JP2019504898A5 - - Google Patents
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- JP2019504898A5 JP2019504898A5 JP2018561293A JP2018561293A JP2019504898A5 JP 2019504898 A5 JP2019504898 A5 JP 2019504898A5 JP 2018561293 A JP2018561293 A JP 2018561293A JP 2018561293 A JP2018561293 A JP 2018561293A JP 2019504898 A5 JP2019504898 A5 JP 2019504898A5
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- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- group
- halogen
- optionally substituted
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 320
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 96
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 80
- 229910052736 halogen Inorganic materials 0.000 claims 72
- 150000002367 halogens Chemical class 0.000 claims 72
- 125000001424 substituent group Chemical group 0.000 claims 50
- 229910052739 hydrogen Inorganic materials 0.000 claims 33
- 239000001257 hydrogen Substances 0.000 claims 33
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 8
- 150000003536 tetrazoles Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 206010016654 Fibrosis Diseases 0.000 claims 6
- 230000004761 fibrosis Effects 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 201000002793 renal fibrosis Diseases 0.000 claims 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 3
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 101001043352 Homo sapiens Lysyl oxidase homolog 2 Proteins 0.000 claims 2
- 101001043354 Homo sapiens Lysyl oxidase homolog 3 Proteins 0.000 claims 2
- 101001043351 Homo sapiens Lysyl oxidase homolog 4 Proteins 0.000 claims 2
- 206010067125 Liver injury Diseases 0.000 claims 2
- 102100021948 Lysyl oxidase homolog 2 Human genes 0.000 claims 2
- 102100021949 Lysyl oxidase homolog 3 Human genes 0.000 claims 2
- 102100021968 Lysyl oxidase homolog 4 Human genes 0.000 claims 2
- 208000007727 Muscle Tissue Neoplasms Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 208000024305 myofibroblastoma Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 1
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims 1
- 206010061424 Anal cancer Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005003 Bladder cancer 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
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010010317 Congenital absence of bile ducts Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 208000010496 Heart Arrest Diseases 0.000 claims 1
- 208000006050 Hemangiopericytoma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023421 Kidney fibrosis Diseases 0.000 claims 1
- 101710159002 L-lactate oxidase Proteins 0.000 claims 1
- -1 LOXLl Proteins 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 206010024612 Lipoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028594 Myocardial fibrosis Diseases 0.000 claims 1
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 108090000854 Oxidoreductases Proteins 0.000 claims 1
- 102000004316 Oxidoreductases Human genes 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000004362 Penile Induration Diseases 0.000 claims 1
- 208000020758 Peyronie disease Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100026858 Protein-lysine 6-oxidase Human genes 0.000 claims 1
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000033626 Renal failure acute Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000003252 Signet Ring Cell Carcinoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 206010047370 Vesicoureteric reflux Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 230000002491 angiogenic effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000011165 anus cancer Diseases 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 201000005271 biliary atresia Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000036952 cancer formation Effects 0.000 claims 1
- 208000002458 carcinoid tumor Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 210000003459 common hepatic duct Anatomy 0.000 claims 1
- 230000008021 deposition Effects 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 206010016629 fibroma Diseases 0.000 claims 1
- 206010049444 fibromatosis Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 239000002657 fibrous material Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000011066 hemangioma Diseases 0.000 claims 1
- 231100000234 hepatic damage Toxicity 0.000 claims 1
- 231100000753 hepatic injury Toxicity 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000010710 hepatitis C virus infection Diseases 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 230000008818 liver damage Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 201000011519 neuroendocrine tumor Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 201000008123 signet ring cell adenocarcinoma Diseases 0.000 claims 1
- 238000007614 solvation Methods 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 201000008618 vesicoureteral reflux Diseases 0.000 claims 1
- 208000031355 vesicoureteral reflux 1 Diseases 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- 230000037314 wound repair Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2016900478 | 2016-02-12 | ||
| AU2016900478A AU2016900478A0 (en) | 2016-02-12 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| AU2016902593A AU2016902593A0 (en) | 2016-07-01 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| AU2016902593 | 2016-07-01 | ||
| PCT/AU2017/000039 WO2017136870A1 (en) | 2016-02-12 | 2017-02-10 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019504898A JP2019504898A (ja) | 2019-02-21 |
| JP2019504898A5 true JP2019504898A5 (https=) | 2020-03-19 |
| JP6843888B2 JP6843888B2 (ja) | 2021-03-17 |
Family
ID=59562850
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018561294A Expired - Fee Related JP6849197B2 (ja) | 2016-02-12 | 2017-02-10 | リジルオキシダーゼのインドールおよびアザインドールハロアリルアミン誘導体阻害剤およびその使用 |
| JP2018561293A Active JP6843888B2 (ja) | 2016-02-12 | 2017-02-10 | リジルオキシダーゼのハロアリルアミンインドールおよびアザインドール誘導体阻害剤およびその使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018561294A Expired - Fee Related JP6849197B2 (ja) | 2016-02-12 | 2017-02-10 | リジルオキシダーゼのインドールおよびアザインドールハロアリルアミン誘導体阻害剤およびその使用 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US10717733B2 (https=) |
| EP (2) | EP3414226A4 (https=) |
| JP (2) | JP6849197B2 (https=) |
| KR (2) | KR20180119582A (https=) |
| CN (2) | CN109071533B (https=) |
| AU (2) | AU2017217239A1 (https=) |
| BR (2) | BR112018067442A8 (https=) |
| CA (2) | CA3013819A1 (https=) |
| CO (2) | CO2018009071A2 (https=) |
| EA (2) | EA037302B9 (https=) |
| IL (2) | IL261119B (https=) |
| MX (1) | MX388745B (https=) |
| PH (2) | PH12018501685A1 (https=) |
| SG (2) | SG11201806700RA (https=) |
| TW (2) | TW201738206A (https=) |
| WO (2) | WO2017136871A1 (https=) |
| ZA (2) | ZA201805675B (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6849197B2 (ja) | 2016-02-12 | 2021-03-24 | ファーマクシス リミテッド | リジルオキシダーゼのインドールおよびアザインドールハロアリルアミン誘導体阻害剤およびその使用 |
| US20200069648A1 (en) * | 2017-03-02 | 2020-03-05 | Pharmaxis Ltd. | Haloallylamine pyrazole derivative inhibitors of lysyl oxidases and uses thereof |
| GB201716871D0 (en) | 2017-10-13 | 2017-11-29 | Inst Of Cancer Research: Royal Cancer Hospital | Compounds |
| CN107903281B (zh) * | 2017-10-27 | 2019-10-29 | 苏州大学 | 一种合成烷基硼酯化合物的方法 |
| AU2019234574A1 (en) | 2018-03-12 | 2020-09-03 | Abbvie Inc. | Inhibitors of tyrosine kinase 2 mediated signaling |
| KR20190110740A (ko) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | 신규의 아릴 또는 헤테로아릴 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물 |
| KR20190110736A (ko) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | 신규의 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물 |
| CN112533897B (zh) | 2018-08-03 | 2023-07-14 | 法玛西斯有限公司 | 赖氨酰氧化酶的卤代烯丙胺砜衍生抑制剂及其用途 |
| TW202039486A (zh) | 2018-12-14 | 2020-11-01 | 南韓商柳韓洋行股份有限公司 | 三唑并吡啶-3-酮化物或其鹽及包含彼之醫藥組合物 |
| TWI835945B (zh) | 2018-12-14 | 2024-03-21 | 南韓商柳韓洋行股份有限公司 | 3,3-二氟烯丙胺化物或其鹽及包含彼的醫藥組合物 |
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| WO2020161209A1 (en) | 2019-02-06 | 2020-08-13 | Syngenta Crop Protection Ag | Herbicidal fused pyridazine compounds |
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| US12578335B2 (en) | 2020-02-05 | 2026-03-17 | Syntara Limited | Bioprobes for lysyl oxidases and uses thereof |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| EP4173639A4 (en) | 2020-06-26 | 2024-03-13 | RaQualia Pharma Inc. | METHOD FOR SELECTING A CANCER PATIENT FOR WHICH COMBINATION THERAPY OF A RETINOID AND A CANCER TREATMENT AGENT WILL BE EFFECTIVE, AND COMBINATION DRUG OF A RETINOID AND A CANCER TREATMENT AGENT |
| JP7384138B2 (ja) * | 2020-09-30 | 2023-11-21 | 株式会社島津製作所 | 電気泳動装置 |
| US11319319B1 (en) | 2021-04-07 | 2022-05-03 | Ventus Therapeutics U.S., Inc. | Compounds for inhibiting NLRP3 and uses thereof |
| AU2022357057A1 (en) * | 2021-10-01 | 2024-04-11 | Yuhan Corporation | Bicyclic fused ring derivative or salt thereof and pharmaceutical composition comprising same |
| US12233056B2 (en) | 2022-04-06 | 2025-02-25 | Syntara Limited | Lysyl oxidase inhibitors for treating myeloid malignancies |
| US12331048B2 (en) | 2022-10-31 | 2025-06-17 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors |
| WO2024151519A2 (en) * | 2023-01-09 | 2024-07-18 | University Of Florida Research Foundatin, Incorporated | Pparg modulators |
| CN117069611A (zh) * | 2023-07-12 | 2023-11-17 | 浙江工业大学 | 一种1-(2,4,6-三氯苯基)丙-2-酮o-甲基肟的制备方法 |
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| JP6849197B2 (ja) | 2016-02-12 | 2021-03-24 | ファーマクシス リミテッド | リジルオキシダーゼのインドールおよびアザインドールハロアリルアミン誘導体阻害剤およびその使用 |
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2017
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