JP2007509054A5 - - Google Patents
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- JP2007509054A5 JP2007509054A5 JP2006535351A JP2006535351A JP2007509054A5 JP 2007509054 A5 JP2007509054 A5 JP 2007509054A5 JP 2006535351 A JP2006535351 A JP 2006535351A JP 2006535351 A JP2006535351 A JP 2006535351A JP 2007509054 A5 JP2007509054 A5 JP 2007509054A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkenyl
- pharmaceutical composition
- cooh
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000008194 pharmaceutical composition Substances 0.000 claims 34
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 29
- 125000003118 aryl group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 238000011282 treatment Methods 0.000 claims 14
- 201000010099 disease Diseases 0.000 claims 10
- 208000035475 disorder Diseases 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000002877 alkyl aryl group Chemical group 0.000 claims 8
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 8
- -1 hydroxy, methoxy , Ethoxy Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 230000006438 vascular health Effects 0.000 claims 7
- 125000001589 carboacyl group Chemical group 0.000 claims 6
- 230000000069 prophylactic effect Effects 0.000 claims 6
- 230000001225 therapeutic effect Effects 0.000 claims 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 5
- 201000001881 impotence Diseases 0.000 claims 5
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 5
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 5
- 125000004149 thio group Chemical group *S* 0.000 claims 5
- 230000002792 vascular Effects 0.000 claims 5
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 4
- 239000004480 active ingredient Substances 0.000 claims 4
- 230000000747 cardiac effect Effects 0.000 claims 4
- 230000004064 dysfunction Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000004970 halomethyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 210000004204 blood vessel Anatomy 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 238000001631 haemodialysis Methods 0.000 claims 3
- 230000000322 hemodialysis Effects 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 230000001590 oxidative effect Effects 0.000 claims 3
- 230000036542 oxidative stress Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- ACMIJDVJWLMBCX-PXAZEXFGSA-N 4-[(3ar,6ar)-2,3,3a,4,6,6a-hexahydro-1h-pyrrolo[2,3-c]pyrrol-5-yl]-6-fluoro-n-methyl-2-(2-methylpyrimidin-5-yl)oxy-9h-pyrimido[4,5-b]indol-8-amine Chemical compound CNC1=CC(F)=CC(C2=C(N3C[C@@H]4NCC[C@@H]4C3)N=3)=C1NC2=NC=3OC1=CN=C(C)N=C1 ACMIJDVJWLMBCX-PXAZEXFGSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- 230000002411 adverse Effects 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 208000020832 chronic kidney disease Diseases 0.000 claims 2
- 125000006371 dihalo methyl group Chemical group 0.000 claims 2
- 208000028208 end stage renal disease Diseases 0.000 claims 2
- 201000000523 end stage renal failure Diseases 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 150000004820 halides Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000036470 plasma concentration Effects 0.000 claims 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- 244000215068 Acacia senegal Species 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 239000005995 Aluminium silicate Substances 0.000 claims 1
- 229920000084 Gum arabic Polymers 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 235000019483 Peanut oil Nutrition 0.000 claims 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 206010059053 Shunt stenosis Diseases 0.000 claims 1
- 229920001615 Tragacanth Polymers 0.000 claims 1
- 235000010489 acacia gum Nutrition 0.000 claims 1
- 239000000205 acacia gum Substances 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 235000012211 aluminium silicate Nutrition 0.000 claims 1
- 239000000305 astragalus gummifer gum Substances 0.000 claims 1
- 230000003416 augmentation Effects 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000001506 calcium phosphate Substances 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000011284 combination treatment Methods 0.000 claims 1
- 239000002270 dispersing agent Substances 0.000 claims 1
- 230000009429 distress Effects 0.000 claims 1
- 238000012377 drug delivery Methods 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 229940057995 liquid paraffin Drugs 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000004006 olive oil Substances 0.000 claims 1
- 235000008390 olive oil Nutrition 0.000 claims 1
- 239000000312 peanut oil Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 238000009117 preventive therapy Methods 0.000 claims 1
- 235000013772 propylene glycol Nutrition 0.000 claims 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
- 239000000661 sodium alginate Substances 0.000 claims 1
- 229940005550 sodium alginate Drugs 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- 239000000080 wetting agent Substances 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51167003P | 2003-10-17 | 2003-10-17 | |
| US51166303P | 2003-10-17 | 2003-10-17 | |
| US51165403P | 2003-10-17 | 2003-10-17 | |
| US53725004P | 2004-01-20 | 2004-01-20 | |
| US53728604P | 2004-01-20 | 2004-01-20 | |
| US53723304P | 2004-01-20 | 2004-01-20 | |
| PCT/US2004/034093 WO2005039596A1 (fr) | 2003-10-17 | 2004-10-18 | Silylphenols pouvant ameliorer la sante vasculaire |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007509054A JP2007509054A (ja) | 2007-04-12 |
| JP2007509054A5 true JP2007509054A5 (fr) | 2007-11-29 |
Family
ID=34528444
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006535351A Pending JP2007509054A (ja) | 2003-10-17 | 2004-10-18 | 血管健康を促進するシリルフェノール |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP1677804A1 (fr) |
| JP (1) | JP2007509054A (fr) |
| WO (1) | WO2005039596A1 (fr) |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5155250A (en) * | 1990-07-05 | 1992-10-13 | Merrell Dow Pharmaceuticals Inc. | 2,6-di-alkyl-4-silyl-phenols as antiatheroscerotic agents |
| US5677291A (en) * | 1993-12-10 | 1997-10-14 | Hoechst Marion Roussel, Inc. | Method of lowering serum cholesterol levels with 2,6-di-alkyl-4-silyl-phenols |
| ES2233937T3 (es) * | 1993-12-10 | 2005-06-16 | Merrell Pharmaceuticals Inc. | Metodo para disminuir los niveles de colesterol serico con 2,6-dialquil-4-silil-fenoles. |
| FR2738817B1 (fr) * | 1995-09-14 | 1997-10-17 | Adir | Nouveaux acides et esters 2,2-dimethyl-omega-phenoxy alcanoiques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US5795876A (en) * | 1996-04-30 | 1998-08-18 | Hoechst Marion Rousssel, Inc. | Method of inhibiting vascular cell adhesion molecule-1 and treating chronic inflammatory diseases with 2, 6-di-alkyl-4-silyl-phenols |
| JP2000509070A (ja) * | 1996-04-30 | 2000-07-18 | ヘキスト・マリオン・ルセル・インコーポレイテツド | ２，６―ジアルキル―４―シリル―フェノールを使用して血管細胞接着分子―１を阻害する方法および慢性炎症性疾患を治療する方法 |
| US5608095A (en) * | 1996-04-30 | 1997-03-04 | Hoechst Marion Roussel, Inc. | Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents |
| EP0971706A2 (fr) * | 1997-03-24 | 2000-01-19 | Gilles Côte | Agent de remodelage vasculaire |
| ATE356113T1 (de) * | 1997-05-14 | 2007-03-15 | Atherogenics Inc | Probucolbernsteinsäureester zur hemmung der expression von vcam-1 |
| ES2190592T3 (es) * | 1997-06-24 | 2003-08-01 | Aventis Pharma Inc | Fenoles y tiofenoles alquil-4-sililheterociclicos como agentes antioxidantes. |
| WO1999024400A1 (fr) * | 1997-11-10 | 1999-05-20 | Vyrex Corporation | Esters de probucol et leurs utilisations |
-
2004
- 2004-10-18 JP JP2006535351A patent/JP2007509054A/ja active Pending
- 2004-10-18 EP EP04795280A patent/EP1677804A1/fr not_active Withdrawn
- 2004-10-18 WO PCT/US2004/034093 patent/WO2005039596A1/fr not_active Ceased
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