JPWO2020092592A5 - - Google Patents
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- Publication number
- JPWO2020092592A5 JPWO2020092592A5 JP2021523278A JP2021523278A JPWO2020092592A5 JP WO2020092592 A5 JPWO2020092592 A5 JP WO2020092592A5 JP 2021523278 A JP2021523278 A JP 2021523278A JP 2021523278 A JP2021523278 A JP 2021523278A JP WO2020092592 A5 JPWO2020092592 A5 JP WO2020092592A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- pharmaceutically acceptable
- acceptable salt
- solvate
- hydrate
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 claims description 133
- 150000003839 salts Chemical class 0.000 claims description 67
- 150000001875 compounds Chemical class 0.000 claims description 58
- 239000012453 solvate Substances 0.000 claims description 35
- 239000002904 solvent Substances 0.000 claims description 17
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 12
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 12
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims description 8
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 claims description 8
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 4
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims description 4
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims description 4
- AQRLNPVMDITEJU-UHFFFAOYSA-N triethylsilane Chemical compound CC[SiH](CC)CC AQRLNPVMDITEJU-UHFFFAOYSA-N 0.000 claims description 4
- 238000011097 chromatography purification Methods 0.000 claims description 3
- 238000001556 precipitation Methods 0.000 claims description 3
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims description 2
- BLRPTPMANUNPDV-UHFFFAOYSA-N Silane Chemical compound [SiH4] BLRPTPMANUNPDV-UHFFFAOYSA-N 0.000 claims description 2
- 239000000010 aprotic solvent Substances 0.000 claims description 2
- 230000005587 bubbling Effects 0.000 claims description 2
- 238000001914 filtration Methods 0.000 claims description 2
- 239000007789 gas Substances 0.000 claims description 2
- 238000000746 purification Methods 0.000 claims description 2
- 229910000077 silane Inorganic materials 0.000 claims description 2
- 239000008280 blood Substances 0.000 description 21
- 210000004369 blood Anatomy 0.000 description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 11
- 230000009424 thromboembolic effect Effects 0.000 description 11
- 238000002618 extracorporeal membrane oxygenation Methods 0.000 description 9
- 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 description 4
- 230000003750 conditioning effect Effects 0.000 description 4
- 229960002897 heparin Drugs 0.000 description 4
- 229920000669 heparin Polymers 0.000 description 4
- 230000002612 cardiopulmonary effect Effects 0.000 description 3
- 230000001143 conditioned effect Effects 0.000 description 3
- 238000005086 pumping Methods 0.000 description 3
- 208000007536 Thrombosis Diseases 0.000 description 2
- 238000000502 dialysis Methods 0.000 description 2
- 210000003709 heart valve Anatomy 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000006213 oxygenation reaction Methods 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- PGOHTUIFYSHAQG-LJSDBVFPSA-N (2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoyl]amino]hexanoic acid Chemical compound CSCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(O)=O PGOHTUIFYSHAQG-LJSDBVFPSA-N 0.000 description 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- 206010051055 Deep vein thrombosis Diseases 0.000 description 1
- 206010014522 Embolism venous Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000010378 Pulmonary Embolism Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 102000002262 Thromboplastin Human genes 0.000 description 1
- 108010000499 Thromboplastin Proteins 0.000 description 1
- 206010047249 Venous thrombosis Diseases 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000035602 clotting Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000004043 venous thromboembolism Diseases 0.000 description 1
- 230000002861 ventricular Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024185222A JP2025011310A (ja) | 2018-10-30 | 2024-10-21 | 治療用化合物および組成物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862752503P | 2018-10-30 | 2018-10-30 | |
| US62/752,503 | 2018-10-30 | ||
| PCT/US2019/058896 WO2020092592A1 (en) | 2018-10-30 | 2019-10-30 | Therapeutic compounds and compositions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024185222A Division JP2025011310A (ja) | 2018-10-30 | 2024-10-21 | 治療用化合物および組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022506110A JP2022506110A (ja) | 2022-01-17 |
| JPWO2020092592A5 true JPWO2020092592A5 (https=) | 2022-10-28 |
| JP2022506110A5 JP2022506110A5 (https=) | 2022-10-28 |
Family
ID=70464752
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021523278A Pending JP2022506110A (ja) | 2018-10-30 | 2019-10-30 | 治療用化合物および組成物 |
| JP2024185222A Pending JP2025011310A (ja) | 2018-10-30 | 2024-10-21 | 治療用化合物および組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024185222A Pending JP2025011310A (ja) | 2018-10-30 | 2024-10-21 | 治療用化合物および組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20210261524A1 (https=) |
| EP (1) | EP3873444A4 (https=) |
| JP (2) | JP2022506110A (https=) |
| KR (1) | KR20210087467A (https=) |
| CN (1) | CN112996495A (https=) |
| AU (1) | AU2019373237A1 (https=) |
| BR (1) | BR112021008345A2 (https=) |
| CA (1) | CA3117470A1 (https=) |
| IL (1) | IL282766A (https=) |
| WO (1) | WO2020092592A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2733405C2 (ru) | 2014-02-07 | 2020-10-01 | Экзитера Фармасьютикалз Инк. | Терапевтические соединения и композиции |
| EP3749662A4 (en) | 2018-02-07 | 2021-07-14 | Exithera Pharmaceuticals Inc. | THERAPEUTIC COMPOUNDS AND COMPOSITIONS |
| KR20210084581A (ko) * | 2018-10-30 | 2021-07-07 | 엑시테라 파마슈티컬스 인코퍼레이티드 | 치료 화합물 및 조성물 |
| IL301410A (en) * | 2020-09-17 | 2023-05-01 | Exithera Pharmaceuticals Inc | FACTOR XIa OR KALLIKREIN INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE THEREOF |
| CN116782911A (zh) * | 2020-09-17 | 2023-09-19 | 艾克赛特赫拉制药有限责任公司 | 治疗性化合物、组合物及其使用方法 |
| TW202346278A (zh) * | 2022-03-28 | 2023-12-01 | 大陸商四川海思科製藥有限公司 | 2-氨基吡啶衍生物製備方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9802206D0 (sv) * | 1998-06-22 | 1998-06-22 | Astra Pharma Inc | Novel compounds |
| CA2648522A1 (en) * | 2005-04-04 | 2006-10-12 | Daiamed, Inc. | Substituted azetidinones |
| WO2008124757A1 (en) * | 2007-04-10 | 2008-10-16 | Bristol-Myers Squibb Company | Thiazolyl compounds useful as kinase inhibitors |
| KR101937514B1 (ko) * | 2011-10-14 | 2019-01-10 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 xia 억제제로서의 치환된 테트라히드로이소퀴놀린 화합물 |
| RU2733405C2 (ru) * | 2014-02-07 | 2020-10-01 | Экзитера Фармасьютикалз Инк. | Терапевтические соединения и композиции |
| US20190315711A1 (en) * | 2016-12-23 | 2019-10-17 | Exithera Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
-
2019
- 2019-10-30 WO PCT/US2019/058896 patent/WO2020092592A1/en not_active Ceased
- 2019-10-30 AU AU2019373237A patent/AU2019373237A1/en not_active Abandoned
- 2019-10-30 CA CA3117470A patent/CA3117470A1/en active Pending
- 2019-10-30 JP JP2021523278A patent/JP2022506110A/ja active Pending
- 2019-10-30 KR KR1020217014647A patent/KR20210087467A/ko not_active Withdrawn
- 2019-10-30 BR BR112021008345-6A patent/BR112021008345A2/pt unknown
- 2019-10-30 CN CN201980072037.6A patent/CN112996495A/zh active Pending
- 2019-10-30 EP EP19877575.1A patent/EP3873444A4/en active Pending
-
2021
- 2021-04-28 US US17/243,120 patent/US20210261524A1/en not_active Abandoned
- 2021-04-28 IL IL282766A patent/IL282766A/en unknown
-
2024
- 2024-10-21 JP JP2024185222A patent/JP2025011310A/ja active Pending
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