JP2018502126A5 - - Google Patents

Info

Publication number

JP2018502126A5

JP2018502126A5 JP2017536934A JP2017536934A JP2018502126A5 JP 2018502126 A5 JP2018502126 A5 JP 2018502126A5 JP 2017536934 A JP2017536934 A JP 2017536934A JP 2017536934 A JP2017536934 A JP 2017536934A JP 2018502126 A5 JP2018502126 A5 JP 2018502126A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

composition according

pulmonary

activator

bmpr2

Prior art date

2016-01-08

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 claims 22
• 102100025422 Bone morphogenetic protein receptor type-2 Human genes 0.000 claims 7
• 101000934635 Homo sapiens Bone morphogenetic protein receptor type-2 Proteins 0.000 claims 7
• 208000002815 pulmonary hypertension Diseases 0.000 claims 7
• 239000012190 activator Substances 0.000 claims 5
• 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 4
• 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 claims 4
• 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 claims 4
• 239000013543 active substance Substances 0.000 claims 4
• 229960000307 avanafil Drugs 0.000 claims 4
• WEAJZXNPAWBCOA-INIZCTEOSA-N avanafil Chemical group C1=C(Cl)C(OC)=CC=C1CNC1=NC(N2[C@@H](CCC2)CO)=NC=C1C(=O)NCC1=NC=CC=N1 WEAJZXNPAWBCOA-INIZCTEOSA-N 0.000 claims 4
• 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims 4
• 239000012453 solvate Substances 0.000 claims 4
• 229950005371 zaprinast Drugs 0.000 claims 4
• REZGGXNDEMKIQB-UHFFFAOYSA-N zaprinast Chemical compound CCCOC1=CC=CC=C1C1=NC(=O)C2=NNNC2=N1 REZGGXNDEMKIQB-UHFFFAOYSA-N 0.000 claims 4
• 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 3
• 239000002308 endothelin receptor antagonist Substances 0.000 claims 3
• 229940126514 guanylate cyclase activator Drugs 0.000 claims 3
• 239000003119 guanylate cyclase activator Substances 0.000 claims 3
• 210000002966 serum Anatomy 0.000 claims 3
• 229960000438 udenafil Drugs 0.000 claims 3
• IYFNEFQTYQPVOC-UHFFFAOYSA-N udenafil Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)NCCC1CCCN1C IYFNEFQTYQPVOC-UHFFFAOYSA-N 0.000 claims 3
• 229940127291 Calcium channel antagonist Drugs 0.000 claims 2
• 229940118365 Endothelin receptor antagonist Drugs 0.000 claims 2
• QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 2
• SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims 2
• 239000003146 anticoagulant agent Substances 0.000 claims 2
• 229940127219 anticoagulant drug Drugs 0.000 claims 2
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
• 239000000480 calcium channel blocker Substances 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 239000002934 diuretic Substances 0.000 claims 2
• 230000001882 diuretic effect Effects 0.000 claims 2
• 229940079593 drug Drugs 0.000 claims 2
• 239000003814 drug Substances 0.000 claims 2
• 239000003112 inhibitor Substances 0.000 claims 2
• 229950002245 mirodenafil Drugs 0.000 claims 2
• MIJFNYMSCFYZNY-UHFFFAOYSA-N mirodenafil Chemical compound C1=C(C=2NC=3C(CCC)=CN(CC)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)N1CCN(CCO)CC1 MIJFNYMSCFYZNY-UHFFFAOYSA-N 0.000 claims 2
• 229910052760 oxygen Inorganic materials 0.000 claims 2
• 239000001301 oxygen Substances 0.000 claims 2
• 229940127293 prostanoid Drugs 0.000 claims 2
• 150000003814 prostanoids Chemical class 0.000 claims 2
• 230000011664 signaling Effects 0.000 claims 2
• 229960003310 sildenafil Drugs 0.000 claims 2
• 229960001967 tacrolimus Drugs 0.000 claims 2
• QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims 2
• 229960000835 tadalafil Drugs 0.000 claims 2
• IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 2
• 229960002381 vardenafil Drugs 0.000 claims 2
• 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
• 101710158332 Diuretic hormone Proteins 0.000 claims 1
• 101710204261 Diuretic hormone class 2 Proteins 0.000 claims 1
• 208000000059 Dyspnea Diseases 0.000 claims 1
• 206010013975 Dyspnoeas Diseases 0.000 claims 1
• 208000005189 Embolism Diseases 0.000 claims 1
• 206010021133 Hypoventilation Diseases 0.000 claims 1
• DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
• 206010025219 Lymphangioma Diseases 0.000 claims 1
• 206010070995 Vascular compression Diseases 0.000 claims 1
• 229960002414 ambrisentan Drugs 0.000 claims 1
• OUJTZYPIHDYQMC-LJQANCHMSA-N ambrisentan Chemical group O([C@@H](C(OC)(C=1C=CC=CC=1)C=1C=CC=CC=1)C(O)=O)C1=NC(C)=CC(C)=N1 OUJTZYPIHDYQMC-LJQANCHMSA-N 0.000 claims 1
• MOTJMGVDPWRKOC-QPVYNBJUSA-N atrasentan Chemical compound C1([C@H]2[C@@H]([C@H](CN2CC(=O)N(CCCC)CCCC)C=2C=C3OCOC3=CC=2)C(O)=O)=CC=C(OC)C=C1 MOTJMGVDPWRKOC-QPVYNBJUSA-N 0.000 claims 1
• 229950010993 atrasentan Drugs 0.000 claims 1
• 229960003065 bosentan Drugs 0.000 claims 1
• GJPICJJJRGTNOD-UHFFFAOYSA-N bosentan Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 GJPICJJJRGTNOD-UHFFFAOYSA-N 0.000 claims 1
• 230000001684 chronic effect Effects 0.000 claims 1
• 230000009547 development abnormality Effects 0.000 claims 1
• 208000035475 disorder Diseases 0.000 claims 1
• 230000000004 hemodynamic effect Effects 0.000 claims 1
• 210000004072 lung Anatomy 0.000 claims 1
• TUYWTLTWNJOZNY-UHFFFAOYSA-N n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2h-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-propan-2-ylpyridine-2-sulfonamide Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2C=C(N=CC=2)C2=NNN=N2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)C)C=N1 TUYWTLTWNJOZNY-UHFFFAOYSA-N 0.000 claims 1
• 210000001147 pulmonary artery Anatomy 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 230000029058 respiratory gaseous exchange Effects 0.000 claims 1
• 229960000529 riociguat Drugs 0.000 claims 1
• WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical group N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 claims 1
• 201000000306 sarcoidosis Diseases 0.000 claims 1
• 229960002578 sitaxentan Drugs 0.000 claims 1
• PHWXUGHIIBDVKD-UHFFFAOYSA-N sitaxentan Chemical compound CC1=NOC(NS(=O)(=O)C2=C(SC=C2)C(=O)CC=2C(=CC=3OCOC=3C=2)C)=C1Cl PHWXUGHIIBDVKD-UHFFFAOYSA-N 0.000 claims 1
• 239000011734 sodium Substances 0.000 claims 1
• 229910052708 sodium Inorganic materials 0.000 claims 1
• 229950000584 tezosentan Drugs 0.000 claims 1
• 230000009424 thromboembolic effect Effects 0.000 claims 1
• 230000001732 thrombotic effect Effects 0.000 claims 1
• 230000007704 transition Effects 0.000 claims 1