JP2008515903A5 - - Google Patents
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- Publication number
- JP2008515903A5 JP2008515903A5 JP2007535795A JP2007535795A JP2008515903A5 JP 2008515903 A5 JP2008515903 A5 JP 2008515903A5 JP 2007535795 A JP2007535795 A JP 2007535795A JP 2007535795 A JP2007535795 A JP 2007535795A JP 2008515903 A5 JP2008515903 A5 JP 2008515903A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- formula
- pharmaceutical composition
- alkoxy
- pharmaceutically acceptable
- 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.)
- Ceased
Links
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims description 14
- 239000002461 renin inhibitor Substances 0.000 claims description 14
- 229940086526 renin-inhibitors Drugs 0.000 claims description 14
- 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 claims description 14
- 229960004699 valsartan Drugs 0.000 claims description 14
- 206010052337 Diastolic dysfunction Diseases 0.000 claims description 10
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 5
- 208000003037 Diastolic Heart Failure Diseases 0.000 claims description 5
- 108050000824 Angiotensin II receptor Proteins 0.000 claims description 3
- 102000008873 Angiotensin II receptor Human genes 0.000 claims description 3
- 230000004064 dysfunction Effects 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 34
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- -1 3-methoxypropyloxy Chemical group 0.000 claims 2
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000005236 alkanoylamino group Chemical group 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000003087 receptor blocking agent Substances 0.000 claims 2
- XPCFTKFZXHTYIP-PMACEKPBSA-N Benazepril Chemical group 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 claims 1
- 108010061435 Enalapril Proteins 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229960004530 benazepril Drugs 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 229960000873 enalapril Drugs 0.000 claims 1
- 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 claims 1
- UXOWGYHJODZGMF-QORCZRPOSA-N Aliskiren Chemical compound COCCCOC1=CC(C[C@@H](C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C)=CC=C1OC UXOWGYHJODZGMF-QORCZRPOSA-N 0.000 description 12
- 229960004601 aliskiren Drugs 0.000 description 12
- 230000014509 gene expression Effects 0.000 description 11
- 230000003205 diastolic effect Effects 0.000 description 9
- 206010020880 Hypertrophy Diseases 0.000 description 8
- 108020004999 messenger RNA Proteins 0.000 description 8
- 206010007572 Cardiac hypertrophy Diseases 0.000 description 5
- 208000006029 Cardiomegaly Diseases 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 4
- 230000007423 decrease Effects 0.000 description 4
- 231100000673 dose–response relationship Toxicity 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 230000002861 ventricular Effects 0.000 description 4
- 102000005862 Angiotensin II Human genes 0.000 description 3
- 101800000733 Angiotensin-2 Proteins 0.000 description 3
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 description 3
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 description 3
- 229950006323 angiotensin ii Drugs 0.000 description 3
- 238000002592 echocardiography Methods 0.000 description 3
- 0 *[C@](C[C@@]([C@](C[C@@](*)C(N*)=O)O)N)Cc1cc(*)c(*)cc1 Chemical compound *[C@](C[C@@]([C@](C[C@@](*)C(N*)=O)O)N)Cc1cc(*)c(*)cc1 0.000 description 2
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 description 2
- 102000002723 Atrial Natriuretic Factor Human genes 0.000 description 2
- 101800001288 Atrial natriuretic factor Proteins 0.000 description 2
- 101800001890 Atrial natriuretic peptide Proteins 0.000 description 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 description 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 2
- 230000001746 atrial effect Effects 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 230000009787 cardiac fibrosis Effects 0.000 description 2
- NSQLIUXCMFBZME-MPVJKSABSA-N carperitide Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)=O)[C@@H](C)CC)C1=CC=CC=C1 NSQLIUXCMFBZME-MPVJKSABSA-N 0.000 description 2
- 230000008602 contraction Effects 0.000 description 2
- 239000003550 marker Substances 0.000 description 2
- 238000011002 quantification Methods 0.000 description 2
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 description 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 description 1
- PXXXJPXDEIYISB-LIVOIKKVSA-N COCO[C@H](CNC[C@@H]1OCc2cc(OC)c(cccc3)c3c2)[C@@H]1c(cc1)ccc1OCCCOCc1ccccc1OC Chemical compound COCO[C@H](CNC[C@@H]1OCc2cc(OC)c(cccc3)c3c2)[C@@H]1c(cc1)ccc1OCCCOCc1ccccc1OC PXXXJPXDEIYISB-LIVOIKKVSA-N 0.000 description 1
- PHEZVSMVAGZWBE-LCFCVFAESA-N COc1ccccc1COCCCOc1ccc([C@@H]([C@H](CO)CNC2)[C@H]2OCc2cc(OC)c(cccc3)c3c2)cc1 Chemical compound COc1ccccc1COCCCOc1ccc([C@@H]([C@H](CO)CNC2)[C@H]2OCc2cc(OC)c(cccc3)c3c2)cc1 PHEZVSMVAGZWBE-LCFCVFAESA-N 0.000 description 1
- 102000009123 Fibrin Human genes 0.000 description 1
- 108010073385 Fibrin Proteins 0.000 description 1
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 description 1
- 206010016807 Fluid retention Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 229960002478 aldosterone Drugs 0.000 description 1
- 229940125364 angiotensin receptor blocker Drugs 0.000 description 1
- 230000003510 anti-fibrotic effect Effects 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000003293 cardioprotective effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 210000003754 fetus Anatomy 0.000 description 1
- 229950003499 fibrin Drugs 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 210000005240 left ventricle Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 210000004165 myocardium Anatomy 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000036454 renin-angiotensin system Effects 0.000 description 1
- 238000003757 reverse transcription PCR Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61720204P | 2004-10-08 | 2004-10-08 | |
| US66789905P | 2005-04-01 | 2005-04-01 | |
| PCT/US2005/035914 WO2006041974A1 (en) | 2004-10-08 | 2005-10-06 | Use of renin inhibitors for the prevention or treatment of diastolic dysfunction or diastolic heart failure |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008515903A JP2008515903A (ja) | 2008-05-15 |
| JP2008515903A5 true JP2008515903A5 (https=) | 2012-03-08 |
Family
ID=35789048
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007535795A Ceased JP2008515903A (ja) | 2004-10-08 | 2005-10-06 | 拡張機能障害または拡張期心不全の予防または処置のためのレニン阻害剤の使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20080085914A1 (https=) |
| EP (2) | EP1799199B1 (https=) |
| JP (1) | JP2008515903A (https=) |
| KR (2) | KR20130048281A (https=) |
| CN (1) | CN101102755B (https=) |
| AT (1) | ATE551052T1 (https=) |
| AU (2) | AU2005294318A1 (https=) |
| BR (1) | BRPI0516128A (https=) |
| CA (1) | CA2580862A1 (https=) |
| ES (1) | ES2384637T3 (https=) |
| MX (1) | MX2007004020A (https=) |
| PL (1) | PL1799199T3 (https=) |
| PT (1) | PT1799199E (https=) |
| RU (1) | RU2407523C2 (https=) |
| WO (1) | WO2006041974A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1972335A1 (en) * | 2007-03-23 | 2008-09-24 | Krka | Solid dosage forms comprising aliskiren and pharmaceutically acceptable salts thereof |
| CA2681746C (en) | 2007-03-27 | 2014-04-29 | Calpis Co., Ltd. | Prophylactic agent for heart failure |
| TW200924737A (en) * | 2007-09-28 | 2009-06-16 | Novartis Ag | Galenical formulations of organic compounds |
| EP2205279B1 (en) * | 2007-09-28 | 2011-04-13 | Novartis AG | Pharmaceutical combination of aliskiren and valsartan |
| PE20110943A1 (es) * | 2009-01-28 | 2012-01-22 | Novartis Ag | Formulacion oral solida de alisquireno |
| EP2216020A1 (en) * | 2009-02-05 | 2010-08-11 | KRKA, tovarna zdravil, d.d., Novo mesto | Moisture-activated granulation process |
| EP2340820A1 (en) * | 2009-12-16 | 2011-07-06 | KRKA, tovarna zdravil, d.d., Novo mesto | Moisture-activated granulation process |
| EA201190091A1 (ru) * | 2009-02-05 | 2012-01-30 | Крка, Товарна Здравил, Д. Д., Ново Место | Активируемый влагой способ грануляции |
| US20120107397A1 (en) * | 2009-07-03 | 2012-05-03 | Hetero Research Foundation | Pharmaceutical compositions of valsartan |
| US20110268797A1 (en) * | 2010-04-30 | 2011-11-03 | Sanovel IIac Sanayi Ve Ticaret Anonim Sirketi | Multicoated aliskiren formulations |
| FR2961105B1 (fr) * | 2010-06-15 | 2013-02-08 | Servier Lab | Utilisation de l'association d'un inhibiteur du courant if sinusal et d'un inhibiteur de l'enzyme de conversion de l'angiotensine pour le traitement de l'insuffisance cardiaque |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1334092C (en) | 1986-07-11 | 1995-01-24 | David John Carini | Angiotensin ii receptor blocking imidazoles |
| CA2018438C (en) | 1989-06-14 | 2000-08-08 | Joseph Alan Finkelstein | Imidazolyl-alkenoic acids |
| IL97219A (en) | 1990-02-19 | 1995-12-08 | Ciba Geigy Ag | Biphenyl substituted aliphatic amino compounds process for their preparation and pharmaceutical compositions containing them |
| TW201738B (https=) | 1990-03-20 | 1993-03-11 | Sanofi Co | |
| US5196444A (en) | 1990-04-27 | 1993-03-23 | Takeda Chemical Industries, Ltd. | 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and compositions and methods of pharmaceutical use thereof |
| BR9106438A (pt) * | 1990-05-11 | 1993-05-18 | Pfizer | Composicoes terapeuticas sinergisticas e processos |
| IE920540A1 (en) | 1991-02-21 | 1992-08-26 | Sankyo Co | 1-biphenylmethylimidazole derivatives, their preparation and¹their therapetuic use |
| DE4121975A1 (de) | 1991-07-03 | 1993-01-07 | Basf Ag | Thermoplastische formmassen auf der basis von polycarbonaten, styrol/acrylnitril-polymerisaten und polyolefinen |
| TW226375B (https=) | 1991-10-24 | 1994-07-11 | American Home Prod | |
| MY119161A (en) | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
| US6197959B1 (en) | 1999-04-27 | 2001-03-06 | Hoffmann-La Roche Inc. | Piperidine derivatives |
| US6376672B1 (en) | 1999-04-27 | 2002-04-23 | Hoffmann-La Roche Inc. | Naphthalenylmethoxypiperidines as renin inhibitors |
| US8168616B1 (en) * | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
| US20040087484A1 (en) * | 2000-12-01 | 2004-05-06 | Sahota Pritam Singh | Combination of organic compounds |
| US7019010B2 (en) * | 2001-09-27 | 2006-03-28 | Novertis Ag | Combinations |
| GB0212410D0 (en) * | 2002-05-29 | 2002-07-10 | Novartis Ag | Organic compounds |
| GB0212412D0 (en) * | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
| CA2490811A1 (en) * | 2002-06-28 | 2004-01-08 | Novartis Ag | Use of organic compounds |
| AU2004293178B8 (en) * | 2003-11-26 | 2009-01-08 | Novartis Ag | Organic compounds |
| ATE440082T1 (de) * | 2003-11-26 | 2009-09-15 | Novartis Pharma Gmbh | 4-phenylpiperidinderivate als renininhibitoren |
| GB0327839D0 (en) * | 2003-12-01 | 2003-12-31 | Novartis Ag | Organic compounds |
| PE20050596A1 (es) * | 2003-12-19 | 2005-10-18 | Novartis Ag | Microemulsion que comprende un inhibidor renina |
| MY146830A (en) * | 2005-02-11 | 2012-09-28 | Novartis Ag | Combination of organic compounds |
-
2005
- 2005-10-06 AU AU2005294318A patent/AU2005294318A1/en not_active Abandoned
- 2005-10-06 PT PT05810560T patent/PT1799199E/pt unknown
- 2005-10-06 WO PCT/US2005/035914 patent/WO2006041974A1/en not_active Ceased
- 2005-10-06 MX MX2007004020A patent/MX2007004020A/es active IP Right Grant
- 2005-10-06 CN CN2005800340394A patent/CN101102755B/zh not_active Expired - Fee Related
- 2005-10-06 KR KR1020137010963A patent/KR20130048281A/ko not_active Withdrawn
- 2005-10-06 PL PL05810560T patent/PL1799199T3/pl unknown
- 2005-10-06 CA CA002580862A patent/CA2580862A1/en not_active Abandoned
- 2005-10-06 EP EP05810560A patent/EP1799199B1/en not_active Revoked
- 2005-10-06 JP JP2007535795A patent/JP2008515903A/ja not_active Ceased
- 2005-10-06 US US11/576,495 patent/US20080085914A1/en not_active Abandoned
- 2005-10-06 BR BRPI0516128-2A patent/BRPI0516128A/pt not_active IP Right Cessation
- 2005-10-06 RU RU2007116863/15A patent/RU2407523C2/ru not_active IP Right Cessation
- 2005-10-06 EP EP10008427A patent/EP2248520A3/en not_active Withdrawn
- 2005-10-06 AT AT05810560T patent/ATE551052T1/de active
- 2005-10-06 KR KR1020077007885A patent/KR20070101843A/ko not_active Ceased
- 2005-10-06 ES ES05810560T patent/ES2384637T3/es not_active Expired - Lifetime
-
2010
- 2010-03-04 AU AU2010200833A patent/AU2010200833B2/en not_active Ceased
-
2012
- 2012-12-10 US US13/709,549 patent/US20130196977A1/en not_active Abandoned
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