JP2018502126A5 - - Google Patents
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- 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
- 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
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- 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562103020P | 2015-01-13 | 2015-01-13 | |
| US62/103,020 | 2015-01-13 | ||
| PCT/US2016/012694 WO2016114993A1 (en) | 2015-01-13 | 2016-01-08 | Combination therapy for pulmonary hypertension |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018502126A JP2018502126A (ja) | 2018-01-25 |
| JP2018502126A5 true JP2018502126A5 (cg-RX-API-DMAC7.html) | 2019-02-21 |
| JP6890540B2 JP6890540B2 (ja) | 2021-06-18 |
Family
ID=56406244
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017536934A Active JP6890540B2 (ja) | 2015-01-13 | 2016-01-08 | 肺高血圧症のための併用療法 |
Country Status (12)
| Country | Link |
|---|---|
| US (4) | US20180325875A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3244968B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6890540B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR102569428B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN107427698A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2016207046B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112017014914B1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2973114C (cg-RX-API-DMAC7.html) |
| IL (1) | IL253325A0 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2017009110A (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ733451A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2016114993A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015089105A1 (en) | 2013-12-09 | 2015-06-18 | Respira Therapeutics, Inc. | Pde5 inhibitor powder formulations and methods relating thereto |
| MA46750A (fr) * | 2016-11-10 | 2019-09-18 | Arena Pharm Inc | Méthodes de traitement de l'htap à l'aide de combinaisons de ralinepag et d'autres agents |
| WO2018112258A1 (en) | 2016-12-14 | 2018-06-21 | Respira Therapeutics, Inc. | Methods and compositions for treatment of pulmonary hypertension and other lung disorders |
| CN112569357B (zh) * | 2019-09-30 | 2023-03-28 | 深圳奥萨制药有限公司 | 双重内皮素受体拮抗剂与利尿剂的组合物 |
| ES2994089T3 (en) * | 2019-11-29 | 2025-01-17 | Actelion Pharmaceuticals Ltd | Initial triple combination therapy with macitentan, tadalafil, and selexipag for treating pulmonary arterial hypertension |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110171193A1 (en) * | 2008-06-12 | 2011-07-14 | The Board Of Trustees Of The University Of Illinois | Compositions and methods for treating pulmonary hypertension |
| WO2012151153A1 (en) * | 2011-05-02 | 2012-11-08 | The Board Of Trustees Of The Leland Stanford Junior University | Use of fk506 for the treatment of pulmonary arterial hypertension |
| SG194901A1 (en) | 2011-05-09 | 2013-12-30 | Univ Glasgow | Methods of modulating micrornas in the treatment of pulmonary arterial hypertension |
| US9233089B2 (en) * | 2012-03-23 | 2016-01-12 | The Board Of Trustees Of The Leland Stanford Junior University | Treatment of pulmonary hypertension with leukotriene inhibitors |
-
2016
- 2016-01-08 WO PCT/US2016/012694 patent/WO2016114993A1/en not_active Ceased
- 2016-01-08 NZ NZ733451A patent/NZ733451A/en unknown
- 2016-01-08 CN CN201680015289.1A patent/CN107427698A/zh active Pending
- 2016-01-08 US US15/543,510 patent/US20180325875A1/en not_active Abandoned
- 2016-01-08 MX MX2017009110A patent/MX2017009110A/es unknown
- 2016-01-08 CA CA2973114A patent/CA2973114C/en active Active
- 2016-01-08 KR KR1020177022273A patent/KR102569428B1/ko active Active
- 2016-01-08 JP JP2017536934A patent/JP6890540B2/ja active Active
- 2016-01-08 AU AU2016207046A patent/AU2016207046B2/en active Active
- 2016-01-08 EP EP16737651.6A patent/EP3244968B1/en active Active
- 2016-01-08 BR BR112017014914-1A patent/BR112017014914B1/pt active IP Right Grant
-
2017
- 2017-07-05 IL IL253325A patent/IL253325A0/en unknown
-
2019
- 2019-04-11 US US16/381,128 patent/US20200069658A1/en not_active Abandoned
-
2021
- 2021-05-11 US US17/317,274 patent/US20210267951A1/en not_active Abandoned
-
2024
- 2024-03-28 US US18/620,058 patent/US20240238259A1/en active Pending
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