HRP20020265A2 - Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives - Google Patents
Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives Download PDFInfo
- Publication number
- HRP20020265A2 HRP20020265A2 HR20020265A HRP20020265A HRP20020265A2 HR P20020265 A2 HRP20020265 A2 HR P20020265A2 HR 20020265 A HR20020265 A HR 20020265A HR P20020265 A HRP20020265 A HR P20020265A HR P20020265 A2 HRP20020265 A2 HR P20020265A2
- Authority
- HR
- Croatia
- Prior art keywords
- mesoprogestin
- estrogen
- estradiol
- pharmaceutical preparation
- dosage units
- Prior art date
Links
- 239000003037 female contraceptive agent Substances 0.000 title description 2
- 229940124566 female contraceptive agent Drugs 0.000 title description 2
- 239000002379 progesterone receptor modulator Substances 0.000 title 1
- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 title 1
- 229940011871 estrogen Drugs 0.000 claims description 48
- 239000000262 estrogen Substances 0.000 claims description 48
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 20
- 239000000126 substance Substances 0.000 claims description 16
- 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 14
- 230000027758 ovulation cycle Effects 0.000 claims description 13
- 230000000740 bleeding effect Effects 0.000 claims description 12
- 229960005309 estradiol Drugs 0.000 claims description 12
- 239000006187 pill Substances 0.000 claims description 10
- 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 9
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical group 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 9
- 229960002568 ethinylestradiol Drugs 0.000 claims description 9
- 201000000736 Amenorrhea Diseases 0.000 claims description 8
- 206010001928 Amenorrhoea Diseases 0.000 claims description 8
- 231100000540 amenorrhea Toxicity 0.000 claims description 8
- 229930182833 estradiol Natural products 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 239000013543 active substance Substances 0.000 claims description 7
- -1 J 912 Chemical compound 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 6
- 239000000902 placebo Substances 0.000 claims description 6
- 229940068196 placebo Drugs 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 230000002441 reversible effect Effects 0.000 claims description 4
- 230000001568 sexual effect Effects 0.000 claims description 4
- BFPYWIDHMRZLRN-SWBPCFCJSA-N (8r,9s,13s,14s,17s)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SWBPCFCJSA-N 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 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 53
- 230000000694 effects Effects 0.000 description 30
- 239000000583 progesterone congener Substances 0.000 description 27
- VKHAHZOOUSRJNA-GCNJZUOMSA-N mifepristone Chemical compound C1([C@@H]2C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]3CC[C@@]([C@]3(C2)C)(O)C#CC)=CC=C(N(C)C)C=C1 VKHAHZOOUSRJNA-GCNJZUOMSA-N 0.000 description 18
- 239000000186 progesterone Substances 0.000 description 17
- 229960003387 progesterone Drugs 0.000 description 17
- 241000283973 Oryctolagus cuniculus Species 0.000 description 15
- 239000003418 antiprogestin Substances 0.000 description 15
- 238000000034 method Methods 0.000 description 15
- 230000016087 ovulation Effects 0.000 description 12
- 230000000708 anti-progestin effect Effects 0.000 description 11
- 230000035935 pregnancy Effects 0.000 description 11
- 238000011282 treatment Methods 0.000 description 11
- 239000000044 progesterone antagonist Substances 0.000 description 10
- 208000032843 Hemorrhage Diseases 0.000 description 9
- 102000003998 progesterone receptors Human genes 0.000 description 9
- 108090000468 progesterone receptors Proteins 0.000 description 9
- 150000002923 oximes Chemical class 0.000 description 8
- 230000002254 contraceptive effect Effects 0.000 description 7
- 210000004696 endometrium Anatomy 0.000 description 7
- 238000012360 testing method Methods 0.000 description 7
- 239000003433 contraceptive agent Substances 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 230000002357 endometrial effect Effects 0.000 description 5
- 230000029849 luteinization Effects 0.000 description 5
- 239000008177 pharmaceutical agent Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- 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 description 4
- 241000282412 Homo Species 0.000 description 4
- 239000004015 abortifacient agent Substances 0.000 description 4
- 231100000641 abortifacient agent Toxicity 0.000 description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 238000011554 guinea pig model Methods 0.000 description 4
- 230000001939 inductive effect Effects 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 230000000757 progestagenic effect Effects 0.000 description 4
- 241000700198 Cavia Species 0.000 description 3
- QMBJSIBWORFWQT-DFXBJWIESA-N Chlormadinone acetate Chemical compound C1=C(Cl)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 QMBJSIBWORFWQT-DFXBJWIESA-N 0.000 description 3
- 241000700159 Rattus Species 0.000 description 3
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- 230000001684 chronic effect Effects 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 230000003054 hormonal effect Effects 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 229940127234 oral contraceptive Drugs 0.000 description 3
- 239000003539 oral contraceptive agent Substances 0.000 description 3
- 230000011599 ovarian follicle development Effects 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- 230000009466 transformation Effects 0.000 description 3
- 241000700199 Cavia porcellus Species 0.000 description 2
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- 238000010171 animal model Methods 0.000 description 2
- 230000001833 anti-estrogenic effect Effects 0.000 description 2
- 230000001838 anti-progestagenic effect Effects 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 238000011888 autopsy Methods 0.000 description 2
- 238000004166 bioassay Methods 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000013066 combination product Substances 0.000 description 2
- 229940127555 combination product Drugs 0.000 description 2
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 description 2
- 229960000978 cyproterone acetate Drugs 0.000 description 2
- 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 2
- 229960004976 desogestrel Drugs 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 230000018109 developmental process Effects 0.000 description 2
- 230000001076 estrogenic effect Effects 0.000 description 2
- 230000035558 fertility Effects 0.000 description 2
- 230000004720 fertilization Effects 0.000 description 2
- SIGSPDASOTUPFS-XUDSTZEESA-N gestodene Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](C=C4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 SIGSPDASOTUPFS-XUDSTZEESA-N 0.000 description 2
- 229960005352 gestodene Drugs 0.000 description 2
- 239000003163 gonadal steroid hormone Substances 0.000 description 2
- 239000007943 implant Substances 0.000 description 2
- 238000002513 implantation Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 230000000977 initiatory effect Effects 0.000 description 2
- 230000000366 juvenile effect Effects 0.000 description 2
- 229960004400 levonorgestrel Drugs 0.000 description 2
- 230000000938 luteal effect Effects 0.000 description 2
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 150000003180 prostaglandins Chemical class 0.000 description 2
- 238000011552 rat model Methods 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 238000011421 subcutaneous treatment Methods 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- WFHDOIKSUKQTLH-IBXXTFBESA-N (8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one;[(8r,9s,13s,14s,17s)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] pentanoate Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 WFHDOIKSUKQTLH-IBXXTFBESA-N 0.000 description 1
- IEXUMDBQLIVNHZ-YOUGDJEHSA-N (8s,11r,13r,14s,17s)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(3-hydroxypropyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(O)CCCO)[C@@]2(C)C1 IEXUMDBQLIVNHZ-YOUGDJEHSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 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 description 1
- 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 description 1
- 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
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
- 108010073521 Luteinizing Hormone Proteins 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 description 1
- 229940123788 Progesterone receptor antagonist Drugs 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 208000036029 Uterine contractions during pregnancy Diseases 0.000 description 1
- 206010046788 Uterine haemorrhage Diseases 0.000 description 1
- 206010046798 Uterine leiomyoma Diseases 0.000 description 1
- 206010046910 Vaginal haemorrhage Diseases 0.000 description 1
- 206010047998 Withdrawal bleed Diseases 0.000 description 1
- RVKFQAJIXCZXQY-CBZIJGRNSA-N [(8r,9s,13s,14s)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-3-yl] sulfamate Chemical compound NS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 RVKFQAJIXCZXQY-CBZIJGRNSA-N 0.000 description 1
- YXYXCSOJKUAPJI-ZBRFXRBCSA-N [(8r,9s,13s,14s,17s)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] sulfamate Chemical compound NS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 YXYXCSOJKUAPJI-ZBRFXRBCSA-N 0.000 description 1
- 229940022663 acetate Drugs 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 230000003509 anti-fertility effect Effects 0.000 description 1
- 230000002513 anti-ovulatory effect Effects 0.000 description 1
- 230000001911 anti-progestational effect Effects 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 230000006406 biphasic response Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229960001616 chlormadinone acetate Drugs 0.000 description 1
- 229940108922 climara Drugs 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 229940035811 conjugated estrogen Drugs 0.000 description 1
- 229940124558 contraceptive agent Drugs 0.000 description 1
- 238000001212 derivatisation Methods 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229960004845 drospirenone Drugs 0.000 description 1
- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000032050 esterification Effects 0.000 description 1
- 238000005886 esterification reaction Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229960001359 estradiol 3-benzoate Drugs 0.000 description 1
- TXHUMRBWIWWBGW-GVGNIZHQSA-N estradiol undecylate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCCC)[C@@]1(C)CC2 TXHUMRBWIWWBGW-GVGNIZHQSA-N 0.000 description 1
- 150000002159 estradiols Chemical class 0.000 description 1
- 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 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 210000003754 fetus Anatomy 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 231100000546 inhibition of ovulation Toxicity 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 201000010260 leiomyoma Diseases 0.000 description 1
- 229940040129 luteinizing hormone Drugs 0.000 description 1
- 230000035800 maturation Effects 0.000 description 1
- 230000002175 menstrual effect Effects 0.000 description 1
- 229960003248 mifepristone Drugs 0.000 description 1
- 229940110234 mirena Drugs 0.000 description 1
- 230000002632 myometrial effect Effects 0.000 description 1
- 229960000417 norgestimate Drugs 0.000 description 1
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 description 1
- VOXZDWNPVJITMN-WKUFJEKOSA-N oestradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-WKUFJEKOSA-N 0.000 description 1
- 229950011093 onapristone Drugs 0.000 description 1
- 210000000287 oocyte Anatomy 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000000624 ovulatory effect Effects 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000032696 parturition Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000011809 primate model Methods 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000003623 progesteronic effect Effects 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
- 230000003442 weekly effect Effects 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
- A61K31/567—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
- 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
- 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
- A61P15/18—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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38613399A | 1999-08-31 | 1999-08-31 | |
| PCT/IB2000/002053 WO2001026603A2 (en) | 1999-08-31 | 2000-08-31 | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20020265A2 true HRP20020265A2 (en) | 2004-02-29 |
Family
ID=23524305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20020265A HRP20020265A2 (en) | 1999-08-31 | 2002-03-28 | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1605949A2 (no) |
| JP (1) | JP2003511399A (no) |
| KR (1) | KR20020038745A (no) |
| CN (1) | CN1384748A (no) |
| AR (1) | AR025455A1 (no) |
| AU (1) | AU781835B2 (no) |
| BG (1) | BG106441A (no) |
| BR (1) | BR0013711A (no) |
| CA (1) | CA2383650A1 (no) |
| CO (1) | CO5190694A1 (no) |
| CZ (1) | CZ2002707A3 (no) |
| EA (1) | EA006805B1 (no) |
| EE (1) | EE200200103A (no) |
| HR (1) | HRP20020265A2 (no) |
| HU (1) | HUP0202515A3 (no) |
| IL (1) | IL148415A0 (no) |
| LT (1) | LT5001B (no) |
| LV (1) | LV12940B (no) |
| MX (1) | MXPA02002186A (no) |
| NO (1) | NO20020998L (no) |
| NZ (1) | NZ517470A (no) |
| PE (1) | PE20010579A1 (no) |
| PL (1) | PL353994A1 (no) |
| SI (1) | SI20853A (no) |
| SK (1) | SK2982002A3 (no) |
| UA (1) | UA77150C2 (no) |
| WO (1) | WO2001026603A2 (no) |
| YU (1) | YU13902A (no) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE50304970D1 (de) * | 2002-08-02 | 2006-10-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper aktivität für die weibliche fertilitätskontrolle und hormonersatztherapie |
| DE10236405A1 (de) | 2002-08-02 | 2004-02-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie |
| EP1624848A4 (en) * | 2003-05-02 | 2009-02-25 | Duramed Pharmaceuticals Inc | METHOD FOR HORMONY TREATMENT WITH CONTRAZEPTVA SCHEMATES WITH EXTENDED CYCLE |
| US20050215535A1 (en) * | 2004-03-24 | 2005-09-29 | Kristof Chwalisz | Sequential SPRM/progestin treatment |
| CA2571377C (en) * | 2004-07-07 | 2014-03-25 | Wyeth | Cyclic progestin regimens and kits |
| DE102005050729A1 (de) * | 2005-10-19 | 2007-04-26 | Schering Ag | Verfahren zur präventiven bedarfsweisen hormonalen Kontrazeption |
| PL2419108T3 (pl) | 2009-04-14 | 2017-08-31 | Laboratoire Hra Pharma | Sposób antykoncepcji na żądanie |
| CN110548034A (zh) * | 2019-07-12 | 2019-12-10 | 广州莎蔓生物科技有限公司 | 一种怀孕阻断药物 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2054271A (en) | 1932-05-17 | 1936-09-15 | Schering Kahlbaum Ag | Production of crystallized hormone esters |
| DE699310C (de) | 1936-11-20 | 1940-11-27 | Chemische Ind Ges | Verfahren zur Herstellung von in 3-Stellung veresterten Verbindungen vom Typus des Oestradiols |
| US2225419A (en) | 1937-03-01 | 1940-12-17 | Schering Corp | Process for the conversion of 17-cisalcohols of the cyclopentanopolyhydrophenanthrene series into the corresponding 17-trans-alcohols |
| US2611773A (en) | 1951-08-21 | 1952-09-23 | Upjohn Co | Estradiol 17-cyclopenetanepropionate |
| US2990414A (en) | 1957-03-26 | 1961-06-27 | Syntex Sa | 17-undecenoate of estradiol |
| DE3337450A1 (de) | 1983-10-12 | 1985-04-25 | Schering AG, 1000 Berlin und 4709 Bergkamen | Prostaglandine und antigestagene fuer den schwangerschaftsabbruch |
| FI101601B (fi) * | 1987-09-24 | 1998-07-31 | Jencap Res Ltd | Ehkäisyvalmiste sekä estrogeenin ja progestiinin käyttö ehkäisyvalmist een valmistusmenetelmässä |
| US5439913A (en) | 1992-05-12 | 1995-08-08 | Schering Aktiengesellschaft | Contraception method using competitive progesterone antagonists and novel compounds useful therein |
| US5516769A (en) | 1993-02-19 | 1996-05-14 | The Medical College Of Hampton Roads | Method of inhibiting fertilization |
| DE4332284C2 (de) * | 1993-09-20 | 1997-05-28 | Jenapharm Gmbh | 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE4332283A1 (de) * | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE4447715C2 (de) | 1994-08-09 | 1998-02-05 | Jenapharm Gmbh | Verwendung von Estra-1,3,5(10)-trien-Derivaten zur hormonalen Behandlung von Prostatakarzinomen |
| DE4429397C2 (de) | 1994-08-09 | 2003-11-20 | Jenapharm Gmbh | Estra-1,3,5(10)-trien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| AU707235B2 (en) * | 1994-10-24 | 1999-07-08 | Schering Aktiengesellschaft | Competitive progesterone antagonists for demand-oriented female birth control |
| US6040340A (en) * | 1996-05-07 | 2000-03-21 | Schering Aktiengesellschaft | Implantation rates after in vitro fertilization, treatment of infertility and early pregnancy loss with a nitric oxide donor alone or in combination with progesterone, and a method for contraception with nitric oxide inhibitors |
| KR20000022189A (ko) * | 1996-06-25 | 2000-04-25 | 에프.지.엠. 헤르만스;이.에이치. 리링크 | 프로제스토젠-항프로제스토젠 섭생 |
| WO1998005679A2 (en) * | 1996-08-05 | 1998-02-12 | Duke University | Mixed agonists of the progesterone receptor and assays therefor |
| DE19809845A1 (de) * | 1998-03-03 | 1999-09-09 | Jenapharm Gmbh | S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen |
| CN1353717A (zh) * | 1999-05-04 | 2002-06-12 | 莱加制药公司 | 四环黄体酮受体调节剂化合物及其方法 |
-
2000
- 2000-08-31 CO CO00065517A patent/CO5190694A1/es not_active Application Discontinuation
- 2000-08-31 NZ NZ517470A patent/NZ517470A/en unknown
- 2000-08-31 WO PCT/IB2000/002053 patent/WO2001026603A2/en not_active Application Discontinuation
- 2000-08-31 EE EEP200200103A patent/EE200200103A/xx unknown
- 2000-08-31 SI SI200020043A patent/SI20853A/sl not_active IP Right Cessation
- 2000-08-31 AR ARP000104536A patent/AR025455A1/es unknown
- 2000-08-31 EP EP00991299A patent/EP1605949A2/en not_active Withdrawn
- 2000-08-31 CA CA002383650A patent/CA2383650A1/en not_active Abandoned
- 2000-08-31 CZ CZ2002707A patent/CZ2002707A3/cs unknown
- 2000-08-31 JP JP2001529395A patent/JP2003511399A/ja active Pending
- 2000-08-31 CN CN00812308A patent/CN1384748A/zh active Pending
- 2000-08-31 UA UA2002032429A patent/UA77150C2/uk unknown
- 2000-08-31 YU YU13902A patent/YU13902A/sh unknown
- 2000-08-31 BR BR0013711-1A patent/BR0013711A/pt not_active IP Right Cessation
- 2000-08-31 IL IL14841500A patent/IL148415A0/xx unknown
- 2000-08-31 AU AU32150/01A patent/AU781835B2/en not_active Ceased
- 2000-08-31 KR KR1020027002785A patent/KR20020038745A/ko not_active Application Discontinuation
- 2000-08-31 HU HU0202515A patent/HUP0202515A3/hu unknown
- 2000-08-31 PE PE2000000894A patent/PE20010579A1/es not_active Application Discontinuation
- 2000-08-31 EA EA200200284A patent/EA006805B1/ru not_active IP Right Cessation
- 2000-08-31 PL PL00353994A patent/PL353994A1/xx not_active Application Discontinuation
- 2000-08-31 SK SK298-2002A patent/SK2982002A3/sk unknown
- 2000-08-31 MX MXPA02002186A patent/MXPA02002186A/es not_active Application Discontinuation
-
2002
- 2002-02-26 BG BG06441A patent/BG106441A/bg unknown
- 2002-02-28 NO NO20020998A patent/NO20020998L/no not_active Application Discontinuation
- 2002-03-26 LT LT2002035A patent/LT5001B/lt not_active IP Right Cessation
- 2002-03-28 HR HR20020265A patent/HRP20020265A2/hr not_active Application Discontinuation
- 2002-03-28 LV LVP-02-52A patent/LV12940B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CZ2002707A3 (cs) | 2002-11-13 |
| BR0013711A (pt) | 2002-05-07 |
| SI20853A (sl) | 2002-10-31 |
| WO2001026603A2 (en) | 2001-04-19 |
| BG106441A (bg) | 2002-09-30 |
| EA006805B1 (ru) | 2006-04-28 |
| CN1384748A (zh) | 2002-12-11 |
| YU13902A (sh) | 2006-01-16 |
| HUP0202515A3 (en) | 2004-06-28 |
| HUP0202515A2 (hu) | 2002-12-28 |
| EE200200103A (et) | 2003-04-15 |
| PE20010579A1 (es) | 2001-06-04 |
| AR025455A1 (es) | 2002-11-27 |
| LT2002035A (lt) | 2002-10-25 |
| UA77150C2 (en) | 2006-11-15 |
| NO20020998L (no) | 2002-03-14 |
| WO2001026603A3 (en) | 2002-01-17 |
| MXPA02002186A (es) | 2002-09-02 |
| PL353994A1 (en) | 2003-12-15 |
| CO5190694A1 (es) | 2002-08-29 |
| LV12940B (en) | 2003-06-20 |
| EA200200284A1 (ru) | 2002-10-31 |
| LT5001B (lt) | 2003-03-25 |
| AU781835B2 (en) | 2005-06-16 |
| NZ517470A (en) | 2004-03-26 |
| EP1605949A2 (en) | 2005-12-21 |
| CA2383650A1 (en) | 2001-04-19 |
| NO20020998D0 (no) | 2002-02-28 |
| IL148415A0 (en) | 2002-09-12 |
| AU3215001A (en) | 2001-04-23 |
| KR20020038745A (ko) | 2002-05-23 |
| SK2982002A3 (en) | 2002-07-02 |
| JP2003511399A (ja) | 2003-03-25 |
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Legal Events
| Date | Code | Title | Description |
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| A1OB | Publication of a patent application | ||
| ARAI | Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application | ||
| PPPP | Transfer of rights |
Owner name: SCHERING AG, DE |
|
| PNAN | Change of the applicant name, address/residence |
Owner name: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT, DE |
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| OBST | Application withdrawn |