JP2018506563A5 - - Google Patents
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- JP2018506563A5 JP2018506563A5 JP2017545289A JP2017545289A JP2018506563A5 JP 2018506563 A5 JP2018506563 A5 JP 2018506563A5 JP 2017545289 A JP2017545289 A JP 2017545289A JP 2017545289 A JP2017545289 A JP 2017545289A JP 2018506563 A5 JP2018506563 A5 JP 2018506563A5
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- 239000008194 pharmaceutical composition Substances 0.000 claims 49
- 150000001875 compounds Chemical class 0.000 claims 44
- 208000007536 Thrombosis Diseases 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000004404 heteroalkyl group Chemical group 0.000 claims 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000004817 pentamethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[*:1] 0.000 claims 11
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical class C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 10
- 239000005977 Ethylene Substances 0.000 claims 10
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 10
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims 10
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims 10
- 125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 208000005189 Embolism Diseases 0.000 claims 6
- 208000001435 Thromboembolism Diseases 0.000 claims 6
- 210000001367 artery Anatomy 0.000 claims 6
- 230000015572 biosynthetic process Effects 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 5
- 206010014522 Embolism venous Diseases 0.000 claims 4
- 102000001399 Kallikrein Human genes 0.000 claims 4
- 108060005987 Kallikrein Proteins 0.000 claims 4
- 238000009098 adjuvant therapy Methods 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 230000002093 peripheral effect Effects 0.000 claims 4
- 208000004043 venous thromboembolism Diseases 0.000 claims 4
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 230000001269 cardiogenic effect Effects 0.000 claims 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 230000000302 ischemic effect Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 208000010125 myocardial infarction Diseases 0.000 claims 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 2
- 206010003178 Arterial thrombosis Diseases 0.000 claims 2
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 2
- 206010014513 Embolism arterial Diseases 0.000 claims 2
- 208000003788 Neoplasm Micrometastasis Diseases 0.000 claims 2
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 2
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 2
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 108090000190 Thrombin Proteins 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 230000003143 atherosclerotic effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000002490 cerebral effect Effects 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- 210000003709 heart valve Anatomy 0.000 claims 2
- 230000004968 inflammatory condition Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 238000013146 percutaneous coronary intervention Methods 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229960004072 thrombin Drugs 0.000 claims 2
- 230000002537 thrombolytic effect Effects 0.000 claims 2
- 230000001052 transient effect Effects 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010062506 Heparin-induced thrombocytopenia Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 102100038297 Kallikrein-1 Human genes 0.000 claims 1
- 101710176219 Kallikrein-1 Proteins 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000011219 Netherton syndrome Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 238000002399 angioplasty Methods 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 238000013176 antiplatelet therapy Methods 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 238000007887 coronary angioplasty Methods 0.000 claims 1
- 230000007547 defect Effects 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000003889 eye drop Substances 0.000 claims 1
- 229940012356 eye drops Drugs 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 230000003480 fibrinolytic effect Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000018578 heart valve disease Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 230000007954 hypoxia Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000001802 infusion Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- -1 methylene, substituted ethylene, substituted propylene, substituted butylene Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 210000003462 vein Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562126424P | 2015-02-27 | 2015-02-27 | |
| US62/126,424 | 2015-02-27 | ||
| PCT/US2016/020116 WO2016138532A1 (en) | 2015-02-27 | 2016-02-29 | Substituted pyrazole compounds as serine protease inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020177836A Division JP2021020939A (ja) | 2015-02-27 | 2020-10-23 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018506563A JP2018506563A (ja) | 2018-03-08 |
| JP2018506563A5 true JP2018506563A5 (https=) | 2019-04-04 |
Family
ID=56789853
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017545289A Pending JP2018506563A (ja) | 2015-02-27 | 2016-02-29 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
| JP2020177836A Pending JP2021020939A (ja) | 2015-02-27 | 2020-10-23 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
| JP2023000535A Pending JP2023040150A (ja) | 2015-02-27 | 2023-01-05 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
| JP2025038259A Pending JP2025090726A (ja) | 2015-02-27 | 2025-03-11 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020177836A Pending JP2021020939A (ja) | 2015-02-27 | 2020-10-23 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
| JP2023000535A Pending JP2023040150A (ja) | 2015-02-27 | 2023-01-05 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
| JP2025038259A Pending JP2025090726A (ja) | 2015-02-27 | 2025-03-11 | セリンプロテアーゼ阻害剤としての置換ピラゾール化合物 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US10532995B2 (https=) |
| EP (1) | EP3261639B1 (https=) |
| JP (4) | JP2018506563A (https=) |
| KR (1) | KR102824411B1 (https=) |
| CN (1) | CN107405333A (https=) |
| AU (2) | AU2016224974B2 (https=) |
| BR (1) | BR112017018092A2 (https=) |
| CA (1) | CA2977993A1 (https=) |
| DK (1) | DK3261639T3 (https=) |
| ES (1) | ES2931460T3 (https=) |
| HK (1) | HK1246164A1 (https=) |
| HR (1) | HRP20221287T1 (https=) |
| HU (1) | HUE060104T2 (https=) |
| IL (1) | IL253876A0 (https=) |
| LT (1) | LT3261639T (https=) |
| MX (1) | MX383930B (https=) |
| PL (1) | PL3261639T3 (https=) |
| PT (1) | PT3261639T (https=) |
| RU (1) | RU2017131562A (https=) |
| SG (2) | SG10201907699YA (https=) |
| SI (1) | SI3261639T1 (https=) |
| WO (1) | WO2016138532A1 (https=) |
| ZA (1) | ZA201705749B (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| CN107405333A (zh) * | 2015-02-27 | 2017-11-28 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物 |
| MY198346A (en) | 2015-10-01 | 2023-08-28 | Biocryst Pharm Inc | Human plasma kallikrein inhibitors |
| IL263235B (en) | 2016-05-31 | 2022-07-01 | Kalvista Pharmaceuticals Ltd | History of pyrazoles as plasma kallikrein inhibitors |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| JP7210540B2 (ja) | 2017-08-04 | 2023-01-23 | 武田薬品工業株式会社 | 血漿カリクレインの阻害剤およびその使用 |
| HUE057912T2 (hu) | 2017-11-29 | 2022-06-28 | Kalvista Pharmaceuticals Ltd | Plazma kallikrein inhibitort tartalmazó dózisformák |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
| AU2019269544B2 (en) * | 2018-05-16 | 2024-03-21 | Infex Therapeutics Limited | Antibacterial compounds |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| EP4463185A4 (en) * | 2022-01-13 | 2026-03-18 | Childrens Hospital Med Ct | Thrombin and fibrinogen as targets for the diagnosis and treatment of atopic dermatitis |
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