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 (enExample) | 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 (enExample) |
| EP (1) | EP3261639B1 (enExample) |
| JP (4) | JP2018506563A (enExample) |
| KR (1) | KR102824411B1 (enExample) |
| CN (1) | CN107405333A (enExample) |
| AU (2) | AU2016224974B2 (enExample) |
| BR (1) | BR112017018092A2 (enExample) |
| CA (1) | CA2977993A1 (enExample) |
| DK (1) | DK3261639T3 (enExample) |
| ES (1) | ES2931460T3 (enExample) |
| HK (1) | HK1246164A1 (enExample) |
| HR (1) | HRP20221287T1 (enExample) |
| HU (1) | HUE060104T2 (enExample) |
| IL (1) | IL253876A0 (enExample) |
| LT (1) | LT3261639T (enExample) |
| MX (1) | MX383930B (enExample) |
| PL (1) | PL3261639T3 (enExample) |
| PT (1) | PT3261639T (enExample) |
| RU (1) | RU2017131562A (enExample) |
| SG (2) | SG11201706411YA (enExample) |
| SI (1) | SI3261639T1 (enExample) |
| WO (1) | WO2016138532A1 (enExample) |
| ZA (1) | ZA201705749B (enExample) |
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 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| AU2016224974B2 (en) * | 2015-02-27 | 2019-09-26 | Verseon Corporation | Substituted pyrazole compounds as serine protease inhibitors |
| PL3355890T3 (pl) | 2015-10-01 | 2022-02-21 | Biocryst Pharmaceuticals, Inc. | Inhibitory ludzkiej kalikreiny osoczowej |
| WO2017207983A1 (en) | 2016-05-31 | 2017-12-07 | Kalvista Pharmaceuticals Limited | Pyrazole derivatives 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 |
| EP3661922B1 (en) * | 2017-08-04 | 2024-10-23 | Takeda Pharmaceutical Company Limited | Inhibitors of plasma kallikrein and uses thereof |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| JP7078722B2 (ja) | 2017-11-29 | 2022-05-31 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレイン阻害剤を含む剤形 |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
| SG11202011298YA (en) * | 2018-05-16 | 2020-12-30 | Infex Therapeutics Ltd | Antibacterial compounds |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | 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 |
| US20250177502A1 (en) * | 2022-01-13 | 2025-06-05 | Children's Hospital Medical Center | Thrombin and fibrinogen as targets for atopic dermatitis diagnosis and treatment |
Family Cites Families (124)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE627393A (enExample) | 1962-01-23 | |||
| BE793955A (fr) | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | Arylpiperazines et leur procede de preparation |
| DE2409753A1 (de) | 1974-03-01 | 1975-09-11 | Basf Ag | Substituierte pyrazole |
| US4160452A (en) | 1977-04-07 | 1979-07-10 | Alza Corporation | Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| PH23506A (en) | 1986-05-23 | 1989-08-16 | Smithkline Beckman Corp | 1-aralkyl-substituted-1,2,4,-triazole-5-thiols as dopamine- -hydroxylase inhibitors |
| JPH089541B2 (ja) | 1988-03-07 | 1996-01-31 | 三井東圧化学株式会社 | ピラゾール類を主成分とする脳浮腫抑制剤 |
| JP2784925B2 (ja) | 1988-09-07 | 1998-08-13 | 日本農薬株式会社 | ３又は５−フェニルピラゾール類又はその塩及び除草剤 |
| DK0495421T3 (da) | 1991-01-15 | 1996-12-09 | Alcon Lab Inc | Anvendelse af carragenaner i topiske ophthalmiske sammensætninger |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| JP3810097B2 (ja) | 1993-01-15 | 2006-08-16 | 明治製菓株式会社 | ピロリジン−２−イルカルボニル複素環式化合物誘導体 |
| US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| RO118291B1 (ro) | 1993-11-30 | 2003-04-30 | Searle & Co | Derivati de pirazol 1,3,4,5 - tetrasubstituiti si compozitie farmaceutica care ii contine |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| DE69532817T2 (de) | 1994-11-10 | 2005-01-13 | Millenium Pharmaceuticals, Inc., Cambridge | Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose |
| US5733955A (en) | 1995-02-10 | 1998-03-31 | The Goodyear Tire & Rubber Company | Asphalt cement modification |
| JP3663522B2 (ja) | 1995-08-12 | 2005-06-22 | 日本農薬株式会社 | 植物生育調節用組成物及びその使用方法 |
| US5756529A (en) | 1995-09-29 | 1998-05-26 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies |
| US5739083A (en) | 1995-10-13 | 1998-04-14 | Otsuka Kagaku Kabushiki Kaisha | Pyrazole derivatives and insecticidal compositions containing the derivative as active component |
| US5792761A (en) | 1996-08-12 | 1998-08-11 | Merck & Co., Inc. | Thrombin inhibitors |
| DE19632773A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Thrombininhibitoren |
| GB9622370D0 (en) | 1996-10-28 | 1997-01-08 | Merck Sharp & Dohme | Therapeutic agents |
| US5869500A (en) | 1996-12-13 | 1999-02-09 | Hoffmann-La Roche Inc. | Pyridone compounds useful in treating Alzheimer's disease |
| CN1246847A (zh) | 1996-12-23 | 2000-03-08 | 杜邦药品公司 | 作为Xa因子抑制剂的含氮杂芳族化合物 |
| AU718048B2 (en) | 1997-03-21 | 2000-04-06 | Novartis Ag | Pyrazole derivatives as herbicides |
| WO2000009500A2 (en) | 1998-08-11 | 2000-02-24 | Nihon Bayer Agrochem K.K. | Nematicidal pyrazoles |
| KR20000047461A (ko) | 1998-12-29 | 2000-07-25 | 성재갑 | 트롬빈 억제제 |
| SE9900070D0 (sv) | 1999-01-13 | 1999-01-13 | Astra Ab | New use |
| AR023510A1 (es) | 1999-04-21 | 2002-09-04 | Astrazeneca Ab | Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina. |
| AU5020400A (en) | 1999-05-20 | 2000-12-12 | E.I. Du Pont De Nemours And Company | Heteroaryloxypyrimidine insecticides and acaricides |
| WO2001012189A1 (en) | 1999-08-12 | 2001-02-22 | Pharmacia Italia S.P.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| US6632815B2 (en) | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| JP2003509412A (ja) | 1999-09-17 | 2003-03-11 | シーオーアール セラピューティクス インコーポレイテッド | Ｘａ因子阻害剤 |
| MXPA02005428A (es) | 1999-12-02 | 2002-11-29 | Novartis Ag | Aminoheterociclilamidas como plaguicidas y agentes antiparasiticos. |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| AU2002308748A1 (en) | 2001-05-16 | 2002-11-25 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
| US6589997B2 (en) | 2001-06-29 | 2003-07-08 | North Shore-Long Island Jewish Health System | Small-molecule modulators of hepatocyte growth factor/scatter factor activities |
| SI21097A (sl) | 2001-12-04 | 2003-06-30 | Univerza V Ljubljani | Inhibitorji trombina |
| SE0200198D0 (sv) | 2002-01-23 | 2002-01-23 | Astrazeneca Ab | New use |
| WO2003062206A2 (en) | 2002-01-23 | 2003-07-31 | Arena Pharmaceuticals, Inc. | Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto |
| JP2003313103A (ja) | 2002-02-20 | 2003-11-06 | Sankyo Agro Kk | ４−アシルアミノピラゾール誘導体を有効成分として含有する農薬 |
| GB0214139D0 (en) | 2002-06-19 | 2002-07-31 | Glaxo Group Ltd | Chemical compounds |
| DE10229070A1 (de) | 2002-06-28 | 2004-01-15 | Merck Patent Gmbh | Phenylderivate 5 |
| TW200424183A (en) | 2002-08-09 | 2004-11-16 | Nps Pharma Inc | New compounds |
| AU2003274025A1 (en) | 2002-10-17 | 2004-05-04 | Syngenta Participations Ag | Pyridine derivatives useful as herbicides |
| US7192976B2 (en) | 2002-12-21 | 2007-03-20 | Angion Biomedica Corporation | Small molecule modulators of hepatocyte growth factor (scatter factor) activity |
| BR0317659A (pt) | 2002-12-23 | 2005-12-06 | Aventis Pharma Gmbh | Derivados de pirazol como inibidores de fator xa |
| WO2004058722A1 (en) | 2002-12-24 | 2004-07-15 | Arena Pharmaceuticals, Inc. | Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a |
| US20040147561A1 (en) | 2002-12-27 | 2004-07-29 | Wenge Zhong | Pyrid-2-one derivatives and methods of use |
| JP2004231528A (ja) | 2003-01-28 | 2004-08-19 | Sankyo Agro Kk | アミド誘導体 |
| GB0308318D0 (en) | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
| ES2350837T3 (es) | 2003-05-01 | 2011-01-27 | Bristol-Myers Squibb Company | Compuestos de pirazol-amida sustituidos con arilo útiles como inhibidores de quinasas. |
| US7417152B2 (en) | 2003-05-02 | 2008-08-26 | Elan Pharmaceuticals, Inc. | 4-bromo-5-(2-chloro-benzoylamino)-1H-pyrazole-3-carboxylic acid amide derivatives and related compounds as bradykinin B1 receptor antagonists for the treatment of inflammatory diseases |
| EP1479679A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Triazole-derivatives as factor Xa inhibitors |
| US7223780B2 (en) | 2003-05-19 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Triazole-derivatives as blood clotting enzyme factor Xa inhibitors |
| WO2005030751A2 (en) | 2003-09-08 | 2005-04-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| MXPA06002853A (es) | 2003-09-11 | 2006-06-14 | Kemia Inc | Inhibidores citoquina. |
| WO2005030128A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
| TW200526588A (en) | 2003-11-17 | 2005-08-16 | Smithkline Beecham Corp | Chemical compounds |
| US20080188527A1 (en) | 2003-12-23 | 2008-08-07 | Cashman John R | Synthetic Compounds and Derivatives as Modulators of Smoking or Nicotine Ingestion and Lung Cancer |
| EP1735319B1 (en) | 2004-03-26 | 2017-05-03 | MethylGene Inc. | Inhibitors of histone deacetylase |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7235530B2 (en) | 2004-09-27 | 2007-06-26 | Dyax Corporation | Kallikrein inhibitors and anti-thrombolytic agents and uses thereof |
| CA2594488C (en) | 2005-01-10 | 2015-04-28 | University Of Connecticut | Novel heteropyrrole analogs acting on cannabinoid receptors |
| JPWO2006109846A1 (ja) | 2005-04-06 | 2008-11-20 | 武田薬品工業株式会社 | トリアゾール誘導体およびその用途 |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| CN100427481C (zh) | 2005-05-26 | 2008-10-22 | 沈阳化工研究院 | 一种芳基醚类化合物及其制备与应用 |
| US20090227588A1 (en) | 2005-12-05 | 2009-09-10 | Roman Wolfgang Fleck | Substituted pyrazole compounds useful as soluble epoxide hyrolase inhibitors |
| EP2016068A1 (en) | 2006-05-03 | 2009-01-21 | AstraZeneca AB | Pyrazole derivatives and their use as pi3k inhibitors |
| CA2691214A1 (en) | 2006-06-09 | 2007-12-21 | Kemia, Inc. | Therapy using cytokine inhibitors |
| MX2008016523A (es) * | 2006-06-30 | 2009-01-19 | Astrazeneca Ab | Derivados de pirimidina utiles en el tratamiento de cancer. |
| DE102006032824A1 (de) | 2006-07-14 | 2008-01-17 | Bayer Healthcare Ag | Substituierte Indazole |
| AR061996A1 (es) | 2006-07-17 | 2008-08-10 | Boehringer Ingelheim Int | Indicaciones para los inhibidores directos de la trombina en el campo cardiovascular |
| JP5322935B2 (ja) | 2006-07-31 | 2013-10-23 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬 |
| WO2008023235A1 (en) | 2006-08-25 | 2008-02-28 | Pfizer Products Inc. | Pyrazole derivatives as anti-platelet and anti-thrombotic agents |
| WO2008062739A1 (en) | 2006-11-20 | 2008-05-29 | Japan Tobacco Inc. | Pyrazoles and use thereof as drugs |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| EP2121619A2 (en) | 2006-11-24 | 2009-11-25 | AC Immune S.A. | Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
| WO2008079277A1 (en) | 2006-12-22 | 2008-07-03 | Millennium Pharmaceuticals, Inc. | Certain pyrazoline derivatives with kinase inhibitory activity |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008105383A1 (ja) | 2007-02-26 | 2008-09-04 | Toray Industries, Inc. | ピラゾール誘導体およびその医薬用途 |
| US20090011833A1 (en) * | 2007-07-03 | 2009-01-08 | Seelig Jerald C | Descending Qualification Community Game |
| GB0714129D0 (en) | 2007-07-19 | 2007-08-29 | Smithkline Beecham Corp | compounds |
| JPWO2009020137A1 (ja) | 2007-08-06 | 2010-11-04 | 大日本住友製薬株式会社 | アミノピラゾールアミド誘導体 |
| EP2196459B1 (en) | 2007-09-28 | 2016-11-02 | Takeda Pharmaceutical Company Limited | 5-membered heterocyclic compound |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US8658685B2 (en) | 2008-01-31 | 2014-02-25 | Activesite Pharmaceuticals, Inc. | Methods for treatment of kallikrein-related disorders |
| CN101990433B (zh) | 2008-02-07 | 2014-11-05 | 马萨诸塞眼科耳科诊所 | 提高Atoh1表达的化合物 |
| CN102088973A (zh) | 2008-05-15 | 2011-06-08 | 杜克大学 | 与热休克转录因子激活化合物及其靶标有关的组合物和方法 |
| CN102099340A (zh) | 2008-05-19 | 2011-06-15 | 先灵公司 | 作为因子ixa抑制剂的杂环化合物 |
| US8772326B2 (en) | 2008-07-10 | 2014-07-08 | Anigion Biomedica Corp. | Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity |
| TW201004941A (en) | 2008-07-16 | 2010-02-01 | Wyeth Corp | Alpha7 nicotinic acetylcholine receptor inhibitors |
| US8273900B2 (en) | 2008-08-07 | 2012-09-25 | Novartis Ag | Organic compounds |
| US20110190365A1 (en) | 2008-08-14 | 2011-08-04 | Bayer Crop Science Ag | Insecticidal 4-phenyl-1H-pyrazoles |
| US20110190352A1 (en) | 2008-08-19 | 2011-08-04 | Boehringer Ingelheim International Gmbh | Use of dabigatranetexilate for treating patients with pulmonary hypertension |
| EA201100358A1 (ru) | 2008-08-19 | 2011-10-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Дабигатран для чрескожной хирургической катетеризации сердца |
| WO2010020601A1 (en) | 2008-08-19 | 2010-02-25 | Boehringer Ingelheim International Gmbh | Dabigatran in tumour therapy |
| CA2758289A1 (en) | 2009-05-07 | 2010-11-11 | Gruenenthal Gmbh | Substituted aromatic carboxamide and urea derivatives as vanilloid receptor ligands |
| JP6155187B2 (ja) | 2010-03-30 | 2017-06-28 | ヴァーセオン コーポレイション | トロンビンの阻害剤としての多置換芳香族化合物 |
| CN101851207B (zh) | 2010-06-11 | 2012-01-25 | 扬州康伊尔医药科技有限公司 | 抗病毒化合物中间体1-酰基-吡唑-3-羧酸及其制备方法 |
| MX2012015292A (es) | 2010-06-24 | 2013-05-30 | Gilead Sciences Inc | Pirazolo[1, 5]pirimidinas en la forma de agentes antivirales. |
| WO2012020820A1 (ja) | 2010-08-11 | 2012-02-16 | 大正製薬株式会社 | ヘテロアリール－ピラゾール誘導体 |
| US8815271B2 (en) | 2010-11-03 | 2014-08-26 | Dow Agrosciences, Llc. | Pesticidal compositions and processes related thereto |
| WO2012065019A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of p13k alpha |
| US9169260B2 (en) | 2011-03-22 | 2015-10-27 | Merck Sharp & Dohme Corp. | Amidopyrazole inhibitors of interleukin receptor-associated kinases |
| WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| WO2012154880A1 (en) | 2011-05-09 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases |
| EP2709622A4 (en) | 2011-05-17 | 2015-03-04 | Plexxikon Inc | CINEMA MODULATION AND INDICATIONS THEREFOR |
| MX2014002208A (es) * | 2011-08-25 | 2014-05-28 | Hoffmann La Roche | Inhibidores de serina/treonina quinasa. |
| WO2013039985A2 (en) | 2011-09-12 | 2013-03-21 | The Johns Hopkins University | Serine protease inhibitors |
| WO2013049591A2 (en) * | 2011-09-29 | 2013-04-04 | Verseon Corporation | Dual inhibitor compounds and methods of use thereof |
| CN104066731B (zh) | 2011-12-27 | 2016-06-15 | 铁木医药有限公司 | 可用作sgc刺激剂的2-苄基、3-(嘧啶-2-基)取代的吡唑类 |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| CA2876382A1 (en) | 2012-06-14 | 2013-12-19 | Daiichi Sankyo Company, Limited | Piperidinylpyrazolopyridine derivative |
| MX2015009270A (es) * | 2013-01-18 | 2015-10-30 | Hoffmann La Roche | Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk). |
| WO2014145986A1 (en) * | 2013-03-15 | 2014-09-18 | Verseon, Inc. | Multisubstituted aromatic compounds as serine protease inhibitors |
| ES2791749T3 (es) * | 2013-03-15 | 2020-11-05 | Verseon Corp | Halogenopirazoles como inhibidores de la trombina |
| WO2015087995A1 (ja) | 2013-12-13 | 2015-06-18 | 第一三共株式会社 | シクロアルキル又はヘテロシクリルピラゾロピリジン誘導体 |
| EP3102568B1 (en) | 2014-02-06 | 2018-06-27 | Heptares Therapeutics Limited | Bicyclic aza compounds as muscarinic m1 receptor agonists. |
| AU2016224974B2 (en) * | 2015-02-27 | 2019-09-26 | Verseon Corporation | Substituted pyrazole compounds as serine protease inhibitors |
| WO2017072020A1 (en) | 2015-10-27 | 2017-05-04 | Boehringer Ingelheim International Gmbh | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
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