JP2005519918A5 - - Google Patents
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- Publication number
- JP2005519918A5 JP2005519918A5 JP2003563540A JP2003563540A JP2005519918A5 JP 2005519918 A5 JP2005519918 A5 JP 2005519918A5 JP 2003563540 A JP2003563540 A JP 2003563540A JP 2003563540 A JP2003563540 A JP 2003563540A JP 2005519918 A5 JP2005519918 A5 JP 2005519918A5
- Authority
- JP
- Japan
- Prior art keywords
- epoxy
- adrenergic
- group
- pharmaceutical composition
- receptor antagonist
- 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.)
- Abandoned
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 56
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 52
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 52
- 229940044551 receptor antagonist Drugs 0.000 claims 52
- 239000002464 receptor antagonist Substances 0.000 claims 52
- RHLJLALHBZGAFM-UHFFFAOYSA-N Bunazosinum Chemical compound C1CN(C(=O)CCC)CCCN1C1=NC(N)=C(C=C(OC)C(OC)=C2)C2=N1 RHLJLALHBZGAFM-UHFFFAOYSA-N 0.000 claims 33
- 229960002467 bunazosin Drugs 0.000 claims 33
- -1 naphthopidyl Chemical compound 0.000 claims 29
- RUZYUOTYCVRMRZ-UHFFFAOYSA-N doxazosin Chemical compound C1OC2=CC=CC=C2OC1C(=O)N(CC1)CCN1C1=NC(N)=C(C=C(C(OC)=C2)OC)C2=N1 RUZYUOTYCVRMRZ-UHFFFAOYSA-N 0.000 claims 27
- 229960001389 doxazosin Drugs 0.000 claims 27
- SGUAFYQXFOLMHL-UHFFFAOYSA-N 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide Chemical compound C=1C=C(O)C(C(N)=O)=CC=1C(O)CNC(C)CCC1=CC=CC=C1 SGUAFYQXFOLMHL-UHFFFAOYSA-N 0.000 claims 23
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 claims 23
- WDZVGELJXXEGPV-YIXHJXPBSA-N Guanabenz Chemical compound NC(N)=N\N=C\C1=C(Cl)C=CC=C1Cl WDZVGELJXXEGPV-YIXHJXPBSA-N 0.000 claims 23
- INJOMKTZOLKMBF-UHFFFAOYSA-N Guanfacine Chemical compound NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl INJOMKTZOLKMBF-UHFFFAOYSA-N 0.000 claims 23
- YSEXMKHXIOCEJA-FVFQAYNVSA-N Nicergoline Chemical compound C([C@@H]1C[C@]2([C@H](N(C)C1)CC=1C3=C2C=CC=C3N(C)C=1)OC)OC(=O)C1=CN=CC(Br)=C1 YSEXMKHXIOCEJA-FVFQAYNVSA-N 0.000 claims 23
- QZVCTJOXCFMACW-UHFFFAOYSA-N Phenoxybenzamine Chemical compound C=1C=CC=CC=1CN(CCCl)C(C)COC1=CC=CC=C1 QZVCTJOXCFMACW-UHFFFAOYSA-N 0.000 claims 23
- DRHKJLXJIQTDTD-OAHLLOKOSA-N Tamsulosine Chemical compound CCOC1=CC=CC=C1OCCN[C@H](C)CC1=CC=C(OC)C(S(N)(=O)=O)=C1 DRHKJLXJIQTDTD-OAHLLOKOSA-N 0.000 claims 23
- BLGXFZZNTVWLAY-CCZXDCJGSA-N Yohimbine Natural products C1=CC=C2C(CCN3C[C@@H]4CC[C@@H](O)[C@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-CCZXDCJGSA-N 0.000 claims 23
- BHIAIPWSVYSKJS-UHFFFAOYSA-N arotinolol Chemical compound S1C(SCC(O)CNC(C)(C)C)=NC(C=2SC(=CC=2)C(N)=O)=C1 BHIAIPWSVYSKJS-UHFFFAOYSA-N 0.000 claims 23
- 229950010731 arotinolol Drugs 0.000 claims 23
- BLGXFZZNTVWLAY-UHFFFAOYSA-N beta-Yohimbin Natural products C1=CC=C2C(CCN3CC4CCC(O)C(C4CC33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-UHFFFAOYSA-N 0.000 claims 23
- 229960002896 clonidine Drugs 0.000 claims 23
- RFWZESUMWJKKRN-UHFFFAOYSA-N dapiprazole Chemical group CC1=CC=CC=C1N1CCN(CCC=2N3CCCCC3=NN=2)CC1 RFWZESUMWJKKRN-UHFFFAOYSA-N 0.000 claims 23
- 229960002947 dapiprazole Drugs 0.000 claims 23
- 229960004553 guanabenz Drugs 0.000 claims 23
- 229960002048 guanfacine Drugs 0.000 claims 23
- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 claims 23
- 229960005417 ketanserin Drugs 0.000 claims 23
- 229960001632 labetalol Drugs 0.000 claims 23
- 229960003642 nicergoline Drugs 0.000 claims 23
- 229960003418 phenoxybenzamine Drugs 0.000 claims 23
- MRBDMNSDAVCSSF-UHFFFAOYSA-N phentolamine Chemical compound C1=CC(C)=CC=C1N(C=1C=C(O)C=CC=1)CC1=NCCN1 MRBDMNSDAVCSSF-UHFFFAOYSA-N 0.000 claims 23
- 229960001999 phentolamine Drugs 0.000 claims 23
- IENZQIKPVFGBNW-UHFFFAOYSA-N prazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1=CC=CO1 IENZQIKPVFGBNW-UHFFFAOYSA-N 0.000 claims 23
- 229960001289 prazosin Drugs 0.000 claims 23
- 229960002613 tamsulosin Drugs 0.000 claims 23
- VCKUSRYTPJJLNI-UHFFFAOYSA-N terazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1CCCO1 VCKUSRYTPJJLNI-UHFFFAOYSA-N 0.000 claims 23
- 229960001693 terazosin Drugs 0.000 claims 23
- 229960002906 trimazosin Drugs 0.000 claims 23
- YNZXWQJZEDLQEG-UHFFFAOYSA-N trimazosin Chemical compound N1=C2C(OC)=C(OC)C(OC)=CC2=C(N)N=C1N1CCN(C(=O)OCC(C)(C)O)CC1 YNZXWQJZEDLQEG-UHFFFAOYSA-N 0.000 claims 23
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 claims 23
- 229960000317 yohimbine Drugs 0.000 claims 23
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 claims 23
- 229960004607 alfuzosin Drugs 0.000 claims 22
- WNMJYKCGWZFFKR-UHFFFAOYSA-N alfuzosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CCCNC(=O)C1CCCO1 WNMJYKCGWZFFKR-UHFFFAOYSA-N 0.000 claims 22
- LVEXHFZHOIWIIP-UHFFFAOYSA-N amosulalol Chemical compound COC1=CC=CC=C1OCCNCC(O)C1=CC=C(C)C(S(N)(=O)=O)=C1 LVEXHFZHOIWIIP-UHFFFAOYSA-N 0.000 claims 22
- 229950010351 amosulalol Drugs 0.000 claims 22
- 229960002610 apraclonidine Drugs 0.000 claims 22
- IEJXVRYNEISIKR-UHFFFAOYSA-N apraclonidine Chemical compound ClC1=CC(N)=CC(Cl)=C1NC1=NCCN1 IEJXVRYNEISIKR-UHFFFAOYSA-N 0.000 claims 22
- AGWFKXDTYITCSP-NHGLSFBUSA-N (8s,9s,10r,13r,14s,17r)-17-(2-carboxyethyl)-10,13-dimethyl-2,3,6,7,8,9,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-7-carboxylic acid Chemical compound C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)CCC(O)=O)[C@@H]4[C@@H]3C(C(O)=O)CC2=C1 AGWFKXDTYITCSP-NHGLSFBUSA-N 0.000 claims 20
- WPNJAUFVNXKLIM-UHFFFAOYSA-N Moxonidine Chemical compound COC1=NC(C)=NC(Cl)=C1NC1=NCCN1 WPNJAUFVNXKLIM-UHFFFAOYSA-N 0.000 claims 20
- CQXADFVORZEARL-UHFFFAOYSA-N Rilmenidine Chemical compound C1CC1C(C1CC1)NC1=NCCO1 CQXADFVORZEARL-UHFFFAOYSA-N 0.000 claims 20
- 125000000457 gamma-lactone group Chemical group 0.000 claims 20
- 229960003938 moxonidine Drugs 0.000 claims 20
- 229960000764 rilmenidine Drugs 0.000 claims 20
- 229960001208 eplerenone Drugs 0.000 claims 18
- JUKPWJGBANNWMW-VWBFHTRKSA-N eplerenone Chemical compound C([C@@H]1[C@]2(C)C[C@H]3O[C@]33[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)C(=O)OC)C[C@@]21CCC(=O)O1 JUKPWJGBANNWMW-VWBFHTRKSA-N 0.000 claims 18
- HKYYMVLLLCHGTL-UNUXFHLRSA-N 3-[(8s,9s,10r,13r,14s,17r)-10,13-dimethyl-2,3,8,9,11,12,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-17-yl]propanoic acid Chemical compound C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)CCC(O)=O)[C@@H]4[C@@H]3C=CC2=C1 HKYYMVLLLCHGTL-UNUXFHLRSA-N 0.000 claims 16
- 208000024172 Cardiovascular disease Diseases 0.000 claims 12
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical class [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 12
- ICMGLRUYEQNHPF-UHFFFAOYSA-N Uraprene Chemical compound COC1=CC=CC=C1N1CCN(CCCNC=2N(C(=O)N(C)C(=O)C=2)C)CC1 ICMGLRUYEQNHPF-UHFFFAOYSA-N 0.000 claims 11
- 229960001130 urapidil Drugs 0.000 claims 11
- 239000004593 Epoxy Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- WFNRNNUZFPVBSM-UHFFFAOYSA-N Monatepil Chemical compound C1=CC(F)=CC=C1N1CCN(CCCC(=O)NC2C3=CC=CC=C3SCC3=CC=CC=C32)CC1 WFNRNNUZFPVBSM-UHFFFAOYSA-N 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 229950003010 monatepil Drugs 0.000 claims 6
- PORJGKBQQFPVED-UNUXFHLRSA-N 3-[(8s,9s,10r,13r,14s,17r)-10,13-dimethyl-8,9,11,12,14,15,16,17-octahydro-3h-cyclopenta[a]phenanthren-17-yl]propanoic acid Chemical compound C1C=C[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)CCC(O)=O)[C@@H]4[C@@H]3C=CC2=C1 PORJGKBQQFPVED-UNUXFHLRSA-N 0.000 claims 4
- 206010019280 Heart failures Diseases 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 125000004494 ethyl ester group Chemical group 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 150000004702 methyl esters Chemical class 0.000 claims 4
- PZQSQRCNMZGWFT-QXMHVHEDSA-N propan-2-yl (z)-octadec-9-enoate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC(C)C PZQSQRCNMZGWFT-QXMHVHEDSA-N 0.000 claims 4
- 229960002256 spironolactone Drugs 0.000 claims 4
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical group C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 claims 4
- 150000003431 steroids Chemical class 0.000 claims 4
- JIVZKJJQOZQXQB-UHFFFAOYSA-N tolazoline Chemical compound C=1C=CC=CC=1CC1=NCCN1 JIVZKJJQOZQXQB-UHFFFAOYSA-N 0.000 claims 4
- 229960002312 tolazoline Drugs 0.000 claims 4
- 229940083712 aldosterone antagonist Drugs 0.000 claims 3
- 239000002170 aldosterone antagonist Substances 0.000 claims 3
- 239000006187 pill Substances 0.000 claims 3
- 206010003445 Ascites Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 2
- 239000000464 adrenergic agent Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000007882 cirrhosis Effects 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 238000004090 dissolution Methods 0.000 claims 2
- 239000012738 dissolution medium Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- 239000002609 medium Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000000977 initiatory effect Effects 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35380102P | 2002-01-30 | 2002-01-30 | |
| PCT/US2003/002723 WO2003063846A2 (en) | 2002-01-30 | 2003-01-30 | Aldosterone receptor antagonist and alpha-adrenergic modulating agent combination therapy for prevention or treatment of cardiovascular conditions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005519918A JP2005519918A (ja) | 2005-07-07 |
| JP2005519918A5 true JP2005519918A5 (https=) | 2006-03-09 |
Family
ID=27663255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003563540A Abandoned JP2005519918A (ja) | 2002-01-30 | 2003-01-30 | 病因性状態を予防または治療するためのアルドステロン受容体拮抗剤およびα−アドレナリン作用変調剤の組み合わせ治療 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20030199483A1 (https=) |
| EP (1) | EP1469862A2 (https=) |
| JP (1) | JP2005519918A (https=) |
| KR (1) | KR20040096540A (https=) |
| CN (1) | CN1625404A (https=) |
| BR (1) | BR0307336A (https=) |
| CA (1) | CA2474845A1 (https=) |
| MX (1) | MXPA04007472A (https=) |
| PL (1) | PL371437A1 (https=) |
| WO (1) | WO2003063846A2 (https=) |
| ZA (1) | ZA200405437B (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100381163C (zh) * | 2006-08-29 | 2008-04-16 | 陈俊云 | 一种含利美尼定的药物 |
| EP2727587A1 (en) * | 2012-10-30 | 2014-05-07 | Pharnext | Compositions, methods and uses for the treatment of diabetes and related conditions by controlling blood glucose level |
| US10350223B2 (en) | 2015-03-03 | 2019-07-16 | Richard W. Yee | Compositions and methods for treating ocular diseases |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5529992A (en) * | 1992-04-21 | 1996-06-25 | Curators Of The University Of Missouri | Method for inhibiting myocardial fibrosis by administering an aldosterone antagonist which suppresses aldoster one receptors |
| US5932538A (en) * | 1996-02-02 | 1999-08-03 | Nitromed, Inc. | Nitrosated and nitrosylated α-adrenergic receptor antagonist compounds, compositions and their uses |
| US20020132001A1 (en) * | 2000-05-11 | 2002-09-19 | Garthwaite Susan M. | Aldosterone antagonist composition for release during aldosterone acrophase |
| US20040235809A1 (en) * | 2000-07-27 | 2004-11-25 | Alexander John C | Epoxy steroidal aldosterone antagonist and beta-adremergic antagonist combination therepy for treatment of congestive heart failure |
| WO2003049745A1 (en) * | 2001-12-12 | 2003-06-19 | Pharmacia Corporation | Method of treating ophthalmic disorders with epoxy-steroidal aldosterone receptor antagonists |
-
2003
- 2003-01-30 PL PL03371437A patent/PL371437A1/xx not_active Application Discontinuation
- 2003-01-30 BR BR0307336-0A patent/BR0307336A/pt not_active IP Right Cessation
- 2003-01-30 US US10/354,653 patent/US20030199483A1/en not_active Abandoned
- 2003-01-30 KR KR10-2004-7011714A patent/KR20040096540A/ko not_active Ceased
- 2003-01-30 CA CA002474845A patent/CA2474845A1/en not_active Abandoned
- 2003-01-30 JP JP2003563540A patent/JP2005519918A/ja not_active Abandoned
- 2003-01-30 MX MXPA04007472A patent/MXPA04007472A/es unknown
- 2003-01-30 WO PCT/US2003/002723 patent/WO2003063846A2/en not_active Ceased
- 2003-01-30 EP EP20030710786 patent/EP1469862A2/en not_active Withdrawn
- 2003-01-30 CN CNA03802988XA patent/CN1625404A/zh active Pending
-
2004
- 2004-07-08 ZA ZA200405437A patent/ZA200405437B/xx unknown
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