JP2015523980A5 - - Google Patents
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- JP2015523980A5 JP2015523980A5 JP2015515172A JP2015515172A JP2015523980A5 JP 2015523980 A5 JP2015523980 A5 JP 2015523980A5 JP 2015515172 A JP2015515172 A JP 2015515172A JP 2015515172 A JP2015515172 A JP 2015515172A JP 2015523980 A5 JP2015523980 A5 JP 2015523980A5
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- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- compound
- halo
- coor
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 61
- 125000000217 alkyl group Chemical group 0.000 claims description 56
- 125000002947 alkylene group Chemical group 0.000 claims description 22
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 239000003814 drug Substances 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- -1 2 -imidazolyl Chemical group 0.000 claims description 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 7
- 239000002792 enkephalinase inhibitor Substances 0.000 claims description 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 206010019280 Heart failures Diseases 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 208000017169 kidney disease Diseases 0.000 claims description 5
- 239000005541 ACE inhibitor Substances 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 4
- 108020001621 Natriuretic Peptide Proteins 0.000 claims description 4
- 102000004571 Natriuretic peptide Human genes 0.000 claims description 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 4
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims description 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000674 adrenergic antagonist Substances 0.000 claims description 4
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 4
- 239000003146 anticoagulant agent Substances 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 230000008878 coupling Effects 0.000 claims description 4
- 238000010168 coupling process Methods 0.000 claims description 4
- 238000005859 coupling reaction Methods 0.000 claims description 4
- 230000009977 dual effect Effects 0.000 claims description 4
- CHNUOJQWGUIOLD-NFZZJPOKSA-N epalrestat Chemical compound C=1C=CC=CC=1\C=C(/C)\C=C1/SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-NFZZJPOKSA-N 0.000 claims description 4
- NBVXSUQYWXRMNV-UHFFFAOYSA-N fluoromethane Chemical compound FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 claims description 4
- 239000003119 guanylate cyclase activator Substances 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 239000000692 natriuretic peptide Substances 0.000 claims description 4
- CTSLXHKWHWQRSH-UHFFFAOYSA-N oxalyl chloride Chemical compound ClC(=O)C(Cl)=O CTSLXHKWHWQRSH-UHFFFAOYSA-N 0.000 claims description 4
- 239000002464 receptor antagonist Substances 0.000 claims description 4
- 229940044551 receptor antagonist Drugs 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 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 claims description 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 2
- PRQUBDQDCAULSW-UHFFFAOYSA-N 2-(2h-triazol-4-yl)pyridine Chemical compound N1N=NC(C=2N=CC=CC=2)=C1 PRQUBDQDCAULSW-UHFFFAOYSA-N 0.000 claims description 2
- QZDDFQLIQRYMBV-UHFFFAOYSA-N 2-[3-nitro-2-(2-nitrophenyl)-4-oxochromen-8-yl]acetic acid Chemical compound OC(=O)CC1=CC=CC(C(C=2[N+]([O-])=O)=O)=C1OC=2C1=CC=CC=C1[N+]([O-])=O QZDDFQLIQRYMBV-UHFFFAOYSA-N 0.000 claims description 2
- MGADZUXDNSDTHW-UHFFFAOYSA-N 2H-pyran Chemical compound C1OC=CC=C1 MGADZUXDNSDTHW-UHFFFAOYSA-N 0.000 claims description 2
- 108010005094 Advanced Glycation End Products Proteins 0.000 claims description 2
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims description 2
- 102400000345 Angiotensin-2 Human genes 0.000 claims description 2
- 101800000733 Angiotensin-2 Proteins 0.000 claims description 2
- 102100030988 Angiotensin-converting enzyme Human genes 0.000 claims description 2
- 102100035765 Angiotensin-converting enzyme 2 Human genes 0.000 claims description 2
- 108090000975 Angiotensin-converting enzyme 2 Proteins 0.000 claims description 2
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims description 2
- 229940122155 Bradykinin receptor antagonist Drugs 0.000 claims description 2
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 2
- LTMHDMANZUZIPE-AMTYYWEZSA-N Digoxin Natural products O([C@H]1[C@H](C)O[C@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@](C)([C@H](O)C4)[C@H](C4=CC(=O)OC4)CC5)CC3)CC2)C[C@@H]1O)[C@H]1O[C@H](C)[C@@H](O[C@H]2O[C@@H](C)[C@H](O)[C@@H](O)C2)[C@@H](O)C1 LTMHDMANZUZIPE-AMTYYWEZSA-N 0.000 claims description 2
- 229940097420 Diuretic Drugs 0.000 claims description 2
- 229940122783 Endothelin converting-enzyme inhibitor Drugs 0.000 claims description 2
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims description 2
- 229940127406 Estrogen Receptor Agonists Drugs 0.000 claims description 2
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 2
- 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 description 2
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims description 2
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims description 2
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical class O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 2
- 102000003840 Opioid Receptors Human genes 0.000 claims description 2
- 108090000137 Opioid Receptors Proteins 0.000 claims description 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims description 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims description 2
- 229940127473 Prostaglandin Receptor Agonists Drugs 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 102000007637 Soluble Guanylyl Cyclase Human genes 0.000 claims description 2
- 108010007205 Soluble Guanylyl Cyclase Proteins 0.000 claims description 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 2
- 229940123445 Tricyclic antidepressant Drugs 0.000 claims description 2
- 239000012190 activator Substances 0.000 claims description 2
- 229940121359 adenosine receptor antagonist Drugs 0.000 claims description 2
- 239000000048 adrenergic agonist Substances 0.000 claims description 2
- 239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 claims description 2
- 239000000332 adrenergic beta-1 receptor antagonist Substances 0.000 claims description 2
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims description 2
- 239000002170 aldosterone antagonist Substances 0.000 claims description 2
- 229940083712 aldosterone antagonist Drugs 0.000 claims description 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 2
- 102000004305 alpha Adrenergic Receptors Human genes 0.000 claims description 2
- 108090000861 alpha Adrenergic Receptors Proteins 0.000 claims description 2
- 239000003098 androgen Substances 0.000 claims description 2
- 239000000400 angiotensin II type 1 receptor blocker Substances 0.000 claims description 2
- 229950006323 angiotensin ii Drugs 0.000 claims description 2
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 230000001142 anti-diarrhea Effects 0.000 claims description 2
- 229940127219 anticoagulant drug Drugs 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 229940125708 antidiabetic agent Drugs 0.000 claims description 2
- 239000003793 antidiarrheal agent Substances 0.000 claims description 2
- 229940125714 antidiarrheal agent Drugs 0.000 claims description 2
- 239000000030 antiglaucoma agent Substances 0.000 claims description 2
- 239000003965 antinociceptive agent Substances 0.000 claims description 2
- 229960004676 antithrombotic agent Drugs 0.000 claims description 2
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims description 2
- 239000012964 benzotriazole Substances 0.000 claims description 2
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims description 2
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims description 2
- 239000003152 bradykinin antagonist Substances 0.000 claims description 2
- 239000000480 calcium channel blocker Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- LTMHDMANZUZIPE-PUGKRICDSA-N digoxin Chemical compound C1[C@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O LTMHDMANZUZIPE-PUGKRICDSA-N 0.000 claims description 2
- 229960005156 digoxin Drugs 0.000 claims description 2
- LTMHDMANZUZIPE-UHFFFAOYSA-N digoxine Natural products C1C(O)C(O)C(C)OC1OC1C(C)OC(OC2C(OC(OC3CC4C(C5C(C6(CCC(C6(C)C(O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)CC2O)C)CC1O LTMHDMANZUZIPE-UHFFFAOYSA-N 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 230000001882 diuretic effect Effects 0.000 claims description 2
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002857 endothelin converting enzyme inhibitor Substances 0.000 claims description 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 2
- 239000000262 estrogen Substances 0.000 claims description 2
- 229940011871 estrogen Drugs 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 2
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims description 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 230000000407 monoamine reuptake Effects 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 229940035363 muscle relaxants Drugs 0.000 claims description 2
- 239000003158 myorelaxant agent Substances 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 239000002840 nitric oxide donor Substances 0.000 claims description 2
- 229910052757 nitrogen Chemical group 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims description 2
- 150000003180 prostaglandins Chemical class 0.000 claims description 2
- 239000000296 purinergic P1 receptor antagonist Substances 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000018 receptor agonist Substances 0.000 claims description 2
- 229940044601 receptor agonist Drugs 0.000 claims description 2
- 239000002461 renin inhibitor Substances 0.000 claims description 2
- 229940086526 renin-inhibitors Drugs 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 claims description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims description 2
- 239000003195 sodium channel blocking agent Substances 0.000 claims description 2
- 150000003536 tetrazoles Chemical class 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 229930192474 thiophene Natural products 0.000 claims description 2
- 150000003852 triazoles Chemical class 0.000 claims description 2
- 239000003029 tricyclic antidepressant agent Substances 0.000 claims description 2
- 229960005486 vaccine Drugs 0.000 claims description 2
- 239000002536 vasopressin receptor antagonist Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 3
- 125000003963 dichloro group Chemical group Cl* 0.000 claims 1
- 0 Cc1c(*)nn[n]1* Chemical compound Cc1c(*)nn[n]1* 0.000 description 5
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- XVNIYPMJNCBPTH-UHFFFAOYSA-N COc1n[o][n+]([O-])c1S(c1ccccc1)(=O)=O Chemical compound COc1n[o][n+]([O-])c1S(c1ccccc1)(=O)=O XVNIYPMJNCBPTH-UHFFFAOYSA-N 0.000 description 1
- VALUMXGSLBMNES-UHFFFAOYSA-N Cc1c(C)nn[nH]1 Chemical compound Cc1c(C)nn[nH]1 VALUMXGSLBMNES-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 102000003729 Neprilysin Human genes 0.000 description 1
- 108090000028 Neprilysin Proteins 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261653564P | 2012-05-31 | 2012-05-31 | |
| US61/653,564 | 2012-05-31 | ||
| PCT/US2013/043252 WO2013181332A1 (en) | 2012-05-31 | 2013-05-30 | Nitric oxide donor neprilysin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015523980A JP2015523980A (ja) | 2015-08-20 |
| JP2015523980A5 true JP2015523980A5 (enExample) | 2016-06-23 |
| JP6088047B2 JP6088047B2 (ja) | 2017-03-01 |
Family
ID=48577953
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015515172A Expired - Fee Related JP6088047B2 (ja) | 2012-05-31 | 2013-05-30 | 一酸化窒素ドナーであるネプリライシン阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9045443B2 (enExample) |
| EP (1) | EP2855464B1 (enExample) |
| JP (1) | JP6088047B2 (enExample) |
| CN (1) | CN104350052B (enExample) |
| CA (1) | CA2871292A1 (enExample) |
| ES (1) | ES2609810T3 (enExample) |
| WO (1) | WO2013181332A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2651896B1 (en) | 2010-12-15 | 2015-08-12 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| SG191175A1 (en) | 2010-12-15 | 2013-07-31 | Theravance Inc | Neprilysin inhibitors |
| CN103380119B (zh) | 2011-02-17 | 2016-02-17 | 施万生物制药研发Ip有限责任公司 | 作为脑啡肽酶抑制剂的经取代的氨基丁酸衍生物 |
| WO2012154249A1 (en) | 2011-02-17 | 2012-11-15 | Theravance, Inc. | Substituted aminobutyric derivatives as neprilysin inhibitors |
| CN103596928B (zh) | 2011-05-31 | 2017-02-15 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| ES2710932T3 (es) | 2012-06-08 | 2019-04-29 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina |
| BR112014030743B1 (pt) | 2012-06-08 | 2022-09-06 | Theravance Biopharma R&D Ip, Llc | Composto inibidor de neprilisina, processo para a preparação do referido composto, composição farmacêutica e uso do referido composto |
| KR102104954B1 (ko) | 2012-08-08 | 2020-04-27 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제 |
| HUE034210T2 (hu) | 2013-03-05 | 2018-02-28 | Theravance Biopharma R&D Ip Llc | Neprilizininhibitorok |
| MX2016009759A (es) | 2014-01-30 | 2016-11-17 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
| CA2934936A1 (en) | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| US10077287B2 (en) | 2014-11-10 | 2018-09-18 | Bristol-Myers Squibb Company | Tubulysin analogs and methods of making and use |
| MY187899A (en) | 2015-02-11 | 2021-10-27 | Theravance Biopharma R&D Ip Llc | (2s,4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor |
| LT3259255T (lt) | 2015-02-19 | 2021-04-26 | Theravance Biopharma R&D Ip, Llc | (2r,4r)-5-(5`-chlor-2`-fluorbifenil-4-il)-2-hidroksi-4-[(5-metiloksazol-2-karbonil)amino]pentano rūgštis |
| KR20220035991A (ko) | 2016-03-08 | 2022-03-22 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | (2s,4r)-5-(5'-클로로-2'-플루오로-[1,1'-비페닐]-4-일)-2-(에톡시메틸)-4-(3-히드록시이속사졸-5-카르복사미도)-2-메틸펜탄산 결정 및 그 용도 |
| UY38072A (es) | 2018-02-07 | 2019-10-01 | Novartis Ag | Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos |
Family Cites Families (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4189604A (en) | 1975-07-22 | 1980-02-19 | Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai | Bestatin |
| US4206232A (en) | 1976-05-10 | 1980-06-03 | E. R. Squibb & Sons, Inc. | Relieving hypertension with carboxyalkylacylamino acids |
| IL58849A (en) | 1978-12-11 | 1983-03-31 | Merck & Co Inc | Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them |
| FR2480747A1 (fr) | 1980-04-17 | 1981-10-23 | Roques Bernard | Derives d'acides amines et leur application therapeutique |
| US4906615A (en) | 1980-12-18 | 1990-03-06 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
| CN1008092B (zh) * | 1983-10-03 | 1990-05-23 | E·R·斯奎布父子公司 | 脑啡肽酶抑制剂的制备方法 |
| US4722810A (en) | 1984-08-16 | 1988-02-02 | E. R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| US4939261A (en) | 1984-06-08 | 1990-07-03 | Ciba-Geigy Corporation | N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase |
| EP0225292A3 (en) | 1985-12-06 | 1988-11-30 | Ciba-Geigy Ag | Certain n-substituted butyramide derivatives |
| US4929641B1 (en) | 1988-05-11 | 1994-08-30 | Schering Corp | Mercapto-acylamino acid antihypertensives |
| KR880007441A (ko) | 1986-12-11 | 1988-08-27 | 알렌 제이.스피겔 | 스피로-치환된 글루타르아미드 이뇨제 |
| FR2623498B1 (fr) | 1987-11-24 | 1990-04-06 | Bioprojet Soc Civ | Nouveaux composes enantiomeres derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques |
| GB8820844D0 (en) | 1988-09-05 | 1988-10-05 | Pfizer Ltd | Therapeutic agents |
| US5599951A (en) | 1989-09-15 | 1997-02-04 | Societe Civile Bioprojet | Amino acid derivatives, the process for their preparation and their applications to therapy |
| US5294632A (en) | 1991-05-01 | 1994-03-15 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipetide derivatives |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| US5217996A (en) | 1992-01-22 | 1993-06-08 | Ciba-Geigy Corporation | Biaryl substituted 4-amino-butyric acid amides |
| US5508272A (en) | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| AU691243B2 (en) * | 1994-02-14 | 1998-05-14 | Aventisub Ii Inc. | Novel mercaptoacetylamido 1,3,4,5-tetrahydro-benzo(c)azepin-3-one disulfide derivatives useful as inhibitors of enkephalinase and ace |
| DE19510566A1 (de) | 1995-03-23 | 1996-09-26 | Kali Chemie Pharma Gmbh | Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| JPH11505522A (ja) | 1995-04-21 | 1999-05-21 | ノバルティス・アクチエンゲゼルシャフト | エンドセリン阻害剤としてのｎ−アロイルアミノ酸アミド |
| US6660756B2 (en) | 2001-03-28 | 2003-12-09 | Pfizer Inc. | N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase |
| GB0119305D0 (en) | 2001-04-12 | 2001-10-03 | Aventis Pharma Gmbh | Mercaptoacetylamide derivatives,a process for their preparation and their use |
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| WO2006091716A2 (en) | 2005-02-24 | 2006-08-31 | Nitromed, Inc. | Nitric oxide enhancing diuretic compounds, compositions and methods of use |
| WO2007055873A2 (en) * | 2005-11-04 | 2007-05-18 | Avanir Pharmaceuticals | Process for the manufacture of peptide facilitators of reverse cholesterol transport |
| 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 |
| US7799784B2 (en) | 2006-02-06 | 2010-09-21 | Nicox S.A. | Quinoxaline derivatives of alpha-2 adrenergic agonists |
| WO2007106708A2 (en) | 2006-03-10 | 2007-09-20 | Novartis Ag | Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril |
| PT2121578T (pt) | 2007-01-12 | 2016-11-14 | Novartis Ag | Processo de preparação de ácido 5-bifenil-4-amino-2-metil-pentanoico |
| EP2125695B1 (en) | 2007-02-05 | 2016-10-26 | Nicox Science Ireland | Nitric oxide donor compounds |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| WO2009049961A2 (en) | 2007-10-19 | 2009-04-23 | Nicox S.A. | New no-donor aspirin derivatives |
| PE20091364A1 (es) | 2008-01-17 | 2009-10-13 | Novartis Ag | Proceso para la preparacion de inhibidores de nep |
| CA2712695A1 (en) | 2008-02-26 | 2009-09-03 | Nicoletta Almirante | New angiotensin ii receptor blocker derivatives |
| AR076731A1 (es) | 2008-05-09 | 2011-07-06 | Pfizer | Prostamidas donadoras de oxido nitrico, uso de los mismos y composiciones farmaceuticas |
| WO2010015447A1 (en) | 2008-08-08 | 2010-02-11 | Nicox S.A. | Angiotensin ii receptor antagonists |
| JP5420761B2 (ja) * | 2009-05-28 | 2014-02-19 | ノバルティス アーゲー | ネプリリシン阻害剤としての置換アミノプロピオン酸誘導体 |
| KR20120041702A (ko) | 2009-05-28 | 2012-05-02 | 노파르티스 아게 | 네프릴리신 억제제로서의 치환된 아미노부티르산 유도체 |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| HRP20151061T1 (hr) | 2010-01-22 | 2015-12-04 | Novartis Ag | Posrednici inhibitora neutralne endopeptidaze i postupak njihove pripreme |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
| SG191175A1 (en) | 2010-12-15 | 2013-07-31 | Theravance Inc | Neprilysin inhibitors |
| EP2651896B1 (en) * | 2010-12-15 | 2015-08-12 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| CN103380119B (zh) * | 2011-02-17 | 2016-02-17 | 施万生物制药研发Ip有限责任公司 | 作为脑啡肽酶抑制剂的经取代的氨基丁酸衍生物 |
| WO2012154249A1 (en) | 2011-02-17 | 2012-11-15 | Theravance, Inc. | Substituted aminobutyric derivatives as neprilysin inhibitors |
| CA2835281A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| CN103596928B (zh) | 2011-05-31 | 2017-02-15 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| US9499487B2 (en) | 2011-05-31 | 2016-11-22 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
-
2013
- 2013-05-30 CA CA2871292A patent/CA2871292A1/en not_active Abandoned
- 2013-05-30 US US13/905,338 patent/US9045443B2/en active Active
- 2013-05-30 ES ES13727784.4T patent/ES2609810T3/es active Active
- 2013-05-30 EP EP13727784.4A patent/EP2855464B1/en active Active
- 2013-05-30 CN CN201380028465.1A patent/CN104350052B/zh not_active Expired - Fee Related
- 2013-05-30 WO PCT/US2013/043252 patent/WO2013181332A1/en not_active Ceased
- 2013-05-30 JP JP2015515172A patent/JP6088047B2/ja not_active Expired - Fee Related
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