NZ536618A - An oily pharmaceutical composition for use as contraceptive and/or HRT comprising etonogesterel undecanoate and/or etonogestrel decanoate and/or etonogestrel dodecanoate - Google Patents
An oily pharmaceutical composition for use as contraceptive and/or HRT comprising etonogesterel undecanoate and/or etonogestrel decanoate and/or etonogestrel dodecanoateInfo
- Publication number
- NZ536618A NZ536618A NZ536618A NZ53661803A NZ536618A NZ 536618 A NZ536618 A NZ 536618A NZ 536618 A NZ536618 A NZ 536618A NZ 53661803 A NZ53661803 A NZ 53661803A NZ 536618 A NZ536618 A NZ 536618A
- Authority
- NZ
- New Zealand
- Prior art keywords
- etonogestrel
- undecanoate
- contraceptively
- therapeutically effective
- decanoate
- Prior art date
Links
- 229960002941 etonogestrel Drugs 0.000 title claims abstract description 126
- GCKFUYQCUCGESZ-BPIQYHPVSA-N etonogestrel Chemical compound O=C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 GCKFUYQCUCGESZ-BPIQYHPVSA-N 0.000 title claims abstract description 123
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 title claims abstract description 46
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 title claims abstract description 21
- POULHZVOKOAJMA-UHFFFAOYSA-M dodecanoate Chemical compound CCCCCCCCCCCC([O-])=O POULHZVOKOAJMA-UHFFFAOYSA-M 0.000 title claims abstract description 19
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 11
- 239000003433 contraceptive agent Substances 0.000 title claims abstract description 7
- 230000002254 contraceptive effect Effects 0.000 title claims abstract description 7
- YSGQGNQWBLYHPE-CFUSNLFHSA-N (7r,8r,9s,10r,13s,14s,17s)-17-hydroxy-7,13-dimethyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3-one Chemical group C1C[C@]2(C)[C@@H](O)CC[C@H]2[C@@H]2[C@H](C)CC3=CC(=O)CC[C@@H]3[C@H]21 YSGQGNQWBLYHPE-CFUSNLFHSA-N 0.000 claims description 25
- 150000002148 esters Chemical class 0.000 claims description 19
- 239000003814 drug Substances 0.000 claims description 14
- 238000002360 preparation method Methods 0.000 claims description 14
- 239000003098 androgen Substances 0.000 claims description 13
- 229940011871 estrogen Drugs 0.000 claims description 10
- 239000000262 estrogen Substances 0.000 claims description 10
- 239000007924 injection Substances 0.000 claims description 9
- 238000002347 injection Methods 0.000 claims description 9
- 238000002560 therapeutic procedure Methods 0.000 abstract description 2
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 32
- 239000000243 solution Substances 0.000 description 31
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 30
- 239000003921 oil Substances 0.000 description 21
- 235000019198 oils Nutrition 0.000 description 21
- 241000220438 Arachis Species 0.000 description 18
- 235000003911 Arachis Nutrition 0.000 description 18
- 238000002657 hormone replacement therapy Methods 0.000 description 18
- 239000002904 solvent Substances 0.000 description 18
- 229960002903 benzyl benzoate Drugs 0.000 description 16
- IAFQYUQIAOWKSB-UHFFFAOYSA-N Ethyl undecanoate Chemical compound CCCCCCCCCCC(=O)OCC IAFQYUQIAOWKSB-UHFFFAOYSA-N 0.000 description 15
- 241000283973 Oryctolagus cuniculus Species 0.000 description 15
- 229960003604 testosterone Drugs 0.000 description 15
- -1 etonogestrel ester Chemical class 0.000 description 14
- 150000001875 compounds Chemical class 0.000 description 11
- 239000000583 progesterone congener Substances 0.000 description 10
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 9
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 9
- VOCBWIIFXDYGNZ-IXKNJLPQSA-N testosterone enanthate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCC)[C@@]1(C)CC2 VOCBWIIFXDYGNZ-IXKNJLPQSA-N 0.000 description 9
- 229960000746 testosterone undecanoate Drugs 0.000 description 9
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 description 8
- 229960003484 testosterone enanthate Drugs 0.000 description 8
- 238000005160 1H NMR spectroscopy Methods 0.000 description 7
- 238000000034 method Methods 0.000 description 7
- UDSFVOAUHKGBEK-CNQKSJKFSA-N testosterone undecanoate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCCC)[C@@]1(C)CC2 UDSFVOAUHKGBEK-CNQKSJKFSA-N 0.000 description 7
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- MNWFXJYAOYHMED-UHFFFAOYSA-N heptanoic acid Chemical compound CCCCCCC(O)=O MNWFXJYAOYHMED-UHFFFAOYSA-N 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 150000003509 tertiary alcohols Chemical class 0.000 description 6
- SZHOJFHSIKHZHA-UHFFFAOYSA-N tridecanoic acid Chemical compound CCCCCCCCCCCCC(O)=O SZHOJFHSIKHZHA-UHFFFAOYSA-N 0.000 description 6
- 239000000654 additive Substances 0.000 description 5
- 229950007169 buciclate Drugs 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 208000035475 disorder Diseases 0.000 description 5
- 238000007918 intramuscular administration Methods 0.000 description 5
- 210000002966 serum Anatomy 0.000 description 5
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 4
- WQEPLUUGTLDZJY-UHFFFAOYSA-M pentadecanoate Chemical compound CCCCCCCCCCCCCCC([O-])=O WQEPLUUGTLDZJY-UHFFFAOYSA-M 0.000 description 4
- 230000000144 pharmacologic effect Effects 0.000 description 4
- 230000002265 prevention Effects 0.000 description 4
- 230000021595 spermatogenesis Effects 0.000 description 4
- 150000003431 steroids Chemical class 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- 238000003556 assay Methods 0.000 description 3
- MNWFXJYAOYHMED-UHFFFAOYSA-M heptanoate Chemical compound CCCCCCC([O-])=O MNWFXJYAOYHMED-UHFFFAOYSA-M 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- 230000036470 plasma concentration Effects 0.000 description 3
- 230000001629 suppression Effects 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 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 description 2
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 2
- VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 description 2
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
- 102000012673 Follicle Stimulating Hormone Human genes 0.000 description 2
- 108010079345 Follicle Stimulating Hormone Proteins 0.000 description 2
- 102000009151 Luteinizing Hormone Human genes 0.000 description 2
- 108010073521 Luteinizing Hormone Proteins 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- 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 description 2
- 230000000996 additive effect Effects 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 239000012267 brine Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 150000001244 carboxylic acid anhydrides Chemical class 0.000 description 2
- 238000004440 column chromatography Methods 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 210000004696 endometrium Anatomy 0.000 description 2
- 229930182833 estradiol Natural products 0.000 description 2
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 description 2
- 229960002568 ethinylestradiol Drugs 0.000 description 2
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 2
- 229940093471 ethyl oleate Drugs 0.000 description 2
- 229940028334 follicle stimulating hormone Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000002583 male contraceptive agent Substances 0.000 description 2
- 239000012074 organic phase Substances 0.000 description 2
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- 229940095055 progestogen systemic hormonal contraceptives Drugs 0.000 description 2
- 238000011555 rabbit model Methods 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- 230000009933 reproductive health Effects 0.000 description 2
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- QAEDZJGFFMLHHQ-UHFFFAOYSA-N trifluoroacetic anhydride Chemical compound FC(F)(F)C(=O)OC(=O)C(F)(F)F QAEDZJGFFMLHHQ-UHFFFAOYSA-N 0.000 description 2
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- QGLVWTFUWVTDEQ-UHFFFAOYSA-N 2-chloro-3-methoxyphenol Chemical compound COC1=CC=CC(O)=C1Cl QGLVWTFUWVTDEQ-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- BALGERHMIXFENA-UHFFFAOYSA-N 4-butylcyclohexane-1-carboxylic acid Chemical compound CCCCC1CCC(C(O)=O)CC1 BALGERHMIXFENA-UHFFFAOYSA-N 0.000 description 1
- 229960000549 4-dimethylaminophenol Drugs 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
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- 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 description 1
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- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class 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 description 1
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- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
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- ODZDZTOROXGJAV-IRWJKHRASA-N [(8r,9s,10r,13s,14s,17s)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 4-butylcyclohexane-1-carboxylate Chemical compound C1CC(CCCC)CCC1C(=O)O[C@@H]1[C@@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4CC[C@H]3[C@@H]2CC1 ODZDZTOROXGJAV-IRWJKHRASA-N 0.000 description 1
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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 description 1
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- 238000003786 synthesis reaction Methods 0.000 description 1
- 150000003515 testosterones Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000005919 time-dependent effect Effects 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- WDQDGKVRHNKEBJ-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O.CCCCCCCCCCC(O)=O WDQDGKVRHNKEBJ-UHFFFAOYSA-N 0.000 description 1
- 229940044953 vaginal ring Drugs 0.000 description 1
- 239000006213 vaginal ring Substances 0.000 description 1
Classifications
-
- 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
- A61K31/568—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 positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
-
- 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
-
- 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
- A61K31/568—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 positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/569—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 positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine 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
- A61P15/18—Feminine contraceptives
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
-
- 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
- A61P5/26—Androgens
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Pregnancy & Childbirth (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02077118 | 2002-05-30 | ||
| PCT/EP2003/050188 WO2003101374A2 (en) | 2002-05-30 | 2003-05-22 | Use of new etonogestrel esters |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ536618A true NZ536618A (en) | 2007-06-29 |
Family
ID=29595013
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ536618A NZ536618A (en) | 2002-05-30 | 2003-05-22 | An oily pharmaceutical composition for use as contraceptive and/or HRT comprising etonogesterel undecanoate and/or etonogestrel decanoate and/or etonogestrel dodecanoate |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US20050222114A1 (enExample) |
| EP (1) | EP1513588B1 (enExample) |
| JP (1) | JP2005532336A (enExample) |
| KR (1) | KR20050005507A (enExample) |
| CN (1) | CN1655848A (enExample) |
| AR (1) | AR040129A1 (enExample) |
| AT (1) | ATE394140T1 (enExample) |
| AU (1) | AU2003246740B2 (enExample) |
| BR (1) | BR0311248A (enExample) |
| CA (1) | CA2487293A1 (enExample) |
| DE (1) | DE60320786D1 (enExample) |
| ES (1) | ES2305498T3 (enExample) |
| HR (1) | HRP20041127A2 (enExample) |
| IL (1) | IL165125A0 (enExample) |
| IS (1) | IS7537A (enExample) |
| MX (1) | MXPA04011798A (enExample) |
| NO (1) | NO20044903L (enExample) |
| NZ (1) | NZ536618A (enExample) |
| PE (1) | PE20040042A1 (enExample) |
| PL (1) | PL373295A1 (enExample) |
| RS (1) | RS101004A (enExample) |
| RU (1) | RU2322986C2 (enExample) |
| TW (1) | TW200400041A (enExample) |
| UA (1) | UA80703C2 (enExample) |
| WO (1) | WO2003101374A2 (enExample) |
| ZA (1) | ZA200409498B (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200403065A (en) * | 2002-05-30 | 2004-03-01 | Akzo Nobel Nv | New etonogestrel esters |
| US20130123523A1 (en) * | 2011-11-10 | 2013-05-16 | Klaus Nickisch | Methods for the preparation of etonogestrel and desogestrel |
| DE102012211511A1 (de) * | 2012-07-03 | 2014-01-09 | Siemens Aktiengesellschaft | Bestimmung der Eignung einer Ressource |
| MX2020003470A (es) * | 2017-10-19 | 2020-10-01 | Evestra Inc | Anticonceptivos de profarmacos de progestina de accion mas prolongada. |
| CN111057120B (zh) * | 2019-12-27 | 2021-04-27 | 苏州翔实医药发展有限公司 | 一种依托孕烯衍生物a及其制备方法和用途 |
| WO2021252761A2 (en) * | 2020-06-11 | 2021-12-16 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Monomeric and oligomeric compound embodiments as contraceptives and therapies and methods of making and using the same |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4227989A1 (de) * | 1992-08-21 | 1994-06-09 | Schering Ag | Mittel zur transdermalen Applikation enthaltend 3-Keto-desogestrel |
| DE4240806A1 (de) * | 1992-12-01 | 1994-06-09 | Schering Ag | Mittel zur transdermalen Applikation enthaltend 14alpha,17alpha-Ethanoestra-1,3,5(10)-trien-3,17beta-diol |
| JPH07101884A (ja) * | 1993-10-01 | 1995-04-18 | Sanei Gen F F I Inc | 水溶性ヘミセルロースを含有する製剤 |
| CZ187796A3 (en) * | 1993-12-27 | 1997-01-15 | Akzo Nobel Nv | Pharmaceutical preparation |
| JPH11509222A (ja) * | 1995-07-17 | 1999-08-17 | シェリング アクチェンゲゼルシャフト | 13−エチル−17β−ヒドロキシ−11−メチレン−18,19−ジノル−17α−プレグン−4−エン−20−イン−3−オンのエステルを含む経皮投与のための剤 |
| CA2333985C (en) * | 1998-06-19 | 2007-04-10 | Dirk Leysen | Testosterone derivative |
| WO1999067270A1 (en) * | 1998-06-19 | 1999-12-29 | Akzo Nobel N.V. | Cycloalkyl-carboxylic acid esters of 7.alpha.methyl-estr-4-en-3-one 17.beta.-ol (19-nor 7.alpha.-methyltestosterone) |
| US6180682B1 (en) * | 1999-01-26 | 2001-01-30 | Virgil A. Place | Buccal drug delivery system for use in male contraception |
| TW200403065A (en) * | 2002-05-30 | 2004-03-01 | Akzo Nobel Nv | New etonogestrel esters |
-
2003
- 2003-05-19 TW TW092113492A patent/TW200400041A/zh unknown
- 2003-05-22 CN CNA038123657A patent/CN1655848A/zh active Pending
- 2003-05-22 US US10/517,362 patent/US20050222114A1/en not_active Abandoned
- 2003-05-22 KR KR10-2004-7019327A patent/KR20050005507A/ko not_active Withdrawn
- 2003-05-22 HR HR20041127A patent/HRP20041127A2/hr not_active Application Discontinuation
- 2003-05-22 PL PL03373295A patent/PL373295A1/xx not_active Application Discontinuation
- 2003-05-22 AT AT03755980T patent/ATE394140T1/de not_active IP Right Cessation
- 2003-05-22 EP EP03755980A patent/EP1513588B1/en not_active Expired - Lifetime
- 2003-05-22 UA UA20041109285A patent/UA80703C2/uk unknown
- 2003-05-22 BR BR0311248-9A patent/BR0311248A/pt not_active IP Right Cessation
- 2003-05-22 DE DE60320786T patent/DE60320786D1/de not_active Expired - Fee Related
- 2003-05-22 RS YU101004A patent/RS101004A/sr unknown
- 2003-05-22 AU AU2003246740A patent/AU2003246740B2/en not_active Ceased
- 2003-05-22 CA CA002487293A patent/CA2487293A1/en not_active Abandoned
- 2003-05-22 WO PCT/EP2003/050188 patent/WO2003101374A2/en not_active Ceased
- 2003-05-22 RU RU2004138809/15A patent/RU2322986C2/ru active
- 2003-05-22 MX MXPA04011798A patent/MXPA04011798A/es unknown
- 2003-05-22 JP JP2004508732A patent/JP2005532336A/ja not_active Withdrawn
- 2003-05-22 ES ES03755980T patent/ES2305498T3/es not_active Expired - Lifetime
- 2003-05-22 NZ NZ536618A patent/NZ536618A/en unknown
- 2003-05-26 PE PE2003000508A patent/PE20040042A1/es not_active Application Discontinuation
- 2003-05-28 AR ARP030101858A patent/AR040129A1/es unknown
-
2004
- 2004-11-09 IL IL16512504A patent/IL165125A0/xx unknown
- 2004-11-10 NO NO20044903A patent/NO20044903L/no not_active Application Discontinuation
- 2004-11-18 IS IS7537A patent/IS7537A/is unknown
- 2004-11-24 ZA ZA200409498A patent/ZA200409498B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2487293A1 (en) | 2003-12-11 |
| IL165125A0 (en) | 2005-12-18 |
| ZA200409498B (en) | 2006-05-31 |
| AU2003246740A1 (en) | 2003-12-19 |
| EP1513588A2 (en) | 2005-03-16 |
| ES2305498T3 (es) | 2008-11-01 |
| DE60320786D1 (de) | 2008-06-19 |
| AR040129A1 (es) | 2005-03-16 |
| BR0311248A (pt) | 2005-03-15 |
| RU2322986C2 (ru) | 2008-04-27 |
| IS7537A (is) | 2004-11-18 |
| CN1655848A (zh) | 2005-08-17 |
| PL373295A1 (en) | 2005-08-22 |
| RS101004A (sr) | 2006-10-27 |
| RU2004138809A (ru) | 2005-06-10 |
| WO2003101374A2 (en) | 2003-12-11 |
| US20050222114A1 (en) | 2005-10-06 |
| NO20044903L (no) | 2005-02-25 |
| HK1072568A1 (en) | 2005-09-02 |
| MXPA04011798A (es) | 2005-03-31 |
| HRP20041127A2 (en) | 2005-02-28 |
| JP2005532336A (ja) | 2005-10-27 |
| ATE394140T1 (de) | 2008-05-15 |
| PE20040042A1 (es) | 2004-01-31 |
| TW200400041A (en) | 2004-01-01 |
| EP1513588B1 (en) | 2008-05-07 |
| KR20050005507A (ko) | 2005-01-13 |
| UA80703C2 (en) | 2007-10-25 |
| WO2003101374A3 (en) | 2004-02-26 |
| AU2003246740B2 (en) | 2009-01-08 |
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| HK1072568B (en) | Use of new etonogestrel esters | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |