JP2008530101A5 - - Google Patents
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- 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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP1863467A2 (OSRAM) |
| JP (1) | JP2008530101A (OSRAM) |
| KR (1) | KR20070102544A (OSRAM) |
| AR (1) | AR053809A1 (OSRAM) |
| AU (1) | AU2006212772B2 (OSRAM) |
| BR (1) | BRPI0606996A2 (OSRAM) |
| CA (1) | CA2596485A1 (OSRAM) |
| GT (1) | GT200600055A (OSRAM) |
| IL (1) | IL184426A0 (OSRAM) |
| MA (1) | MA29326B1 (OSRAM) |
| MY (1) | MY146830A (OSRAM) |
| NO (1) | NO20074509L (OSRAM) |
| NZ (1) | NZ556275A (OSRAM) |
| PE (1) | PE20060999A1 (OSRAM) |
| TN (1) | TNSN07312A1 (OSRAM) |
| TW (1) | TW200716081A (OSRAM) |
| WO (1) | WO2006086456A2 (OSRAM) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101102755B (zh) * | 2004-10-08 | 2013-01-02 | 诺瓦提斯公司 | 肾素抑制剂在制备预防或治疗舒张功能障碍或舒张性心力衰竭的药物中的用途 |
| 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 |
| SG185318A1 (en) | 2007-01-12 | 2012-11-29 | Novartis Ag | Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid |
| 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 |
| EP2200975A1 (en) | 2007-09-07 | 2010-06-30 | Theravance, Inc. | Dual-acting antihypertensive agents |
| AR066168A1 (es) * | 2007-09-28 | 2009-07-29 | Novartis Ag | Formulaciones galenicas de compuestos organicos |
| WO2009040427A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Galenical formulations of organic compounds |
| MY148266A (en) * | 2007-09-28 | 2013-03-29 | Novartis Ag | Galenical formulations of aliskiren |
| EP2225210B1 (en) | 2007-12-11 | 2012-04-25 | Theravance, Inc. | Dual-acting benzoimidazole derivative and their use as antihypertensive agents |
| US7989484B2 (en) | 2008-04-29 | 2011-08-02 | Theravance, Inc. | Dual-acting antihypertensive agents |
| US8569381B2 (en) | 2008-05-23 | 2013-10-29 | Targacept, Inc. | Combination therapy for the management of hypertension |
| JP2010031006A (ja) * | 2008-07-17 | 2010-02-12 | Novartis Ag | 有機化合物の使用 |
| 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 |
| WO2010107966A1 (en) * | 2009-03-20 | 2010-09-23 | Novartis Ag | Pharmaceutical composition comprising aliskiren |
| BRPI1011657A2 (pt) | 2009-05-28 | 2019-04-16 | Novartis Ag | derivados aminopropiônicos substituídos como inibidores de neprilisina |
| 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 |
| US8372984B2 (en) | 2009-07-22 | 2013-02-12 | Theravance, Inc. | Dual-acting oxazole antihypertensive agents |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| EP2526095A1 (en) | 2010-01-19 | 2012-11-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| ES2576179T3 (es) | 2010-08-23 | 2016-07-06 | Novartis Ag | Proceso para la preparación de intermediarios para la elaboración de inhibidores de NEP |
| US8673974B2 (en) * | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| US8877815B2 (en) * | 2010-11-16 | 2014-11-04 | Novartis Ag | Substituted carbamoylcycloalkyl acetic acid derivatives as NEP |
| EP3943084A1 (en) * | 2012-08-24 | 2022-01-26 | Novartis AG | Nep inhibitors for treating diseases characterized by atrial enlargement or remodeling |
| KR20150119107A (ko) | 2013-02-14 | 2015-10-23 | 노파르티스 아게 | 개선된 생체내 효능을 갖는 nep 억제제로서의 치환된 비스페닐 부탄산 유도체 |
| SG11201506018PA (en) | 2013-02-14 | 2015-08-28 | Novartis Ag | Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors |
| 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 |
|---|---|---|---|---|
| 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 |
| ES2290429T3 (es) * | 2002-01-17 | 2008-02-16 | Novartis Ag | Composiciones farmaceuticas que comprenden valsartan e inhibidores de nep. |
| US7468390B2 (en) * | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
| NZ536555A (en) * | 2002-05-17 | 2007-03-30 | Novartis Ag | Pharmaceutical composition comprising a renin inhibitor, a calcium channel blocker and a diuretic |
| GB0212412D0 (en) * | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
| 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 |
| 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 |
| 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 AR ARP060100468A patent/AR053809A1/es not_active Application Discontinuation
- 2006-02-09 AU AU2006212772A patent/AU2006212772B2/en not_active Ceased
- 2006-02-09 PE PE2006000152A patent/PE20060999A1/es not_active Application Discontinuation
- 2006-02-09 BR BRPI0606996-7A patent/BRPI0606996A2/pt not_active IP Right Cessation
- 2006-02-09 KR KR1020077018445A patent/KR20070102544A/ko not_active Ceased
- 2006-02-09 CA CA002596485A patent/CA2596485A1/en not_active Abandoned
- 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 WO PCT/US2006/004401 patent/WO2006086456A2/en not_active Ceased
- 2006-02-09 US US11/813,530 patent/US20080119557A1/en not_active Abandoned
- 2006-02-09 EP EP06734563A patent/EP1863467A2/en not_active Withdrawn
- 2006-02-10 TW TW095104610A patent/TW200716081A/zh unknown
- 2006-02-10 GT GT200600055A patent/GT200600055A/es 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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