JPWO2019156929A5 - - Google Patents
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- Publication number
- JPWO2019156929A5 JPWO2019156929A5 JP2020542552A JP2020542552A JPWO2019156929A5 JP WO2019156929 A5 JPWO2019156929 A5 JP WO2019156929A5 JP 2020542552 A JP2020542552 A JP 2020542552A JP 2020542552 A JP2020542552 A JP 2020542552A JP WO2019156929 A5 JPWO2019156929 A5 JP WO2019156929A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- subject
- compound according
- pharmaceutically acceptable
- acceptable salt
- 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.)
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- 239000000203 mixture Substances 0.000 claims description 240
- 150000001875 compounds Chemical class 0.000 claims description 239
- 150000003839 salts Chemical class 0.000 claims description 124
- 125000000217 alkyl group Chemical group 0.000 claims description 46
- 206010020772 Hypertension Diseases 0.000 claims description 26
- 208000010378 Pulmonary Embolism Diseases 0.000 claims description 22
- 230000000302 ischemic effect Effects 0.000 claims description 22
- 239000003814 drug Substances 0.000 claims description 21
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- 229940124597 therapeutic agent Drugs 0.000 claims description 20
- 206010051055 Deep vein thrombosis Diseases 0.000 claims description 18
- 206010047249 Venous thrombosis Diseases 0.000 claims description 18
- 125000005843 halogen group Chemical group 0.000 claims description 18
- 230000002265 prevention Effects 0.000 claims description 17
- 125000001544 thienyl group Chemical group 0.000 claims description 16
- 238000001356 surgical procedure Methods 0.000 claims description 13
- 206010062506 Heparin-induced thrombocytopenia Diseases 0.000 claims description 12
- 208000006011 Stroke Diseases 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 12
- 230000008085 renal dysfunction Effects 0.000 claims description 12
- 230000009424 thromboembolic effect Effects 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 238000011282 treatment Methods 0.000 claims description 11
- 239000003146 anticoagulant agent Substances 0.000 claims description 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 208000005189 Embolism Diseases 0.000 claims description 8
- 208000007536 Thrombosis Diseases 0.000 claims description 8
- 229940127219 anticoagulant drug Drugs 0.000 claims description 8
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000002883 imidazolyl group Chemical group 0.000 claims description 8
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 8
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 230000009885 systemic effect Effects 0.000 claims description 8
- 125000000335 thiazolyl group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 206010061481 Renal injury Diseases 0.000 claims description 6
- 208000035868 Vascular inflammations Diseases 0.000 claims description 6
- 208000037849 arterial hypertension Diseases 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 6
- 208000028867 ischemia Diseases 0.000 claims description 6
- 208000037806 kidney injury Diseases 0.000 claims description 6
- 201000002793 renal fibrosis Diseases 0.000 claims description 6
- 230000002792 vascular Effects 0.000 claims description 6
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 4
- 102000005862 Angiotensin II Human genes 0.000 claims description 4
- 101800000733 Angiotensin-2 Proteins 0.000 claims description 4
- 206010003162 Arterial injury Diseases 0.000 claims description 4
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 4
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 claims description 4
- 206010061218 Inflammation Diseases 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- 206010030113 Oedema Diseases 0.000 claims description 4
- 206010000891 acute myocardial infarction Diseases 0.000 claims description 4
- 229950006323 angiotensin ii Drugs 0.000 claims description 4
- 230000004054 inflammatory process Effects 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 230000000399 orthopedic effect Effects 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 208000034841 Thrombotic Microangiopathies Diseases 0.000 claims description 3
- 230000001732 thrombotic effect Effects 0.000 claims description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims description 2
- 208000009304 Acute Kidney Injury Diseases 0.000 claims description 2
- 206010002329 Aneurysm Diseases 0.000 claims description 2
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims description 2
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims description 2
- 206010048554 Endothelial dysfunction Diseases 0.000 claims description 2
- 108010080805 Factor XIa Proteins 0.000 claims description 2
- 206010019280 Heart failures Diseases 0.000 claims description 2
- 208000031220 Hemophilia Diseases 0.000 claims description 2
- 208000009292 Hemophilia A Diseases 0.000 claims description 2
- 108060005987 Kallikrein Proteins 0.000 claims description 2
- 102000001399 Kallikrein Human genes 0.000 claims description 2
- 208000033626 Renal failure acute Diseases 0.000 claims description 2
- 208000006117 ST-elevation myocardial infarction Diseases 0.000 claims description 2
- 108090000190 Thrombin Proteins 0.000 claims description 2
- 208000032109 Transient ischaemic attack Diseases 0.000 claims description 2
- 238000012084 abdominal surgery Methods 0.000 claims description 2
- 201000011040 acute kidney failure Diseases 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 229940127218 antiplatelet drug Drugs 0.000 claims description 2
- 210000001765 aortic valve Anatomy 0.000 claims description 2
- 210000001367 artery Anatomy 0.000 claims description 2
- 210000004204 blood vessel Anatomy 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 238000013153 catheter ablation Methods 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 230000008694 endothelial dysfunction Effects 0.000 claims description 2
- 238000001631 haemodialysis Methods 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 230000000322 hemodialysis Effects 0.000 claims description 2
- 230000002440 hepatic effect Effects 0.000 claims description 2
- 238000011540 hip replacement Methods 0.000 claims description 2
- 238000002513 implantation Methods 0.000 claims description 2
- 230000008595 infiltration Effects 0.000 claims description 2
- 238000001764 infiltration Methods 0.000 claims description 2
- 210000003127 knee Anatomy 0.000 claims description 2
- 238000013150 knee replacement Methods 0.000 claims description 2
- 210000000265 leukocyte Anatomy 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 229940127066 new oral anticoagluant drug Drugs 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 238000013146 percutaneous coronary intervention Methods 0.000 claims description 2
- 230000002093 peripheral effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- -1 pyridyl N-oxide Chemical class 0.000 claims description 2
- 238000012959 renal replacement therapy Methods 0.000 claims description 2
- 208000037803 restenosis Diseases 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 230000002195 synergetic effect Effects 0.000 claims description 2
- 229960004072 thrombin Drugs 0.000 claims description 2
- 201000010875 transient cerebral ischemia Diseases 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 230000002861 ventricular Effects 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000034 method Methods 0.000 description 148
- 229940079593 drug Drugs 0.000 description 5
- 239000008177 pharmaceutical agent Substances 0.000 description 2
- 241000282465 Canis Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000007675 cardiac surgery Methods 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023203652A JP2024023490A (ja) | 2018-02-07 | 2023-12-01 | 治療用化合物および組成物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862627435P | 2018-02-07 | 2018-02-07 | |
| US62/627,435 | 2018-02-07 | ||
| PCT/US2019/016503 WO2019156929A1 (en) | 2018-02-07 | 2019-02-04 | Therapeutic compounds and compositions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023203652A Division JP2024023490A (ja) | 2018-02-07 | 2023-12-01 | 治療用化合物および組成物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021512894A JP2021512894A (ja) | 2021-05-20 |
| JPWO2019156929A5 true JPWO2019156929A5 (https=) | 2022-02-14 |
| JP2021512894A5 JP2021512894A5 (https=) | 2022-02-14 |
| JP7397797B2 JP7397797B2 (ja) | 2023-12-13 |
Family
ID=67548561
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020542552A Active JP7397797B2 (ja) | 2018-02-07 | 2019-02-04 | 治療用化合物および組成物 |
| JP2023203652A Pending JP2024023490A (ja) | 2018-02-07 | 2023-12-01 | 治療用化合物および組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023203652A Pending JP2024023490A (ja) | 2018-02-07 | 2023-12-01 | 治療用化合物および組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US11691962B2 (https=) |
| EP (1) | EP3749662A4 (https=) |
| JP (2) | JP7397797B2 (https=) |
| KR (1) | KR20200118088A (https=) |
| CN (1) | CN111902404A (https=) |
| AU (1) | AU2019217366B2 (https=) |
| BR (1) | BR112020016123A2 (https=) |
| CA (1) | CA3089970A1 (https=) |
| IL (2) | IL276563B1 (https=) |
| WO (1) | WO2019156929A1 (https=) |
Families Citing this family (2)
| 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 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4595532A (en) | 1983-02-02 | 1986-06-17 | University Of Notre Dame Du Lac | N-(substituted-methyl)-azetidin-2-ones |
| EP1051431A1 (de) | 1998-01-26 | 2000-11-15 | Basf Aktiengesellschaft | Thrombininhibitoren |
| US6335324B1 (en) | 1998-06-25 | 2002-01-01 | Bristol-Myers Squibb Co. | Beta lactam compounds and their use as inhibitors of tryptase |
| AU752320B2 (en) | 1998-06-25 | 2002-09-12 | Bristol-Myers Squibb Company | Amidino and guanidino azetidinone tryptase inhibitors |
| AU4654199A (en) | 1998-07-23 | 2000-02-14 | Shionogi & Co., Ltd. | Monocyclic beta-lactam compounds and chymase inhibitors containing the same |
| US20070032466A1 (en) | 2003-08-22 | 2007-02-08 | Teijin Pharma Limited | Drug containing chymase inhibitor as the active ingredient |
| CA2648522A1 (en) * | 2005-04-04 | 2006-10-12 | Daiamed, Inc. | Substituted azetidinones |
| TW200745084A (en) | 2006-03-08 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
| JP5756800B2 (ja) | 2009-06-16 | 2015-07-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｂ２受容体を調節するアゼチジン２−カルボキサミド誘導体 |
| ES2674745T3 (es) | 2010-02-11 | 2018-07-03 | Bristol-Myers Squibb Company | Macrociclos como inhibidores del factor XIa |
| KR101937514B1 (ko) | 2011-10-14 | 2019-01-10 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 xia 억제제로서의 치환된 테트라히드로이소퀴놀린 화합물 |
| US9730921B2 (en) | 2012-03-27 | 2017-08-15 | Duke University | Compositions and methods for the prevention and treatment of mast cell-induced vascular leakage |
| 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 |
| 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 |
| 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
- 2019-02-04 EP EP19751349.2A patent/EP3749662A4/en not_active Withdrawn
- 2019-02-04 BR BR112020016123-3A patent/BR112020016123A2/pt unknown
- 2019-02-04 CA CA3089970A patent/CA3089970A1/en active Pending
- 2019-02-04 AU AU2019217366A patent/AU2019217366B2/en active Active
- 2019-02-04 JP JP2020542552A patent/JP7397797B2/ja active Active
- 2019-02-04 CN CN201980021810.6A patent/CN111902404A/zh active Pending
- 2019-02-04 WO PCT/US2019/016503 patent/WO2019156929A1/en not_active Ceased
- 2019-02-04 KR KR1020207024907A patent/KR20200118088A/ko active Pending
-
2020
- 2020-08-06 US US16/986,658 patent/US11691962B2/en active Active
- 2020-08-06 IL IL276563A patent/IL276563B1/en unknown
-
2023
- 2023-02-17 US US18/170,858 patent/US12152014B2/en active Active
- 2023-12-01 JP JP2023203652A patent/JP2024023490A/ja active Pending
-
2025
- 2025-12-21 IL IL325484A patent/IL325484A/en unknown
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