AR040188A1 - Estratrienos 9-alfa-sustituidos como estrogenos de eficacia selectiva - Google Patents
Estratrienos 9-alfa-sustituidos como estrogenos de eficacia selectivaInfo
- Publication number
- AR040188A1 AR040188A1 ARP030102079A ARP030102079A AR040188A1 AR 040188 A1 AR040188 A1 AR 040188A1 AR P030102079 A ARP030102079 A AR P030102079A AR P030102079 A ARP030102079 A AR P030102079A AR 040188 A1 AR040188 A1 AR 040188A1
- Authority
- AR
- Argentina
- Prior art keywords
- radical
- group
- optionally substituted
- straight
- independently
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0055—Estrane derivatives not substituted in position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
-
- 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
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Como ingredientes activos farmacéuticos, que presentan un vitro una mayor afinidad en preparaciones de receptores de estrógeno de próstata de rata que en preparaciones de receptores de estrógeno de útero de rata y que presentan in vivo, con preferencia, un efecto preferencial en el ovario en comparación con el útero, a su preparación, su aplicación terapéutica y a formas farmacéuticas que contienen los nuevos compuestos. Describe, además, el uso de estos compuestos para el tratamiento de enfermedades y estados originados por deficiencia de estrógenos. Reivindicación 1: Derivados de estra-1,3,5(10)-trieno 9a-sustituidos de la fórmula general (1) donde los radicales R3, R7, R7', R9, R13, R16, así como R17 y R17' poseen, independientemente entre sí, el siguiente significado: R3 es un átomo de hidrógeno o un grupo R18, donde R18 es un radical hidrocarburo de cadena lineal o ramificada, saturado o no saturado con hasta 6 átomos de carbono, un grupo trifluorometilo, un radical arilo, heteroarilo aralquilo opcionalmente sustituido, un radical acilo COR19, donde R19 es un radical hidrocarburo opcionalmente sustituido, de cadena lineal o ramificada, saturado o hasta tres veces no saturado, opcionalmente halogenado en forma parcial o total con hasta 10 átomos de carbono; o R18 es un grupo R20SO2, donde R20 es un grupo R21R22N, donde R21 y R22 son, independientemente entre sí, un átomo de hidrógeno, un radical alquilo C1-5, un grupo C(O)R23, donde R23 es un radical hidrocarburo opcionalmente sustituido, de cadena lineal o ramificada, saturado o hasta tres veces no saturado, opcionalmente halogenado en forma parcial o total con hasta 10 átomos de carbono, un radical cicloalquilo C3-7 opcionalmente sustituido, un radical cicloalquilo C4-15 opcionalmente sustituido o un radical arilo, heteroarilo o aralquilo opcionalmente sustituido o, junto con el átomo de N, es un radical polimetilenimino C4-6 o un radical morfolino; R7 y R7' son en cada caso, independientemente entre sí, un átomo de hidrógeno o un átomo de halógeno; R9 es un radical alquenilo o alquinilo de cadena lineal o ramificada C2-6, que puede estar opcionalmente fluorado en forma parcial o total, o un radical etinilo o prop-1-inilo; R13 es un grupo metilo o un grupo etilo; R16 es un grupo hidroxi o un grupo R18O-, R20SO2- u OC(O)R23 con R18, R20 y R23 con el correspondiente significado indicado en R3; R17 y R17' son en cada caso, independientemente entre sí, un átomo de hidrógeno o un átomo de halógeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10226326A DE10226326A1 (de) | 2002-06-11 | 2002-06-11 | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040188A1 true AR040188A1 (es) | 2005-03-16 |
Family
ID=29723144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030102079A AR040188A1 (es) | 2002-06-11 | 2003-06-11 | Estratrienos 9-alfa-sustituidos como estrogenos de eficacia selectiva |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP1517914B1 (es) |
| JP (1) | JP4615998B2 (es) |
| KR (1) | KR101006612B1 (es) |
| CN (1) | CN1293090C (es) |
| AR (1) | AR040188A1 (es) |
| AT (1) | ATE303397T1 (es) |
| AU (1) | AU2003242683B9 (es) |
| BR (1) | BR0312140A (es) |
| CA (1) | CA2486495C (es) |
| CR (1) | CR10289A (es) |
| CU (1) | CU23414B7 (es) |
| DE (2) | DE10226326A1 (es) |
| DK (1) | DK1517914T3 (es) |
| EA (1) | EA008442B1 (es) |
| EC (1) | ECSP055530A (es) |
| ES (1) | ES2248770T3 (es) |
| HK (1) | HK1081203A1 (es) |
| HR (1) | HRP20050009B1 (es) |
| IL (1) | IL165321A (es) |
| MX (1) | MXPA04012491A (es) |
| NO (1) | NO329563B1 (es) |
| PE (1) | PE20040613A1 (es) |
| PL (1) | PL209910B1 (es) |
| RS (1) | RS50878B (es) |
| TW (1) | TWI286140B (es) |
| UA (1) | UA78062C2 (es) |
| UY (1) | UY27844A1 (es) |
| WO (1) | WO2003104253A2 (es) |
| ZA (1) | ZA200500217B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| PT1689410E (pt) * | 2003-11-26 | 2008-08-18 | Bayer Schering Pharma Ag | Prevenção e tratamento de doenças cardíacas hipertensivas pelos estrogénios selectivos 8beta-vinil-estra-1,3,5(10)-trieno-3,17beta-diol e 17beta-fluoro-9alfa-vinil-estra-1,3,5(10)-trieno-3,16alfa-diol |
| US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
| DE102005057224A1 (de) | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| JP2011511816A (ja) * | 2008-02-13 | 2011-04-14 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 安定化効果を有する薬物送達システム |
| EP2143432A1 (en) | 2008-07-11 | 2010-01-13 | Bayer Schering Pharma AG | 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer |
| CA2744127A1 (en) * | 2008-11-21 | 2010-05-27 | Bayer Schering Pharma Aktiengesellschaft | Drug delivery system |
| AU2015308987B2 (en) | 2014-08-26 | 2021-02-18 | Betanien Hospital | Methods, agents and compositions for treatment of inflammatory conditions |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2336432A1 (de) | 1973-07-13 | 1975-01-30 | Schering Ag | 3.17.18-trihydroxy-1.3.5(10)-oestratriene |
| US6154158A (en) * | 1998-06-30 | 2000-11-28 | Qualcomm Incorporated | Digital-to-analog converter D.C. offset correction comparing converter input and output signals |
| DE19906159A1 (de) * | 1999-02-09 | 2000-08-10 | Schering Ag | 16-Hydroxyestratriene als selektiv wirksame Estrogene |
| PT1226155E (pt) * | 1999-11-02 | 2007-07-26 | Bayer Schering Pharma Ag | 18-nor-esteróides como estrogénios selectivamente activos |
| IL152248A0 (en) * | 2000-04-12 | 2003-05-29 | Schering Ag | 8beta-HYDROCARBYL-SUBSTITUTED ESTRATRIENES FOR USE AS SELECTIVE ESTROGENS |
-
2002
- 2002-06-11 DE DE10226326A patent/DE10226326A1/de not_active Ceased
-
2003
- 2003-06-10 PE PE2003000575A patent/PE20040613A1/es not_active Application Discontinuation
- 2003-06-11 KR KR1020047020133A patent/KR101006612B1/ko not_active IP Right Cessation
- 2003-06-11 MX MXPA04012491A patent/MXPA04012491A/es active IP Right Grant
- 2003-06-11 ES ES03757065T patent/ES2248770T3/es not_active Expired - Lifetime
- 2003-06-11 RS YUP-1070/04A patent/RS50878B/sr unknown
- 2003-06-11 PL PL373090A patent/PL209910B1/pl not_active IP Right Cessation
- 2003-06-11 CN CNB038135027A patent/CN1293090C/zh not_active Expired - Fee Related
- 2003-06-11 JP JP2004511321A patent/JP4615998B2/ja not_active Expired - Fee Related
- 2003-06-11 DE DE50301116T patent/DE50301116D1/de not_active Expired - Lifetime
- 2003-06-11 EP EP03757065A patent/EP1517914B1/de not_active Expired - Lifetime
- 2003-06-11 DK DK03757065T patent/DK1517914T3/da active
- 2003-06-11 TW TW092115863A patent/TWI286140B/zh not_active IP Right Cessation
- 2003-06-11 CA CA2486495A patent/CA2486495C/en not_active Expired - Fee Related
- 2003-06-11 AT AT03757065T patent/ATE303397T1/de active
- 2003-06-11 UY UY27844A patent/UY27844A1/es not_active Application Discontinuation
- 2003-06-11 AU AU2003242683A patent/AU2003242683B9/en not_active Ceased
- 2003-06-11 WO PCT/EP2003/006172 patent/WO2003104253A2/de active IP Right Grant
- 2003-06-11 AR ARP030102079A patent/AR040188A1/es active IP Right Grant
- 2003-06-11 BR BR0312140-2A patent/BR0312140A/pt not_active IP Right Cessation
- 2003-06-11 EA EA200401544A patent/EA008442B1/ru not_active IP Right Cessation
- 2003-11-06 UA UAA200500212A patent/UA78062C2/uk unknown
-
2004
- 2004-11-22 IL IL165321A patent/IL165321A/en not_active IP Right Cessation
- 2004-12-10 CU CU20040282A patent/CU23414B7/es not_active IP Right Cessation
-
2005
- 2005-01-05 HR HRP20050009AA patent/HRP20050009B1/hr not_active IP Right Cessation
- 2005-01-10 NO NO20050127A patent/NO329563B1/no not_active IP Right Cessation
- 2005-01-10 EC EC2005005530A patent/ECSP055530A/es unknown
-
2006
- 2006-01-10 ZA ZA200500217A patent/ZA200500217B/en unknown
- 2006-01-27 HK HK06101276A patent/HK1081203A1/xx not_active IP Right Cessation
-
2008
- 2008-09-16 CR CR10289A patent/CR10289A/es not_active Application Discontinuation
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Legal Events
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| FG | Grant, registration |