JP2003508426A5 - - Google Patents
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- JP2003508426A5 JP2003508426A5 JP2001519887A JP2001519887A JP2003508426A5 JP 2003508426 A5 JP2003508426 A5 JP 2003508426A5 JP 2001519887 A JP2001519887 A JP 2001519887A JP 2001519887 A JP2001519887 A JP 2001519887A JP 2003508426 A5 JP2003508426 A5 JP 2003508426A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- inhibitor
- acceptable derivative
- ras
- pharmaceutical formulation
- 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.)
- Granted
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- 239000003112 inhibitor Substances 0.000 description 8
- 230000002401 inhibitory effect Effects 0.000 description 8
- 230000036454 renin-angiotensin system Effects 0.000 description 7
- -1 ancobenin Chemical compound 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 230000003042 antagnostic Effects 0.000 description 5
- 239000005557 antagonist Substances 0.000 description 5
- 239000005541 ACE inhibitor Substances 0.000 description 4
- 206010007559 Cardiac failure congestive Diseases 0.000 description 4
- 201000006233 congestive heart failure Diseases 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 239000002053 C09CA06 - Candesartan Substances 0.000 description 3
- SGZAIDDFHDDFJU-UHFFFAOYSA-N Candesartan Chemical compound CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SGZAIDDFHDDFJU-UHFFFAOYSA-N 0.000 description 3
- GHOSNRCGJFBJIB-UHFFFAOYSA-N Candesartan cilexetil Chemical compound C=12N(CC=3C=CC(=CC=3)C=3C(=CC=CC=3)C3=NNN=N3)C(OCC)=NC2=CC=CC=1C(=O)OC(C)OC(=O)OC1CCCCC1 GHOSNRCGJFBJIB-UHFFFAOYSA-N 0.000 description 3
- 229960000873 Enalapril Drugs 0.000 description 3
- 108010061435 Enalapril Proteins 0.000 description 3
- GBXSMTUPTTWBMN-XIRDDKMYSA-N Enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 description 3
- 108010066671 Enalaprilat Proteins 0.000 description 3
- LZFZMUMEGBBDTC-QEJZJMRPSA-N Enalaprilat Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 LZFZMUMEGBBDTC-QEJZJMRPSA-N 0.000 description 3
- 229960002394 Lisinopril Drugs 0.000 description 3
- 108010007859 Lisinopril Proteins 0.000 description 3
- 229960003401 Ramipril Drugs 0.000 description 3
- HDACQVRGBOVJII-JBDAPHQKSA-N Ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 description 3
- 229960002231 Ramiprilat Drugs 0.000 description 3
- 229960000932 candesartan Drugs 0.000 description 3
- 229960004349 candesartan cilexetil Drugs 0.000 description 3
- 229960002680 enalaprilat Drugs 0.000 description 3
- RLAWWYSOJDYHDC-BZSNNMDCSA-N lisinopril Chemical compound C([C@H](N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 RLAWWYSOJDYHDC-BZSNNMDCSA-N 0.000 description 3
- KEDYTOTWMPBSLG-HILJTLORSA-N ramiprilat Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)C(O)=O)CC1=CC=CC=C1 KEDYTOTWMPBSLG-HILJTLORSA-N 0.000 description 3
- BIDNLKIUORFRQP-XYGFDPSESA-N (2S,4S)-4-cyclohexyl-1-[2-[[(1S)-2-methyl-1-propanoyloxypropoxy]-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid Chemical compound C([P@@](=O)(O[C@H](OC(=O)CC)C(C)C)CC(=O)N1[C@@H](C[C@H](C1)C1CCCCC1)C(O)=O)CCCC1=CC=CC=C1 BIDNLKIUORFRQP-XYGFDPSESA-N 0.000 description 2
- FIQOFIRCTOWDOW-BJLQDIEVSA-N 2-[(2S,6R)-6-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]azaniumyl]-5-oxo-2-thiophen-2-yl-1,4-thiazepan-4-yl]acetate Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C[C@H](SC1)C=1SC=CC=1)=O)CC1=CC=CC=C1 FIQOFIRCTOWDOW-BJLQDIEVSA-N 0.000 description 2
- XRKXJJYSKUIIEN-LLVKDONJSA-N 2-[cyclopentyl-[(2S)-3-(2,2-dimethylpropanoylsulfanyl)-2-methylpropanoyl]amino]acetic acid Chemical compound CC(C)(C)C(=O)SC[C@@H](C)C(=O)N(CC(O)=O)C1CCCC1 XRKXJJYSKUIIEN-LLVKDONJSA-N 0.000 description 2
- 239000002083 C09CA01 - Losartan Substances 0.000 description 2
- 239000002080 C09CA02 - Eprosartan Substances 0.000 description 2
- 239000004072 C09CA03 - Valsartan Substances 0.000 description 2
- 239000002947 C09CA04 - Irbesartan Substances 0.000 description 2
- 239000002081 C09CA05 - Tasosartan Substances 0.000 description 2
- 239000005537 C09CA07 - Telmisartan Substances 0.000 description 2
- 206010012601 Diabetes mellitus Diseases 0.000 description 2
- OROAFUQRIXKEMV-LDADJPATSA-N Eprosartan Chemical compound C=1C=C(C(O)=O)C=CC=1CN1C(CCCC)=NC=C1\C=C(C(O)=O)/CC1=CC=CS1 OROAFUQRIXKEMV-LDADJPATSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- YCPOHTHPUREGFM-UHFFFAOYSA-N Irbesartan Chemical compound O=C1N(CC=2C=CC(=CC=2)C=2C(=CC=CC=2)C=2[N]N=NN=2)C(CCCC)=NC21CCCC2 YCPOHTHPUREGFM-UHFFFAOYSA-N 0.000 description 2
- 229960004773 Losartan Drugs 0.000 description 2
- KJJZZJSZUJXYEA-UHFFFAOYSA-N Losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 description 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 description 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 description 2
- JSDRRTOADPPCHY-HSQYWUDLSA-N Quinapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 JSDRRTOADPPCHY-HSQYWUDLSA-N 0.000 description 2
- HRWCVUIFMSZDJS-SZMVWBNQSA-N Spirapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2(C1)SCCS2)C(O)=O)CC1=CC=CC=C1 HRWCVUIFMSZDJS-SZMVWBNQSA-N 0.000 description 2
- ADXGNEYLLLSOAR-UHFFFAOYSA-N Tasosartan Chemical compound C12=NC(C)=NC(C)=C2CCC(=O)N1CC(C=C1)=CC=C1C1=CC=CC=C1C=1N=NNN=1 ADXGNEYLLLSOAR-UHFFFAOYSA-N 0.000 description 2
- RMMXLENWKUUMAY-UHFFFAOYSA-N Telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 description 2
- SJSNUMAYCRRIOM-QFIPXVFZSA-N Valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 description 2
- IAIDUHCBNLFXEF-MNEFBYGVSA-N Zofenopril Chemical compound C([C@@H](C)C(=O)N1[C@@H](C[C@@H](C1)SC=1C=CC=CC=1)C(O)=O)SC(=O)C1=CC=CC=C1 IAIDUHCBNLFXEF-MNEFBYGVSA-N 0.000 description 2
- 229960004563 eprosartan Drugs 0.000 description 2
- 229960002490 fosinopril Drugs 0.000 description 2
- WOIWWYDXDVSWAZ-RTWAWAEBSA-N fosinoprilat Chemical compound C([C@@H](C[C@H]1C(=O)O)C2CCCCC2)N1C(=O)CP(O)(=O)CCCCC1=CC=CC=C1 WOIWWYDXDVSWAZ-RTWAWAEBSA-N 0.000 description 2
- 229960002198 irbesartan Drugs 0.000 description 2
- 229960001455 quinapril Drugs 0.000 description 2
- 229960002909 spirapril Drugs 0.000 description 2
- 229960000651 tasosartan Drugs 0.000 description 2
- 229960005187 telmisartan Drugs 0.000 description 2
- 229960004084 temocapril Drugs 0.000 description 2
- 229960004699 valsartan Drugs 0.000 description 2
- 229960002769 zofenopril Drugs 0.000 description 2
- QKIVRALZQSUWHH-SFYZADRCSA-N (1S,2R)-2-[[2-(hydroxyamino)-2-oxoethyl]-methylcarbamoyl]cyclohexane-1-carboxylic acid Chemical compound ONC(=O)CN(C)C(=O)[C@@H]1CCCC[C@@H]1C(O)=O QKIVRALZQSUWHH-SFYZADRCSA-N 0.000 description 1
- NVXFXLSOGLFXKQ-JMSVASOKSA-N (2S)-1-[(2R,4R)-5-ethoxy-2,4-dimethyl-5-oxopentanoyl]-2,3-dihydroindole-2-carboxylic acid Chemical compound C1=CC=C2N(C(=O)[C@H](C)C[C@@H](C)C(=O)OCC)[C@H](C(O)=O)CC2=C1 NVXFXLSOGLFXKQ-JMSVASOKSA-N 0.000 description 1
- OMGPCTGQLHHVDU-SSXGPBTGSA-N (2S)-3-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-3-azabicyclo[2.2.2]octane-2-carboxylic acid Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C2CCC1CC2)C(O)=O)CC1=CC=CC=C1 OMGPCTGQLHHVDU-SSXGPBTGSA-N 0.000 description 1
- CMPAGYDKASJORH-YSSFQJQWSA-N (3S)-2-[(2S)-2-[[(1S)-1-carboxy-3-phenylpropyl]amino]propanoyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-3-carboxylic acid Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](CC=2C=C(C(=CC=2C1)OC)OC)C(O)=O)C(O)=O)CC1=CC=CC=C1 CMPAGYDKASJORH-YSSFQJQWSA-N 0.000 description 1
- NZFXQRHFBLVEQA-GXOSTJLWSA-N (6R)-2-[[(4S)-4-[[(2S)-2-[2-[(2S,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxypropanoylamino]propanoyl]amino]-4-carboxybutanoyl]amino]-6,7-diamino-7-oxoheptanoic acid Chemical compound NC(=O)[C@H](N)CCCC(C(O)=O)NC(=O)CC[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)C(C)O[C@H]1[C@H](O)[C@@H](CO)O[C@H](O)[C@@H]1NC(C)=O NZFXQRHFBLVEQA-GXOSTJLWSA-N 0.000 description 1
- VPSRQEHTHIMDQM-FDOHDBATSA-N 2-[(3R)-3-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid;hydrochloride Chemical compound Cl.C([C@@H](C(=O)OCC)N[C@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 VPSRQEHTHIMDQM-FDOHDBATSA-N 0.000 description 1
- FHHHOYXPRDYHEZ-COXVUDFISA-N Alacepril Chemical compound CC(=O)SC[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 FHHHOYXPRDYHEZ-COXVUDFISA-N 0.000 description 1
- 229950007884 Alacepril Drugs 0.000 description 1
- 229960003619 Benazepril hydrochloride Drugs 0.000 description 1
- MADRIHWFJGRSBP-ROUUACIJSA-N Benazeprilat Chemical compound C([C@H](N[C@H]1CCC2=CC=CC=C2N(C1=O)CC(=O)O)C(O)=O)CC1=CC=CC=C1 MADRIHWFJGRSBP-ROUUACIJSA-N 0.000 description 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N Captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 description 1
- NEEBNBLVYKFVTK-VGMNWLOBSA-N Captopril-cysteine disulfide Chemical compound OC(=O)[C@@H](N)CSSC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O NEEBNBLVYKFVTK-VGMNWLOBSA-N 0.000 description 1
- 229960005025 Cilazapril Drugs 0.000 description 1
- HHHKFGXWKKUNCY-FHWLQOOXSA-N Cilazapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N2[C@@H](CCCN2CCC1)C(O)=O)=O)CC1=CC=CC=C1 HHHKFGXWKKUNCY-FHWLQOOXSA-N 0.000 description 1
- 229950010233 Cilazaprilat Drugs 0.000 description 1
- UVAUYSRYXACKSC-ULQDDVLXSA-N Cilazaprilat Chemical compound C([C@@H](C(=O)O)N[C@@H]1C(N2[C@@H](CCCN2CCC1)C(O)=O)=O)CC1=CC=CC=C1 UVAUYSRYXACKSC-ULQDDVLXSA-N 0.000 description 1
- 229960005227 DELAPRIL Drugs 0.000 description 1
- WOUOLAUOZXOLJQ-MBSDFSHPSA-N Delapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N(CC(O)=O)C1CC2=CC=CC=C2C1)CC1=CC=CC=C1 WOUOLAUOZXOLJQ-MBSDFSHPSA-N 0.000 description 1
- 229960003018 Fosinoprilat Drugs 0.000 description 1
- WEGGKZQIJMQCGR-RECQUVTISA-N Hemorphin-4 Chemical compound C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H]([C@H](O)C)C(O)=O)C1=CC=C(O)C=C1 WEGGKZQIJMQCGR-RECQUVTISA-N 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 229950010375 Idrapril Drugs 0.000 description 1
- KLZWOWYOHUKJIG-BPUTZDHNSA-N Imidapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1C(N(C)C[C@H]1C(O)=O)=O)CC1=CC=CC=C1 KLZWOWYOHUKJIG-BPUTZDHNSA-N 0.000 description 1
- 229960005170 MOEXIPRIL Drugs 0.000 description 1
- UWWDHYUMIORJTA-HSQYWUDLSA-N Moexipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC(OC)=C(OC)C=C2C1)C(O)=O)CC1=CC=CC=C1 UWWDHYUMIORJTA-HSQYWUDLSA-N 0.000 description 1
- 229960000937 Moexiprilat Drugs 0.000 description 1
- 229950008492 PENTOPRIL Drugs 0.000 description 1
- 229960002582 Perindopril Drugs 0.000 description 1
- IPVQLZZIHOAWMC-QXKUPLGCSA-N Perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 description 1
- ODAIHABQVKJNIY-PEDHHIEDSA-N Perindoprilat Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(O)=O)[C@H]21 ODAIHABQVKJNIY-PEDHHIEDSA-N 0.000 description 1
- 229960005226 Perindoprilat Drugs 0.000 description 1
- 229950008688 Pivopril Drugs 0.000 description 1
- FLSLEGPOVLMJMN-YSSFQJQWSA-N Quinaprilat Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)C(O)=O)CC1=CC=CC=C1 FLSLEGPOVLMJMN-YSSFQJQWSA-N 0.000 description 1
- 229940083542 Sodium Drugs 0.000 description 1
- 229940091252 Sodium supplements Drugs 0.000 description 1
- FMMDBLMCSDRUPA-BPUTZDHNSA-N Spiraprilat Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](CC2(C1)SCCS2)C(O)=O)C(O)=O)CC1=CC=CC=C1 FMMDBLMCSDRUPA-BPUTZDHNSA-N 0.000 description 1
- 229950006297 Spiraprilat Drugs 0.000 description 1
- 229950010186 Teprotide Drugs 0.000 description 1
- UUUHXMGGBIUAPW-CSCXCSGISA-N Teprotide Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(O)=O)C(=O)[C@@H]1CCC(=O)N1 UUUHXMGGBIUAPW-CSCXCSGISA-N 0.000 description 1
- 108010045759 Teprotide Proteins 0.000 description 1
- AHYHTSYNOHNUSH-HXFGRODQSA-N Trandolaprilat Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)C(O)=O)CC1=CC=CC=C1 AHYHTSYNOHNUSH-HXFGRODQSA-N 0.000 description 1
- VXFJYXUZANRPDJ-WTNASJBWSA-N Trandopril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 VXFJYXUZANRPDJ-WTNASJBWSA-N 0.000 description 1
- 102000010913 Type 1 Angiotensin Receptor Human genes 0.000 description 1
- 108010062481 Type 1 Angiotensin Receptor Proteins 0.000 description 1
- 229950009999 Zabicipril Drugs 0.000 description 1
- 229960004530 benazepril Drugs 0.000 description 1
- 229960004067 benazeprilat Drugs 0.000 description 1
- XPCFTKFZXHTYIP-PMACEKPBSA-N benzazepril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 XPCFTKFZXHTYIP-PMACEKPBSA-N 0.000 description 1
- IVBOFTGCTWVBLF-GOSISDBHSA-N benzyl 2-[[(2S)-2-(acetylsulfanylmethyl)-3-(1,3-benzodioxol-5-yl)propanoyl]amino]acetate Chemical compound O=C([C@H](CC=1C=C2OCOC2=CC=1)CSC(=O)C)NCC(=O)OCC1=CC=CC=C1 IVBOFTGCTWVBLF-GOSISDBHSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 229960000830 captopril Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- OYFJQPXVCSSHAI-QFPUQLAESA-N enalapril maleate Chemical compound OC(=O)\C=C/C(O)=O.C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 OYFJQPXVCSSHAI-QFPUQLAESA-N 0.000 description 1
- 230000001747 exhibiting Effects 0.000 description 1
- 108010047748 hemorphin 4 Proteins 0.000 description 1
- 230000001077 hypotensive Effects 0.000 description 1
- 229960001195 imidapril Drugs 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229960001007 quinaprilat Drugs 0.000 description 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229960002051 trandolapril Drugs 0.000 description 1
- 229960002651 trandolaprilat Drugs 0.000 description 1
Description
【特許請求の範囲】
【請求項1】 卒中を予防するための医薬の製造における、レニン−アンギオテンシン系(RAS)の阻害剤またはその製薬上許容される誘導体の使用。
【請求項2】 正常血圧または低血圧を示す患者の卒中を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項3】 糖尿病を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項4】 うっ血性心不全(CHF)が先在しない患者のCHFの発生を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項5】 RASの阻害剤が、アンギオテンシン変換酵素(ACE)阻害剤またはアンギオテンシンII型1受容体(AT II)拮抗剤またはこれら何れかの製薬上許容される誘導体である、請求項1〜4の何れかに記載の使用。
【請求項6】 ACE阻害剤またはその製薬上許容される誘導体が、アラセプリル、アラトリオプリル、アルチオプリルカルシウム、アンコベニン、ベナゼプリル、塩酸ベナゼプリル、ベナゼプリラット、ベンゾイルカプトプリル、カプトプリル、カプトプリル−システイン、カプトプリル−グルタチオン、セラナプリル、セラノプリル、セロナプリル、シラザプリル、シラザプリラット、デラプリル、デラプリル−ジ酸、エナラプリル、エナラプリラット、エナプリル、エピカプトプリル、ホロキシミチン、ホスフェノプリル、ホセノプリル、ホセノプリルナトリウム、ホシノプリル、ホシノプリルナトリウム、ホシノプリラット、ホシノプリル酸、グリコプリル、へモルフィン−4、イドラプリル、イミダプリル、インドラプリル、インドラプリラット、リベンザプリル、リシノプリル、リシウミンA、リシウミンB、ミキサンプリル、モエキシプリル、モエキシプリラット、モベルチプリル、ムラセインA、ムラセインB、ムラセインC、ペントプリル、ペリンドプリル、ペリンドプリラット、ピバロプリル、ピボプリル、キナプリル、塩酸キナプリル、キナプリラット、ラミプリル、ラミプリラット、スピラプリル、塩酸スピラプリル、スピラプリラット、スピロプリル、塩酸スピロプリル、テモカプリル、塩酸テモカプリル、テプロチド、トランドラプリル、トランドラプリラット、ウチバプリル、ザビシプリル、ザビシプリラット、ゾフェノプリルおよびゾフェノプリラットからなる群から選択される、請求項5に記載の使用。
【請求項7】 ACE阻害剤が、ラミプリル、ラミプリラット、リシノプリル、エナラプリルおよびエナラプリラットからなる群から選択される、請求項6に記載の使用。
【請求項8】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタン、カンデサルタンシレキセチル、ロサルタン、バルサルタン、イルベサルタン、タソサルタン、テルミサルタンおよびエプロサルタンからなる群から選択される、請求項5に記載の使用。
【請求項9】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタンおよびカンデサルタンシレキセチルからなる群から選択される、請求項8に記載の使用。
【請求項10】 治療上有効量のRASの阻害剤またはその製薬上許容される誘導体を含む、卒中、糖尿病および/またはCHFの予防に使用するための医薬処方物。
【請求項11】 RASの阻害剤が、ACE阻害剤またはAT II拮抗剤またはこれら何れかの製薬上許容される誘導体である、請求項10に記載の医薬処方物。
【請求項12】 ACE阻害剤が、ラミプリル、ラミプリラット、リシノプリル、エナラプリルおよびエナラプリラットからなる群から選択される、請求項11に記載の医薬処方物。
【請求項13】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタン、カンデサルタンシレキセチル、ロサルタン、バルサルタン、イルベサルタン、タソサルタン、テルミサルタンおよびエプロサルタンからなる群から選択される、請求項11に記載の医薬処方物。
【請求項14】 製薬上許容される補助剤、希釈剤および/または担体との混合物である、請求項10〜13の何れか1項に記載の医薬処方物。
【請求項15】 単位用量形態にある、請求項10〜14の何れか1項に記載の医薬処方物。
【請求項1】 卒中を予防するための医薬の製造における、レニン−アンギオテンシン系(RAS)の阻害剤またはその製薬上許容される誘導体の使用。
【請求項2】 正常血圧または低血圧を示す患者の卒中を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項3】 糖尿病を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項4】 うっ血性心不全(CHF)が先在しない患者のCHFの発生を予防するための医薬の製造における、RASの阻害剤またはその製薬上許容される誘導体の使用。
【請求項5】 RASの阻害剤が、アンギオテンシン変換酵素(ACE)阻害剤またはアンギオテンシンII型1受容体(AT II)拮抗剤またはこれら何れかの製薬上許容される誘導体である、請求項1〜4の何れかに記載の使用。
【請求項6】 ACE阻害剤またはその製薬上許容される誘導体が、アラセプリル、アラトリオプリル、アルチオプリルカルシウム、アンコベニン、ベナゼプリル、塩酸ベナゼプリル、ベナゼプリラット、ベンゾイルカプトプリル、カプトプリル、カプトプリル−システイン、カプトプリル−グルタチオン、セラナプリル、セラノプリル、セロナプリル、シラザプリル、シラザプリラット、デラプリル、デラプリル−ジ酸、エナラプリル、エナラプリラット、エナプリル、エピカプトプリル、ホロキシミチン、ホスフェノプリル、ホセノプリル、ホセノプリルナトリウム、ホシノプリル、ホシノプリルナトリウム、ホシノプリラット、ホシノプリル酸、グリコプリル、へモルフィン−4、イドラプリル、イミダプリル、インドラプリル、インドラプリラット、リベンザプリル、リシノプリル、リシウミンA、リシウミンB、ミキサンプリル、モエキシプリル、モエキシプリラット、モベルチプリル、ムラセインA、ムラセインB、ムラセインC、ペントプリル、ペリンドプリル、ペリンドプリラット、ピバロプリル、ピボプリル、キナプリル、塩酸キナプリル、キナプリラット、ラミプリル、ラミプリラット、スピラプリル、塩酸スピラプリル、スピラプリラット、スピロプリル、塩酸スピロプリル、テモカプリル、塩酸テモカプリル、テプロチド、トランドラプリル、トランドラプリラット、ウチバプリル、ザビシプリル、ザビシプリラット、ゾフェノプリルおよびゾフェノプリラットからなる群から選択される、請求項5に記載の使用。
【請求項7】 ACE阻害剤が、ラミプリル、ラミプリラット、リシノプリル、エナラプリルおよびエナラプリラットからなる群から選択される、請求項6に記載の使用。
【請求項8】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタン、カンデサルタンシレキセチル、ロサルタン、バルサルタン、イルベサルタン、タソサルタン、テルミサルタンおよびエプロサルタンからなる群から選択される、請求項5に記載の使用。
【請求項9】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタンおよびカンデサルタンシレキセチルからなる群から選択される、請求項8に記載の使用。
【請求項10】 治療上有効量のRASの阻害剤またはその製薬上許容される誘導体を含む、卒中、糖尿病および/またはCHFの予防に使用するための医薬処方物。
【請求項11】 RASの阻害剤が、ACE阻害剤またはAT II拮抗剤またはこれら何れかの製薬上許容される誘導体である、請求項10に記載の医薬処方物。
【請求項12】 ACE阻害剤が、ラミプリル、ラミプリラット、リシノプリル、エナラプリルおよびエナラプリラットからなる群から選択される、請求項11に記載の医薬処方物。
【請求項13】 AT II拮抗剤またはその製薬上許容される誘導体が、カンデサルタン、カンデサルタンシレキセチル、ロサルタン、バルサルタン、イルベサルタン、タソサルタン、テルミサルタンおよびエプロサルタンからなる群から選択される、請求項11に記載の医薬処方物。
【請求項14】 製薬上許容される補助剤、希釈剤および/または担体との混合物である、請求項10〜13の何れか1項に記載の医薬処方物。
【請求項15】 単位用量形態にある、請求項10〜14の何れか1項に記載の医薬処方物。
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PCT/EP2000/008341 WO2001015673A2 (en) | 1999-08-27 | 2000-08-25 | Pharmaceutical formulations and use thereof in the prevention of stroke, diabetes and/or congestive heart failure |
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