JP2007538027A5 - - Google Patents
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- JP2007538027A5 JP2007538027A5 JP2007517048A JP2007517048A JP2007538027A5 JP 2007538027 A5 JP2007538027 A5 JP 2007538027A5 JP 2007517048 A JP2007517048 A JP 2007517048A JP 2007517048 A JP2007517048 A JP 2007517048A JP 2007538027 A5 JP2007538027 A5 JP 2007538027A5
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- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000002560 nitrile group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- PROQIPRRNZUXQM-ZXXIGWHRSA-N Estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims 1
- 229960001348 Estriol Drugs 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrugs Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 0 CC(CC(O)=O)c1c(*)c(*)c(*)c(*)c1* Chemical compound CC(CC(O)=O)c1c(*)c(*)c(*)c(*)c1* 0.000 description 1
Claims (1)
R1は、基-SO2NH2 又は-NHSO2NH2であり、ここでR2、R3及びX, X1は、水素原子、ハロゲン原子、ニトリル基、ニトロ基、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、CpF2p+1基（ｐは１〜３である）、基OC(O)-R20 , COOR20, OR20, C(O)NHR20 又は OC(O)NH- R21を表し、ここでR20 及びR21 R 22は、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、単環若しくは二環の置換された若しくは非置換のC3-8−シクロアルキル基、置換された若しくは非置換のアリール基、置換された若しくは非置換のC1-4−アルキレンアリール基、置換された若しくは非置換のC1-4−アルキレン−C3-8−シクロアルキル基又は置換された若しくは非置換のC3-8−シクロアルキレン−C1-4−アルキル基であり、そしてさらにR20は水素であってもよく、あるいは
R2は、基-SO2NH2 又は-NHSO2NH2であり、ここでR 1 、R3及びX, X1は、水素原子、ハロゲン原子、ニトリル基、ニトロ基、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、CpF2p+1基（ｐは１〜３である）、基OC(O)-R20 , COOR20, OR20, C(O)NHR20 又は OC(O)NH- R21を表し、ここでR20及びR21は、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、単環若しくは二環の置換された若しくは非置換のC3-8−シクロアルキル基、置換された若しくは非置換のアリール基、置換された若しくは非置換のC1-4−アルキレンアリール基、置換された若しくは非置換のC1-4−アルキレン−C3-8−シクロアルキル基又は置換された若しくは非置換の、分岐した若しくは直鎖のC3-8−シクロアルキレン−C1-4−アルキル基であり、そしてさらにR20は水素であってもよく、あるいは
R3は、基-SO2NH2 又は-NHSO2NH2であり、ここでR1、R2及びX, X1は、水素原子、ハロゲン原子、ニトリル基、ニトロ基、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、CpF2p+1基（ｐは１〜３である）、基OC(O)-R20 , COOR20, OR20, C(O)NHR20 又は OC(O)NH- R21を表し、ここでR20、及びR21 は、置換された若しくは非置換の、分岐した若しくは直鎖のC1-5−アルキル基、単環若しくは二環の置換された若しくは非置換のC3-8−シクロアルキル基、置換された若しくは非置換のアリール基、置換された若しくは非置換のC1-4−アルキレンアリール基、置換された若しくは非置換のC1-4−アルキレン−C3-8−シクロアルキル基又は置換された若しくは非置換のC3-8−シクロアルキレン−C1-4−アルキル基であり、そしてさらにR20は水素であってもよく、そして
STEROIDは、下記一般式（IIA）−（IID）：
ここで、R4, R16, R17は、ヒドロキシ基、トリ（C1-C6−アルキル）シリルオキシ基、基OC(O)-R20、C2-5−ヘテロシクロアルキルオキシ基、又は基Yを表わし、そして
R15は、水素原子、ヒドロキシ基、トリ（C1-C6−アルキル）シリルオキシ基、基OC(O)-R20、C2-5−ヘテロシクロアルキルオキシ基、又は基Yを表わす］
で表されるエストリオール及びエステトロールプロドラッグ類、及びそれらの医薬的に許容できる塩類。 The following general formula (I):
R 1 is a group --SO 2 NH 2 or --NHSO 2 NH 2 where R 2 , R 3 and X, X 1 are a hydrogen atom, halogen atom, nitrile group, nitro group, substituted or non- Substituted, branched or straight chain C 1-5 -alkyl groups, CpF 2p + 1 groups (p is 1 to 3), groups OC (O) -R 20 , COOR 20 , OR 20 , C (O ) represents NHR 20 or OC (O) NHR 21, wherein R 20 and R 2 1 R 22 is of or unsubstituted substituted, branched or straight chain C 1-5 - alkyl group, a single Ring or bicyclic substituted or unsubstituted C 3-8 -cycloalkyl group, substituted or unsubstituted aryl group, substituted or unsubstituted C 1-4 -alkylenearyl group, substituted or unsubstituted C 1-4 - alkylene -C 3-8 - cycloalkyl group or a substituted or unsubstituted C 3-8 - cycloalkylene -C 1-4 - alkyl group, and further R 20 is There may be a prime, or
R 2 is a group --SO 2 NH 2 or --NHSO 2 NH 2 , where R 1 , R 3 and X, X 1 are a hydrogen atom, a halogen atom, a nitrile group, a nitro group, substituted or non- Substituted, branched or straight chain C 1-5 -alkyl groups, CpF 2p + 1 groups (p is 1 to 3), groups OC (O) -R 20 , COOR 20 , OR 20 , C (O ) NHR 20 or OC (O) NH—R 21 , wherein R 20 and R 21 are substituted or unsubstituted, branched or straight-chain C 1-5 -alkyl groups, monocyclic or dicyclic Ring substituted or unsubstituted C 3-8 -cycloalkyl group, substituted or unsubstituted aryl group, substituted or unsubstituted C 1-4 -alkylenearyl group, substituted or unsubstituted A C 1-4 -alkylene-C 3-8 -cycloalkyl group or a substituted or unsubstituted, branched or straight chain C 3-8 -cycloalkylene-C 1-4 -alkyl group. , And further R 20 may be hydrogen, or
R 3 is a group --SO 2 NH 2 or --NHSO 2 NH 2 where R 1 , R 2 and X, X 1 are a hydrogen atom, halogen atom, nitrile group, nitro group, substituted or non- Substituted, branched or straight chain C 1-5 -alkyl groups, CpF 2p + 1 groups (p is 1 to 3), groups OC (O) -R 20 , COOR 20 , OR 20 , C (O ) represents NHR 20 or OC (O) NHR 21, wherein R 20, and R 2 1 is a substituted or unsubstituted, branched or straight chain C 1-5 - alkyl group, a monocyclic Or a bicyclic substituted or unsubstituted C 3-8 -cycloalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted C 1-4 -alkylenearyl group, substituted or An unsubstituted C 1-4 -alkylene-C 3-8 -cycloalkyl group or a substituted or unsubstituted C 3-8 -cycloalkylene-C 1-4 -alkyl group, and R 20 is water Can be plain, and
STEROID has the following general formula (IIA)-(IID):
Here, R 4 , R 16 and R 17 are a hydroxy group, a tri (C 1 -C 6 -alkyl) silyloxy group, a group OC (O) -R 20 , a C 2-5 -heterocycloalkyloxy group, or Represents the group Y, and
R 15 represents a hydrogen atom, a hydroxy group, a tri (C 1 -C 6 -alkyl) silyloxy group, a group OC (O) —R 20 , a C 2-5 -heterocycloalkyloxy group, or a group Y]
And estriol prodrugs represented by the formula: and pharmaceutically acceptable salts thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004025985A DE102004025985A1 (en) | 2004-05-21 | 2004-05-21 | Estriol and estetrol prodrugs |
| PCT/EP2005/005258 WO2005113576A1 (en) | 2004-05-21 | 2005-05-10 | Aminosulphonyl- or aminosulphonylamino-substituted phenyl esters as estriol and estetrol prodrugs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007538027A JP2007538027A (en) | 2007-12-27 |
| JP2007538027A5 true JP2007538027A5 (en) | 2008-06-26 |
Family
ID=34969311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007517048A Pending JP2007538027A (en) | 2004-05-21 | 2005-05-10 | Estriol and Estetrol prodrugs |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP1747231A1 (en) |
| JP (1) | JP2007538027A (en) |
| AR (1) | AR049108A1 (en) |
| DE (1) | DE102004025985A1 (en) |
| GT (1) | GT200500120A (en) |
| PA (1) | PA8633801A1 (en) |
| PE (1) | PE20060314A1 (en) |
| SV (1) | SV2006002122A (en) |
| TW (1) | TW200612962A (en) |
| UY (1) | UY28910A1 (en) |
| WO (1) | WO2005113576A1 (en) |
Families Citing this family (7)
| 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 |
| DE102004025966A1 (en) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estradiol 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 |
| 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 |
| CN100396693C (en) * | 2006-11-08 | 2008-06-25 | 浙江大学 | Preparation method of 1,4-dipregnene-16-beta-methyl-17-alpha-21-bihydroxy object |
| CN102079771B (en) * | 2010-12-10 | 2012-10-03 | 郑州大学 | Estrogen amino-acid ester compound with antitumor activity as well as synthetic method thereof |
Family Cites Families (12)
| 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 |
| US5116828A (en) * | 1989-10-26 | 1992-05-26 | Nippon Zoki Pharmaceutical Co., Ltd. | Pharmaceutical composition for treatment of osteoporosis |
| 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 |
| US6953785B2 (en) * | 2000-04-24 | 2005-10-11 | 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 |
| DE102004025966A1 (en) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estradiol prodrugs |
-
2004
- 2004-05-21 DE DE102004025985A patent/DE102004025985A1/en not_active Ceased
-
2005
- 2005-05-10 EP EP05747926A patent/EP1747231A1/en not_active Withdrawn
- 2005-05-10 JP JP2007517048A patent/JP2007538027A/en active Pending
- 2005-05-10 WO PCT/EP2005/005258 patent/WO2005113576A1/en active Application Filing
- 2005-05-19 UY UY28910A patent/UY28910A1/en not_active Application Discontinuation
- 2005-05-20 PA PA20058633801A patent/PA8633801A1/en unknown
- 2005-05-20 AR ARP050102085A patent/AR049108A1/en unknown
- 2005-05-20 GT GT200500120A patent/GT200500120A/en unknown
- 2005-05-20 PE PE2005000555A patent/PE20060314A1/en not_active Application Discontinuation
- 2005-05-20 TW TW094116505A patent/TW200612962A/en unknown
- 2005-05-23 SV SV2005002122A patent/SV2006002122A/en not_active Application Discontinuation
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