JP2020536924A5 - - Google Patents
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- JP2020536924A5 JP2020536924A5 JP2020520592A JP2020520592A JP2020536924A5 JP 2020536924 A5 JP2020536924 A5 JP 2020536924A5 JP 2020520592 A JP2020520592 A JP 2020520592A JP 2020520592 A JP2020520592 A JP 2020520592A JP 2020536924 A5 JP2020536924 A5 JP 2020536924A5
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- JP
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- Prior art keywords
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- cancer
- pharmaceutically acceptable
- acceptable salt
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- Prior art date
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- 125000005842 heteroatom Chemical group 0.000 claims description 34
- 125000000217 alkyl group Chemical group 0.000 claims description 33
- 229910052760 oxygen Inorganic materials 0.000 claims description 32
- 229910052717 sulfur Inorganic materials 0.000 claims description 31
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 14
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 13
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 11
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 6
- 125000003107 substituted aryl group Chemical group 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 125000002837 carbocyclic group Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 42
- 150000003839 salts Chemical class 0.000 claims 33
- 206010028980 Neoplasm Diseases 0.000 claims 14
- 101001041393 Homo sapiens Serine protease HTRA1 Proteins 0.000 claims 11
- 102000055008 Matrilin Proteins Human genes 0.000 claims 11
- 108010072582 Matrilin Proteins Proteins 0.000 claims 11
- 102100021119 Serine protease HTRA1 Human genes 0.000 claims 11
- 201000011510 cancer Diseases 0.000 claims 11
- 238000000034 method Methods 0.000 claims 11
- 239000003795 chemical substances by application Substances 0.000 claims 10
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 10
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 10
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 10
- 229940121922 Lysyl oxidase inhibitor Drugs 0.000 claims 8
- 239000012472 biological sample Substances 0.000 claims 7
- 239000013074 reference sample Substances 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 102000004669 Protein-Lysine 6-Oxidase Human genes 0.000 claims 5
- 108010003894 Protein-Lysine 6-Oxidase Proteins 0.000 claims 5
- 238000011282 treatment Methods 0.000 claims 5
- 102000010909 Monoamine Oxidase Human genes 0.000 claims 4
- 108010062431 Monoamine oxidase Proteins 0.000 claims 4
- 102100026858 Protein-lysine 6-oxidase Human genes 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 230000004043 responsiveness Effects 0.000 claims 4
- 201000009030 Carcinoma Diseases 0.000 claims 3
- 230000003197 catalytic effect Effects 0.000 claims 3
- 230000014509 gene expression Effects 0.000 claims 3
- 125000001288 lysyl group Chemical group 0.000 claims 3
- 206010004593 Bile duct cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 210000000013 bile duct Anatomy 0.000 claims 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims 2
- 239000000090 biomarker Substances 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 230000000112 colonic effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 230000035800 maturation Effects 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 229940127557 pharmaceutical product Drugs 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 206010038038 rectal cancer Diseases 0.000 claims 2
- 201000001275 rectum cancer Diseases 0.000 claims 2
- 230000035945 sensitivity Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 238000011269 treatment regimen Methods 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 101100422577 Danio rerio stil gene Proteins 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Natural products C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- 101710143123 Mothers against decapentaplegic homolog 2 Proteins 0.000 claims 1
- 229940087098 Oxidase inhibitor Drugs 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 102000057208 Smad2 Human genes 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 150000002780 morpholines Chemical class 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 150000003053 piperidines Chemical class 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 230000004044 response Effects 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 150000004886 thiomorpholines Chemical class 0.000 claims 1
- 230000003827 upregulation Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 description 1
- 125000001188 haloalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1716871.7A GB201716871D0 (en) | 2017-10-13 | 2017-10-13 | Compounds |
| GB1716871.7 | 2017-10-13 | ||
| PCT/GB2018/052934 WO2019073251A1 (en) | 2017-10-13 | 2018-10-12 | INHIBITORS OF LYSYL OXIDASE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020536924A JP2020536924A (ja) | 2020-12-17 |
| JP2020536924A5 true JP2020536924A5 (https=) | 2021-11-11 |
| JP7385561B2 JP7385561B2 (ja) | 2023-11-22 |
Family
ID=60419229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020520592A Active JP7385561B2 (ja) | 2017-10-13 | 2018-10-12 | 化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11325915B2 (https=) |
| EP (1) | EP3694857A1 (https=) |
| JP (1) | JP7385561B2 (https=) |
| CN (1) | CN111212836B (https=) |
| CA (1) | CA3076566A1 (https=) |
| GB (1) | GB201716871D0 (https=) |
| IL (1) | IL273727B2 (https=) |
| WO (1) | WO2019073251A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201716871D0 (en) | 2017-10-13 | 2017-11-29 | Inst Of Cancer Research: Royal Cancer Hospital | Compounds |
| GB201809295D0 (en) | 2018-06-06 | 2018-07-25 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| 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 |
| GB201818750D0 (en) * | 2018-11-16 | 2019-01-02 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| AU2020317374A1 (en) * | 2019-07-25 | 2022-02-03 | Pharmaxis Ltd. | Difluorohaloallylamine sulfone derivative inhibitors of lysyl oxidases, methods of preparation, and uses thereof |
| IL326597A (en) | 2019-10-07 | 2026-04-01 | Contineum Therapeutics Inc | Muscarinic M1 acetylcholine receptor antagonists |
| US11752149B2 (en) | 2019-12-02 | 2023-09-12 | Pipeline Therapeutics, Inc. | Muscarinic acetylcholine M1 receptor antagonists |
| US12578335B2 (en) | 2020-02-05 | 2026-03-17 | Syntara Limited | Bioprobes for lysyl oxidases and uses thereof |
| US20230310445A1 (en) * | 2020-04-21 | 2023-10-05 | Anovia Biosciences, Inc. | Lox enzyme inhibiting methods and compositions |
| US12233056B2 (en) | 2022-04-06 | 2025-02-25 | Syntara Limited | Lysyl oxidase inhibitors for treating myeloid malignancies |
| CN116763899B (zh) * | 2023-07-17 | 2026-02-24 | 大连医科大学附属第一医院 | Htra1抑制剂在制备治疗胰腺炎-癌转化的药物中的应用 |
| CN119732928B (zh) * | 2024-12-26 | 2026-04-07 | 国家纳米科学中心 | 一种抑制胶原纤维形成的药物分子及其应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4992546A (en) | 1987-07-31 | 1991-02-12 | Warner-Lambert Company | Process for preparing 6,8-diazabicyclo[3.2.2]nonane derivatives |
| DE4402933A1 (de) | 1994-02-01 | 1995-08-03 | Kali Chemie Pharma Gmbh | Neue 3-Benzoyl-3,7-diazabicyclo[3,3,1] nonan-Verbindungen enthaltende Arzneimittel |
| CA2657623A1 (en) * | 2006-07-14 | 2008-01-17 | Merck & Co., Inc. | Bridged diazepan orexin receptor antagonists |
| BRPI0821676A2 (pt) | 2007-12-21 | 2015-06-16 | Astrazeneca Ab | Composto, composição farmacêutica, e, processo para a preparação dos compostos. |
| WO2010028011A1 (en) | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclononanes and uses thereof |
| WO2011119345A2 (en) | 2010-03-25 | 2011-09-29 | Abbott Laboratories | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
| AU2014348518B2 (en) * | 2013-11-14 | 2019-01-03 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| US9994570B2 (en) | 2014-11-26 | 2018-06-12 | Merck Sharp & Dohme Corp. | Bridged diazepane orexin receptor antagonists |
| EP3267996B1 (en) * | 2015-03-12 | 2020-11-11 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of irak4 activity |
| EP3317258A4 (en) * | 2015-07-01 | 2019-06-26 | Pharmakea, Inc. | LYSYL OXIDASE LIKE 2 INHIBITORS AND USES THEREOF |
| ES2880766T3 (es) | 2016-02-09 | 2021-11-25 | Pharmakea Inc | Inhibidores de quinolinona lisil oxidasa similar al tipo 2 y usos de los mismos |
| 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 |
| GB201602934D0 (en) | 2016-02-19 | 2016-04-06 | Cancer Res Inst Royal | Compounds |
| US20210009551A1 (en) | 2016-06-02 | 2021-01-14 | The Regents Of The University Of California | Compounds and methods for treating fibrosis or cancer |
| WO2018048928A1 (en) | 2016-09-07 | 2018-03-15 | Pharmakea, Inc. | Chemical probes of lysyl oxidase-like 2 and uses thereof |
| WO2018048930A1 (en) | 2016-09-07 | 2018-03-15 | Pharmakea, Inc. | Lysyl oxidase-like 2 inhibitors and uses thereof |
| KR102587178B1 (ko) | 2016-09-07 | 2023-10-06 | 파마케아, 인크. | 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법 |
| 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 |
-
2017
- 2017-10-13 GB GBGB1716871.7A patent/GB201716871D0/en not_active Ceased
-
2018
- 2018-10-12 CN CN201880065806.5A patent/CN111212836B/zh active Active
- 2018-10-12 WO PCT/GB2018/052934 patent/WO2019073251A1/en not_active Ceased
- 2018-10-12 EP EP18792450.1A patent/EP3694857A1/en active Pending
- 2018-10-12 US US16/755,739 patent/US11325915B2/en active Active
- 2018-10-12 JP JP2020520592A patent/JP7385561B2/ja active Active
- 2018-10-12 CA CA3076566A patent/CA3076566A1/en active Pending
-
2020
- 2020-03-31 IL IL273727A patent/IL273727B2/en unknown
-
2022
- 2022-04-04 US US17/712,541 patent/US12060360B2/en active Active
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