AR050335A1 - ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS - Google Patents
ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THISInfo
- Publication number
- AR050335A1 AR050335A1 ARP050102083A ARP050102083A AR050335A1 AR 050335 A1 AR050335 A1 AR 050335A1 AR P050102083 A ARP050102083 A AR P050102083A AR P050102083 A ARP050102083 A AR P050102083A AR 050335 A1 AR050335 A1 AR 050335A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- atom
- cycloalkyl
- halogen atom
- Prior art date
Links
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 title abstract 3
- 229960005309 estradiol Drugs 0.000 title abstract 3
- 229930182833 estradiol Natural products 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 101100240526 Caenorhabditis elegans nhr-20 gene Proteins 0.000 abstract 3
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 3
- 125000005275 alkylenearyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 125000002560 nitrile group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940011871 estrogen Drugs 0.000 abstract 1
- 239000000262 estrogen Substances 0.000 abstract 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 150000003431 steroids Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Prodrogas de estradiol de la formula general (1), un procedimiento para su preparacion, composiciones farmacéuticas que contienen estos compuestos y su uso para preparar medicamentos con efecto estrogeno. Reivindicacion 1: Prodrogas de estradiol de la formula general (1) caracterizadas porque n es un numero de 0 a 4; R1 es un radical -SO2NH2 o -NHSO2NH2; donde R2, R3 y X, X1 es un átomo de H, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1, con p = 1-3, un grupo OC(O)-R20, COOR20, OR20, C(O)NHR20 o OC(O)NH-R21; donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, un grupo arilo, un grupo alquilenarilo C1-4, un grupo alquileno-C1-4-cicloalquilo C3-8 o cicloalquileno-C3- 8-alquilo C1-4 y R20 puede ser además, un H, o R2 es un radical -SO2NH2 o -NHSO2NH2, donde R2, R3 y X, X1 es un átomo de H, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1, con p =1-3, un grupo OC(O)- R20, COOR20, OR20, C(O)NHR20 o OC(O)NH-R21; donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, un grupo arilo, un grupo alquilenarilo C1-4, un grupo alquileno-C1-4-cicloalquilo C3-8 o cicloalquileno- C3-8-alquilo C1-4, y R20 puede ser, además un H o R3 es un radical -SO2NH2 o -NHSO2NH2; donde R2, R3 y X, X1 es un átomo de H, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1 con p =1-3, un grupo OC(O)-R20, COOR20, OR20, C(O)NHR20 o OC(O)NH-R21; donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, u grupo arilo, un grupo alquilenarilo C1-4, un grupo alquileno-C1-4-cicloalquilo C3-8 o cicloalquileno-C3-8-alquilo C1-4, y R20 puede ser, además, un H, y esteroide es un sistema de anillo ABCD esteroide de las formulas generales parciales (2)-(3), donde R5, R6, R8 son, cada uno, un átomo de H y R7 es un átomo de H, un grupo metilo o etilo o R5+R6, R7+R8 o R6+R7 son juntos, una union doble; R9 es un átomo de H, un átomo de halogeno, un grupo hidroxi, un grupo metoxi, un grupo OC(O)-R20, un grupo metilo o un grupo etilo; R10 es un grupo hidroxi, un grupo metoxi, un grupo tri(alquil C1-6)sililoxi, un grupo OC(O)-R20, un grupo heterocicloalquiloxi C2-5 o un grupo Z; R11 es un átomo de H o de halogeno; R12 es un grupo hidroxi, un grupo metoxi, un grupo tri(alquilo C1-6)sililoxi, un grupo OC(O)-R20, un grupo heterocicloalquiloxi C2-5 o un grupo Z; R14 es átomo de H, un grupo metilo, o un grupo etilo; R15 es átomo de H, un grupo hidroxi, un grupo metoxi, un grupo etoxi, un grupo tri(alquilo C1-6)sililoxi, un grupo OC(O)-R20 o un grupo heterocicloalquiloxi C2-5, y sus sales farmacéuticamente aceptables.Prodiges of estradiol of the general formula (1), a process for its preparation, pharmaceutical compositions containing these compounds and their use for preparing drugs with estrogen effect. Claim 1: Estradiol prodrugs of the general formula (1) characterized in that n is a number from 0 to 4; R1 is a radical -SO2NH2 or -NHSO2NH2; where R2, R3 and X, X1 is an H atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group, with p = 1-3, an OC group (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21; where R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, an aryl group, a C1-4 alkylenearyl group, a C1-4 alkylene-C3-8 cycloalkyl or C3-8 cycloalkylene group -C1-4 and R20 alkyl may also be an H, or R2 is a radical -SO2NH2 or -NHSO2NH2, where R2, R3 and X, X1 is an H atom, a halogen atom, a nitrile group, a group nitro, a C1-5 alkyl group, a CpF2p + 1 group, with p = 1-3, an OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21 group; where R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, an aryl group, a C1-4 alkylenearyl group, a C1-4 alkylene-C3-8 cycloalkyl or C3-8 cycloalkylene group -C1-4 alkyl, and R20 may also be an H or R3 is a radical -SO2NH2 or -NHSO2NH2; where R2, R3 and X, X1 is an H atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group with p = 1-3, an OC group ( O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21; wherein R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, or aryl group, a C1-4 alkylenearyl group, a C1-4 alkylene-C3-8 cycloalkyl or C3-8 cycloalkylene group -C1-4 alkyl, and R20 may also be an H, and steroid is a steroid ABCD ring system of the partial general formulas (2) - (3), where R5, R6, R8 are each a H and R7 atom is an H atom, a methyl or ethyl group or R5 + R6, R7 + R8 or R6 + R7 are together, a double bond; R9 is an H atom, a halogen atom, a hydroxy group, a methoxy group, an OC (O) -R20 group, a methyl group or an ethyl group; R10 is a hydroxy group, a methoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group, a C2-5 heterocycloalkyloxy group or a Z group; R11 is an H or halogen atom; R12 is a hydroxy group, a methoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group, a C2-5 heterocycloalkyloxy group or a Z group; R14 is an atom of H, a methyl group, or an ethyl group; R15 is an H atom, a hydroxy group, a methoxy group, an ethoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group or a C2-5 heterocycloalkyloxy group, and their pharmaceutically acceptable salts .
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004025966A DE102004025966A1 (en) | 2004-05-21 | 2004-05-21 | Estradiol prodrugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050335A1 true AR050335A1 (en) | 2006-10-18 |
Family
ID=34969196
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102083A AR050335A1 (en) | 2004-05-21 | 2005-05-20 | ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP1747230A1 (en) |
| JP (1) | JP2007538025A (en) |
| AR (1) | AR050335A1 (en) |
| DE (1) | DE102004025966A1 (en) |
| GT (1) | GT200500121A (en) |
| PA (1) | PA8633701A1 (en) |
| PE (1) | PE20060359A1 (en) |
| SV (1) | SV2006002121A (en) |
| TW (1) | TW200613315A (en) |
| UY (1) | UY28909A1 (en) |
| WO (1) | WO2005113574A1 (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10027887A1 (en) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds |
| US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
| DE102004025985A1 (en) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estriol and estetrol prodrugs |
| DE102005057224A1 (en) * | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | New 9-alpha substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders |
| DE102005057225A1 (en) * | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | New 8-beta-substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders |
| DE102005057408A1 (en) * | 2005-11-30 | 2007-05-31 | Bayer Schering Pharma Ag | New sulfamoylsulfonate prodrugs e.g. useful for protecting red blood cells from attack by parasites or for hormone replacement therapy, female fertility control or treating hormone-associated diseases |
| RU2667942C2 (en) * | 2013-07-11 | 2018-09-27 | Эвестра, Инк. | Prodrug forming compounds |
| CN115368427B (en) * | 2022-08-17 | 2024-02-13 | 南宁师范大学 | Estradiol selenocyanate compounds and their preparation methods and applications |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR1238739A (en) * | 1958-08-04 | 1960-08-19 | Chimiotherapie Lab Franc | Process for the preparation of water-soluble testosterone derivatives |
| FR8290M (en) * | 1968-12-31 | 1970-11-09 | Rech Chimiques Et Ind Mar Lab | |
| US5001234A (en) * | 1987-04-16 | 1991-03-19 | The Upjohn Company | Cyclic hydrocarbons with an aminoalkyl sidechain |
| US5571933A (en) * | 1994-11-17 | 1996-11-05 | Duquesne University Of The Holy Ghost | Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use |
| DE19712488A1 (en) * | 1997-03-25 | 1998-10-01 | Knoell Hans Forschung Ev | Steroid sulfamates, processes for their preparation and use thereof |
| AU2001248849A1 (en) * | 2000-04-24 | 2001-11-07 | Kyowa Hakko Kogyo Co. Ltd. | Estra-1,3,5(10)-triene derivatives |
| DE10027887A1 (en) * | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds |
| GB0015876D0 (en) * | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| GB0316290D0 (en) * | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
| TWI331154B (en) * | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
| DE102004025985A1 (en) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estriol and estetrol prodrugs |
-
2004
- 2004-05-21 DE DE102004025966A patent/DE102004025966A1/en not_active Withdrawn
-
2005
- 2005-05-10 WO PCT/EP2005/005254 patent/WO2005113574A1/en not_active Ceased
- 2005-05-10 EP EP05747458A patent/EP1747230A1/en not_active Withdrawn
- 2005-05-10 JP JP2007517046A patent/JP2007538025A/en active Pending
- 2005-05-19 UY UY28909A patent/UY28909A1/en not_active Application Discontinuation
- 2005-05-20 AR ARP050102083A patent/AR050335A1/en unknown
- 2005-05-20 PE PE2005000557A patent/PE20060359A1/en not_active Application Discontinuation
- 2005-05-20 TW TW094116503A patent/TW200613315A/en unknown
- 2005-05-20 PA PA20058633701A patent/PA8633701A1/en unknown
- 2005-05-20 GT GT200500121A patent/GT200500121A/en unknown
- 2005-05-23 SV SV2005002121A patent/SV2006002121A/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PA8633701A1 (en) | 2006-07-03 |
| UY28909A1 (en) | 2005-12-30 |
| TW200613315A (en) | 2006-05-01 |
| DE102004025966A1 (en) | 2005-12-15 |
| PE20060359A1 (en) | 2006-05-25 |
| SV2006002121A (en) | 2006-02-15 |
| JP2007538025A (en) | 2007-12-27 |
| WO2005113574A1 (en) | 2005-12-01 |
| EP1747230A1 (en) | 2007-01-31 |
| GT200500121A (en) | 2006-01-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |