DE60036723T2 - Mesoprogestine zur behandlung und vorbeugung von hormonabhängigen gutartigen gynekologischen störungen - Google Patents
Mesoprogestine zur behandlung und vorbeugung von hormonabhängigen gutartigen gynekologischen störungen Download PDFInfo
- Publication number
- DE60036723T2 DE60036723T2 DE60036723T DE60036723T DE60036723T2 DE 60036723 T2 DE60036723 T2 DE 60036723T2 DE 60036723 T DE60036723 T DE 60036723T DE 60036723 T DE60036723 T DE 60036723T DE 60036723 T2 DE60036723 T2 DE 60036723T2
- Authority
- DE
- Germany
- Prior art keywords
- treatment
- endometriosis
- dysmenorrhea
- prevention
- mesoprogestins
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 238000011282 treatment Methods 0.000 title claims description 48
- 230000002265 prevention Effects 0.000 title claims description 14
- 206010013935 Dysmenorrhoea Diseases 0.000 claims description 38
- 201000009273 Endometriosis Diseases 0.000 claims description 27
- 208000005171 Dysmenorrhea Diseases 0.000 claims description 16
- 208000007106 menorrhagia Diseases 0.000 claims description 14
- 206010027514 Metrorrhagia Diseases 0.000 claims description 13
- 229940079593 drug Drugs 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 206010046798 Uterine leiomyoma Diseases 0.000 claims description 8
- 201000010260 leiomyoma Diseases 0.000 claims description 8
- 206010013908 Dysfunctional uterine bleeding Diseases 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 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 30
- 230000000694 effects Effects 0.000 description 28
- 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
- 239000003418 antiprogestin Substances 0.000 description 16
- 241000283973 Oryctolagus cuniculus Species 0.000 description 15
- 208000032843 Hemorrhage Diseases 0.000 description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 13
- 239000000186 progesterone Substances 0.000 description 13
- 229960003387 progesterone Drugs 0.000 description 13
- 230000000708 anti-progestin effect Effects 0.000 description 12
- 230000000740 bleeding effect Effects 0.000 description 12
- 239000000556 agonist Substances 0.000 description 9
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 9
- 102000003998 progesterone receptors Human genes 0.000 description 9
- 108090000468 progesterone receptors Proteins 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 8
- POZRVZJJTULAOH-LHZXLZLDSA-N danazol Chemical compound C1[C@]2(C)[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=CC2=C1C=NO2 POZRVZJJTULAOH-LHZXLZLDSA-N 0.000 description 8
- 229960000766 danazol Drugs 0.000 description 8
- 208000035475 disorder Diseases 0.000 description 8
- 230000035935 pregnancy Effects 0.000 description 8
- 239000000583 progesterone congener Substances 0.000 description 8
- NMJREATYWWNIKX-UHFFFAOYSA-N GnRH Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CC(C)C)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 NMJREATYWWNIKX-UHFFFAOYSA-N 0.000 description 7
- 230000002357 endometrial effect Effects 0.000 description 7
- 241000700198 Cavia Species 0.000 description 6
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 6
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 6
- 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 5
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 description 5
- 208000000450 Pelvic Pain Diseases 0.000 description 5
- 102100024028 Progonadoliberin-1 Human genes 0.000 description 5
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 description 5
- 208000036029 Uterine contractions during pregnancy Diseases 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 238000002560 therapeutic procedure Methods 0.000 description 5
- 208000002193 Pain Diseases 0.000 description 4
- 241000700159 Rattus Species 0.000 description 4
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 4
- 206010000210 abortion Diseases 0.000 description 4
- 231100000176 abortion Toxicity 0.000 description 4
- 230000001270 agonistic effect Effects 0.000 description 4
- 230000001911 anti-progestational effect Effects 0.000 description 4
- 230000007423 decrease Effects 0.000 description 4
- 230000000977 initiatory effect Effects 0.000 description 4
- 230000001629 suppression Effects 0.000 description 4
- 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 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 3
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 230000001154 acute effect Effects 0.000 description 3
- 230000001548 androgenic effect Effects 0.000 description 3
- 230000003042 antagnostic effect Effects 0.000 description 3
- 230000033228 biological regulation Effects 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 229960005309 estradiol Drugs 0.000 description 3
- 229930182833 estradiol Natural products 0.000 description 3
- 230000035558 fertility Effects 0.000 description 3
- 229940088597 hormone Drugs 0.000 description 3
- 239000005556 hormone Substances 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 238000013160 medical therapy Methods 0.000 description 3
- 230000005906 menstruation Effects 0.000 description 3
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 3
- 229960003248 mifepristone Drugs 0.000 description 3
- 229940110234 mirena Drugs 0.000 description 3
- 229940053934 norethindrone Drugs 0.000 description 3
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 description 3
- 229950011093 onapristone Drugs 0.000 description 3
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 3
- QNGNSVIICDLXHT-UHFFFAOYSA-N para-ethylbenzaldehyde Natural products CCC1=CC=C(C=O)C=C1 QNGNSVIICDLXHT-UHFFFAOYSA-N 0.000 description 3
- 230000007170 pathology Effects 0.000 description 3
- 230000000757 progestagenic effect Effects 0.000 description 3
- 239000000044 progesterone antagonist Substances 0.000 description 3
- 239000002379 progesterone receptor modulator Substances 0.000 description 3
- 150000003180 prostaglandins Chemical class 0.000 description 3
- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 description 3
- 150000003431 steroids Chemical class 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 241000700199 Cavia porcellus Species 0.000 description 2
- 208000004483 Dyspareunia Diseases 0.000 description 2
- BJJXHLWLUDYTGC-ANULTFPQSA-N Gestrinone Chemical compound C1CC(=O)C=C2CC[C@@H]([C@H]3[C@@](CC)([C@](CC3)(O)C#C)C=C3)C3=C21 BJJXHLWLUDYTGC-ANULTFPQSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 206010030247 Oestrogen deficiency Diseases 0.000 description 2
- 208000001132 Osteoporosis Diseases 0.000 description 2
- 206010047139 Vasoconstriction Diseases 0.000 description 2
- 125000002015 acyclic group Chemical group 0.000 description 2
- 230000001838 anti-progestagenic effect Effects 0.000 description 2
- 238000011888 autopsy Methods 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000027455 binding Effects 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- 210000004696 endometrium Anatomy 0.000 description 2
- 229940011871 estrogen Drugs 0.000 description 2
- 239000000262 estrogen Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229960004761 gestrinone Drugs 0.000 description 2
- 238000011554 guinea pig model Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 208000000509 infertility Diseases 0.000 description 2
- 230000036512 infertility Effects 0.000 description 2
- 231100000535 infertility Toxicity 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 230000002175 menstrual effect Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000036961 partial effect Effects 0.000 description 2
- 210000004197 pelvis Anatomy 0.000 description 2
- 230000003623 progesteronic effect Effects 0.000 description 2
- 229940095743 selective estrogen receptor modulator Drugs 0.000 description 2
- 239000000333 selective estrogen receptor modulator Substances 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 230000025033 vasoconstriction Effects 0.000 description 2
- 150000000319 19-nortestosterones Chemical class 0.000 description 1
- 206010000234 Abortion spontaneous Diseases 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 206010003694 Atrophy Diseases 0.000 description 1
- 206010065687 Bone loss Diseases 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 102000006771 Gonadotropins Human genes 0.000 description 1
- 108010086677 Gonadotropins Proteins 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 108010000817 Leuprolide Proteins 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 206010067572 Oestrogenic effect Diseases 0.000 description 1
- 208000034424 Painful defaecation Diseases 0.000 description 1
- 206010034650 Peritoneal adhesions Diseases 0.000 description 1
- 229940123788 Progesterone receptor antagonist Drugs 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 206010039792 Seborrhoea Diseases 0.000 description 1
- 206010046788 Uterine haemorrhage Diseases 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 239000000808 adrenergic beta-agonist Substances 0.000 description 1
- 230000001195 anabolic effect Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000001833 anti-estrogenic effect Effects 0.000 description 1
- 230000003509 anti-fertility effect Effects 0.000 description 1
- 230000001567 anti-fibrinolytic effect Effects 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000003454 betamimetic effect Effects 0.000 description 1
- 238000004166 bioassay Methods 0.000 description 1
- 230000002051 biphasic effect Effects 0.000 description 1
- 208000034158 bleeding Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000013872 defecation Effects 0.000 description 1
- 230000001419 dependent effect Effects 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
- 238000003745 diagnosis Methods 0.000 description 1
- 210000003717 douglas' pouch Anatomy 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 206010013990 dysuria Diseases 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 201000006828 endometrial hyperplasia Diseases 0.000 description 1
- 239000000328 estrogen antagonist Substances 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 229960000445 ethisterone Drugs 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 230000003152 gestagenic effect Effects 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 description 1
- 239000002622 gonadotropin Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 238000009802 hysterectomy Methods 0.000 description 1
- 229960001680 ibuprofen Drugs 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 208000003243 intestinal obstruction Diseases 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 150000002545 isoxazoles Chemical class 0.000 description 1
- RGLRXNKKBLIBQS-XNHQSDQCSA-N leuprolide acetate Chemical compound CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 RGLRXNKKBLIBQS-XNHQSDQCSA-N 0.000 description 1
- 210000003041 ligament Anatomy 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 230000004807 localization Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940087857 lupron Drugs 0.000 description 1
- HYYBABOKPJLUIN-UHFFFAOYSA-N mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 description 1
- 229960003464 mefenamic acid Drugs 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 230000004066 metabolic change Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000002395 mineralocorticoid Substances 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 230000002632 myometrial effect Effects 0.000 description 1
- 230000037312 oily skin Effects 0.000 description 1
- 229940127234 oral contraceptive Drugs 0.000 description 1
- 239000003539 oral contraceptive agent Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000011599 ovarian follicle development Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 230000016087 ovulation Effects 0.000 description 1
- 230000000624 ovulatory effect Effects 0.000 description 1
- 150000002923 oximes Chemical class 0.000 description 1
- 210000004303 peritoneum Anatomy 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000001817 pituitary effect Effects 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 150000003146 progesterones Chemical class 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229960004622 raloxifene Drugs 0.000 description 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 1
- 238000011552 rat model Methods 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 230000000284 resting effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 208000000995 spontaneous abortion Diseases 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000003867 tiredness Effects 0.000 description 1
- 208000016255 tiredness Diseases 0.000 description 1
- 230000003195 tocolytic effect Effects 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- 238000002646 transcutaneous electrical nerve stimulation Methods 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 210000003708 urethra Anatomy 0.000 description 1
- 208000010422 uterine anomalies Diseases 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 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
-
- 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
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- 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
- A61P5/34—Gestagens
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38614199A | 1999-08-31 | 1999-08-31 | |
| US386141 | 1999-08-31 | ||
| PCT/US2000/023770 WO2001015679A2 (en) | 1999-08-31 | 2000-08-31 | Mesoprogestins for the treatment and prevention of benign hormone dependent gynecological disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60036723D1 DE60036723D1 (de) | 2007-11-22 |
| DE60036723T2 true DE60036723T2 (de) | 2008-07-17 |
Family
ID=23524338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60036723T Expired - Lifetime DE60036723T2 (de) | 1999-08-31 | 2000-08-31 | Mesoprogestine zur behandlung und vorbeugung von hormonabhängigen gutartigen gynekologischen störungen |
Country Status (34)
| Country | Link |
|---|---|
| EP (1) | EP1229906B1 (https=) |
| JP (1) | JP2003535029A (https=) |
| KR (3) | KR20080066095A (https=) |
| AR (1) | AR025457A1 (https=) |
| AT (1) | ATE375160T1 (https=) |
| AU (1) | AU781840B2 (https=) |
| BG (1) | BG65817B1 (https=) |
| BR (1) | BR0014161A (https=) |
| CA (1) | CA2382580C (https=) |
| CO (1) | CO5200772A1 (https=) |
| CZ (1) | CZ2002704A3 (https=) |
| DE (1) | DE60036723T2 (https=) |
| DK (1) | DK1229906T3 (https=) |
| EA (1) | EA007854B1 (https=) |
| EE (1) | EE05172B1 (https=) |
| ES (1) | ES2295050T3 (https=) |
| HR (1) | HRP20020267A2 (https=) |
| HU (1) | HUP0202429A3 (https=) |
| IL (1) | IL148416A0 (https=) |
| LT (1) | LT5034B (https=) |
| LV (1) | LV12941B (https=) |
| ME (1) | MEP13808A (https=) |
| MX (1) | MXPA02002191A (https=) |
| NO (1) | NO20020999L (https=) |
| NZ (1) | NZ517471A (https=) |
| PE (1) | PE20010578A1 (https=) |
| PL (1) | PL198790B1 (https=) |
| PT (1) | PT1229906E (https=) |
| RO (1) | RO122179B1 (https=) |
| RS (1) | RS50283B (https=) |
| SI (1) | SI20852B (https=) |
| SK (1) | SK287192B6 (https=) |
| UA (1) | UA78184C2 (https=) |
| WO (1) | WO2001015679A2 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003255355A1 (en) * | 2002-08-02 | 2004-02-25 | Schering Aktiengesellschaft | Progesterone receptor modulators having an increased antigonadotropic activity for use in female fertility testing and hormone replacement therapy |
| DE10236405A1 (de) | 2002-08-02 | 2004-02-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie |
| US20040097591A1 (en) * | 2002-11-18 | 2004-05-20 | Kristof Chwalisz | Use of selective progesterone receptor modulators for the treatment of androgen deficiency |
| RU2301691C1 (ru) * | 2005-12-20 | 2007-06-27 | Государственное учреждение Научный центр акушерства, гинекологии и перинатологии Российской академии медицинских наук | Способ восстановительного лечения женщин репродуктивного возраста с тазовыми перитонеальными спайками с фиксированной или субфиксированной ретродевиацией матки |
| DE102007011105A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Schering Pharma Aktiengesellschaft | Mineralcorticoid-Rezeptor-Antagonisten zur Behandlung von Endometriose |
| RU2339392C1 (ru) * | 2007-05-21 | 2008-11-27 | Федеральное Государственное учреждение Научный центр акушерства, гинекологии и перинатологии Росмедтехнологий | Способ остановки маточных кровотечений в пубертатном периоде |
| JP4709328B2 (ja) * | 2009-06-17 | 2011-06-22 | 国立大学法人 熊本大学 | 月経困難症の予防及び／又は治療薬 |
| US8399432B2 (en) * | 2009-10-27 | 2013-03-19 | Lipogen Ltd. | Compositions and methods of treatment for alleviating premenstrual syndrome symptoms |
| JP2022548314A (ja) * | 2019-09-23 | 2022-11-17 | ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー | 妊娠を遷延させるためおよび月経または妊娠の合併症の処置の方法 |
| US12426782B2 (en) | 2020-11-06 | 2025-09-30 | The Board Of Trustees Of The Leland Stanford Junior University | Systems and temporal alignment methods for evaluation of gestational age and time to delivery |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3633244A1 (de) | 1986-09-26 | 1988-03-31 | Schering Ag | Antigestagene zur hemmung der uterinen prostaglandinsynthese |
| 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 |
| US5681817A (en) * | 1994-02-04 | 1997-10-28 | The Medical College Of Hampton Roads | Treatment of ovarian estrogen dependent conditions |
| US5576310A (en) * | 1994-09-20 | 1996-11-19 | Jenapharm Gmbh | 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds |
| US5696127A (en) * | 1994-12-22 | 1997-12-09 | Ligand Pharmaceuticals Incorporated | Steroid receptor modulator compounds and methods |
| EP1043325B1 (en) * | 1994-12-22 | 2004-06-16 | Ligand Pharmaceuticals Incorporated | Steroid receptor modulator compounds and methods |
| UA37259C2 (uk) | 1995-02-02 | 2001-05-15 | Шерінг Актієнгезеллшафт | Активна речовина для одержання лікарських засобів при лікуванні дисфункціональних маткових кровотеч |
| DE19604231A1 (de) * | 1996-01-29 | 1997-07-31 | Schering Ag | Pharmazeutisches Kombinationspräparat und seine Verwendung zur Behandlung von gynäkologischen Störungen |
| WO1997041145A1 (en) * | 1996-05-01 | 1997-11-06 | The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | 21-substituted progesterone derivatives as new antiprogestational agents |
| 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 |
| EP1144396A2 (en) * | 1999-01-14 | 2001-10-17 | Bayer Corporation | Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents |
| HK1043788A1 (zh) * | 1999-05-04 | 2002-09-27 | American Home Products Corporation | 四環黃體酮受體調節劑化合物及方法 |
-
2000
- 2000-08-31 CA CA002382580A patent/CA2382580C/en not_active Expired - Lifetime
- 2000-08-31 IL IL14841600A patent/IL148416A0/xx unknown
- 2000-08-31 AT AT00957914T patent/ATE375160T1/de not_active IP Right Cessation
- 2000-08-31 ES ES00957914T patent/ES2295050T3/es not_active Expired - Lifetime
- 2000-08-31 PT PT00957914T patent/PT1229906E/pt unknown
- 2000-08-31 CO CO00065515A patent/CO5200772A1/es not_active Application Discontinuation
- 2000-08-31 PL PL353930A patent/PL198790B1/pl not_active IP Right Cessation
- 2000-08-31 KR KR1020087016247A patent/KR20080066095A/ko not_active Withdrawn
- 2000-08-31 KR KR1020027002790A patent/KR100755109B1/ko not_active Expired - Fee Related
- 2000-08-31 ME MEP-138/08A patent/MEP13808A/xx unknown
- 2000-08-31 DE DE60036723T patent/DE60036723T2/de not_active Expired - Lifetime
- 2000-08-31 HU HU0202429A patent/HUP0202429A3/hu unknown
- 2000-08-31 SI SI200020042A patent/SI20852B/sl not_active IP Right Cessation
- 2000-08-31 EE EEP200200104A patent/EE05172B1/xx not_active IP Right Cessation
- 2000-08-31 BR BR0014161-5A patent/BR0014161A/pt not_active Application Discontinuation
- 2000-08-31 SK SK299-2002A patent/SK287192B6/sk unknown
- 2000-08-31 PE PE2000000893A patent/PE20010578A1/es not_active Application Discontinuation
- 2000-08-31 KR KR1020077011455A patent/KR100864547B1/ko not_active Expired - Fee Related
- 2000-08-31 AU AU69466/00A patent/AU781840B2/en not_active Ceased
- 2000-08-31 EP EP00957914A patent/EP1229906B1/en not_active Expired - Lifetime
- 2000-08-31 CZ CZ2002704A patent/CZ2002704A3/cs unknown
- 2000-08-31 UA UA2002032430A patent/UA78184C2/uk unknown
- 2000-08-31 RS YUP-140/02A patent/RS50283B/sr unknown
- 2000-08-31 DK DK00957914T patent/DK1229906T3/da active
- 2000-08-31 AR ARP000104538A patent/AR025457A1/es unknown
- 2000-08-31 JP JP2001519893A patent/JP2003535029A/ja active Pending
- 2000-08-31 NZ NZ517471A patent/NZ517471A/en unknown
- 2000-08-31 WO PCT/US2000/023770 patent/WO2001015679A2/en not_active Ceased
- 2000-08-31 EA EA200200282A patent/EA007854B1/ru not_active IP Right Cessation
- 2000-08-31 RO ROA200200229A patent/RO122179B1/ro unknown
- 2000-08-31 HR HR20020267A patent/HRP20020267A2/xx not_active Application Discontinuation
-
2002
- 2002-02-26 BG BG106442A patent/BG65817B1/bg unknown
- 2002-02-28 MX MXPA02002191A patent/MXPA02002191A/es active IP Right Grant
- 2002-02-28 NO NO20020999A patent/NO20020999L/no not_active Application Discontinuation
- 2002-03-21 LT LT2002031A patent/LT5034B/lt not_active IP Right Cessation
- 2002-03-28 LV LVP-02-53A patent/LV12941B/lv unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP0723439B1 (de) | Kombination von progesteronantagonisten und antiöstrogenen mit partialer agonistischer wirkung für die hormonsubstitutions-therapie für peri- und postmenopausale frauen | |
| DE19739916C2 (de) | Verwendung einer Kombination aus einem Gestagen und einem Estrogen zur kontinuierlichen Ovulationshemmung und ggf. gleichzeitigen Behandlung und/oder Prophylaxe von Tumoren der Brustdrüsen | |
| DE3855606T2 (de) | Verwendung von Melatonin zur Herstellung einer kontrazeptiven Zusammensetzung | |
| DE69804918T2 (de) | Sehr niedrigdosiertes orales Kontrazeptiv mit weniger Menstruationsblutungen und verzögerter Wirkung | |
| EP2445491B1 (de) | Pharmazeutische zusammensetzung zur notfallempfängnisverhütung | |
| EP2552404B1 (de) | Parenterale arzneiform, die aromatasehemmer und gestagene freisetzt, für die behandlung von endometriose | |
| EP0799042A1 (de) | Progesteronantagonistisch- und antiöstrogen wirksame verbindungen zur gemeinsamen verwendung für die weibliche kontrazeption | |
| DE60218881T2 (de) | Verfahren zur vorbeugung oder behandlung von benignen gynäkologischen störungen | |
| DE69327319T2 (de) | Minimierung von mit progesteron verbundenen durchbruckblutungen | |
| WO1998035682A1 (de) | Mittel zur hormonalen kontrazeption und/oder behandlung und/oder prophylaxe von tumoren der brustdrüsen mit drei hormonkomponente | |
| DE60036723T2 (de) | Mesoprogestine zur behandlung und vorbeugung von hormonabhängigen gutartigen gynekologischen störungen | |
| DE69430732T2 (de) | Kit zur verhütung oder hemmung der befruchtung | |
| DE4329344A1 (de) | Progesteronantagonistisch- und antiöstrogen wirksame Verbindungen für die Behandlung des Leiomyomata uteri | |
| DE69827017T2 (de) | Kombinationen von endometrium schonenden gestagenen und endometrium atrophisierenden gestagenen mit estrogenen, bei der oralen empfängnisverhütung | |
| US8193252B1 (en) | Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders | |
| WO2006087173A1 (de) | Pharmazeutisches präparat zur kontrazeption | |
| DE4406915A1 (de) | Ovulationshemmendes Mittel zur hormonalen Kontrazeption | |
| CN1450892A (zh) | 中孕酮(孕酮受体调节剂)用于治疗和预防激素依赖性良性妇科疾病 | |
| WO1996029078A1 (de) | OVULATIONSHEMMENDES MITTEL ZUR HORMONALEN KONTRAZEPTION DAS 50-70 νg LEVONORGESTREL UND MEHR ALS 30-40 νg ETHINYLESTRADIOL ENTHÄLT |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8327 | Change in the person/name/address of the patent owner |
Owner name: BAYER SCHERING PHARMA AKIENGESELLSCHAFT, 13353, DE |
|
| 8364 | No opposition during term of opposition |