HRP20140691T1 - Supstituirani derivati karbamoilmetilamino octene kiseline kao novi nep-inhibitori - Google Patents
Supstituirani derivati karbamoilmetilamino octene kiseline kao novi nep-inhibitori Download PDFInfo
- Publication number
- HRP20140691T1 HRP20140691T1 HRP20140691AT HRP20140691T HRP20140691T1 HR P20140691 T1 HRP20140691 T1 HR P20140691T1 HR P20140691A T HRP20140691A T HR P20140691AT HR P20140691 T HRP20140691 T HR P20140691T HR P20140691 T1 HRP20140691 T1 HR P20140691T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound according
- hydroxy
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title claims 2
- AWEZYTUWDZADKR-UHFFFAOYSA-N 2-[(2-amino-2-oxoethyl)azaniumyl]acetate Chemical class NC(=O)CNCC(O)=O AWEZYTUWDZADKR-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 208000001647 Renal Insufficiency Diseases 0.000 claims 3
- -1 benzyloxy, hydroxy Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 201000006370 kidney failure Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 208000010496 Heart Arrest Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 2
- 208000030761 polycystic kidney disease Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 150000003536 tetrazoles Chemical class 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- XRNSYNJTRANIJE-SJCJKPOMSA-N (2s)-2-[[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-[(1-methyltetrazol-5-yl)amino]-1-oxopropan-2-yl]amino]propanoic acid Chemical compound C([C@H](N[C@@H](C)C(O)=O)C(=O)NC=1N(N=NN=1)C)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 XRNSYNJTRANIJE-SJCJKPOMSA-N 0.000 claims 1
- LATSUHPVCHACDZ-IRXDYDNUSA-N (2s)-2-[[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-oxo-1-(2h-tetrazol-5-ylamino)propan-2-yl]amino]-3-methoxypropanoic acid Chemical compound C([C@H](N[C@@H](COC)C(O)=O)C(=O)NC=1NN=NN=1)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 LATSUHPVCHACDZ-IRXDYDNUSA-N 0.000 claims 1
- SDRHPEXZXZNXLX-ZBEGNZNMSA-N (2s)-2-[[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-oxo-1-(2h-tetrazol-5-ylamino)propan-2-yl]amino]propanoic acid Chemical compound C([C@H](N[C@@H](C)C(O)=O)C(=O)NC=1NN=NN=1)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 SDRHPEXZXZNXLX-ZBEGNZNMSA-N 0.000 claims 1
- WTZARVQRNNDSGI-SJCJKPOMSA-N (2s)-2-[[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-oxo-1-[(3-oxo-1,2-oxazol-5-yl)amino]propan-2-yl]amino]propanoic acid Chemical compound C([C@H](N[C@@H](C)C(O)=O)C(=O)NC=1ON=C(O)C=1)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 WTZARVQRNNDSGI-SJCJKPOMSA-N 0.000 claims 1
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 239000005541 ACE inhibitor Substances 0.000 claims 1
- 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 claims 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 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 102000015427 Angiotensins Human genes 0.000 claims 1
- 108010064733 Angiotensins Proteins 0.000 claims 1
- 206010003445 Ascites Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003662 Atrial flutter Diseases 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010052337 Diastolic dysfunction Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010048554 Endothelial dysfunction Diseases 0.000 claims 1
- 206010057671 Female sexual dysfunction Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010020571 Hyperaldosteronism Diseases 0.000 claims 1
- 206010020590 Hypercalciuria Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 claims 1
- 206010057672 Male sexual dysfunction Diseases 0.000 claims 1
- 208000019255 Menstrual disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 1
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 229910003827 NRaRb Inorganic materials 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 102000003729 Neprilysin Human genes 0.000 claims 1
- 108090000028 Neprilysin Proteins 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 208000005107 Premature Birth Diseases 0.000 claims 1
- 206010036590 Premature baby Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 229940123934 Reductase inhibitor Drugs 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010042600 Supraventricular arrhythmias Diseases 0.000 claims 1
- 206010042957 Systolic hypertension Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 229960002478 aldosterone Drugs 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000001627 detrimental effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 201000000523 end stage renal failure Diseases 0.000 claims 1
- 230000008694 endothelial dysfunction Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- RBFYWBHUGPWSSJ-UGSOOPFHSA-N ethyl (2s)-2-[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-oxo-1-(2h-tetrazol-5-ylamino)propan-2-yl]oxypropanoate Chemical compound C([C@H](O[C@@H](C)C(=O)OCC)C(=O)NC=1NN=NN=1)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 RBFYWBHUGPWSSJ-UGSOOPFHSA-N 0.000 claims 1
- SAPRXCUXOWRKQA-UGSOOPFHSA-N ethyl (2s)-2-[[(2s)-3-[4-(3-chlorophenyl)phenyl]-1-oxo-1-(2h-tetrazol-5-ylamino)propan-2-yl]amino]propanoate Chemical compound C([C@H](N[C@@H](C)C(=O)OCC)C(=O)NC=1NN=NN=1)C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 SAPRXCUXOWRKQA-UGSOOPFHSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000027119 gastric acid secretion Effects 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 206010020871 hypertrophic cardiomyopathy Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000001797 obstructive sleep apnea Diseases 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 239000003087 receptor blocking agent Substances 0.000 claims 1
- 238000007634 remodeling Methods 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 230000001850 reproductive effect Effects 0.000 claims 1
- 208000015658 resistant hypertension Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 230000006641 stabilisation Effects 0.000 claims 1
- 238000011105 stabilization Methods 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 210000005166 vasculature Anatomy 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
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Claims (14)
1. Spoj, naznačen time, da ima formulu (III):
[image]
u kojoj:
X1 je OH, -O-C1-7-alkil, -NRaRb, -NHS(O)2-C1-7-alkil ili -NHS(O)2-benzil, gdje su Ra i Rb svaki puta kad se pojave, neovisno H ili C1-7-alkil;
R1 je C1-6-alkil ili C6-10-aril-C1-6alkil, pri čemu je alkil opcijski supstituiran s benziloksi, hidroksi ili C1-6-alkoksi;
svaki puta kad se pojavi, R2 je neovisno C1-6-alkoksi, hidroksi, halogen, C1-6-alkil, cijano ili trifluorometil;
R4 i R5 su neovisno H ili C1-6-alkil;
A1 je veza ili C1-3-alkilen-lanac;
R3 je 5- ili 6-člani heteroaril, C6-10-aril ili C3-7-cikloalkil, gdje je svaki heteroaril, aril ili cikloalkil opcijski supstituiran s jednom ili više skupina neovisno odabranih iz skupine koju čine: C1-6-alkil, halogen, halo-C1-6-alkil, C1-6-alkoksi, hidroksi, CO2H i CO2C1-6-alkil;
R6 je, svaki puta kad se pojavi, neovisno halogen, hidroksi, C1-7-alkoksi, halo-C1-7-alkil ili halo-C1-7-alkil; ili
R4, A1-R3, zajedno s dušikom na kojega su R4 i A1-R3 priključeni, tvore 4- do 7-člani heterociklil ili 5- do 6- člani heteroaril, od kojih je svaki opcijski supstituiran s jednom ili više skupina neovisno odabranih iz skupine koju čine: C1-6-alkil,halogen, halo-C1-6-alkil, C1-6-alkoksi, hidroksi, CO2H i CO2C1-6-alkil; i
m je 0 ili cijeli broj od 1 do 5;
s je 0 ili cijeli broj od 1 do 4;
X2 je halogen; i
p je 0 ili cijeli broj od 1 do 4;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, naznačen time, da ima formulu IV:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time, da
X1 predstavlja OH ili O-C1-6-alkil;
R1 je C1-6-alkil;
R2 je, za svako pojavljivanje, neovisno C1-6-alkoksi, hidroksi, halogen, C1-6-alkil, cijano ili trifluorometil;
R4 i R5 su neovisno H ili C1-6-alkil;
A1 je veza ili C1-3-alkilen-lanac;
R3 je 5- ili 6-člani heteroaril opcijski supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine: C1-6-alkil, halogen, halo-C1-6-alkil, C1-6-alkoksi, hidroksi, CO2H i CO2C1-6-alkil;
R6 je, za svako pojavljivanje, neovisno halogen, hidroksi, C1-7-alkoksi, halo-C1-7-alkil ili halo-C1-7-alkil;
m je 0 ili cijeli broj od 1 do 5;
s je 0 ili cijeli broj od 1 do 4;
X2 je halogen; i
p je 0 ili cijeli broj od 1 do 4;
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da
A1 je veza ili CH2;
li njegova farmaceutski prihvatljiva sol.
5. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da
R1 je metil ili etil;
R5 i R4 su H;
ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da
R3 je 5-člani heteroaril-prsten odabran iz skupine koju čine: oksazol, pirol, pirazol, izooksazol, triazol, tetrazol, oksadiazol, tiazol, izotiazol, tiofen, imidazol i tiadiazol; od kojih je svaki opcijski supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine: C1-6-alkil, halogen, halo-C1-6-alkil, C1-6-alkoksi, hidroksi, CO2H i CO2C1-6-alkil;
ili njegova farmaceutski prihvatljiva sol.
7. Spojevi prema bilo kojem od prethodnih zahtjeva, naznačeni time, da
R3 je tetrazol;
ili njegova farmaceutski prihvatljiva sol.
8. Spojevi prema bilo kojem od prethodnih zahtjeva, naznačeni time, da
X2 je Cl,
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je odabran između sljedećih:
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(1H-tetrazol-5-ilkarbamoil)-etilamino]-propionska kiselina-etil ester;
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(1H-tetrazol-5-ilkarbamoil)-etoksi]-propionska kiselina etil ester;
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(1H-tetrazol-5-ilkarbamoil)-etilamino]-propionska kiselina;
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(3-hidroksi-izoksazol-5-ilkarbamoil)-etilamino]-propionska kiselina;
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(1-metil-1H-tetrazol-5-ilkarbamoil)-etilamino]-propionska kiselina; i
(S)-2-[(S)-2-(3’-kloro-bifenil-4-il)-1-(1H-tetrazol-5-ilkarbamoil)-etilamino]-3-metoksi-propionska kiselina;
ili njegova farmaceutski prihvatljiva sol.
10. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od prethodnih zahtjeva ili njegovu farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih nosača.
11. Kombinacija, naznačena time, da obuhvaća spoj prema bilo kojem zahtjevu od 1 do 9 ili njegovu farmaceutski prihvatljivu sol i jedan ili više terapeutski djelotvornih sredstava odabranih između sljedećih: inhibitor reduktaze HMG-Co-A, blokator receptora angiotenzina, inhibitor enzima koji pretvara angiotenzin, blokator kanala kalcija, antagonist endotelina, inhibitor renina, diuretik, ApoA-I-mimetik, anti-dijabetičko sredstvo, sredstvo za redukciju pretilosti, blokator receptora aldosterona, blokator receptora endotelina, inhibitor sinteze aldosterona, CETP-inhibitor ili inhibitor fosfodiesteraze tipa 5 (PDE5-inhibitor).
12. Spoj prema bilo kojem zahtjevu od 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen(a) time, da se upotrebljava kao lijek.
13. Spoj prema bilo kojem zahtjevu od 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen(a) time, da se upotrebljava za liječenje poremećaja ili bolesti povezanih s djelovanjem neutralne endopeptidaze EC.3.4.24.11. kod pojedinca kojemu je potrebno takvo liječenje.
14. Spoj prema bilo kojem zahtjevu od 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen(a) time, da se upotrebljava za liječenje poremećaja ili bolesti odabranih između sljedećih: hipertenzija, rezistentna hipertenzija, pulmonarna hipertenzija, pulmonarna arterijska hipertenzija, izolirana sistolička hipertenzija, periferna vaskularna bolest, srčani zastoj, kongestivni srčani zastoj, lijeva ventrikularna hipertrofija, angina, renalna insuficijencija, renalni zastoj, dijabetička nefropatija, ne-dijabetička nefropatija, nefrotski sindrom, glomerulonefritis, skleroderma, glomerularna skleroza, proteinurea u primarnoj bolesti bubrega, renalna vaskularna hipertenzija, dijabetička retinopatija i zadnji stadij bolesti bubrega (ESRD), endotelijalna disfunkcija, dijastolička disfunkcija, hipertrofijska kardiomiopatija, dijabetička kardijska miopatija, supraventrikularne i ventrikularne aritmije, atrijska fibrilacija (AF), kardijska fibroza, atrijsko podrhtavanje, detrimentalno vaskularno remodeliranje, koronarna stabilizacija plaka, infarkt miokarda (MI), renalna fibroza, bolest policističnih bubrega (PKD), renalni zastoj, ciklički edem, Menièresova bolest, hiperaldosteronizam, hiperkalciuria, ascites, glaukom, menstrualni poremećaji, preuranjeni porod, predeklampsija, endometrioza i reproduktivni poremećaji, astma, opstrukcijska apneja kod spavanja, upale, leukemija, bolovi, epilepsija, efektivni poremećaji, depresija, psihotička stanja, demencija, gerijatrijska konfuzija, pretilost, gastrointestinalni poremećaji, zacjeljivanje rana, septički šok, disfunkcija sekrecije gastričke kiseline, hiperreninemija, cistična fibroza, restenoza, dijabetes tipa 2, metabolički sindrom, dijabetičke komplikacije, ateroskleroza, muška i ženska seksualna disfunkcija.
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