CO5190694A1 - MESOPROGESTINES (PROGESTERONE RECEPTORS MODULATORS) AS COMPONENTS OF FEMALE ANTI-CONCEPTIVES - Google Patents
MESOPROGESTINES (PROGESTERONE RECEPTORS MODULATORS) AS COMPONENTS OF FEMALE ANTI-CONCEPTIVESInfo
- Publication number
- CO5190694A1 CO5190694A1 CO00065517A CO00065517A CO5190694A1 CO 5190694 A1 CO5190694 A1 CO 5190694A1 CO 00065517 A CO00065517 A CO 00065517A CO 00065517 A CO00065517 A CO 00065517A CO 5190694 A1 CO5190694 A1 CO 5190694A1
- Authority
- CO
- Colombia
- Prior art keywords
- progesterone
- mcphail
- mesoprogestins
- female
- contraception
- Prior art date
Links
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)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Diabetes (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)
Abstract
La presente invención hace referencia al uso de mesoprogestinas para producir un producto farmacéutico para la anticoncepción femenina, a una preparación farmacéutica para la anticoncepción femenina y a un método anticonceptivo femenino que administra cantidades efectivas de una mesoprogestina en una mujer que desea contar con anticoncepción.Opcionalmente, la mesoprogestina puede utilizarse en combinación con un estrógeno.Las mesoprogestinas se definen como compuestos que disponen de actividad tanto agonística como antagonística en el receptor de progesterona (RP) in vivo. Estabilizan la función de RP en un nivel intermedio entre agonístico y antagonístico. Con las progestinas o las antiprogestinas no es posible lograr estados funcionales correspondientes.J867, J912, J956 y J1042 son las mesoprogestinas preferibles 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="00065517_1" ID="1" IMF=JPEG >vehículo - progesterona - RU486 - J867 - J956 - J1042Figura 1B:Resultado de McPhail<EMI FILE="00065517_2" ID="2" IMF=JPEG >Mg/animal/día (dosis de sustancias de prueba + 1,0 mg de progesterona).The present invention refers to the use of mesoprogestins to produce a pharmaceutical product for female contraception, a pharmaceutical preparation for female contraception and a female contraceptive method that administers effective amounts of a mesoprogestin in a woman who wishes to have contraception. Mesoprogestin can be used in combination with an estrogen. Mesoprogestins are defined as compounds that have both agonistic and antagonistic activity in the progesterone receptor (RP) in vivo. They stabilize the function of RP at an intermediate level between agonistic and antagonistic. With progestins or antiprogestins it is not possible to achieve corresponding functional states. J867, J912, J956 and J1042 are the preferable mesoprogestins according to the invention. Figures 1A and 1B progesterone-like effects (above, Figure 1A) and progesterone antagonists (below, Figure 1B) of RP modulators in the uterus of immature rabbits prepared with estrogen (McPhail test). Figure 1A: McPhail result <EMI FILE = "00065517_1" ID = "1" MFI = JPEG> vehicle - progesterone - RU486 - J867 - J956 - J1042 Figure 1B: McPhail result <EMI FILE = "00065517_2" ID = "2" MFI = JPEG> Mg / animal / day (dose of test substances + 1.0 mg progesterone).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38613399A | 1999-08-31 | 1999-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5190694A1 true CO5190694A1 (en) | 2002-08-29 |
Family
ID=23524305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00065517A CO5190694A1 (en) | 1999-08-31 | 2000-08-31 | MESOPROGESTINES (PROGESTERONE RECEPTORS MODULATORS) AS COMPONENTS OF FEMALE ANTI-CONCEPTIVES |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1605949A2 (en) |
| JP (1) | JP2003511399A (en) |
| KR (1) | KR20020038745A (en) |
| CN (1) | CN1384748A (en) |
| AR (1) | AR025455A1 (en) |
| AU (1) | AU781835B2 (en) |
| BG (1) | BG106441A (en) |
| BR (1) | BR0013711A (en) |
| CA (1) | CA2383650A1 (en) |
| CO (1) | CO5190694A1 (en) |
| CZ (1) | CZ2002707A3 (en) |
| EA (1) | EA006805B1 (en) |
| EE (1) | EE200200103A (en) |
| HR (1) | HRP20020265A2 (en) |
| HU (1) | HUP0202515A3 (en) |
| IL (1) | IL148415A0 (en) |
| LT (1) | LT5001B (en) |
| LV (1) | LV12940B (en) |
| MX (1) | MXPA02002186A (en) |
| NO (1) | NO20020998L (en) |
| NZ (1) | NZ517470A (en) |
| PE (1) | PE20010579A1 (en) |
| PL (1) | PL353994A1 (en) |
| SI (1) | SI20853A (en) |
| SK (1) | SK2982002A3 (en) |
| UA (1) | UA77150C2 (en) |
| WO (1) | WO2001026603A2 (en) |
| YU (1) | YU13902A (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10236405A1 (en) | 2002-08-02 | 2004-02-19 | Schering Ag | New 4-(3-oxo-estra-4,9-dien-11 beta-yl)-benzaldehyde oximes, are progesterone receptor modulators useful in female contraception, hormone replacement therapy and treatment of gynecological disorders |
| ES2273061T3 (en) * | 2002-08-02 | 2007-05-01 | Schering Aktiengesellschaft | PROGESTERONE RECEPTORS MODULATING AGENTS WITH ELEVATED ANTIGONADOTROP ACTIVITY FOR FEMALE FERTILITY CONTROL AND FOR HORMONAL REPLACEMENT THERAPY. |
| 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 |
| SV2006002165A (en) * | 2004-07-07 | 2006-05-09 | Wyeth Corp | CYCLICAL PROGESTINE REGIMES AND KITS REF. AM101677 |
| DE102005050729A1 (en) * | 2005-10-19 | 2007-04-26 | Schering Ag | Method of preventive on-demand hormonal contraception |
| NZ595790A (en) * | 2009-04-14 | 2013-11-29 | Hra Pharma Lab | Method for on-demand contraception |
| CN110548034A (en) * | 2019-07-12 | 2019-12-10 | 广州莎蔓生物科技有限公司 | Pregnancy-blocking medicine |
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 (en) | 1936-11-20 | 1940-11-27 | Chemische Ind Ges | Process for the preparation of compounds of the estradiol type which are esterified in the 3-position |
| 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 (en) | 1983-10-12 | 1985-04-25 | Schering AG, 1000 Berlin und 4709 Bergkamen | PROSTAGLANDINE AND ANTIGESTAGE FOR PREGNANCY ABORT |
| EP0559240B1 (en) * | 1987-09-24 | 2001-12-05 | Jencap Research Limited | Contraceptive packages containing oestrogen and progestin |
| 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 (en) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Novel 11-benzaldoximestradiene derivatives, processes for their preparation and medicaments containing these compounds |
| DE4332284C2 (en) * | 1993-09-20 | 1997-05-28 | Jenapharm Gmbh | 11-Benzaldoxime-17beta-methoxy-17alpha-methoxymethyl-estradiene derivatives, process for their preparation and medicaments containing these compounds |
| DE4429398C2 (en) | 1994-08-09 | 1997-09-11 | Jenapharm Gmbh | Use of Estra-1,3,5 (10) -triene derivatives for hormonal contraception |
| DE4429397C2 (en) | 1994-08-09 | 2003-11-20 | Jenapharm Gmbh | Estra-1,3,5 (10) -triene derivatives, processes for their preparation and pharmaceutical compositions containing these compounds |
| DE59511071D1 (en) * | 1994-10-24 | 2007-01-25 | Schering Ag | COMPETITIVE PROGESTERONANT AGONISTS FOR THE FOCUSED FEMININE FERTILITY CONTROL |
| US6040340A (en) * | 1996-05-07 | 2000-03-21 | Schering Aktiengesellschaft | Implantation rates after in vitro fertilization, treatment of infertility and early pregnancy loss with a nitric oxide donor alone or in combination with progesterone, and a method for contraception with nitric oxide inhibitors |
| KR20000022189A (en) * | 1996-06-25 | 2000-04-25 | 에프.지.엠. 헤르만스;이.에이치. 리링크 | Progestogen-anti-progestogen regimens |
| WO1998005679A2 (en) * | 1996-08-05 | 1998-02-12 | Duke University | Mixed agonists of the progesterone receptor and assays therefor |
| DE19809845A1 (en) * | 1998-03-03 | 1999-09-09 | Jenapharm Gmbh | S-substituted 11beta-benzaldoxime-estra-4,9-diene-carbonic acid thiol esters, processes for their preparation and pharmaceutical preparations containing these compounds |
| WO2000066590A2 (en) * | 1999-05-04 | 2000-11-09 | Ligand Pharmaceuticals, Inc. | Tetracyclic progesterone receptor modulator compounds and methods |
-
2000
- 2000-08-31 PL PL00353994A patent/PL353994A1/en not_active Application Discontinuation
- 2000-08-31 SK SK298-2002A patent/SK2982002A3/en unknown
- 2000-08-31 IL IL14841500A patent/IL148415A0/en unknown
- 2000-08-31 BR BR0013711-1A patent/BR0013711A/en not_active IP Right Cessation
- 2000-08-31 HU HU0202515A patent/HUP0202515A3/en unknown
- 2000-08-31 UA UA2002032429A patent/UA77150C2/en unknown
- 2000-08-31 CN CN00812308A patent/CN1384748A/en active Pending
- 2000-08-31 SI SI200020043A patent/SI20853A/en not_active IP Right Cessation
- 2000-08-31 EA EA200200284A patent/EA006805B1/en not_active IP Right Cessation
- 2000-08-31 YU YU13902A patent/YU13902A/en unknown
- 2000-08-31 AU AU32150/01A patent/AU781835B2/en not_active Ceased
- 2000-08-31 EP EP00991299A patent/EP1605949A2/en not_active Withdrawn
- 2000-08-31 KR KR1020027002785A patent/KR20020038745A/en not_active Application Discontinuation
- 2000-08-31 WO PCT/IB2000/002053 patent/WO2001026603A2/en not_active Application Discontinuation
- 2000-08-31 CZ CZ2002707A patent/CZ2002707A3/en unknown
- 2000-08-31 PE PE2000000894A patent/PE20010579A1/en not_active Application Discontinuation
- 2000-08-31 MX MXPA02002186A patent/MXPA02002186A/en not_active Application Discontinuation
- 2000-08-31 JP JP2001529395A patent/JP2003511399A/en active Pending
- 2000-08-31 NZ NZ517470A patent/NZ517470A/en unknown
- 2000-08-31 CA CA002383650A patent/CA2383650A1/en not_active Abandoned
- 2000-08-31 AR ARP000104536A patent/AR025455A1/en unknown
- 2000-08-31 EE EEP200200103A patent/EE200200103A/en unknown
- 2000-08-31 CO CO00065517A patent/CO5190694A1/en not_active Application Discontinuation
-
2002
- 2002-02-26 BG BG06441A patent/BG106441A/en unknown
- 2002-02-28 NO NO20020998A patent/NO20020998L/en not_active Application Discontinuation
- 2002-03-26 LT LT2002035A patent/LT5001B/en not_active IP Right Cessation
- 2002-03-28 HR HR20020265A patent/HRP20020265A2/en not_active Application Discontinuation
- 2002-03-28 LV LVP-02-52A patent/LV12940B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2003511399A (en) | 2003-03-25 |
| CN1384748A (en) | 2002-12-11 |
| AU3215001A (en) | 2001-04-23 |
| BR0013711A (en) | 2002-05-07 |
| PE20010579A1 (en) | 2001-06-04 |
| HRP20020265A2 (en) | 2004-02-29 |
| LT2002035A (en) | 2002-10-25 |
| WO2001026603A3 (en) | 2002-01-17 |
| KR20020038745A (en) | 2002-05-23 |
| NO20020998D0 (en) | 2002-02-28 |
| NZ517470A (en) | 2004-03-26 |
| SI20853A (en) | 2002-10-31 |
| NO20020998L (en) | 2002-03-14 |
| EA200200284A1 (en) | 2002-10-31 |
| EE200200103A (en) | 2003-04-15 |
| AU781835B2 (en) | 2005-06-16 |
| PL353994A1 (en) | 2003-12-15 |
| LV12940B (en) | 2003-06-20 |
| BG106441A (en) | 2002-09-30 |
| LT5001B (en) | 2003-03-25 |
| AR025455A1 (en) | 2002-11-27 |
| EP1605949A2 (en) | 2005-12-21 |
| EA006805B1 (en) | 2006-04-28 |
| MXPA02002186A (en) | 2002-09-02 |
| HUP0202515A3 (en) | 2004-06-28 |
| WO2001026603A2 (en) | 2001-04-19 |
| IL148415A0 (en) | 2002-09-12 |
| CA2383650A1 (en) | 2001-04-19 |
| UA77150C2 (en) | 2006-11-15 |
| SK2982002A3 (en) | 2002-07-02 |
| CZ2002707A3 (en) | 2002-11-13 |
| YU13902A (en) | 2006-01-16 |
| HUP0202515A2 (en) | 2002-12-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |