限公司	一种包含去氧孕烯和炔雌醇的药物组合物及其制备方法和应用
WO2022246634A1 (fr) *	2021-05-25	2022-12-01	Zhejiang Jiachi Development Pharmaceuticals Ltd.	Compositions pour le traitement de l'insomnie et leurs utilisations

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20070111975A1 (en) *	2004-10-07	2007-05-17	Duramed Pharmaceuticals, Inc.	Methods of Hormonal Treatment Utilizing Ascending-Dose Extended Cycle Regimens
BRPI0819571A2 (pt) *	2007-12-20	2019-09-24	Teva Womenss Health Inc	"método para contracepção de emergência, pacote farmacêutico para contracepção de emergência e composição farmacêutica"

2004
- 2004-03-26 CN CNA2004100296007A patent/CN1672685A/zh active Pending
- 2004-04-14 WO PCT/CN2004/000348 patent/WO2005092346A1/fr not_active Ceased

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN101848716B (zh) *	2007-11-05	2012-11-28	拜耳先灵医药股份有限公司	与雌激素以及一种或多种药学上可接受的赋形剂/载体组合的助孕剂用于无乳糖口服避孕药的用途
CN101455644B (zh) *	2008-02-05	2013-05-01	北京紫竹药业有限公司	一种长效复方避孕微球及其制备
CN102302779A (zh) *	2011-07-29	2012-01-04	岳中瑾	治疗包茎的乳膏制剂及其应用
CN107995864A (zh) *	2015-05-18	2018-05-04	敏捷治疗公司	避孕组合物及提高效能和调节副作用的方法
WO2022246634A1 (fr) *	2021-05-25	2022-12-01	Zhejiang Jiachi Development Pharmaceuticals Ltd.	Compositions pour le traitement de l'insomnie et leurs utilisations
CN114259498A (zh) *	2021-12-02	2022-04-01	南通联亚药业有限公司	一种包含去氧孕烯和炔雌醇的药物组合物及其制备方法和应用
CN114259498B (zh) *	2021-12-02	2023-04-28	南通联亚药业股份有限公司	一种包含去氧孕烯和炔雌醇的药物组合物及其制备方法和应用

Also Published As

Publication number	Publication date
WO2005092346A1 (fr)	2005-10-06

Publication	Publication Date	Title
US5108995A (en)	1992-04-28	Hormone preparation and method
US5585370A (en)	1996-12-17	Hormone preparation and method
EP0559240B1 (fr)	2001-12-05	Packages contraceptives contenant de l'estrogen et du progestin
CA2256977C (fr)	2008-11-25	Methodes de contraception orale comprenant une utilisation prolongee de l'agent contraceptif
US5256421A (en)	1993-10-26	Hormone preparation and method
KR100847346B1 (ko)	2008-07-21	여성 성기능장애를 치료하기 위한 방법 및 제제
RU2114621C1 (ru)	1998-07-10	Композиции и способ предупреждения зачатия
JP5563227B2 (ja)	2014-07-30	ホルモン置換療法のためのドロスピレノン
KR100849919B1 (ko)	2008-08-04	에스트로겐 대체 요법으로 치료중인 여성의 호르몬결핍증을 치료하기 위한 에스트로겐 및 안드로겐의 조합
JP2015163646A (ja)	2015-09-10	緊急避妊のための医薬組成物及び処置方法
CN1358104A (zh)	2002-07-10	低剂量雌激素间断激素补偿治疗
US20030191096A1 (en)	2003-10-09	Method of hormonal therapy
PT646008E (pt)	2000-04-28	Minimizacao de hemorragias secundarias associadas a progestina
CN1672685A (zh)	2005-09-28	一种新的避孕药物
US20030018018A1 (en)	2003-01-23	Ultra low dose oral contraceptives with sustained efficacy and induced amenorrhea
JP2001523639A (ja)	2001-11-27	プロゲストゲン−抗プロゲストゲンレジメン
EP0472628A1 (fr)	1992-03-04	Utilisation de derives de melatonine afin d'effectuer la contraception
CA1332228C (fr)	1994-10-04	Formulation et methode pour le traitement de remplacement de l'estrogene
CN1395932A (zh)	2003-02-12	雌激素/孕激素/抗孕激素的应用,其组合物和药盒
JP2007197459A (ja)	2007-08-09	月経の出血を少なくし維持された効力を持つ超低投与量避妊薬
US20210386757A1 (en)	2021-12-16	Methods of Treating Menopausal Symptoms Using Low Dose Progesterone
IE83631B1 (en)		Hormone preparation and method
IL94411A (en)	1996-10-16	Compositions comprising an analog of melatonin in combination with progestogen and/or estrogen for effecting contraception
IE84449B1 (en)	2006-12-13	Contraceptive packages containing oestrogen and progestin

Legal Events

Date	Code	Title
2005-09-28	C06	Publication
2005-09-28	PB01	Publication
2005-11-23	C10	Entry into substantive examination
2005-11-23	SE01	Entry into force of request for substantive examination
2007-06-27	C02	Deemed withdrawal of patent application after publication (patent law 2001)
2007-06-27	WD01	Invention patent application deemed withdrawn after publication