JPWO2021032938A5 - - Google Patents
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- JPWO2021032938A5 JPWO2021032938A5 JP2022503834A JP2022503834A JPWO2021032938A5 JP WO2021032938 A5 JPWO2021032938 A5 JP WO2021032938A5 JP 2022503834 A JP2022503834 A JP 2022503834A JP 2022503834 A JP2022503834 A JP 2022503834A JP WO2021032938 A5 JPWO2021032938 A5 JP WO2021032938A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- alkyl
- heterocyclyl
- independently selected
- optionally
- 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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- 125000000623 heterocyclic group Chemical group 0.000 claims 47
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 125000005843 halogen group Chemical group 0.000 claims 46
- 125000003118 aryl group Chemical group 0.000 claims 25
- 229910052717 sulfur Inorganic materials 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000004474 heteroalkylene group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 5
- 108010071241 Factor XIIa Proteins 0.000 claims 5
- 208000007536 Thrombosis Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 4
- 208000028185 Angioedema Diseases 0.000 claims 3
- 101800004538 Bradykinin Proteins 0.000 claims 3
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 3
- 102100035792 Kininogen-1 Human genes 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical group NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 3
- 150000002430 hydrocarbons Chemical class 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 239000004215 Carbon black (E152) Substances 0.000 claims 2
- 206010014522 Embolism venous Diseases 0.000 claims 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 235000010290 biphenyl Nutrition 0.000 claims 2
- 239000004305 biphenyl Substances 0.000 claims 2
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- 208000004043 venous thromboembolism Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000007257 Budd-Chiari syndrome Diseases 0.000 claims 1
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 208000032843 Hemorrhage 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
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000010183 Papilledema Diseases 0.000 claims 1
- 206010038886 Retinal oedema Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- -1 alkylb 1 Chemical group 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 238000011882 arthroplasty Methods 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000005008 bacterial sepsis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 238000002618 extracorporeal membrane oxygenation Methods 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 210000003709 heart valve Anatomy 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 230000002314 neuroinflammatory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000003331 prothrombotic effect Effects 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 201000011195 retinal edema Diseases 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 208000013223 septicemia Diseases 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2019/052358 WO2021032935A1 (en) | 2019-08-21 | 2019-08-21 | Enzyme inhibitors |
| GBPCT/GB2019/052358 | 2019-08-21 | ||
| PCT/GB2020/050334 WO2021032938A1 (en) | 2019-08-21 | 2020-02-13 | Enzyme inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022545159A JP2022545159A (ja) | 2022-10-26 |
| JP2022545159A5 JP2022545159A5 (https=) | 2023-02-20 |
| JPWO2021032938A5 true JPWO2021032938A5 (https=) | 2023-02-20 |
Family
ID=67777358
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022503834A Ceased JP2022545159A (ja) | 2019-08-21 | 2020-02-13 | 酵素阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20220289727A1 (https=) |
| EP (1) | EP4017850A1 (https=) |
| JP (1) | JP2022545159A (https=) |
| KR (1) | KR20220050925A (https=) |
| CN (1) | CN114258392A (https=) |
| AR (1) | AR118083A1 (https=) |
| AU (1) | AU2020331720A1 (https=) |
| BR (1) | BR112022001390A2 (https=) |
| CA (1) | CA3148028A1 (https=) |
| CO (1) | CO2022000270A2 (https=) |
| IL (1) | IL289778A (https=) |
| MX (1) | MX2022000811A (https=) |
| PH (1) | PH12022550118A1 (https=) |
| TW (1) | TW202115021A (https=) |
| WO (2) | WO2021032935A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| EP4017587A1 (en) * | 2019-08-21 | 2022-06-29 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| CN119264065A (zh) * | 2023-07-05 | 2025-01-07 | 中国科学院上海有机化学研究所 | 一类细胞程序性坏死抑制剂及其制备方法和用途 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL123986A (en) * | 1997-04-24 | 2011-10-31 | Organon Nv | Medicinal compounds |
| ATE306481T1 (de) * | 1999-05-12 | 2005-10-15 | Ortho Mcneil Pharm Inc | Pyrazolecarboxamide zur behandlung von fettleibigkeit und anderen erkrankungen |
| US7320992B2 (en) * | 2003-08-25 | 2008-01-22 | Amgen Inc. | Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use |
| NZ592039A (en) | 2003-08-27 | 2013-03-28 | Ophthotech Corp | Combination therapy for the treatment of ocular neovascular disorders |
| GB0518237D0 (en) * | 2005-09-07 | 2005-10-19 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| US8338437B2 (en) * | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| US8658635B2 (en) * | 2008-06-05 | 2014-02-25 | Glaxosmithkline Intellectual Property Development Limited | Benzpyrazol derivatives as inhibitors of PI3 kinases |
| EP2149552A1 (de) * | 2008-07-30 | 2010-02-03 | Bayer Schering Pharma AG | 5,6 substituierte Benzamid-Derivate als Modulatoren des EP2-Rezeptors |
| US9290485B2 (en) * | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| RU2013130019A (ru) * | 2010-12-03 | 2015-01-10 | Аллерган, Инк. | Новые производные азетидина в качестве модуляторов рецептора сфингозин 1-фосфата (s1p) |
| CN103415301A (zh) * | 2011-03-09 | 2013-11-27 | 德国杰特贝林生物制品有限公司 | 用于与包括与人造表面接触的医疗操作一起施用的fxii抑制剂 |
| US8404859B2 (en) * | 2011-03-16 | 2013-03-26 | Hoffmann-La Roche Inc. | Thiazole and thiophene compounds |
| US20120252853A1 (en) * | 2011-04-01 | 2012-10-04 | H. Lundbeck A/S | Positive allosteric modulators of nicotinic acetylcholine receptor |
| JP2014514302A (ja) * | 2011-04-13 | 2014-06-19 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｂａｃｅ阻害薬としての５−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用 |
| US9340500B2 (en) * | 2011-04-20 | 2016-05-17 | Shionogi & Co., Ltd. | Aromatic heterocyclic derivative having TRPV4-inhibiting activity |
| US9938269B2 (en) * | 2011-06-30 | 2018-04-10 | Abbvie Inc. | Inhibitor compounds of phosphodiesterase type 10A |
| BR112014013136B1 (pt) * | 2011-11-30 | 2020-05-26 | F. Hoffmann-La Roche Ag | Novos derivados de dihidroisoquinolina-1-ona biciclicos |
| AR091022A1 (es) * | 2012-05-11 | 2014-12-30 | Abbvie Inc | Inhibidores del nampt |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| MY174018A (en) | 2013-05-23 | 2020-03-04 | Kalvista Pharmaceuticals Ltd | Heterocyclic derivates |
| CN106257976B (zh) * | 2014-03-07 | 2021-02-02 | 拜奥克里斯特制药公司 | 人类血浆激肽释放酶抑制剂 |
| US10772881B2 (en) * | 2017-02-27 | 2020-09-15 | Russell Dahl | Quinolines that modulate SERCA and their use for treating disease |
| GB201421088D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| CN104592204B (zh) * | 2014-12-26 | 2017-05-17 | 华润赛科药业有限责任公司 | 达比加群衍生物及其制备方法和用途 |
| WO2017123518A1 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
| GB201604647D0 (en) * | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| WO2017176958A1 (en) * | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| AU2017269256B2 (en) | 2016-05-23 | 2021-02-25 | The Rockefeller University | Aminoacylindazole immunomodulators for treatment of autoimmune diseases |
| US10858319B2 (en) * | 2016-10-03 | 2020-12-08 | Iomet Pharma Ltd. | Indole derivatives for use in medicine |
| WO2018093695A1 (en) | 2016-11-18 | 2018-05-24 | Merck Sharp & Dohme Corp. | FACTOR XIIa INHIBITORS |
| EP3541381B1 (en) | 2016-11-18 | 2022-12-28 | Merck Sharp & Dohme LLC | Inhibitors of factor xiia |
| JP2021504490A (ja) | 2017-11-29 | 2021-02-15 | ザ ロックフェラー ユニバーシティーＴｈｅ Ｒｏｃｋｅｆｅｌｌｅｒ Ｕｎｉｖｅｒｓｉｔｙ | 自己免疫疾患治療用ピラノピラゾールおよびピラゾロピリジン免疫調節薬 |
| CN112585119A (zh) * | 2018-08-14 | 2021-03-30 | Epizyme股份有限公司 | 经取代的吲哚及其使用方法 |
| WO2021028645A1 (en) * | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| EP4017587A1 (en) * | 2019-08-21 | 2022-06-29 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
-
2019
- 2019-08-21 WO PCT/GB2019/052358 patent/WO2021032935A1/en not_active Ceased
- 2019-08-21 CN CN201980099443.1A patent/CN114258392A/zh active Pending
- 2019-08-21 EP EP19759702.4A patent/EP4017850A1/en not_active Withdrawn
-
2020
- 2020-02-13 PH PH1/2022/550118A patent/PH12022550118A1/en unknown
- 2020-02-13 KR KR1020227008854A patent/KR20220050925A/ko not_active Withdrawn
- 2020-02-13 AR ARP200100397A patent/AR118083A1/es not_active Application Discontinuation
- 2020-02-13 JP JP2022503834A patent/JP2022545159A/ja not_active Ceased
- 2020-02-13 WO PCT/GB2020/050334 patent/WO2021032938A1/en not_active Ceased
- 2020-02-13 US US17/634,593 patent/US20220289727A1/en active Pending
- 2020-02-13 BR BR112022001390A patent/BR112022001390A2/pt not_active Application Discontinuation
- 2020-02-13 CA CA3148028A patent/CA3148028A1/en active Pending
- 2020-02-13 TW TW109104466A patent/TW202115021A/zh unknown
- 2020-02-13 AU AU2020331720A patent/AU2020331720A1/en active Pending
- 2020-02-13 MX MX2022000811A patent/MX2022000811A/es unknown
-
2022
- 2022-01-12 IL IL289778A patent/IL289778A/en unknown
- 2022-01-17 CO CONC2022/0000270A patent/CO2022000270A2/es unknown
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