MXPA03000845A - Estrogenos substituidos por 16alfa-metilo o etilo. - Google Patents
Estrogenos substituidos por 16alfa-metilo o etilo.Info
- Publication number
- MXPA03000845A MXPA03000845A MXPA03000845A MXPA03000845A MXPA03000845A MX PA03000845 A MXPA03000845 A MX PA03000845A MX PA03000845 A MXPA03000845 A MX PA03000845A MX PA03000845 A MXPA03000845 A MX PA03000845A MX PA03000845 A MXPA03000845 A MX PA03000845A
- Authority
- MX
- Mexico
- Prior art keywords
- methyl
- 16alpha
- substituted
- ethyl substituted
- halogens
- Prior art date
Links
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title abstract 2
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 abstract 1
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 230000003637 steroidlike Effects 0.000 abstract 1
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
-
- 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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- 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
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La invencion hace disponible un compuesto de esteroides substituidos-16a que tienen la formula I en donde el anillo punteado es un anillo completamente saturado, completamente aromatico o saturado con un enlace doble ?5-10; R1 es (C1-C3)alquilo o (C2-C3)alquenilo, y cada uno de estos grupos puede ser substituido por uno o mas halogenos; R2 es (C1-C4)alquilo, (C2-C4)alquenilo o metileno, y cada uno de estos grupos puede ser substituido por uno o mas halogenos; R3 es metilo o etilo; o un profarmaco del mismo cuyo compuesto puede ser usado para un tratamiento selectivo del receptor de estrogeno a.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00202697 | 2000-07-28 | ||
| PCT/EP2001/008535 WO2002010188A1 (en) | 2000-07-28 | 2001-07-23 | 16alpha-methyl or ethyl substituted estrogens |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA03000845A true MXPA03000845A (es) | 2004-04-05 |
Family
ID=8171866
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA03000845A MXPA03000845A (es) | 2000-07-28 | 2001-07-23 | Estrogenos substituidos por 16alfa-metilo o etilo. |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7696190B2 (es) |
| EP (1) | EP1307471B1 (es) |
| JP (1) | JP2004505093A (es) |
| KR (1) | KR20030029640A (es) |
| CN (1) | CN1220696C (es) |
| AR (1) | AR029989A1 (es) |
| AT (1) | ATE294812T1 (es) |
| AU (2) | AU2001282016B2 (es) |
| BR (1) | BR0112791A (es) |
| CA (1) | CA2416311C (es) |
| CZ (1) | CZ2003270A3 (es) |
| DE (1) | DE60110606T2 (es) |
| EC (1) | ECSP034448A (es) |
| ES (1) | ES2241854T3 (es) |
| HR (1) | HRP20030060A2 (es) |
| HU (1) | HUP0301592A2 (es) |
| IL (2) | IL153934A0 (es) |
| IS (1) | IS6692A (es) |
| MX (1) | MXPA03000845A (es) |
| NO (1) | NO20030419L (es) |
| PE (1) | PE20020331A1 (es) |
| PL (1) | PL366235A1 (es) |
| SK (1) | SK882003A3 (es) |
| WO (1) | WO2002010188A1 (es) |
| ZA (1) | ZA200300417B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE453659T1 (de) * | 2002-01-21 | 2010-01-15 | Organon Nv | Verfahren zur herstellung von 7-alpha- methylsteroide |
| DE10213371C1 (de) * | 2002-03-21 | 2003-12-24 | Schering Ag | Verfahren zur Herstellung von 7alpha-Methylsteroiden |
| CN101014610B (zh) * | 2004-09-08 | 2012-08-22 | Msd欧斯股份有限公司 | 具有选择性雌激素活性的15β-取代的类固醇 |
| UA89964C2 (ru) * | 2004-09-08 | 2010-03-25 | Н.В. Органон | 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ |
| CN114409717B (zh) * | 2021-12-17 | 2023-03-17 | 湖南科益新生物医药有限公司 | 替勃龙中间体醚化物和替勃龙的制备方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL226738A (es) | 1957-04-11 | |||
| DE1084261B (de) | 1957-04-11 | 1960-06-30 | Syntex Sa | Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate |
| US3257429A (en) | 1957-11-12 | 1966-06-21 | Syntex Corp | 16-methylene derivatives of estrone and estradiol |
| US3007946A (en) | 1958-11-06 | 1961-11-07 | Searle & Co | 3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones |
| US3049555A (en) | 1959-12-22 | 1962-08-14 | Searle & Co | 3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones |
| US3092645A (en) | 1961-12-28 | 1963-06-04 | Searle & Co | Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols |
| GB1112840A (en) | 1964-04-07 | 1968-05-08 | Res Inst Medicine Chem | Steroids having pro-oestrogenic activity |
| US3299108A (en) | 1965-10-18 | 1967-01-17 | Searle & Co | 17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto |
| US3465010A (en) | 1966-11-22 | 1969-09-02 | Searle & Co | 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof |
| US3377366A (en) | 1966-12-02 | 1968-04-09 | Searle & Co | 17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof |
| ZA712312B (en) | 1970-04-28 | 1972-01-26 | Ochsner Med Found Alton | 4,14-estradiene compounds |
| US3652606A (en) | 1970-08-07 | 1972-03-28 | Searle & Co | 3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof |
| US3704253A (en) | 1970-09-23 | 1972-11-28 | American Home Prod | 13 - polycarbonalkyl - 16 - methylgona-1,3,5(10)-trienes and 13-polycarbonalkyl-16-methylgon - 4 - en-3-ones and intermediates for their production |
| FR2377419A1 (fr) | 1977-01-13 | 1978-08-11 | Roussel Uclaf | Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament |
| DE2757157C3 (de) | 1977-12-19 | 1980-10-09 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Verfahren zur Herstellung von 16 a -alkylierten Steroiden |
| AU572589B2 (en) | 1983-12-14 | 1988-05-12 | Upjohn Company, The | 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids |
| US5116830A (en) * | 1984-08-17 | 1992-05-26 | Sri International | Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses |
| DE3822770A1 (de) * | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| ZA94715B (en) | 1993-02-08 | 1994-10-24 | Akzo Nv | Steroids for treating menopausal complaints |
| ATE180669T1 (de) | 1993-03-05 | 1999-06-15 | Akzo Nobel Nv | Verwendung von pregnanderivaten zur behandlung von tumoren |
| PL343428A1 (en) | 1998-03-09 | 2001-08-13 | Akzo Nobel Nv | New contraceptive kit |
| TR200003743T2 (tr) * | 1998-06-19 | 2001-07-23 | Akzo Nobel N.V. | Testosteron türevi. |
| EP1131336B1 (en) | 1998-11-20 | 2002-08-28 | Akzo Nobel N.V. | Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11 |
| TW548277B (en) * | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| AU770331B2 (en) * | 1999-09-06 | 2004-02-19 | N.V. Organon | Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11 |
-
2001
- 2001-07-23 JP JP2002515917A patent/JP2004505093A/ja not_active Withdrawn
- 2001-07-23 CN CNB018133983A patent/CN1220696C/zh not_active Expired - Fee Related
- 2001-07-23 AU AU2001282016A patent/AU2001282016B2/en not_active Ceased
- 2001-07-23 AU AU8201601A patent/AU8201601A/xx active Pending
- 2001-07-23 WO PCT/EP2001/008535 patent/WO2002010188A1/en active IP Right Grant
- 2001-07-23 HU HU0301592A patent/HUP0301592A2/hu unknown
- 2001-07-23 HR HR20030060A patent/HRP20030060A2/hr not_active Application Discontinuation
- 2001-07-23 PL PL01366235A patent/PL366235A1/xx unknown
- 2001-07-23 SK SK88-2003A patent/SK882003A3/sk unknown
- 2001-07-23 CZ CZ2003270A patent/CZ2003270A3/cs unknown
- 2001-07-23 IL IL15393401A patent/IL153934A0/xx active IP Right Grant
- 2001-07-23 ES ES01960546T patent/ES2241854T3/es not_active Expired - Lifetime
- 2001-07-23 AT AT01960546T patent/ATE294812T1/de not_active IP Right Cessation
- 2001-07-23 DE DE60110606T patent/DE60110606T2/de not_active Expired - Lifetime
- 2001-07-23 US US10/343,293 patent/US7696190B2/en not_active Expired - Fee Related
- 2001-07-23 BR BR0112791-8A patent/BR0112791A/pt not_active IP Right Cessation
- 2001-07-23 MX MXPA03000845A patent/MXPA03000845A/es active IP Right Grant
- 2001-07-23 EP EP01960546A patent/EP1307471B1/en not_active Expired - Lifetime
- 2001-07-23 CA CA002416311A patent/CA2416311C/en not_active Expired - Fee Related
- 2001-07-23 KR KR10-2003-7001186A patent/KR20030029640A/ko not_active Withdrawn
- 2001-07-25 PE PE2001000751A patent/PE20020331A1/es not_active Application Discontinuation
- 2001-07-26 AR ARP010103558A patent/AR029989A1/es unknown
-
2003
- 2003-01-14 IL IL153934A patent/IL153934A/en not_active IP Right Cessation
- 2003-01-15 ZA ZA200300417A patent/ZA200300417B/xx unknown
- 2003-01-20 IS IS6692A patent/IS6692A/is unknown
- 2003-01-24 EC EC2003004448A patent/ECSP034448A/es unknown
- 2003-01-27 NO NO20030419A patent/NO20030419L/no not_active Application Discontinuation
-
2009
- 2009-05-29 US US12/475,096 patent/US20100029603A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN1220696C (zh) | 2005-09-28 |
| AR029989A1 (es) | 2003-07-23 |
| WO2002010188A1 (en) | 2002-02-07 |
| ZA200300417B (en) | 2004-04-15 |
| DE60110606T2 (de) | 2005-12-01 |
| SK882003A3 (en) | 2003-07-01 |
| CZ2003270A3 (cs) | 2003-06-18 |
| KR20030029640A (ko) | 2003-04-14 |
| PE20020331A1 (es) | 2002-04-30 |
| EP1307471B1 (en) | 2005-05-04 |
| JP2004505093A (ja) | 2004-02-19 |
| PL366235A1 (en) | 2005-01-24 |
| CA2416311A1 (en) | 2002-02-07 |
| ECSP034448A (es) | 2003-03-10 |
| NO20030419D0 (no) | 2003-01-27 |
| NO20030419L (no) | 2003-01-27 |
| IL153934A (en) | 2007-07-24 |
| AU8201601A (en) | 2002-02-13 |
| CN1444596A (zh) | 2003-09-24 |
| US7696190B2 (en) | 2010-04-13 |
| EP1307471A1 (en) | 2003-05-07 |
| BR0112791A (pt) | 2003-06-24 |
| ATE294812T1 (de) | 2005-05-15 |
| US20040043976A1 (en) | 2004-03-04 |
| ES2241854T3 (es) | 2005-11-01 |
| AU2001282016B2 (en) | 2005-11-10 |
| CA2416311C (en) | 2009-04-28 |
| IL153934A0 (en) | 2003-07-31 |
| HRP20030060A2 (en) | 2004-06-30 |
| HUP0301592A2 (hu) | 2003-09-29 |
| US20100029603A1 (en) | 2010-02-04 |
| IS6692A (is) | 2003-01-20 |
| DE60110606D1 (de) | 2005-06-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration | ||
| GB | Transfer or rights |