BG106441A - Мезопрогестини (модулатори на прогестероновия рецептор) като компоненти на женски контрацептиви - Google Patents
Мезопрогестини (модулатори на прогестероновия рецептор) като компоненти на женски контрацептиви Download PDFInfo
- Publication number
- BG106441A BG106441A BG06441A BG10644102A BG106441A BG 106441 A BG106441 A BG 106441A BG 06441 A BG06441 A BG 06441A BG 10644102 A BG10644102 A BG 10644102A BG 106441 A BG106441 A BG 106441A
- Authority
- BG
- Bulgaria
- Prior art keywords
- mesoprogestin
- days
- estrogen
- estradiol
- use according
- Prior art date
Links
- 229940124566 female contraceptive agent Drugs 0.000 title description 6
- 239000003037 female contraceptive agent Substances 0.000 title description 5
- 239000002379 progesterone receptor modulator Substances 0.000 title description 2
- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 title description 2
- 229940011871 estrogen Drugs 0.000 claims abstract description 41
- 239000000262 estrogen Substances 0.000 claims abstract description 41
- 239000000583 progesterone congener Substances 0.000 claims abstract description 24
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract description 21
- 150000001875 compounds Chemical class 0.000 claims abstract description 10
- 238000004519 manufacturing process Methods 0.000 claims abstract description 5
- 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 claims description 44
- 229960005309 estradiol Drugs 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 14
- 230000000740 bleeding effect Effects 0.000 claims description 14
- 230000027758 ovulation cycle Effects 0.000 claims description 12
- 239000003433 contraceptive agent Substances 0.000 claims description 11
- 229930182833 estradiol Natural products 0.000 claims description 11
- -1 estradiol ester Chemical class 0.000 claims description 11
- 206010001928 Amenorrhoea Diseases 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
- 201000000736 Amenorrhea Diseases 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
- 231100000540 amenorrhea Toxicity 0.000 claims description 9
- 229960002568 ethinylestradiol Drugs 0.000 claims description 9
- 239000008177 pharmaceutical agent Substances 0.000 claims description 8
- 239000006187 pill Substances 0.000 claims description 8
- 239000004480 active ingredient Substances 0.000 claims description 7
- 125000004122 cyclic group Chemical group 0.000 claims description 7
- 229940124558 contraceptive agent Drugs 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 239000004615 ingredient Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 239000000902 placebo Substances 0.000 claims description 5
- 229940068196 placebo Drugs 0.000 claims description 5
- 230000000306 recurrent effect Effects 0.000 claims description 3
- 230000001568 sexual effect Effects 0.000 claims description 3
- 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
- 229940094984 other estrogen in atc Drugs 0.000 claims 1
- 239000003418 antiprogestin Substances 0.000 abstract description 16
- 230000000708 anti-progestin effect Effects 0.000 abstract description 12
- 238000000034 method Methods 0.000 abstract description 12
- 102000003998 progesterone receptors Human genes 0.000 abstract description 11
- 108090000468 progesterone receptors Proteins 0.000 abstract description 11
- 230000001270 agonistic effect Effects 0.000 abstract description 3
- 230000003042 antagnostic effect Effects 0.000 abstract description 3
- 238000001727 in vivo Methods 0.000 abstract description 3
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 27
- 230000000694 effects Effects 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 19
- 239000000186 progesterone Substances 0.000 description 18
- 229960003387 progesterone Drugs 0.000 description 18
- 238000002360 preparation method Methods 0.000 description 16
- 206010000210 abortion Diseases 0.000 description 13
- QNGNSVIICDLXHT-UHFFFAOYSA-N para-ethylbenzaldehyde Natural products CCC1=CC=C(C=O)C=C1 QNGNSVIICDLXHT-UHFFFAOYSA-N 0.000 description 13
- 208000032843 Hemorrhage Diseases 0.000 description 12
- 230000016087 ovulation Effects 0.000 description 12
- 238000011282 treatment Methods 0.000 description 12
- 230000035935 pregnancy Effects 0.000 description 11
- 241000283973 Oryctolagus cuniculus Species 0.000 description 10
- 231100000176 abortion Toxicity 0.000 description 10
- 150000002923 oximes Chemical class 0.000 description 10
- 239000000044 progesterone antagonist Substances 0.000 description 10
- 230000002254 contraceptive effect Effects 0.000 description 8
- 210000004696 endometrium Anatomy 0.000 description 8
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 8
- 241000700198 Cavia Species 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- 241000282412 Homo Species 0.000 description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 230000035558 fertility Effects 0.000 description 4
- 230000003054 hormonal effect Effects 0.000 description 4
- 230000029849 luteinization Effects 0.000 description 4
- 230000000757 progestagenic effect Effects 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 3
- 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 3
- 239000000556 agonist Substances 0.000 description 3
- 239000005557 antagonist Substances 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- 230000027455 binding Effects 0.000 description 3
- 230000033228 biological regulation Effects 0.000 description 3
- 230000001684 chronic effect Effects 0.000 description 3
- 239000007933 dermal patch Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 230000002357 endometrial effect Effects 0.000 description 3
- 239000007941 film coated tablet Substances 0.000 description 3
- 238000002513 implantation Methods 0.000 description 3
- 230000001939 inductive effect Effects 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 229940127234 oral contraceptive Drugs 0.000 description 3
- 239000003539 oral contraceptive agent Substances 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000033458 reproduction Effects 0.000 description 3
- 150000003431 steroids Chemical class 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 230000009466 transformation Effects 0.000 description 3
- QIDKBIHFEGQWGX-ZFCZOSEKSA-N COC[C@@]12[C@@H](CC[C@H]1[C@@H]1CCC3=CC(CCC3=C1CC2)=O)COC Chemical compound COC[C@@]12[C@@H](CC[C@H]1[C@@H]1CCC3=CC(CCC3=C1CC2)=O)COC QIDKBIHFEGQWGX-ZFCZOSEKSA-N 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 230000001838 anti-progestagenic effect Effects 0.000 description 2
- 238000011888 autopsy Methods 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 229960000978 cyproterone acetate 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
- 230000003111 delayed effect Effects 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
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 229960004845 drospirenone Drugs 0.000 description 2
- 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 2
- 210000003754 fetus Anatomy 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
- 238000011554 guinea pig model Methods 0.000 description 2
- 238000011835 investigation Methods 0.000 description 2
- 230000000938 luteal effect Effects 0.000 description 2
- 230000011599 ovarian follicle development Effects 0.000 description 2
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 2
- 150000003180 prostaglandins Chemical class 0.000 description 2
- 230000003442 weekly effect Effects 0.000 description 2
- 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 1
- 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
- MGAFPXGQLWFEPK-UHFFFAOYSA-N 1,3,2-dioxathiepane 2,2-dioxide Chemical compound O=S1(=O)OCCCCO1 MGAFPXGQLWFEPK-UHFFFAOYSA-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
- 241000700199 Cavia porcellus Species 0.000 description 1
- 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 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
- 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 description 1
- 102100027909 Folliculin Human genes 0.000 description 1
- 101710182803 Folliculin Proteins 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
- 241000282560 Macaca mulatta Species 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
- 241000288906 Primates Species 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
- HPFVBGJFAYZEBE-XNBTXCQYSA-N [(8r,9s,10r,13s,14s)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 3-cyclopentylpropanoate Chemical compound C([C@H]1[C@H]2[C@@H]([C@]3(CCC(=O)C=C3CC2)C)CC[C@@]11C)CC1OC(=O)CCC1CCCC1 HPFVBGJFAYZEBE-XNBTXCQYSA-N 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
- 229940022663 acetate Drugs 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 230000001833 anti-estrogenic effect Effects 0.000 description 1
- 230000003509 anti-fertility effect Effects 0.000 description 1
- 230000001911 anti-progestational effect Effects 0.000 description 1
- 230000009286 beneficial effect 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
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000035606 childbirth Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 229940035811 conjugated estrogen Drugs 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000000254 damaging effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- 150000001993 dienes Chemical class 0.000 description 1
- NXFNZLHFBJYCPG-UHFFFAOYSA-N diethylsulfamic acid Chemical compound CCN(CC)S(O)(=O)=O NXFNZLHFBJYCPG-UHFFFAOYSA-N 0.000 description 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000002552 dosage form Substances 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
- 150000002159 estradiols Chemical class 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 125000004705 ethylthio group Chemical group C(C)S* 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000004720 fertilization Effects 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 229940094892 gonadotropins Drugs 0.000 description 1
- MNWFXJYAOYHMED-UHFFFAOYSA-M heptanoate Chemical compound CCCCCCC([O-])=O MNWFXJYAOYHMED-UHFFFAOYSA-M 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 230000006698 induction Effects 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
- 230000007246 mechanism Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 230000009245 menopause Effects 0.000 description 1
- 230000002175 menstrual effect Effects 0.000 description 1
- 229960003248 mifepristone Drugs 0.000 description 1
- 230000002632 myometrial effect Effects 0.000 description 1
- MYMDOKBFMTVEGE-UHFFFAOYSA-M n-methylsulfamate Chemical compound CNS([O-])(=O)=O MYMDOKBFMTVEGE-UHFFFAOYSA-M 0.000 description 1
- 238000006396 nitration reaction Methods 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
- 239000003217 oral combined contraceptive Substances 0.000 description 1
- 239000007935 oral tablet Substances 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
- 230000002085 persistent effect Effects 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 230000003623 progesteronic effect Effects 0.000 description 1
- 230000000750 progressive 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
- 230000009467 reduction Effects 0.000 description 1
- 230000008844 regulatory mechanism Effects 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000011421 subcutaneous treatment Methods 0.000 description 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-M undecanoate Chemical compound CCCCCCCCCCC([O-])=O ZDPHROOEEOARMN-UHFFFAOYSA-M 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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 |
|---|---|
| BG106441A true BG106441A (bg) | 2002-09-30 |
Family
ID=23524305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BG06441A BG106441A (bg) | 1999-08-31 | 2002-02-26 | Мезопрогестини (модулатори на прогестероновия рецептор) като компоненти на женски контрацептиви |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1605949A2 (lt) |
| JP (1) | JP2003511399A (lt) |
| KR (1) | KR20020038745A (lt) |
| CN (1) | CN1384748A (lt) |
| AR (1) | AR025455A1 (lt) |
| AU (1) | AU781835B2 (lt) |
| BG (1) | BG106441A (lt) |
| BR (1) | BR0013711A (lt) |
| CA (1) | CA2383650A1 (lt) |
| CO (1) | CO5190694A1 (lt) |
| CZ (1) | CZ2002707A3 (lt) |
| EA (1) | EA006805B1 (lt) |
| EE (1) | EE200200103A (lt) |
| HR (1) | HRP20020265A2 (lt) |
| HU (1) | HUP0202515A3 (lt) |
| IL (1) | IL148415A0 (lt) |
| LT (1) | LT5001B (lt) |
| LV (1) | LV12940B (lt) |
| MX (1) | MXPA02002186A (lt) |
| NO (1) | NO20020998L (lt) |
| NZ (1) | NZ517470A (lt) |
| PE (1) | PE20010579A1 (lt) |
| PL (1) | PL353994A1 (lt) |
| SI (1) | SI20853A (lt) |
| SK (1) | SK2982002A3 (lt) |
| UA (1) | UA77150C2 (lt) |
| WO (1) | WO2001026603A2 (lt) |
| YU (1) | YU13902A (lt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005539016A (ja) * | 2002-08-02 | 2005-12-22 | シエーリング アクチエンゲゼルシャフト | 女性用受胎調節及びホルモン置換療法のための高められた抗ゴナドトロピン活性を有するプロゲステロン受容体モジュレーター |
| DE10236405A1 (de) | 2002-08-02 | 2004-02-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie |
| US7772219B2 (en) * | 2003-05-02 | 2010-08-10 | Teva Women's Health, Inc. | Methods of hormonal treatment utilizing extended cycle contraceptive regimens |
| US20050215535A1 (en) * | 2004-03-24 | 2005-09-29 | Kristof Chwalisz | Sequential SPRM/progestin treatment |
| JP5288796B2 (ja) * | 2004-07-07 | 2013-09-11 | ワイス・エルエルシー | 周期的プロゲスチンレジメン及びキット |
| DE102005050729A1 (de) * | 2005-10-19 | 2007-04-26 | Schering Ag | Verfahren zur präventiven bedarfsweisen hormonalen Kontrazeption |
| US9616073B2 (en) | 2009-04-14 | 2017-04-11 | Laboratoire Hra-Pharma | Method for on-demand contraception |
| 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 |
| FI101601B1 (fi) * | 1987-09-24 | 1998-07-31 | Jencap Research Ltd | Ehkäisyvalmiste sekä estrogeenin ja progestiinin käyttö ehkäisyvalmisteen 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 |
| DE4332283A1 (de) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| 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 |
| 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 |
| DE4429398C2 (de) | 1994-08-09 | 1997-09-11 | Jenapharm Gmbh | Verwendung von Estra-1,3,5(10)-trien-Derivaten zur hormonalen Kontrazeption |
| NZ295365A (en) * | 1994-10-24 | 1999-07-29 | Schering Ag | Competitive progesterone antagonists for regulating female fertility as required |
| 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 |
| ATE213947T1 (de) * | 1996-06-25 | 2002-03-15 | Akzo Nobel Nv | Progestogen-anti-progestogen therapien |
| 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 SI SI200020043A patent/SI20853A/sl not_active IP Right Cessation
- 2000-08-31 IL IL14841500A patent/IL148415A0/xx unknown
- 2000-08-31 AR ARP000104536A patent/AR025455A1/es unknown
- 2000-08-31 UA UA2002032429A patent/UA77150C2/uk unknown
- 2000-08-31 KR KR1020027002785A patent/KR20020038745A/ko not_active Ceased
- 2000-08-31 PE PE2000000894A patent/PE20010579A1/es not_active Application Discontinuation
- 2000-08-31 JP JP2001529395A patent/JP2003511399A/ja active Pending
- 2000-08-31 BR BR0013711-1A patent/BR0013711A/pt not_active IP Right Cessation
- 2000-08-31 WO PCT/IB2000/002053 patent/WO2001026603A2/en not_active Ceased
- 2000-08-31 CA CA002383650A patent/CA2383650A1/en not_active Abandoned
- 2000-08-31 EE EEP200200103A patent/EE200200103A/xx unknown
- 2000-08-31 YU YU13902A patent/YU13902A/sh unknown
- 2000-08-31 MX MXPA02002186A patent/MXPA02002186A/es not_active Application Discontinuation
- 2000-08-31 HU HU0202515A patent/HUP0202515A3/hu unknown
- 2000-08-31 CO CO00065517A patent/CO5190694A1/es not_active Application Discontinuation
- 2000-08-31 CN CN00812308A patent/CN1384748A/zh active Pending
- 2000-08-31 NZ NZ517470A patent/NZ517470A/en unknown
- 2000-08-31 CZ CZ2002707A patent/CZ2002707A3/cs unknown
- 2000-08-31 PL PL00353994A patent/PL353994A1/xx not_active Application Discontinuation
- 2000-08-31 EA EA200200284A patent/EA006805B1/ru not_active IP Right Cessation
- 2000-08-31 EP EP00991299A patent/EP1605949A2/en not_active Withdrawn
- 2000-08-31 SK SK298-2002A patent/SK2982002A3/sk unknown
- 2000-08-31 HR HR20020265A patent/HRP20020265A2/hr not_active Application Discontinuation
- 2000-08-31 AU AU32150/01A patent/AU781835B2/en not_active Ceased
-
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 LV LVP-02-52A patent/LV12940B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20020038745A (ko) | 2002-05-23 |
| LT5001B (lt) | 2003-03-25 |
| JP2003511399A (ja) | 2003-03-25 |
| MXPA02002186A (es) | 2002-09-02 |
| IL148415A0 (en) | 2002-09-12 |
| EP1605949A2 (en) | 2005-12-21 |
| AU781835B2 (en) | 2005-06-16 |
| SK2982002A3 (en) | 2002-07-02 |
| LT2002035A (lt) | 2002-10-25 |
| WO2001026603A3 (en) | 2002-01-17 |
| EE200200103A (et) | 2003-04-15 |
| YU13902A (sh) | 2006-01-16 |
| NO20020998L (no) | 2002-03-14 |
| AR025455A1 (es) | 2002-11-27 |
| EA200200284A1 (ru) | 2002-10-31 |
| EA006805B1 (ru) | 2006-04-28 |
| CZ2002707A3 (cs) | 2002-11-13 |
| PL353994A1 (en) | 2003-12-15 |
| WO2001026603A2 (en) | 2001-04-19 |
| NZ517470A (en) | 2004-03-26 |
| HRP20020265A2 (en) | 2004-02-29 |
| HUP0202515A3 (en) | 2004-06-28 |
| AU3215001A (en) | 2001-04-23 |
| UA77150C2 (en) | 2006-11-15 |
| HUP0202515A2 (hu) | 2002-12-28 |
| NO20020998D0 (no) | 2002-02-28 |
| CO5190694A1 (es) | 2002-08-29 |
| PE20010579A1 (es) | 2001-06-04 |
| SI20853A (sl) | 2002-10-31 |
| LV12940B (en) | 2003-06-20 |
| CN1384748A (zh) | 2002-12-11 |
| CA2383650A1 (en) | 2001-04-19 |
| BR0013711A (pt) | 2002-05-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US6143754A (en) | Competitive progesterone antagonist for demand-oriented female birth control | |
| BG106441A (bg) | Мезопрогестини (модулатори на прогестероновия рецептор) като компоненти на женски контрацептиви | |
| KR100729311B1 (ko) | 호르몬 대체 요법(hrt)용 조성물의 성분으로서의메조프로게스틴 (프로게스테론 수용체 조절물질) | |
| US7629334B1 (en) | Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT) | |
| ZA200201614B (en) | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives. | |
| HK1051810A (en) | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives |