JP2017528486A5 - - Google Patents
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- JP2017528486A5 JP2017528486A5 JP2017514899A JP2017514899A JP2017528486A5 JP 2017528486 A5 JP2017528486 A5 JP 2017528486A5 JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017528486 A5 JP2017528486 A5 JP 2017528486A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- medicament
- compound
- aryl
- 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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- 150000001875 compounds Chemical class 0.000 claims 31
- 239000003814 drug Substances 0.000 claims 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 26
- 125000003118 aryl group Chemical group 0.000 claims 17
- -1 3- (hydroxymethyl) phenyl Chemical group 0.000 claims 15
- 208000035475 disorder Diseases 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 12
- 125000004404 heteroalkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 208000007536 Thrombosis Diseases 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 102000001399 Kallikrein Human genes 0.000 claims 4
- 108060005987 Kallikrein Proteins 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 4
- 208000005189 Embolism Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000001435 Thromboembolism Diseases 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims 3
- 230000004968 inflammatory condition Effects 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 208000032382 Ischaemic stroke Diseases 0.000 claims 2
- 208000003788 Neoplasm Micrometastasis Diseases 0.000 claims 2
- 108090000190 Thrombin Proteins 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 229960004072 thrombin Drugs 0.000 claims 2
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease 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
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 206010014522 Embolism venous Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102100038297 Kallikrein-1 Human genes 0.000 claims 1
- 101710176219 Kallikrein-1 Proteins 0.000 claims 1
- 206010067125 Liver injury 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
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 1
- 108090000113 Plasma Kallikrein Proteins 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
- 206010063837 Reperfusion injury 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
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000001548 androgenic effect Effects 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
- 230000023555 blood coagulation Effects 0.000 claims 1
- 230000001269 cardiogenic effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 231100000012 chronic liver injury Toxicity 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 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
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 208000012947 ischemia reperfusion injury Diseases 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
- 230000009401 metastasis Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 150000003217 pyrazoles Chemical group 0.000 claims 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical group OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 1
- 230000002207 retinal effect Effects 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
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 230000008728 vascular permeability Effects 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462051511P | 2014-09-17 | 2014-09-17 | |
| US201462051585P | 2014-09-17 | 2014-09-17 | |
| US62/051,511 | 2014-09-17 | ||
| US62/051,585 | 2014-09-17 | ||
| PCT/US2015/050809 WO2016044662A1 (en) | 2014-09-17 | 2015-09-17 | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020087253A Division JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017528486A JP2017528486A (ja) | 2017-09-28 |
| JP2017528486A5 true JP2017528486A5 (OSRAM) | 2018-11-01 |
Family
ID=55533876
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514899A Pending JP2017528486A (ja) | 2014-09-17 | 2015-09-17 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
| JP2020087253A Pending JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020087253A Pending JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US10189810B2 (OSRAM) |
| EP (1) | EP3194369A4 (OSRAM) |
| JP (2) | JP2017528486A (OSRAM) |
| KR (1) | KR20170048410A (OSRAM) |
| CN (1) | CN106687445A (OSRAM) |
| AU (2) | AU2015317522A1 (OSRAM) |
| BR (1) | BR112017004704A2 (OSRAM) |
| CA (1) | CA2960790A1 (OSRAM) |
| IL (1) | IL250965A0 (OSRAM) |
| MX (1) | MX2017003624A (OSRAM) |
| RU (1) | RU2017112739A (OSRAM) |
| SG (1) | SG11201701940UA (OSRAM) |
| WO (1) | WO2016044662A1 (OSRAM) |
| ZA (1) | ZA201701799B (OSRAM) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2968297T3 (pl) * | 2013-03-15 | 2019-04-30 | Verseon Corp | Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej |
| 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 |
| EP3194369A4 (en) * | 2014-09-17 | 2018-02-28 | Verseon Corporation | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
| 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 |
| CN108884067B (zh) | 2016-02-19 | 2021-01-08 | 思普瑞特生物科学公司 | 可用于治疗癌症和糖尿病的6-杂环基-4-吗啉-4-基吡啶-2-酮化合物 |
| PT3416945T (pt) * | 2016-02-19 | 2020-09-11 | Sprint Bioscience Ab | Compostos de 6-aril-4-(morfolin-4-il)-1h-piridina-2-ona úteis para o tratamento do cancro e da diabetes |
| CN106008362B (zh) * | 2016-05-24 | 2018-08-10 | 杰达维（上海）医药科技发展有限公司 | 一种嘧啶衍生物的制备方法 |
| SG11201809922YA (en) | 2016-05-31 | 2018-12-28 | Kalvista Pharmaceuticals Ltd | 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 |
| EP3575286B1 (en) * | 2017-01-26 | 2022-05-11 | Mitsui Chemicals Agro, Inc. | Pyridone compound and bactericide for agricultural and horticultural use, which uses said compound as active ingredient |
| EP3612522A4 (en) | 2017-04-18 | 2021-07-07 | Celgene Quanticel Research, Inc. | THERAPEUTIC COMPOUNDS |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| RS63069B1 (sr) | 2017-11-29 | 2022-04-29 | Kalvista Pharmaceuticals Ltd | Dozni oblici koji sadrže inhibitor kalikreina plazme |
| CN110386932A (zh) | 2018-04-20 | 2019-10-29 | 艾科思莱德制药公司 | 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂 |
| WO2020014669A1 (en) * | 2018-07-13 | 2020-01-16 | Verseon Corporation | Thrombin inhibitors, formulations, and uses thereof |
| CN114206852A (zh) | 2019-08-09 | 2022-03-18 | 卡尔维斯塔制药有限公司 | 血浆激肽释放酶抑制剂 |
| CN110467601B (zh) * | 2019-08-29 | 2021-07-02 | 杭州市西溪医院 | 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用 |
| DE102020103516B4 (de) | 2020-02-11 | 2023-12-07 | Universität Zu Lübeck | Antivirale Wirkstoffe mit breiter Aktivität |
| BR102020009679A2 (pt) | 2020-05-14 | 2021-11-23 | Fundação Universidade Federal Do Abc - Ufabc | Anticorpos recombinantes humanos para inibição da calicreína tecidual humana 7 (klk7) e uso em doenças relacionadas ao processo de descamação da pele |
| WO2022115562A1 (en) | 2020-11-25 | 2022-06-02 | Deciphera Pharmaceuticals, Llc | Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection |
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-
2015
- 2015-09-17 EP EP15841577.8A patent/EP3194369A4/en not_active Withdrawn
- 2015-09-17 JP JP2017514899A patent/JP2017528486A/ja active Pending
- 2015-09-17 CA CA2960790A patent/CA2960790A1/en not_active Abandoned
- 2015-09-17 SG SG11201701940UA patent/SG11201701940UA/en unknown
- 2015-09-17 KR KR1020177007352A patent/KR20170048410A/ko not_active Withdrawn
- 2015-09-17 BR BR112017004704A patent/BR112017004704A2/pt not_active Application Discontinuation
- 2015-09-17 US US15/512,037 patent/US10189810B2/en active Active
- 2015-09-17 RU RU2017112739A patent/RU2017112739A/ru not_active Application Discontinuation
- 2015-09-17 MX MX2017003624A patent/MX2017003624A/es unknown
- 2015-09-17 AU AU2015317522A patent/AU2015317522A1/en not_active Abandoned
- 2015-09-17 CN CN201580050088.0A patent/CN106687445A/zh active Pending
- 2015-09-17 WO PCT/US2015/050809 patent/WO2016044662A1/en not_active Ceased
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2017
- 2017-03-06 IL IL250965A patent/IL250965A0/en unknown
- 2017-03-13 ZA ZA2017/01799A patent/ZA201701799B/en unknown
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2018
- 2018-12-07 US US16/213,272 patent/US20190359586A1/en not_active Abandoned
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2020
- 2020-03-26 AU AU2020202167A patent/AU2020202167A1/en not_active Abandoned
- 2020-05-19 JP JP2020087253A patent/JP2020143112A/ja active Pending
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