JP2008530101A5 - - Google Patents
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- Publication number
- JP2008530101A5 JP2008530101A5 JP2007555186A JP2007555186A JP2008530101A5 JP 2008530101 A5 JP2008530101 A5 JP 2008530101A5 JP 2007555186 A JP2007555186 A JP 2007555186A JP 2007555186 A JP2007555186 A JP 2007555186A JP 2008530101 A5 JP2008530101 A5 JP 2008530101A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- propionyl
- carboxy
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 60
- 150000003839 salts Chemical class 0.000 claims 54
- -1 3-methoxypropyloxy Chemical group 0.000 claims 23
- 239000002461 renin inhibitor Substances 0.000 claims 20
- 229940086526 renin-inhibitors Drugs 0.000 claims 20
- 102000003729 Neprilysin Human genes 0.000 claims 14
- 108090000028 Neprilysin Proteins 0.000 claims 14
- 229940000635 beta-alanine Drugs 0.000 claims 12
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 8
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 8
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 8
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 8
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 8
- 239000002934 diuretic Substances 0.000 claims 8
- 230000001882 diuretic effect Effects 0.000 claims 8
- 239000002792 enkephalinase inhibitor Substances 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 239000003087 receptor blocking agent Substances 0.000 claims 8
- 102000005862 Angiotensin II Human genes 0.000 claims 6
- 101800000733 Angiotensin-2 Proteins 0.000 claims 6
- 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 claims 6
- 229950006323 angiotensin ii Drugs 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- KDQWIKMBLSWIPD-ABLWVSNPSA-N (2s)-2-[(2-benzyl-3-sulfanylpropanoyl)amino]-4,4-bis(methylsulfanyl)butanoic acid Chemical compound CSC(SC)C[C@@H](C(O)=O)NC(=O)C(CS)CC1=CC=CC=C1 KDQWIKMBLSWIPD-ABLWVSNPSA-N 0.000 claims 4
- QAQRHURCJWHRJU-FHWLQOOXSA-N (2s)-2-[[(2s)-1-[[(2s)-2-carboxy-2-hydroxyethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-phenylbutanoic acid Chemical compound C([C@@H](C(=O)NC[C@H](O)C(O)=O)N[C@@H](CCC=1C=CC=CC=1)C(O)=O)C1=CC=CC=C1 QAQRHURCJWHRJU-FHWLQOOXSA-N 0.000 claims 4
- FGXXIAHRYGHABD-KGLIPLIRSA-N (2s)-2-[[(2s)-2-[(2-methylphenyl)methyl]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoic acid Chemical compound CSCC[C@@H](C(O)=O)NC(=O)[C@@H](CS)CC1=CC=CC=C1C FGXXIAHRYGHABD-KGLIPLIRSA-N 0.000 claims 4
- PQSUQDFBGSIHKA-NEPJUHHUSA-N (2s)-2-hydroxy-3-[[(2s)-2-[(2-methylphenyl)methyl]-3-sulfanylpropanoyl]amino]propanoic acid Chemical compound CC1=CC=CC=C1C[C@H](CS)C(=O)NC[C@H](O)C(O)=O PQSUQDFBGSIHKA-NEPJUHHUSA-N 0.000 claims 4
- NLCRGAWADQQVEK-VXKWHMMOSA-N (2s)-2-hydroxy-3-[[1-[[(2s)-1-oxo-4-phenyl-1-phenylmethoxybutan-2-yl]amino]cyclopentanecarbonyl]amino]propanoic acid Chemical compound N([C@@H](CCC=1C=CC=CC=1)C(=O)OCC=1C=CC=CC=1)C1(C(=O)NC[C@H](O)C(O)=O)CCCC1 NLCRGAWADQQVEK-VXKWHMMOSA-N 0.000 claims 4
- AYOUMVNNOAOYLV-UHFFFAOYSA-N 2-[(3-phenyl-2-sulfanylbutanoyl)amino]-1,3-thiazole-4-carboxylic acid Chemical compound C=1C=CC=CC=1C(C)C(S)C(=O)NC1=NC(C(O)=O)=CS1 AYOUMVNNOAOYLV-UHFFFAOYSA-N 0.000 claims 4
- OSJSRBCOQRHXEC-LYKKTTPLSA-N 2-[[1-[[(2s)-2-carboxy-2-hydroxyethyl]carbamoyl]cyclopentyl]methyl]-4-phenylbutanoic acid Chemical compound C=1C=CC=CC=1CCC(C(O)=O)CC1(C(=O)NC[C@H](O)C(O)=O)CCCC1 OSJSRBCOQRHXEC-LYKKTTPLSA-N 0.000 claims 4
- UXTJLCWDHLUAQF-UHFFFAOYSA-N 3-[[2-(acetylsulfanylmethyl)-3-phenylpropanoyl]amino]benzoic acid Chemical compound C=1C=CC(C(O)=O)=CC=1NC(=O)C(CSC(=O)C)CC1=CC=CC=C1 UXTJLCWDHLUAQF-UHFFFAOYSA-N 0.000 claims 4
- REPVVNYZORKKPQ-UHFFFAOYSA-N 3-oxo-3-[(1-phenyl-3-sulfanylpropan-2-yl)amino]propanoic acid Chemical compound OC(=O)CC(=O)NC(CS)CC1=CC=CC=C1 REPVVNYZORKKPQ-UHFFFAOYSA-N 0.000 claims 4
- NCSNXXXLRVRXIM-UHFFFAOYSA-N 4-[(2-benzyl-3-sulfanylpropanoyl)amino]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1NC(=O)C(CS)CC1=CC=CC=C1 NCSNXXXLRVRXIM-UHFFFAOYSA-N 0.000 claims 4
- VCFGVPMALWRCTK-UHFFFAOYSA-N 4-[(2-benzyl-3-sulfanylpropanoyl)amino]thiophene-2-carboxylic acid Chemical compound S1C(C(=O)O)=CC(NC(=O)C(CS)CC=2C=CC=CC=2)=C1 VCFGVPMALWRCTK-UHFFFAOYSA-N 0.000 claims 4
- KJVKOEVEFLXJES-UHFFFAOYSA-N 7-[(2-benzyl-3-sulfanylpropanoyl)amino]heptanoic acid Chemical compound OC(=O)CCCCCCNC(=O)C(CS)CC1=CC=CC=C1 KJVKOEVEFLXJES-UHFFFAOYSA-N 0.000 claims 4
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 4
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims 4
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 claims 4
- 239000004471 Glycine Substances 0.000 claims 4
- 229930195722 L-methionine Natural products 0.000 claims 4
- ZPHBZEQOLSRPAK-UHFFFAOYSA-N Phosphoramidon Natural products C=1NC2=CC=CC=C2C=1CC(C(O)=O)NC(=O)C(CC(C)C)NP(O)(=O)OC1OC(C)C(O)C(O)C1O ZPHBZEQOLSRPAK-UHFFFAOYSA-N 0.000 claims 4
- 108010036928 Thiorphan Proteins 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 235000010290 biphenyl Nutrition 0.000 claims 4
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- WYPJYXKWBXYEBI-ZDUSSCGKSA-N ethyl (2s)-2-[[1-(acetylsulfanylmethyl)cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoate Chemical compound CCOC(=O)[C@H](CCSC)NC(=O)C1(CSC(C)=O)CCCC1 WYPJYXKWBXYEBI-ZDUSSCGKSA-N 0.000 claims 4
- ZVQXPUMRSJGLSF-ZVAWYAOSSA-N ethyl (2s)-2-[[2-(acetylsulfanylmethyl)-3-(2-methylphenyl)propanoyl]amino]-4-methylsulfanylbutanoate Chemical compound CCOC(=O)[C@H](CCSC)NC(=O)C(CSC(C)=O)CC1=CC=CC=C1C ZVQXPUMRSJGLSF-ZVAWYAOSSA-N 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 229960002003 hydrochlorothiazide Drugs 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- YACKEPLHDIMKIO-UHFFFAOYSA-N methylphosphonic acid Chemical compound CP(O)(O)=O YACKEPLHDIMKIO-UHFFFAOYSA-N 0.000 claims 4
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 4
- 108010072906 phosphoramidon Proteins 0.000 claims 4
- BWSDNRQVTFZQQD-AYVHNPTNSA-N phosphoramidon Chemical compound O([P@@](O)(=O)N[C@H](CC(C)C)C(=O)N[C@H](CC=1[C]2C=CC=CC2=NC=1)C(O)=O)[C@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@@H]1O BWSDNRQVTFZQQD-AYVHNPTNSA-N 0.000 claims 4
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 108700016891 retrothiorphan Proteins 0.000 claims 4
- 150000003536 tetrazoles Chemical class 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- LJJKNPQAGWVLDQ-SNVBAGLBSA-N thiorphan Chemical compound OC(=O)CNC(=O)[C@@H](CS)CC1=CC=CC=C1 LJJKNPQAGWVLDQ-SNVBAGLBSA-N 0.000 claims 4
- ACWBQPMHZXGDFX-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=NN1 ACWBQPMHZXGDFX-QFIPXVFZSA-N 0.000 claims 4
- 229960004699 valsartan Drugs 0.000 claims 4
- BOWUOGIPSRVRSJ-UHFFFAOYSA-N 2-aminohexano-6-lactam Chemical compound NC1CCCCNC1=O BOWUOGIPSRVRSJ-UHFFFAOYSA-N 0.000 claims 3
- UHXFGTQBGJWZEZ-UHFFFAOYSA-N 3-[(3-phenyl-2-sulfanylbutanoyl)amino]benzoic acid Chemical compound C=1C=CC=CC=1C(C)C(S)C(=O)NC1=CC=CC(C(O)=O)=C1 UHXFGTQBGJWZEZ-UHFFFAOYSA-N 0.000 claims 3
- 206010002383 Angina Pectoris Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 3
- 206010003662 Atrial flutter Diseases 0.000 claims 3
- 208000026372 Congenital cystic kidney disease Diseases 0.000 claims 3
- 208000026292 Cystic Kidney disease Diseases 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 3
- 208000032781 Diabetic cardiomyopathy Diseases 0.000 claims 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
- 206010052337 Diastolic dysfunction Diseases 0.000 claims 3
- 206010048554 Endothelial dysfunction Diseases 0.000 claims 3
- 208000004248 Familial Primary Pulmonary Hypertension Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 125000003412 L-alanyl group Chemical group [H]N([H])[C@@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 3
- 206010049694 Left Ventricular Dysfunction Diseases 0.000 claims 3
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 3
- 208000019695 Migraine disease Diseases 0.000 claims 3
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 3
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 3
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 3
- 208000003782 Raynaud disease Diseases 0.000 claims 3
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 3
- 208000001647 Renal Insufficiency Diseases 0.000 claims 3
- 201000003099 Renovascular Hypertension Diseases 0.000 claims 3
- 206010039710 Scleroderma Diseases 0.000 claims 3
- 206010039808 Secondary aldosteronism Diseases 0.000 claims 3
- 206010042600 Supraventricular arrhythmias Diseases 0.000 claims 3
- 208000032594 Vascular Remodeling Diseases 0.000 claims 3
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 3
- 230000002411 adverse Effects 0.000 claims 3
- 210000004556 brain Anatomy 0.000 claims 3
- 230000009787 cardiac fibrosis Effects 0.000 claims 3
- 208000020832 chronic kidney disease Diseases 0.000 claims 3
- 208000033679 diabetic kidney disease Diseases 0.000 claims 3
- 208000028208 end stage renal disease Diseases 0.000 claims 3
- 201000000523 end stage renal failure Diseases 0.000 claims 3
- 230000008694 endothelial dysfunction Effects 0.000 claims 3
- 239000000835 fiber Substances 0.000 claims 3
- 206010061989 glomerulosclerosis Diseases 0.000 claims 3
- 206010020718 hyperplasia Diseases 0.000 claims 3
- 206010020871 hypertrophic cardiomyopathy Diseases 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 201000006370 kidney failure Diseases 0.000 claims 3
- 206010027599 migraine Diseases 0.000 claims 3
- 208000010125 myocardial infarction Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 201000008312 primary pulmonary hypertension Diseases 0.000 claims 3
- 201000001474 proteinuria Diseases 0.000 claims 3
- 208000037812 secondary pulmonary hypertension Diseases 0.000 claims 3
- 230000006641 stabilisation Effects 0.000 claims 3
- 238000011105 stabilization Methods 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- FGXXIAHRYGHABD-KZUDCZAMSA-N (2s)-2-[[2-[(2-methylphenyl)methyl]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoic acid Chemical compound CSCC[C@@H](C(O)=O)NC(=O)C(CS)CC1=CC=CC=C1C FGXXIAHRYGHABD-KZUDCZAMSA-N 0.000 claims 2
- OLLRCBHPDQHWJH-QRMWWUJWSA-N (2s)-2-[[3-(2-methylphenyl)-2-sulfanylbutanoyl]amino]-4-methylsulfanylbutanoic acid Chemical compound CSCC[C@@H](C(O)=O)NC(=O)C(S)C(C)C1=CC=CC=C1C OLLRCBHPDQHWJH-QRMWWUJWSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- SUKNXYMRQLQQMI-UHFFFAOYSA-N 3-[(2-benzyl-3-sulfanylpropanoyl)amino]benzoic acid Chemical compound OC(=O)C1=CC=CC(NC(=O)C(CS)CC=2C=CC=CC=2)=C1 SUKNXYMRQLQQMI-UHFFFAOYSA-N 0.000 claims 1
- LDOFBCFBEJQIIY-PKHIMPSTSA-N C(C)(=O)SCC(C(=O)[C@@]1(C(=O)NCCCC1)N)CC1=CC=CC=C1 Chemical compound C(C)(=O)SCC(C(=O)[C@@]1(C(=O)NCCCC1)N)CC1=CC=CC=C1 LDOFBCFBEJQIIY-PKHIMPSTSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000001294 propane Substances 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65232505P | 2005-02-11 | 2005-02-11 | |
| US65510205P | 2005-02-22 | 2005-02-22 | |
| US67009005P | 2005-04-11 | 2005-04-11 | |
| PCT/US2006/004401 WO2006086456A2 (en) | 2005-02-11 | 2006-02-09 | Combination of organic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008530101A JP2008530101A (ja) | 2008-08-07 |
| JP2008530101A5 true JP2008530101A5 (https=) | 2009-04-09 |
Family
ID=36793671
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007555186A Pending JP2008530101A (ja) | 2005-02-11 | 2006-02-09 | 有機化合物の組合わせ剤 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20080119557A1 (https=) |
| EP (1) | EP1863467A2 (https=) |
| JP (1) | JP2008530101A (https=) |
| KR (1) | KR20070102544A (https=) |
| AR (1) | AR053809A1 (https=) |
| AU (1) | AU2006212772B2 (https=) |
| BR (1) | BRPI0606996A2 (https=) |
| CA (1) | CA2596485A1 (https=) |
| GT (1) | GT200600055A (https=) |
| IL (1) | IL184426A0 (https=) |
| MA (1) | MA29326B1 (https=) |
| MY (1) | MY146830A (https=) |
| NO (1) | NO20074509L (https=) |
| NZ (1) | NZ556275A (https=) |
| PE (1) | PE20060999A1 (https=) |
| TN (1) | TNSN07312A1 (https=) |
| TW (1) | TW200716081A (https=) |
| WO (1) | WO2006086456A2 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005294318A1 (en) * | 2004-10-08 | 2006-04-20 | Novartis Ag | Use of renin inhibitors for the prevention or treatment of diastolic dysfunction or diastolic heart failure |
| WO2007051007A2 (en) * | 2005-10-28 | 2007-05-03 | Novartis Ag | Combination of antihypertensives with cholesterol-lowering agent |
| AR057882A1 (es) * | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
| GB0612540D0 (en) * | 2006-06-23 | 2006-08-02 | Novartis Ag | Galenical formulations of organic compounds |
| KR101580067B1 (ko) | 2007-01-12 | 2015-12-23 | 노파르티스 아게 | 5-바이페닐-4-아미노-2-메틸 펜탄산의 제조 방법 |
| TW200838501A (en) * | 2007-02-02 | 2008-10-01 | Theravance Inc | Dual-acting antihypertensive agents |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| TWI406850B (zh) | 2007-06-05 | 2013-09-01 | Theravance Inc | 雙效苯并咪唑抗高血壓劑 |
| JP2010538071A (ja) | 2007-09-07 | 2010-12-09 | セラヴァンス， インコーポレーテッド | 二重作用性降圧剤 |
| KR20100076996A (ko) * | 2007-09-28 | 2010-07-06 | 노파르티스 아게 | 알리스키렌의 생약 제형 |
| TW200924737A (en) * | 2007-09-28 | 2009-06-16 | Novartis Ag | Galenical formulations of organic compounds |
| WO2009040427A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Galenical formulations of organic compounds |
| JP2011506459A (ja) | 2007-12-11 | 2011-03-03 | セラヴァンス， インコーポレーテッド | 抗高血圧剤としての二重作用性ベンゾイミダゾール誘導体およびその使用 |
| EP2297113A1 (en) | 2008-04-29 | 2011-03-23 | Theravance, Inc. | Dual-acting antihypertensive agents |
| WO2009143403A1 (en) * | 2008-05-23 | 2009-11-26 | Targacept, Inc. | Combination therapy for the management hypertension |
| US20100093603A1 (en) * | 2008-07-17 | 2010-04-15 | Kenneth Baker | Use of organic compounds |
| WO2010011821A2 (en) | 2008-07-24 | 2010-01-28 | Theravance, Inc. | Dual-acting antihypertensive agents |
| DE102008059206A1 (de) | 2008-11-27 | 2010-06-10 | Bayer Schering Pharma Aktiengesellschaft | Pharmazeutische Darreichungsform enthaltend Nifedipin oder Nisoldipin und einen Angiotensin-II Antagonisten und/oder ein Diuretikum |
| CN102361633A (zh) * | 2009-03-20 | 2012-02-22 | 诺瓦提斯公司 | 包含阿利吉仑的药物组合物 |
| CN103896796B (zh) | 2009-05-28 | 2016-04-27 | 诺华股份有限公司 | 作为脑啡肽酶抑制剂的取代的氨基丙酸衍生物 |
| EP2435402B1 (en) | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| EP2451782B1 (en) | 2009-07-07 | 2016-11-09 | Theravance Biopharma R&D IP, LLC | Dual-acting pyrazole antihypertensive agents |
| JP2012533626A (ja) | 2009-07-22 | 2012-12-27 | セラヴァンス， インコーポレーテッド | 二重作用オキサゾール降圧剤 |
| JO2967B1 (en) * | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| WO2011090929A1 (en) | 2010-01-19 | 2011-07-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| RU2588572C2 (ru) | 2010-08-23 | 2016-07-10 | Новартис Аг | Способ получения промежуточных соединений для получения ингибиторов nep |
| US8877815B2 (en) * | 2010-11-16 | 2014-11-04 | Novartis Ag | Substituted carbamoylcycloalkyl acetic acid derivatives as NEP |
| US8673974B2 (en) * | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| ES2879550T3 (es) * | 2012-08-24 | 2021-11-22 | Novartis Ag | Inhibidores de epn para tratar enfermedades caracterizadas por la dilatación o remodelación auriculares. |
| CU24330B1 (es) | 2013-02-14 | 2018-03-13 | Novartis Ag | Derivados del ácido 4-((1,1) bifenil-4-il)-3-(3-fosfonopropanamido) butanoico, activos como inhibidores de nep (endopeptidasa neutral) |
| US9102635B2 (en) | 2013-02-14 | 2015-08-11 | Novartis Ag | Substituted bisphenyl butanoic acid derivatives as NEP inhibitors with improved in vivo efficacy |
| CN105348209B (zh) | 2015-12-09 | 2017-12-26 | 浙江天宇药业股份有限公司 | 一种抗心衰药lcz696的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AU1256692A (en) * | 1991-02-06 | 1992-09-07 | Schering Corporation | Combination of an angiotensin II antagonist or renin inhibitor with a neutral endopeptidase inhibitor |
| US5217996A (en) * | 1992-01-22 | 1993-06-08 | Ciba-Geigy Corporation | Biaryl substituted 4-amino-butyric acid amides |
| DE19750529A1 (de) * | 1997-11-14 | 1999-05-20 | Basf Ag | Neue heterocyclisch substituierte alpha-Hydroxycarbonsäurederivate, ihre Herstellung und Verwendung als Endothelinrezeptorantagonisten |
| US6506785B2 (en) * | 1998-05-22 | 2003-01-14 | Pfizer, Inc. | Treating or preventing the early stages of degeneration of articular cartilage or subchondral bone in mammals using carprofen and derivatives |
| US8168616B1 (en) * | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
| US7468390B2 (en) * | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
| DK1467728T3 (da) * | 2002-01-17 | 2007-12-27 | Novartis Ag | Farmaceutiske sammensætninger indeholdende valsartan og NEP-inhibitorer |
| DK1507558T3 (da) * | 2002-05-17 | 2011-12-05 | Novartis Pharma Ag | Farmaceutisk sammensætning omfattende en renininhibitor, en calciumkanalblokker og et diuretikum |
| GB0212412D0 (en) * | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
| CL2004000545A1 (es) * | 2003-03-18 | 2005-01-28 | Pharmacia Corp Sa Organizada B | Uso de un antagonista de los receptores de aldosterona y un antagonista de receptores de endotelina para el tratamiento o profilaxis de una condicion patologica relacionada con hipertension, disfuncion renal, insulinopatia y enfermedades cardiovascul |
| CL2004000544A1 (es) * | 2003-03-18 | 2005-01-28 | Pharmacia Corp Sa Organizada B | Uso de una combinacion farmaceutica, de un antagonista del receptor de aldosterona y un inhibidor de endopeptidasa neutral, util para el tratamiento y prevencion de una condicion patologica relacionada con hipertension, disfuncion renal, insulinopati |
| US20040214804A1 (en) * | 2003-04-25 | 2004-10-28 | Pharmacia Corporation | Combination of an aldosterone receptor antagonist and an anti-obesity agent |
-
2006
- 2006-02-07 MY MYPI20060499A patent/MY146830A/en unknown
- 2006-02-09 EP EP06734563A patent/EP1863467A2/en not_active Withdrawn
- 2006-02-09 KR KR1020077018445A patent/KR20070102544A/ko not_active Ceased
- 2006-02-09 US US11/813,530 patent/US20080119557A1/en not_active Abandoned
- 2006-02-09 BR BRPI0606996-7A patent/BRPI0606996A2/pt not_active IP Right Cessation
- 2006-02-09 AR ARP060100468A patent/AR053809A1/es not_active Application Discontinuation
- 2006-02-09 AU AU2006212772A patent/AU2006212772B2/en not_active Ceased
- 2006-02-09 NZ NZ556275A patent/NZ556275A/en not_active IP Right Cessation
- 2006-02-09 JP JP2007555186A patent/JP2008530101A/ja active Pending
- 2006-02-09 PE PE2006000152A patent/PE20060999A1/es not_active Application Discontinuation
- 2006-02-09 WO PCT/US2006/004401 patent/WO2006086456A2/en not_active Ceased
- 2006-02-09 CA CA002596485A patent/CA2596485A1/en not_active Abandoned
- 2006-02-10 GT GT200600055A patent/GT200600055A/es unknown
- 2006-02-10 TW TW095104610A patent/TW200716081A/zh unknown
-
2007
- 2007-07-05 IL IL184426A patent/IL184426A0/en unknown
- 2007-08-10 TN TNP2007000312A patent/TNSN07312A1/en unknown
- 2007-09-06 NO NO20074509A patent/NO20074509L/no not_active Application Discontinuation
- 2007-09-10 MA MA30209A patent/MA29326B1/fr unknown
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