RU2008116571A - Новые с18 модифицированные ретростероиды в качестве модулятора рецептора прогестерона - Google Patents
Новые с18 модифицированные ретростероиды в качестве модулятора рецептора прогестерона Download PDFInfo
- Publication number
- RU2008116571A RU2008116571A RU2008116571/04A RU2008116571A RU2008116571A RU 2008116571 A RU2008116571 A RU 2008116571A RU 2008116571/04 A RU2008116571/04 A RU 2008116571/04A RU 2008116571 A RU2008116571 A RU 2008116571A RU 2008116571 A RU2008116571 A RU 2008116571A
- Authority
- RU
- Russia
- Prior art keywords
- ethyl
- group
- dione
- alkyl
- pregna
- Prior art date
Links
- 239000002379 progesterone receptor modulator Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 20
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 16
- 239000001257 hydrogen Substances 0.000 claims abstract 16
- 229910052736 halogen Inorganic materials 0.000 claims abstract 15
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 13
- 125000003118 aryl group Chemical group 0.000 claims abstract 12
- 125000004122 cyclic group Chemical group 0.000 claims abstract 10
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 9
- 125000005842 heteroatom Chemical group 0.000 claims abstract 9
- 125000004430 oxygen atom Chemical group O* 0.000 claims abstract 9
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 6
- 239000000651 prodrug Substances 0.000 claims abstract 6
- 229940002612 prodrug Drugs 0.000 claims abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- 150000003839 salts Chemical class 0.000 claims abstract 5
- 125000001424 substituent group Chemical group 0.000 claims abstract 5
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 5
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 4
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims abstract 3
- 125000003367 polycyclic group Chemical group 0.000 claims abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 28
- -1 4-hydroxyaminoformylphenyl Chemical group 0.000 claims 16
- 238000000034 method Methods 0.000 claims 9
- 102000003998 progesterone receptors Human genes 0.000 claims 9
- 108090000468 progesterone receptors Proteins 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 6
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 6
- 230000001419 dependent effect Effects 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 5
- 229940088597 hormone Drugs 0.000 claims 5
- 239000005556 hormone Substances 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 102000005962 receptors Human genes 0.000 claims 5
- 108020003175 receptors Proteins 0.000 claims 5
- 206010027514 Metrorrhagia Diseases 0.000 claims 4
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000004494 ethyl ester group Chemical group 0.000 claims 4
- 201000010260 leiomyoma Diseases 0.000 claims 4
- 208000007106 menorrhagia Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 229940011871 estrogen Drugs 0.000 claims 3
- 239000000262 estrogen Substances 0.000 claims 3
- 238000011282 treatment Methods 0.000 claims 3
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000014311 Cushing syndrome Diseases 0.000 claims 2
- 208000016192 Demyelinating disease Diseases 0.000 claims 2
- 206010013908 Dysfunctional uterine bleeding Diseases 0.000 claims 2
- 208000005171 Dysmenorrhea Diseases 0.000 claims 2
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- 208000033830 Hot Flashes Diseases 0.000 claims 2
- 206010060800 Hot flush Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 201000006828 endometrial hyperplasia Diseases 0.000 claims 2
- 230000035558 fertility Effects 0.000 claims 2
- 238000002657 hormone replacement therapy Methods 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 208000022168 hypermenorrhea Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 206010027191 meningioma Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 201000007954 uterine fibroid Diseases 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- JGMOKGBVKVMRFX-HQZYFCCVSA-N dydrogesterone Chemical compound C1=CC2=CC(=O)CC[C@@]2(C)[C@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 JGMOKGBVKVMRFX-HQZYFCCVSA-N 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- AIHDCSAXVMAMJH-GFBKWZILSA-N levan Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)OC[C@@H]1[C@@H](O)[C@H](O)[C@](CO)(CO[C@@H]2[C@H]([C@H](O)[C@@](O)(CO)O2)O)O1 AIHDCSAXVMAMJH-GFBKWZILSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J15/00—Stereochemically pure steroids containing carbon, hydrogen, halogen or oxygen having a partially or totally inverted skeleton, e.g. retrosteroids, L-isomers
- C07J15/005—Retrosteroids (9 beta 10 alfa)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/36—Antigestagens
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05109126 | 2005-09-30 | ||
| EP05109126.2 | 2005-09-30 | ||
| EP06118034.5 | 2006-07-28 | ||
| EP06118034 | 2006-07-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2008116571A true RU2008116571A (ru) | 2009-11-10 |
Family
ID=37688673
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008116571/04A RU2008116571A (ru) | 2005-09-30 | 2006-09-28 | Новые с18 модифицированные ретростероиды в качестве модулятора рецептора прогестерона |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1928894A1 (https=) |
| JP (1) | JP2009512633A (https=) |
| CA (1) | CA2624015A1 (https=) |
| RU (1) | RU2008116571A (https=) |
| WO (1) | WO2007039544A1 (https=) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1247661A (en) * | 1967-07-11 | 1971-09-29 | Philips Nv | NEW 9beta,10alpha-STEROIDS AND METHODS OF PRODUCING THE SAME |
-
2006
- 2006-09-28 EP EP06806867A patent/EP1928894A1/en not_active Withdrawn
- 2006-09-28 RU RU2008116571/04A patent/RU2008116571A/ru not_active Application Discontinuation
- 2006-09-28 JP JP2008532784A patent/JP2009512633A/ja not_active Withdrawn
- 2006-09-28 CA CA002624015A patent/CA2624015A1/en not_active Abandoned
- 2006-09-28 WO PCT/EP2006/066842 patent/WO2007039544A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP1928894A1 (en) | 2008-06-11 |
| WO2007039544A1 (en) | 2007-04-12 |
| JP2009512633A (ja) | 2009-03-26 |
| CA2624015A1 (en) | 2007-04-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA200201052A1 (ru) | 8β-ГИДРОКАРБИЛЗАМЕЩЕННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ | |
| RU2007101303A (ru) | Модуляторы рецепторов прогестерона, содержащие производные пиррол-оксиндола и их применение | |
| US5272141A (en) | Contraceptive and menstrual cycle controlling drug having oncostatic therapeutic properties for treatment of mammary tumors and melanomas, and method therefor | |
| ES2280766T3 (es) | 5-(2-hidroxi-3'-1-(3-trifluorometilfenil)-ciclopropil)-propionilamino)-ftalida y compuestos afines con actividad moduladora del receptor de progesterona, para uso en control de la fertilidad y terapia de reemplazamiento hormonal. | |
| AU2012210691B2 (en) | Testosterone formulations | |
| RU2007101304A (ru) | Модуляторы рецептора прогестерона, содержащие производные пиррол-оксиндола и применение | |
| RU2000116270A (ru) | Новые антиэстрогенные стероиды и связанные с ними фармацевтические композиции и способы получения | |
| AR071516A1 (es) | Regimenes de dosificacion con antiprogestinas que comprende la administracion de un antagonista de progesterona como el compuesto cdb-4124 | |
| ES2548723T3 (es) | Geles a base de testosterona que comprenden propilenglicol y miristato de isopropilo como promotores de penetración | |
| US20070093548A1 (en) | Use of progesterone receptor modulators | |
| RU2008116571A (ru) | Новые с18 модифицированные ретростероиды в качестве модулятора рецептора прогестерона | |
| TWI234458B (en) | Inhibition of the growth factor dependency of tumor cells | |
| JP2006504736A5 (https=) | ||
| Tator et al. | The effect of exogenous thyroid hormones on functional recovery of the rat after acute spinal cord compression injury | |
| KR20020086905A (ko) | 노르에티스테론을 포함하는 남성 피임약 제형 | |
| RU2005128284A (ru) | Продленные режимы чрескожной контрацепции | |
| JP2001525807A (ja) | プレグナン−３−オール−２０−オン | |
| WO2012142029A2 (en) | Serms for the treatment of estrogen receptor-mediated disorders | |
| JP2009512633A5 (https=) | ||
| TW200902028A (en) | Combination of progesterone-receptor antagonist together with an aromatase inhibitor for use in BRCA mediated diseases | |
| Pasqualini et al. | Biological responses of 3-and 17-estrogen sulfates in the mammary cancer cell line MCF-7 | |
| Karl et al. | An approach to develop platinum complexes with a specific activity on hormone-dependent breast cancer | |
| Pronzato et al. | Danazol treatment for advanced breast cancer | |
| Schuderer et al. | Mammary tumor inhibiting cytotoxic-linked estrogens of the triphenylbutene-type | |
| WO2005048956A2 (en) | Estradiol-related compounds and methods of use as anti-tumor agents |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20101012 |