SI2956464T1 - Substituirani derivati bisfenil butanojske fosfonske kisline kot inhibitorji NEP (nevtralne endopeptidaze) - Google Patents
Substituirani derivati bisfenil butanojske fosfonske kisline kot inhibitorji NEP (nevtralne endopeptidaze) Download PDFInfo
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- SI2956464T1 SI2956464T1 SI201430761T SI201430761T SI2956464T1 SI 2956464 T1 SI2956464 T1 SI 2956464T1 SI 201430761 T SI201430761 T SI 201430761T SI 201430761 T SI201430761 T SI 201430761T SI 2956464 T1 SI2956464 T1 SI 2956464T1
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- alkyl
- pharmaceutically acceptable
- acceptable salt
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- 102000003729 Neprilysin Human genes 0.000 title claims 4
- 108090000028 Neprilysin Proteins 0.000 title claims 4
- 239000003112 inhibitor Substances 0.000 title claims 3
- 229940042400 direct acting antivirals phosphonic acid derivative Drugs 0.000 title claims 2
- 150000003007 phosphonic acid derivatives Chemical class 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 150000003839 salts Chemical class 0.000 claims abstract 19
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 230000001225 therapeutic effect Effects 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- -1 5-chloro-2'-fluoro- [1,1'-biphenyl] -4-yl Chemical group 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 208000001647 Renal Insufficiency Diseases 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 3
- 201000006370 kidney failure Diseases 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 2
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 2
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 2
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 2
- 206010042957 Systolic hypertension Diseases 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
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 2
- 208000030761 polycystic kidney disease Diseases 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 208000015658 resistant hypertension Diseases 0.000 claims 2
- TWKJROJSAYIJLA-OAHLLOKOSA-N (3r)-4-[4-(5-chloro-2-fluorophenyl)phenyl]-3-(3-phosphonopropanoylamino)butanoic acid Chemical compound C1=CC(C[C@H](CC(=O)O)NC(=O)CCP(O)(O)=O)=CC=C1C1=CC(Cl)=CC=C1F TWKJROJSAYIJLA-OAHLLOKOSA-N 0.000 claims 1
- 239000005541 ACE inhibitor Substances 0.000 claims 1
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims 1
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 1
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 1
- 206010003445 Ascites Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims 1
- 108090000312 Calcium Channels Proteins 0.000 claims 1
- 102000003922 Calcium Channels Human genes 0.000 claims 1
- 229910016523 CuKa Inorganic materials 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
- 208000032781 Diabetic cardiomyopathy 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
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000002193 Pain 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
- 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
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 239000002981 blocking agent Substances 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 239000003638 chemical reducing agent 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
- 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
- 230000000694 effects 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
- 239000012530 fluid Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 206010020871 hypertrophic cardiomyopathy Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
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- 208000001797 obstructive sleep apnea Diseases 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 1
- 239000003087 receptor blocking agent Substances 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
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
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- 230000029663 wound healing Effects 0.000 claims 1
- 239000013543 active substance Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
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- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
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Claims (19)
- Substituirani derivati bisfenil butanojske fosfonske kisline kot inhibitorji NEP (nevtralne endopeptidaze) Patentni zahtevki1. Spojina s formulo (I): kjer:R1 je H; -Ci_7alkil ali C6_i0aril; kjer je alkil po izbiri substituiran z enim ali več substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo -O-C(O)-O-C3.7cikloalkil, -O-C(O)-C3.7cikloalkil, -O-C(O)-C6.i0aril, -O-C(O)-O-C6.10aril, -O-C(O)-O-Ci_7alkil, -O-C(O)-Ci.7alkil, heteroaril, heterociklil, -C(O)-heterociklil, -C(O)NH2, -C(O)NH-C!.7alkil in -C(O)N(Ci.7alkil)2; kjer je C3.7-cikloalkil nasičena ali nenasičena, vendar nearomatska monocikliČna, biciklična ali triciklična C3.7-ogljikovodikova skupina, R2 je Cl, CH3 ali F; R3 je H, F, Cl, CH3 ali OCH3, ali njena farmacevtsko sprejemljiva sol.
- 2. Spojina po zahtevku 1 s formulo II:kjer: R1 je H; -Ci_7alkil ali C6_i0aril; kjer je alkil po izbiri substituiran z enim ali več substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo -O-C(O)-O-C3.7cikloalkil, -O-C(O)-C3.7cikloalkil, -O-C(O)-C6.10aril, -O-C(O)-0-C6.ioaril> -O-C(O)-O-Ci.7alkil, -O-C(O)-Ci.7alkil, heteroaril, heterociklil, -C(O)-heterociklil, -C(O)NH2, -C(O)NH-C!.7alkil in -C(O)N(C1.7alkil)2; kjer je C3.7cikloalkil nasičena ali nenasičena, vendar nearomatska monociklična, biciklična ali triciklična C3.7-ogljikovodikova skupina, R2jeCl, CH3aliF; R3je H, F, Cl, CH3 ali OCH3, ali njena farmacevtsko sprejemljiva sol.
- 3. Spojina po zahtevku 1 ali 2, kjer R2 pomeni Cl in R3 pomeni F; ali njena farmacevtsko sprejemljiva sol.
- 4. Spojina po zahtevku 1, 2 ali 3, ki ima formulo III:ali njena farmacevtsko sprejemljiva sol.
- 5. Spojina po katerem koli od zahtevkov 1-4, ki ima formulo IV:ali njena farmacevtsko sprejemljiva sol.
- 6. Spojina po zahtevku 1, 2 ali 3, kjer R1 pomeni -C^alkil ali C6.i0aril; kjer je alkil po izbiri substituiran z enim ali več substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo -O-C(O)-O-C3.7cikloalkil, -O-C(O)-C3.7cikloalkil, -O-C(O)-C6.i0aril> -0-C(0)-0-C6_ioaril, -O-C(O)-O-Ci.7alkil, -O-C(O)-Ci_7alkil, heteroaril, heterociklil, -C(O)-heterociklil, -C(O)NH2, -C(O)NH-Ci.7alkil in -C(O)N(Ci.7alkil)2;kjer je C3_7cikloalkil nasičena ali nenasičena, vendar nearomatska monocikliČna, biciklična ali triciklična C3.7-ogljikovodikova skupina, ali njena farmacevtsko sprejemljiva sol.
- 7. Spojina po zahtevku 1, 2 ali 3, kjer R1 pomeni -Ci.4alkil ali je R1 izbran izmed naslednjih skupin:kjer sta Ra in Re neodvisno izbrana izmed H in Ci.4alkila in Rb pomeni Ci_4alkil; ali njena farmacevtsko sprejemljiva sol.
- 8. Spojina po zahtevku 1, 2 ali 3, kjer R1 pomeni -CMalkil, kjer je alkil po izbiri substituiran z enim ali več substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo -C(O)NH2, -C(O)NH-C1.7alkil in -C(O)N(C1.7alkil)2; ali njena farmacevtsko sprejemljiva sol.
- 9. Spojina po zahtevku 1, 2 ali 3, kjer R1 pomeni Me, Et ali je izbran iz skupine naslednjih formul:inc kjer R pomeni H ali Ci_4alkil in R pomeni Ci_4alkil; ali njena farmacevtsko sprejemljiva sol.
- 10. Spojina po zahtevku 1, 2 ali 3, kjer R1 pomeni Me, Et ali je izbran iz skupine naslednjih formul:ali njena farmacevtsko sprejemljiva sol.
- 11. Spojina po zahtevku 1, ki je (R)-4-(5’-kloro-2’-fluoro-[l,l’-bifenil]-4-il)-3-(3-fosfonopropanamido)butanojska kislina ali njena farmacevtsko sprejemljiva sol.
- 12. Spojina po zahtevku 1, kije (3-(((2R)-l-(5’-kloro-2’-fluoro-[l,l’-bifenil]-4-il)-4-(l-(((cikloheksiloksi)karbonil)oksi)etoksi)-4-oksobutan-2-il)amino)-3-oksopropil)fosfonska kislina ali njena farmacevtsko sprejemljiva sol.
- 13. Spojina po zahtevku 1, kije (3-(((R)-l-(5’-kloro-2’-fluoro-[l,l’-bifenil]-4-il)-4-((S)-l-(((cikloheksiloksi)karbonil)oksi)etoksi)-4-oksobutan-2-il)amino)-3-oksopropil)fosfonska kislina ali njena farmacevtsko sprejemljiva sol.
- 14. Kristalinična oblika A proste kisline spojine po zahtevku 1, ki je (3-(((R)-l-(5’-kloro-2 ’ -fluoro-[ 1,1’ -bi fenil] -4-il)-4-((S)-1 -(((cikloheksiloksi)karbonil)oksi)etoksi)-4-oksobutan-2-il)amino)-3-oksopropil)fosfonska kislina, označena z rentgenskim praškovnim diffakcijskim vzorcem, ki obsega štiri ali več vrednosti 2Θ (CuKa λ = 1,5418 A), izbranih iz skupine, ki jo sestavljajo 16,5° ± 0,2°, 17,5° ± 0,2°, 17,8° ± 0,2°, 18,7° ± 0,2°, 20,2° ± 0,2°, 20,7° ± 0,2°, 21,7° ± 0,2°, 21,9° ± 0,2°, 24,1° ± 0,2°, 24,6° ± 0,2°, 25,0° ± 0,2°, 25,5° ± 0,2° in 27,4° ± 0,2°, izmerjenih pri temperaturi približno 22 °C in rentgenski valovni dolžini λ = 1,5418 A.
- 15. Farmacevtski sestavek, ki obsega spojino po katerem koli od zahtevkov 1-14 ali njeno farmacevtsko sprejemljivo sol in en ali več farmacevtsko sprejmljivih nosilcev.
- 16. Kombinacija, ki obsega: spojino po katerem koli od zahtevkov 1-14 ali njeno farmacevtsko sprejemljivo sol in eno ali več terapevtskih učinkovin, izbranih izmed inhibitorja HMG-Co-A reduktaze, blokatorja anigiotenzinskega receptorja, inhibitorja encima, ki pretvarja angiotenzin, blokatorja kalcijevega kanalčka, endotelinskega antagonista, reninskega inhibitorja, diuretika, ApoA-I mimetika, antidiabetičnega sredstva, sredstva za zmanjševanje debelosti, blokatorja aldosteronskega receptorja, blokatorja endotelinskega receptorja, inhibitorja aldosteron sintaze, CETP inhibitorja in inhibitorja fosfodiesteraze tipa 5 (PDE5).
- 17. Spojina po katerem koli od zahtevkov 1-14 ali njena farmacevtsko sprejemljiva sol za uporabo kot zdravilo.
- 18. Spojina po katerem koli od zahtevkov 1-14 ali njena farmacevtsko sprejemljiva sol za uporabo pri zdravljenu motnje ali bolezni, povezane z aktivnostjo nevtralne endopeptidaze in izbrane iz skupine, ki jo sestavljajo hipertenzija, rezistentna hipertenzija, pljučna hipertenzija, pljučna arterijska hipertenzija, izolirana sistolična hipertenzija, periferna vaskulama bolezen, srčna insuficienca, kongestivna srčna insuficienca, leva ventrikulama hipertrofija, angina, renalna insuficienca, renalna odpoved, diabetična nefropatija, nediabetična nefropatija, kontrastna nefropatija, neffotični sindrom, glomerulonefritis, skleroderma, glomerulama skleroza, proteinurija primarne renalne bolezni, renalna vaskulama hipertenzija, diabetična retinopatija in renalna bolezen v končnem stadiju (ESRD), endotelijska disfunkcija, diastolična disfunkcija, hipertrofična kardiomiopatija, diabetična kardiomiopatija, supraventrikulame in ventrikulame aritmije, atrijska fibrilacija (AF), srčna fibroza, atrijkso plapolanje, detrimentalno vaskulamo remodeliranje, stabilizacija plakov, miokardni infarkt (MI), renalna fibroza, bolezen policističnih ledvic (PKD), renalna odpove, ciklični edem, Menierova bolezen, hiperaldosteronizem, hiperkalciurija, ascites, glavkom, menstrualne motnje, prezgodnji porod, preeklampsija, endometrioza in reproduktivne motnje, astma, obstruktivna apneja v spanju, vnetje, levkemija, bolečina, epilepsija, afektivne motnje, depresija, psihotično stanje, demenca, geriatrična konfuzija, debelost, gastrointestinalne motnje, celjenje ran, septični šok, disfunkcija izločanja želodčne tekočine, hiperreninemija, cistična fibroza, restenoza, diabetes tipa 2, metabolični sindrom, diabetični zapleti, ateroskleroza in moška ter ženska spolna disfunkcija, pri individuumu, ki potrebuje tako zdravljenje.
- 19. Spojina po katerem koli od zahtevkov 1-14 ali njena farmacevtsko sprejemljiva sol za uporabo po zahtevku 18, kjer je motnja ali bolezen izbrana izmed hipertenzije, pljučne hipertenzije, izolirane sistolične hipertenzije, rezistentene hipertenzije, periferne vaskulame bolezni, kongestivne srčne insuficience ali pljučne arterijske hipertenzije.
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