CO5200773A1 - Mesoprogestinas (moduladores de receptores para progestero- na) como componente de composiciones utilizadas para la terapia de sustitucion hormonal (trh) - Google Patents
Mesoprogestinas (moduladores de receptores para progestero- na) como componente de composiciones utilizadas para la terapia de sustitucion hormonal (trh)Info
- Publication number
- CO5200773A1 CO5200773A1 CO00065516A CO00065516A CO5200773A1 CO 5200773 A1 CO5200773 A1 CO 5200773A1 CO 00065516 A CO00065516 A CO 00065516A CO 00065516 A CO00065516 A CO 00065516A CO 5200773 A1 CO5200773 A1 CO 5200773A1
- Authority
- CO
- Colombia
- Prior art keywords
- hrt
- progesterone
- mcphail
- mesoprogestins
- component
- Prior art date
Links
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound 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 title abstract 5
- 230000003054 hormonal effect Effects 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title 1
- 238000009256 replacement therapy Methods 0.000 title 1
- 238000002657 hormone replacement therapy Methods 0.000 abstract 3
- 102000005962 receptors Human genes 0.000 abstract 3
- 108020003175 receptors Proteins 0.000 abstract 3
- 230000001270 agonistic effect Effects 0.000 abstract 2
- 230000003042 antagnostic effect Effects 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 229940011871 estrogen Drugs 0.000 abstract 2
- 239000000262 estrogen Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000186 progesterone Substances 0.000 abstract 2
- 229960003387 progesterone Drugs 0.000 abstract 2
- 241001465754 Metazoa Species 0.000 abstract 1
- 241000283973 Oryctolagus cuniculus Species 0.000 abstract 1
- 230000000708 anti-progestin effect Effects 0.000 abstract 1
- 239000003418 antiprogestin Substances 0.000 abstract 1
- 239000000306 component Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 239000005426 pharmaceutical component Substances 0.000 abstract 1
- 239000000044 progesterone antagonist Substances 0.000 abstract 1
- 239000000583 progesterone congener Substances 0.000 abstract 1
- 102000003998 progesterone receptors Human genes 0.000 abstract 1
- 108090000468 progesterone receptors Proteins 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 210000004291 uterus Anatomy 0.000 abstract 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
- 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
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Epidemiology (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)
Abstract
La presente invención hace referencia a al uso de mesoprogestinas como componentes farmacéuticos para la fabricación de un medicamento para la terapia de sustitución hormonal (TRH) y como componente para el uso combinado junto con un estrógeno para la fabricación de un medicamento para TRH así como en métodos de TRH respectivos y en métodos para tratar la insuficiencia hormonal y síntomas de irregularidad hormonal. Las mesoprogestinas se definen como compuestos que disponen de actividades tanto agonísticas como antagonísticas en el receptor de progesterona (RP) in vivo.Estabilizan la f´unción del RP en un nivel intermedio entre agonístico y antagonístico. Las progestinas y las antiprogestinas no permiten alcanzar estados funcionales correspondientes.J867, J912, J956 y J1042 son las mesoprogestinas preferidas de acuerdo con la invención.Figuras 1A y 1BEfectos tipo progesterona (arriba, Figura 1A) y antagonísticos de progesterona (debajo, Figura 1B) de los moduladores de RP en el útero de conejos inmaduros preparados con estrógeno (prueba de McPhail).Figura 1A:Resultado de McPhail<EMI FILE="00065516_1" ID="1" IMF=JPEG >vehículo - progesterona - RU486 - J867 - J956 - J1042Figura 1B:Resultado de McPhail<EMI FILE="00065516_2" ID="2" IMF=JPEG >mg/animal/día (dosis de sustancias de prueba + 1,0 mg de progesterona).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38614099A | 1999-08-31 | 1999-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5200773A1 true CO5200773A1 (es) | 2002-09-27 |
Family
ID=23524333
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00065516A CO5200773A1 (es) | 1999-08-31 | 2000-08-31 | Mesoprogestinas (moduladores de receptores para progestero- na) como componente de composiciones utilizadas para la terapia de sustitucion hormonal (trh) |
Country Status (33)
| Country | Link |
|---|---|
| EP (1) | EP1605924B1 (es) |
| JP (1) | JP2003513908A (es) |
| KR (1) | KR100729311B1 (es) |
| CN (1) | CN1454088A (es) |
| AR (1) | AR025456A1 (es) |
| AT (1) | ATE413168T1 (es) |
| AU (1) | AU781836B2 (es) |
| BG (1) | BG65846B1 (es) |
| BR (1) | BR0013710A (es) |
| CA (1) | CA2383659C (es) |
| CO (1) | CO5200773A1 (es) |
| CZ (1) | CZ301412B6 (es) |
| DE (1) | DE60040764D1 (es) |
| EA (1) | EA007840B1 (es) |
| EE (1) | EE200200102A (es) |
| ES (1) | ES2316402T3 (es) |
| HR (1) | HRP20020266A2 (es) |
| HU (1) | HUP0202460A3 (es) |
| IL (2) | IL148417A0 (es) |
| LT (1) | LT5011B (es) |
| LV (1) | LV12942B (es) |
| MX (1) | MXPA02002190A (es) |
| NO (1) | NO20021000L (es) |
| NZ (1) | NZ517469A (es) |
| PE (1) | PE20010581A1 (es) |
| PL (1) | PL198798B1 (es) |
| RO (1) | RO122180B1 (es) |
| RS (1) | RS50396B (es) |
| SI (1) | SI20851B (es) |
| SK (1) | SK287121B6 (es) |
| UA (1) | UA75339C2 (es) |
| WO (1) | WO2001034126A2 (es) |
| ZA (1) | ZA200201621B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10236405A1 (de) | 2002-08-02 | 2004-02-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie |
| ATE338763T1 (de) * | 2002-08-02 | 2006-09-15 | 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 |
| RU2611370C1 (ru) * | 2016-01-12 | 2017-02-21 | Общество с ограниченной ответственностью Медицинская Корпорация "РАНА" | Применение препарата Лаеннек для уменьшения или устранения проявления менопаузальных симптомов (варианты) |
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 |
| US4729999A (en) * | 1984-10-12 | 1988-03-08 | Bcm Technologies | Antiestrogen therapy for symptoms of estrogen deficiency |
| MX9301121A (es) * | 1992-03-02 | 1993-09-01 | Schering Ag | Metodo y equipo para la contracepcion oral y regulacion de la menstruacion con estrogeno/progestina/aniprogestina. |
| TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| DE4225623C2 (de) * | 1992-08-03 | 1994-06-30 | Karl Hehl | Verfahren zur Herstellung einer pulverförmigen Spritzgußmasse für die Herstellung von Porzellan und deren Verwendung |
| US5468736A (en) * | 1993-02-25 | 1995-11-21 | The Medical College Of Hampton Road | Hormone replacement therapy |
| 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 |
| US5391557A (en) * | 1993-10-15 | 1995-02-21 | Eli Lilly And Company | Methods for the treatment of peri-menopausal syndrome |
| EP0787002B1 (de) * | 1994-10-24 | 2006-12-13 | Schering Aktiengesellschaft | Kompetitive progesteronantagonisten zur bedarfsorientierten weiblichen fertilitätskontrolle |
| DE19610635A1 (de) * | 1996-03-11 | 1997-09-18 | Schering Ag | Sequentielle Estrogen/Progesteronantagonist-Kombination für die Hormonersatz-Therapie |
| CA2255863A1 (en) * | 1996-06-25 | 1997-12-31 | Akzo Nobel Nv | Progestogen-anti-progestogen regimens |
| 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 |
| TR200102041T2 (tr) * | 1999-01-14 | 2001-12-21 | Bayer Corporation | Progesteron reseptör bağlama aktif maddeleri olarak ikameli 2-arilimino heterosaykıllar |
-
2000
- 2000-08-31 AU AU36332/01A patent/AU781836B2/en not_active Ceased
- 2000-08-31 AR ARP000104537A patent/AR025456A1/es unknown
- 2000-08-31 CO CO00065516A patent/CO5200773A1/es not_active Application Discontinuation
- 2000-08-31 HU HU0202460A patent/HUP0202460A3/hu unknown
- 2000-08-31 KR KR1020027002815A patent/KR100729311B1/ko not_active Expired - Fee Related
- 2000-08-31 UA UA2002032428A patent/UA75339C2/uk unknown
- 2000-08-31 CA CA002383659A patent/CA2383659C/en not_active Expired - Lifetime
- 2000-08-31 PE PE2000000892A patent/PE20010581A1/es not_active Application Discontinuation
- 2000-08-31 CN CN00812257A patent/CN1454088A/zh active Pending
- 2000-08-31 EA EA200200285A patent/EA007840B1/ru not_active IP Right Cessation
- 2000-08-31 BR BR0013710-3A patent/BR0013710A/pt not_active Application Discontinuation
- 2000-08-31 SI SI200020041A patent/SI20851B/sl not_active IP Right Cessation
- 2000-08-31 DE DE60040764T patent/DE60040764D1/de not_active Expired - Lifetime
- 2000-08-31 RO ROA200200230A patent/RO122180B1/ro unknown
- 2000-08-31 PL PL353931A patent/PL198798B1/pl not_active IP Right Cessation
- 2000-08-31 EP EP00991840A patent/EP1605924B1/en not_active Expired - Lifetime
- 2000-08-31 HR HR20020266A patent/HRP20020266A2/hr not_active Application Discontinuation
- 2000-08-31 EE EEP200200102A patent/EE200200102A/xx unknown
- 2000-08-31 SK SK297-2002A patent/SK287121B6/sk not_active IP Right Cessation
- 2000-08-31 CZ CZ20020706A patent/CZ301412B6/cs not_active IP Right Cessation
- 2000-08-31 IL IL14841700A patent/IL148417A0/xx unknown
- 2000-08-31 ES ES00991840T patent/ES2316402T3/es not_active Expired - Lifetime
- 2000-08-31 RS YUP-141/02A patent/RS50396B/sr unknown
- 2000-08-31 JP JP2001536126A patent/JP2003513908A/ja active Pending
- 2000-08-31 WO PCT/US2000/023771 patent/WO2001034126A2/en not_active Ceased
- 2000-08-31 NZ NZ517469A patent/NZ517469A/en unknown
- 2000-08-31 AT AT00991840T patent/ATE413168T1/de not_active IP Right Cessation
-
2002
- 2002-02-26 ZA ZA200201621A patent/ZA200201621B/en unknown
- 2002-02-26 BG BG106443A patent/BG65846B1/bg unknown
- 2002-02-27 IL IL148417A patent/IL148417A/en not_active IP Right Cessation
- 2002-02-28 NO NO20021000A patent/NO20021000L/no not_active Application Discontinuation
- 2002-02-28 MX MXPA02002190A patent/MXPA02002190A/es active IP Right Grant
- 2002-03-27 LT LT2002037A patent/LT5011B/lt not_active IP Right Cessation
- 2002-03-28 LV LVP-02-54A patent/LV12942B/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |