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
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- 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 |
|---|---|---|---|
| AU2016900478A AU2016900478A0 (en) | 2016-02-12 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| AU2016900478 | 2016-02-12 | ||
| AU2016902593 | 2016-07-01 | ||
| AU2016902593A AU2016902593A0 (en) | 2016-07-01 | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof | |
| 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 (enExample) | 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 (enExample) |
| EP (2) | EP3414244A4 (enExample) |
| JP (2) | JP6849197B2 (enExample) |
| KR (2) | KR20180119582A (enExample) |
| CN (2) | CN109071533B (enExample) |
| AU (2) | AU2017217238B2 (enExample) |
| BR (2) | BR112018016484B1 (enExample) |
| CA (2) | CA3013819A1 (enExample) |
| CO (2) | CO2018009068A2 (enExample) |
| EA (2) | EA037302B9 (enExample) |
| IL (2) | IL261118A (enExample) |
| MX (1) | MX388745B (enExample) |
| PH (2) | PH12018501686A1 (enExample) |
| SG (2) | SG11201806700RA (enExample) |
| TW (2) | TW201738206A (enExample) |
| WO (2) | WO2017136871A1 (enExample) |
| ZA (2) | ZA201805664B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201806700RA (en) * | 2016-02-12 | 2018-09-27 | Pharmaxis Ltd | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof |
| CN110709385A (zh) * | 2017-03-02 | 2020-01-17 | 法玛西斯有限公司 | 赖氨酰氧化酶的卤代烯丙胺吡唑衍生物抑制剂及其用途 |
| GB201716871D0 (en) | 2017-10-13 | 2017-11-29 | Inst Of Cancer Research: Royal Cancer Hospital | Compounds |
| CN110605143B (zh) * | 2017-10-27 | 2022-07-19 | 苏州大学 | 有机铁盐作为催化剂在合成烷基硼酯化合物中的应用 |
| TW201940483A (zh) | 2018-03-12 | 2019-10-16 | 美商艾伯維有限公司 | 酪胺酸激酶２介導的傳訊之抑制劑 |
| 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 |
| AR115906A1 (es) | 2018-08-03 | 2021-03-10 | Pharmaxis Ltd | Derivados de haloalilamina sulfona como inhibidores de lisil oxidasas |
| 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 |
| 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 |
| WO2020146639A2 (en) * | 2019-01-11 | 2020-07-16 | Viscient Biosciences, Inc. | Compositions and methods for the diagnosis and treatment of diseases of the liver |
| WO2020161209A1 (en) | 2019-02-06 | 2020-08-13 | Syngenta Crop Protection Ag | Herbicidal fused pyridazine compounds |
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| MX2022001031A (es) * | 2019-07-25 | 2022-02-23 | Pharmaxis Ltd | Inhibidores derivados de difluorohaloalilamina-sulfona de lisil-oxidasas, metodos de preparacion y usos de los mismos. |
| JP7629442B2 (ja) | 2019-07-29 | 2025-02-13 | ヘパリジェニックス ゲーエムベーハー | 肝臓再生を促進または肝細胞死を縮減もしくは防止するためのヘテロアリール置換ピラゾロ－ピリジンタンパク質キナーゼ阻害剤 |
| CA3164361A1 (en) | 2020-01-15 | 2021-07-22 | Heparegenix Gmbh | 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases |
| WO2021155439A1 (en) * | 2020-02-05 | 2021-08-12 | Pharmaxis Ltd. | 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 |
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| US12686665B2 (en) | 2021-10-01 | 2026-07-21 | 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 |
| IL321907A (en) * | 2023-01-09 | 2025-09-01 | Univ Florida | 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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| SG11201806700RA (en) | 2016-02-12 | 2018-09-27 | Pharmaxis Ltd | Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof |
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2017
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