JPWO2020092594A5 - - Google Patents
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- Publication number
- JPWO2020092594A5 JPWO2020092594A5 JP2021523277A JP2021523277A JPWO2020092594A5 JP WO2020092594 A5 JPWO2020092594 A5 JP WO2020092594A5 JP 2021523277 A JP2021523277 A JP 2021523277A JP 2021523277 A JP2021523277 A JP 2021523277A JP WO2020092594 A5 JPWO2020092594 A5 JP WO2020092594A5
- Authority
- JP
- Japan
- Prior art keywords
- acceptable salt
- pharmaceutically acceptable
- composition
- subject
- blood
- 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 73
- 150000003839 salts Chemical class 0.000 claims description 58
- 150000001875 compounds Chemical class 0.000 claims description 36
- 239000008280 blood Substances 0.000 claims description 30
- 210000004369 blood Anatomy 0.000 claims description 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 230000009424 thromboembolic effect Effects 0.000 claims description 14
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 12
- 238000002618 extracorporeal membrane oxygenation Methods 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 238000005086 pumping Methods 0.000 claims description 6
- 230000001143 conditioned effect Effects 0.000 claims description 5
- 230000003750 conditioning effect Effects 0.000 claims description 5
- 230000002612 cardiopulmonary effect Effects 0.000 claims description 4
- 238000006213 oxygenation reaction Methods 0.000 claims description 4
- 230000036470 plasma concentration Effects 0.000 claims description 4
- 208000007536 Thrombosis Diseases 0.000 claims description 3
- 238000000502 dialysis Methods 0.000 claims description 3
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims description 3
- 210000003709 heart valve Anatomy 0.000 claims description 3
- 239000012528 membrane Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 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 claims description 2
- 241001465754 Metazoa Species 0.000 claims description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 2
- 102000002262 Thromboplastin Human genes 0.000 claims description 2
- 108010000499 Thromboplastin Proteins 0.000 claims description 2
- 230000000747 cardiac effect Effects 0.000 claims description 2
- 239000000155 melt Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 18
- 208000035475 disorder Diseases 0.000 description 11
- 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
- 229960002897 heparin Drugs 0.000 description 4
- 229920000669 heparin Polymers 0.000 description 4
- 206010051055 Deep vein thrombosis Diseases 0.000 description 2
- 206010047249 Venous thrombosis Diseases 0.000 description 2
- 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
- 206010014522 Embolism venous Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 208000010378 Pulmonary Embolism Diseases 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
- 230000000302 ischemic effect Effects 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862752510P | 2018-10-30 | 2018-10-30 | |
| US62/752,510 | 2018-10-30 | ||
| PCT/US2019/058898 WO2020092594A1 (en) | 2018-10-30 | 2019-10-30 | Therapeutic compounds and compositions |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022506109A JP2022506109A (ja) | 2022-01-17 |
| JPWO2020092594A5 true JPWO2020092594A5 (https=) | 2022-10-28 |
| JP2022506109A5 JP2022506109A5 (https=) | 2022-10-28 |
Family
ID=70464743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021523277A Pending JP2022506109A (ja) | 2018-10-30 | 2019-10-30 | 治療用化合物および組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20210253550A1 (https=) |
| EP (1) | EP3873446A4 (https=) |
| JP (1) | JP2022506109A (https=) |
| KR (1) | KR20210084581A (https=) |
| CN (1) | CN113056263A (https=) |
| AU (1) | AU2019369518A1 (https=) |
| BR (1) | BR112021008462A2 (https=) |
| CA (1) | CA3117549A1 (https=) |
| IL (1) | IL282765A (https=) |
| WO (1) | WO2020092594A1 (https=) |
Families Citing this family (3)
| 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 |
| TW202345825A (zh) * | 2022-03-30 | 2023-12-01 | 大陸商四川海思科製藥有限公司 | 環狀內醯胺類化合物的注射用藥物組合物及其製備方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| GB0205527D0 (en) | 2002-03-08 | 2002-04-24 | Ferring Bv | Inhibitors |
| CA2648522A1 (en) * | 2005-04-04 | 2006-10-12 | Daiamed, Inc. | Substituted azetidinones |
| 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 |
| WO2020092592A1 (en) * | 2018-10-30 | 2020-05-07 | Exithera Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
| EP3917910A4 (en) * | 2019-01-29 | 2022-11-09 | Exithera Pharmaceuticals Inc. | THERAPEUTIC COMPOUNDS AND COMPOSITIONS |
-
2019
- 2019-10-30 KR KR1020217016347A patent/KR20210084581A/ko not_active Withdrawn
- 2019-10-30 AU AU2019369518A patent/AU2019369518A1/en not_active Abandoned
- 2019-10-30 BR BR112021008462-2A patent/BR112021008462A2/pt unknown
- 2019-10-30 EP EP19880599.6A patent/EP3873446A4/en active Pending
- 2019-10-30 CN CN201980072155.7A patent/CN113056263A/zh active Pending
- 2019-10-30 JP JP2021523277A patent/JP2022506109A/ja active Pending
- 2019-10-30 WO PCT/US2019/058898 patent/WO2020092594A1/en not_active Ceased
- 2019-10-30 CA CA3117549A patent/CA3117549A1/en active Pending
-
2021
- 2021-04-28 IL IL282765A patent/IL282765A/en unknown
- 2021-04-30 US US17/245,691 patent/US20210253550A1/en not_active Abandoned
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