RU2011102471A - Диарилмочевины для лечения сердечной недостаточности - Google Patents
Диарилмочевины для лечения сердечной недостаточности Download PDFInfo
- Publication number
- RU2011102471A RU2011102471A RU2011102471/15A RU2011102471A RU2011102471A RU 2011102471 A RU2011102471 A RU 2011102471A RU 2011102471/15 A RU2011102471/15 A RU 2011102471/15A RU 2011102471 A RU2011102471 A RU 2011102471A RU 2011102471 A RU2011102471 A RU 2011102471A
- Authority
- RU
- Russia
- Prior art keywords
- formula
- inhibitors
- alkyl
- optionally substituted
- heart
- Prior art date
Links
- 206010019280 Heart failures Diseases 0.000 title claims abstract 20
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- -1 hydrate Substances 0.000 claims abstract 21
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims abstract 18
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims abstract 15
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims abstract 12
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims abstract 12
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims abstract 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 11
- 229910052736 halogen Inorganic materials 0.000 claims abstract 9
- 239000001257 hydrogen Substances 0.000 claims abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 6
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims abstract 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims abstract 6
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims abstract 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims abstract 6
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims abstract 6
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims abstract 6
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims abstract 6
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims abstract 6
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims abstract 6
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 6
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims abstract 6
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000002207 metabolite Substances 0.000 claims abstract 6
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000000651 prodrug Substances 0.000 claims abstract 6
- 229940002612 prodrug Drugs 0.000 claims abstract 6
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims abstract 6
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims abstract 6
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 150000003536 tetrazoles Chemical class 0.000 claims abstract 6
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims abstract 6
- 229930192474 thiophene Natural products 0.000 claims abstract 6
- 150000003852 triazoles Chemical class 0.000 claims abstract 6
- 239000012453 solvate Substances 0.000 claims abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 4
- 239000003814 drug Substances 0.000 claims abstract 4
- 230000002265 prevention Effects 0.000 claims abstract 4
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims abstract 3
- NQPJDJVGBDHCAD-UHFFFAOYSA-N 1,3-diazinan-2-one Chemical compound OC1=NCCCN1 NQPJDJVGBDHCAD-UHFFFAOYSA-N 0.000 claims abstract 3
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 claims abstract 3
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical compound C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 claims abstract 3
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims abstract 3
- BJMOTQQVVMGOHA-UHFFFAOYSA-N O1C=CC2=C1C=CC=C2.N2=CN=C1N=CNC1=C2 Chemical compound O1C=CC2=C1C=CC=C2.N2=CN=C1N=CNC1=C2 BJMOTQQVVMGOHA-UHFFFAOYSA-N 0.000 claims abstract 3
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims abstract 3
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims abstract 3
- YPWFISCTZQNZAU-UHFFFAOYSA-N Thiane Chemical compound C1CCSCC1 YPWFISCTZQNZAU-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 3
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 claims abstract 3
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 claims abstract 3
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims abstract 3
- 208000019622 heart disease Diseases 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 239000003112 inhibitor Substances 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- LNTHITQWFMADLM-UHFFFAOYSA-N gallic acid Chemical compound OC(=O)C1=CC(O)=C(O)C(O)=C1 LNTHITQWFMADLM-UHFFFAOYSA-N 0.000 claims 8
- 239000005557 antagonist Substances 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 208000009525 Myocarditis Diseases 0.000 claims 6
- 206010030113 Oedema Diseases 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 210000003709 heart valve Anatomy 0.000 claims 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 230000007547 defect Effects 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 4
- 238000002399 angioplasty Methods 0.000 claims 4
- 230000015572 biosynthetic process Effects 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- ZOOGRGPOEVQQDX-KHLHZJAASA-N cyclic guanosine monophosphate Chemical compound C([C@H]1O2)O[P@](O)(=O)O[C@@H]1[C@H](O)[C@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-KHLHZJAASA-N 0.000 claims 4
- 229940074391 gallic acid Drugs 0.000 claims 4
- 235000004515 gallic acid Nutrition 0.000 claims 4
- 150000003278 haem Chemical class 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 claims 3
- 101000851058 Homo sapiens Neutrophil elastase Proteins 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 208000006887 mitral valve stenosis Diseases 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 230000002093 peripheral effect Effects 0.000 claims 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 claims 2
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 229940123073 Angiotensin antagonist Drugs 0.000 claims 2
- 208000003017 Aortic Valve Stenosis Diseases 0.000 claims 2
- 206010002915 Aortic valve incompetence Diseases 0.000 claims 2
- 206010003130 Arrhythmia supraventricular Diseases 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 2
- 206010048962 Brain oedema Diseases 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 2
- 229940122434 Calcium sensitizer Drugs 0.000 claims 2
- 206010007556 Cardiac failure acute Diseases 0.000 claims 2
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 229940127328 Cholesterol Synthesis Inhibitors Drugs 0.000 claims 2
- 208000002330 Congenital Heart Defects Diseases 0.000 claims 2
- 206010056370 Congestive cardiomyopathy Diseases 0.000 claims 2
- 201000010046 Dilated cardiomyopathy Diseases 0.000 claims 2
- 102000002045 Endothelin Human genes 0.000 claims 2
- 108050009340 Endothelin Proteins 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 229940123583 Factor Xa inhibitor Drugs 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 102100025306 Integrin alpha-IIb Human genes 0.000 claims 2
- 101710149643 Integrin alpha-IIb Proteins 0.000 claims 2
- 206010048858 Ischaemic cardiomyopathy Diseases 0.000 claims 2
- 229940127470 Lipase Inhibitors Drugs 0.000 claims 2
- 208000007101 Muscle Cramp Diseases 0.000 claims 2
- 201000002481 Myositis Diseases 0.000 claims 2
- 108020001621 Natriuretic Peptide Proteins 0.000 claims 2
- 102000004571 Natriuretic peptide Human genes 0.000 claims 2
- 108010028924 PPAR alpha Proteins 0.000 claims 2
- 102000023984 PPAR alpha Human genes 0.000 claims 2
- 108010015181 PPAR delta Proteins 0.000 claims 2
- 108010016731 PPAR gamma Proteins 0.000 claims 2
- 102000000536 PPAR gamma Human genes 0.000 claims 2
- 206010037423 Pulmonary oedema Diseases 0.000 claims 2
- 206010037448 Pulmonary valve incompetence Diseases 0.000 claims 2
- 208000005392 Spasm Diseases 0.000 claims 2
- 208000007718 Stable Angina Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 claims 2
- 101000712605 Theromyzon tessulatum Theromin Proteins 0.000 claims 2
- 229940122388 Thrombin inhibitor Drugs 0.000 claims 2
- 208000001435 Thromboembolism Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 229940127535 Thyroid Hormone Receptor Agonists Drugs 0.000 claims 2
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 2
- 206010044642 Tricuspid valve stenosis Diseases 0.000 claims 2
- 208000007814 Unstable Angina Diseases 0.000 claims 2
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 201000005180 acute myocarditis Diseases 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 150000003973 alkyl amines Chemical class 0.000 claims 2
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 2
- 239000002369 angiotensin antagonist Substances 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 230000002785 anti-thrombosis Effects 0.000 claims 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 229940127219 anticoagulant drug Drugs 0.000 claims 2
- 229940127218 antiplatelet drug Drugs 0.000 claims 2
- 206010002906 aortic stenosis Diseases 0.000 claims 2
- 201000002064 aortic valve insufficiency Diseases 0.000 claims 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 2
- 210000001367 artery Anatomy 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 230000001746 atrial effect Effects 0.000 claims 2
- 239000002876 beta blocker Substances 0.000 claims 2
- 230000036772 blood pressure Effects 0.000 claims 2
- 208000006752 brain edema Diseases 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 230000000747 cardiac effect Effects 0.000 claims 2
- 230000015556 catabolic process Effects 0.000 claims 2
- 230000001906 cholesterol absorption Effects 0.000 claims 2
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 208000028831 congenital heart disease Diseases 0.000 claims 2
- 238000007887 coronary angioplasty Methods 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 210000004351 coronary vessel Anatomy 0.000 claims 2
- 238000006731 degradation reaction Methods 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 125000005265 dialkylamine group Chemical group 0.000 claims 2
- 230000003205 diastolic effect Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000002934 diuretic Substances 0.000 claims 2
- 229940030606 diuretics Drugs 0.000 claims 2
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims 2
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 claims 2
- 230000037149 energy metabolism Effects 0.000 claims 2
- 239000002792 enkephalinase inhibitor Substances 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 239000003119 guanylate cyclase activator Substances 0.000 claims 2
- 229960002897 heparin Drugs 0.000 claims 2
- 229920000669 heparin Polymers 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 230000004060 metabolic process Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 239000000692 natriuretic peptide Substances 0.000 claims 2
- 229940082615 organic nitrates used in cardiac disease Drugs 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 2
- 230000009090 positive inotropic effect Effects 0.000 claims 2
- 230000000019 pro-fibrinolytic effect Effects 0.000 claims 2
- 208000005333 pulmonary edema Diseases 0.000 claims 2
- 201000010298 pulmonary valve insufficiency Diseases 0.000 claims 2
- 208000009138 pulmonary valve stenosis Diseases 0.000 claims 2
- 230000009103 reabsorption Effects 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 239000002461 renin inhibitor Substances 0.000 claims 2
- 229940086526 renin-inhibitors Drugs 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 230000035939 shock Effects 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- 229940031439 squalene Drugs 0.000 claims 2
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 claims 2
- 239000000021 stimulant Substances 0.000 claims 2
- 238000003860 storage Methods 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 238000003786 synthesis reaction Methods 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 239000003868 thrombin inhibitor Substances 0.000 claims 2
- 230000002537 thrombolytic effect Effects 0.000 claims 2
- 231100000331 toxic Toxicity 0.000 claims 2
- 230000002588 toxic effect Effects 0.000 claims 2
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 2
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 2
- 206010047470 viral myocarditis Diseases 0.000 claims 2
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 102100040214 Apolipoprotein(a) Human genes 0.000 claims 1
- 108010078321 Guanylate Cyclase Proteins 0.000 claims 1
- 102000014469 Guanylate cyclase Human genes 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 108010033266 Lipoprotein(a) Proteins 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 201000001943 Tricuspid Valve Insufficiency Diseases 0.000 claims 1
- 229940083712 aldosterone antagonist Drugs 0.000 claims 1
- 239000003698 antivitamin K Substances 0.000 claims 1
- 208000037849 arterial hypertension Diseases 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 239000003602 elastase inhibitor Substances 0.000 claims 1
- RQFCJASXJCIDSX-UUOKFMHZSA-N guanosine 5'-monophosphate Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O RQFCJASXJCIDSX-UUOKFMHZSA-N 0.000 claims 1
- 239000002628 heparin derivative Substances 0.000 claims 1
- 102000052502 human ELANE Human genes 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000003591 leukocyte elastase inhibitor Substances 0.000 claims 1
- 239000003055 low molecular weight heparin Substances 0.000 claims 1
- 229940127215 low-molecular weight heparin Drugs 0.000 claims 1
- 230000036244 malformation Effects 0.000 claims 1
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 239000002394 mineralocorticoid antagonist Substances 0.000 claims 1
- 208000005907 mitral valve insufficiency Diseases 0.000 claims 1
- 210000004165 myocardium Anatomy 0.000 claims 1
- 230000003448 neutrophilic effect Effects 0.000 claims 1
- PIRWNASAJNPKHT-SHZATDIYSA-N pamp Chemical compound C([C@@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)N)C(C)C)C1=CC=CC=C1 PIRWNASAJNPKHT-SHZATDIYSA-N 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 210000003102 pulmonary valve Anatomy 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 230000036262 stenosis Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 125000005490 tosylate group Chemical class 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 229940019333 vitamin k antagonists Drugs 0.000 claims 1
- 229940124629 β-receptor antagonist Drugs 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08011471 | 2008-06-25 | ||
| EP08011471.3 | 2008-06-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2011102471A true RU2011102471A (ru) | 2012-07-27 |
Family
ID=41136709
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011102471/15A RU2011102471A (ru) | 2008-06-25 | 2009-06-18 | Диарилмочевины для лечения сердечной недостаточности |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20110263657A1 (enExample) |
| EP (1) | EP2293792A1 (enExample) |
| JP (1) | JP2011525506A (enExample) |
| KR (1) | KR20110031294A (enExample) |
| CN (1) | CN102076338A (enExample) |
| AU (1) | AU2009262599A1 (enExample) |
| BR (1) | BRPI0914636A2 (enExample) |
| CA (1) | CA2729050A1 (enExample) |
| IL (1) | IL209647A0 (enExample) |
| MX (1) | MX2010014441A (enExample) |
| RU (1) | RU2011102471A (enExample) |
| WO (1) | WO2009156089A1 (enExample) |
| ZA (1) | ZA201009063B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102718703B (zh) * | 2011-03-31 | 2016-09-14 | 中国医学科学院药物研究所 | Gk和ppar双重激动活性的含有二甲基的芳基脲类衍生物 |
| EP2723718A1 (en) | 2011-06-24 | 2014-04-30 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| AP2013007331A0 (en) | 2011-06-24 | 2013-12-31 | Amgen Inc | TRPM8 antagonists and their use in treatments |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| RU2646454C2 (ru) * | 2013-11-12 | 2018-03-05 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | Способ моделирования алкогольной кардиомиопатии |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1636585B2 (en) * | 2003-05-20 | 2012-06-13 | Bayer HealthCare LLC | Diaryl ureas with kinase inhibiting activity |
| PL1663978T3 (pl) * | 2003-07-23 | 2008-04-30 | Bayer Healthcare Llc | Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów |
| WO2007087575A2 (en) * | 2006-01-24 | 2007-08-02 | University Of Chicago | Compositions and methods for treating pulmonary hypertension |
| WO2009092442A1 (en) * | 2008-01-23 | 2009-07-30 | Universidad De Barcelona | Treatment of portal hypertension and related conditions by combined inhibition of the vegf and pdgf signalling pathways |
-
2009
- 2009-06-18 CN CN2009801240616A patent/CN102076338A/zh active Pending
- 2009-06-18 CA CA2729050A patent/CA2729050A1/en not_active Abandoned
- 2009-06-18 US US13/001,145 patent/US20110263657A1/en not_active Abandoned
- 2009-06-18 MX MX2010014441A patent/MX2010014441A/es not_active Application Discontinuation
- 2009-06-18 WO PCT/EP2009/004390 patent/WO2009156089A1/en not_active Ceased
- 2009-06-18 KR KR1020107029143A patent/KR20110031294A/ko not_active Withdrawn
- 2009-06-18 BR BRPI0914636A patent/BRPI0914636A2/pt not_active IP Right Cessation
- 2009-06-18 JP JP2011515168A patent/JP2011525506A/ja not_active Withdrawn
- 2009-06-18 AU AU2009262599A patent/AU2009262599A1/en not_active Abandoned
- 2009-06-18 EP EP09768938A patent/EP2293792A1/en not_active Withdrawn
- 2009-06-18 RU RU2011102471/15A patent/RU2011102471A/ru not_active Application Discontinuation
-
2010
- 2010-11-30 IL IL209647A patent/IL209647A0/en unknown
- 2010-12-17 ZA ZA2010/09063A patent/ZA201009063B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009262599A1 (en) | 2009-12-30 |
| IL209647A0 (en) | 2011-02-28 |
| JP2011525506A (ja) | 2011-09-22 |
| KR20110031294A (ko) | 2011-03-25 |
| MX2010014441A (es) | 2011-01-21 |
| BRPI0914636A2 (pt) | 2015-10-20 |
| ZA201009063B (en) | 2012-02-29 |
| US20110263657A1 (en) | 2011-10-27 |
| CN102076338A (zh) | 2011-05-25 |
| CA2729050A1 (en) | 2009-12-30 |
| EP2293792A1 (en) | 2011-03-16 |
| WO2009156089A1 (en) | 2009-12-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR100204433B1 (ko) | 4-아미노피리미딘 유도체 | |
| RU2012136473A (ru) | Кислородзамещенные производные 3-гетероароиламинопропионовых кислот и их применение в качестве фармацевтических средств | |
| JP2023501599A (ja) | Ｌｐａ受容体アンタゴニストとしてのトリアゾールカルバメートピリジルスルホンアミド及びその使用 | |
| US20200255375A1 (en) | Phenylpyrrolidinone formyl peptide 2 receptor agonists | |
| JP2011520967A5 (enExample) | ||
| JP2019518041A5 (enExample) | ||
| RU2013125480A (ru) | Стимуляторы sgc | |
| JP2007507551A5 (enExample) | ||
| JP2010513272A5 (enExample) | ||
| HRP20170506T1 (hr) | Dihidropiridon p1 kao inhibitori xia faktora | |
| JPWO2003064410A1 (ja) | 新規１，２，４−トリアゾール系化合物 | |
| JP2015164972A5 (enExample) | ||
| US10508119B2 (en) | Pyrazole derivatives useful as 5-lipdxygenase activating protein (FLAP) inhibitors | |
| EP2925322A1 (en) | Inhibitors of the renal outer medullary potassium channel | |
| RU2012144332A (ru) | Циклоалкил-замещенное производное имидазола | |
| JP5116681B2 (ja) | ２−アミノエトキシ酢酸誘導体およびそれらの使用 | |
| JP7856575B2 (ja) | Ｐｈｄ阻害剤化合物、組成物、及びそれらの使用 | |
| JP2011525506A5 (enExample) | ||
| EP3675858B1 (en) | Imidazo[1,5-a]pyrazine compounds and compositions for ire1 inhibition | |
| RU2014107000A (ru) | Производные 3-гетероароиламинопропионовой кислоты и их применение в качестве лекарственных средств | |
| US9745282B2 (en) | Indoline compounds as aldosterone synthase inhibitors | |
| RU2014106999A (ru) | Замещенные производные 3-тиазолоаминопропионовой кислоты и их применение в качестве фармацевтических препаратов | |
| RU2013139352A (ru) | Аминозамещенные производные 3-гетероароиламинопропионовой кислоты и их применение в качестве фармацевтических средств | |
| CA2634216A1 (en) | Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery | |
| JP2009538846A5 (enExample) |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20130626 |