JPWO2019228403A5 - - Google Patents
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- Publication number
- JPWO2019228403A5 JPWO2019228403A5 JP2020540731A JP2020540731A JPWO2019228403A5 JP WO2019228403 A5 JPWO2019228403 A5 JP WO2019228403A5 JP 2020540731 A JP2020540731 A JP 2020540731A JP 2020540731 A JP2020540731 A JP 2020540731A JP WO2019228403 A5 JPWO2019228403 A5 JP WO2019228403A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocycloalkyl
- cycloalkyl
- aryl
- heteroaryl
- 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.)
- Pending
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- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 82
- 125000000753 cycloalkyl group Chemical group 0.000 claims 75
- 125000000217 alkyl group Chemical group 0.000 claims 64
- 125000003118 aryl group Chemical group 0.000 claims 61
- 125000001072 heteroaryl group Chemical group 0.000 claims 60
- 229910052736 halogen Inorganic materials 0.000 claims 50
- 150000002367 halogens Chemical class 0.000 claims 50
- 150000001875 compounds Chemical class 0.000 claims 42
- 150000003839 salts Chemical class 0.000 claims 41
- 239000012453 solvate Substances 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 29
- 239000001257 hydrogen Substances 0.000 claims 29
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 23
- 229910052805 deuterium Inorganic materials 0.000 claims 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims 22
- 150000002431 hydrogen Chemical class 0.000 claims 20
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 6
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- -1 C1 -C 6 alkyl Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- BKIMMITUMNQMOS-UHFFFAOYSA-N nonane Chemical compound CCCCCCCCC BKIMMITUMNQMOS-UHFFFAOYSA-N 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- OXPIFHNJGOJJQZ-UHFFFAOYSA-N 2,7-diazaspiro[3.4]octane Chemical compound C1NCC11CNCC1 OXPIFHNJGOJJQZ-UHFFFAOYSA-N 0.000 claims 1
- DROZYMFJWSYDRY-UHFFFAOYSA-N 2,7-diazaspiro[3.5]nonane Chemical compound C1NCC11CCNCC1 DROZYMFJWSYDRY-UHFFFAOYSA-N 0.000 claims 1
- DDVRNOMZDQTUNS-UHFFFAOYSA-N 2,7-diazaspiro[4.4]nonane Chemical compound C1NCCC11CNCC1 DDVRNOMZDQTUNS-UHFFFAOYSA-N 0.000 claims 1
- WYZZNMWIWHRXRM-UHFFFAOYSA-N 2,8-diazaspiro[4.5]decane Chemical compound C1NCCC21CCNCC2 WYZZNMWIWHRXRM-UHFFFAOYSA-N 0.000 claims 1
- QPEJAHMNOVMSOZ-UHFFFAOYSA-N 2-azaspiro[3.3]heptane Chemical compound C1CCC21CNC2 QPEJAHMNOVMSOZ-UHFFFAOYSA-N 0.000 claims 1
- VSWICNJIUPRZIK-UHFFFAOYSA-N 2-piperideine Chemical compound C1CNC=CC1 VSWICNJIUPRZIK-UHFFFAOYSA-N 0.000 claims 1
- RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical compound C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 claims 1
- RHVACWSWOHDPBX-UHFFFAOYSA-N 5-azaspiro[2.3]hexane Chemical compound C1CC11CNC1 RHVACWSWOHDPBX-UHFFFAOYSA-N 0.000 claims 1
- GIBPTWPJEVCTGR-UHFFFAOYSA-N 6-azaspiro[2.5]octane Chemical compound C1CC11CCNCC1 GIBPTWPJEVCTGR-UHFFFAOYSA-N 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862677459P | 2018-05-29 | 2018-05-29 | |
| US62/677,459 | 2018-05-29 | ||
| US201862731003P | 2018-09-13 | 2018-09-13 | |
| US62/731,003 | 2018-09-13 | ||
| PCT/CN2019/089025 WO2019228403A1 (en) | 2018-05-29 | 2019-05-29 | Autotaxin inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021526123A JP2021526123A (ja) | 2021-09-30 |
| JP2021526123A5 JP2021526123A5 (https=) | 2022-05-27 |
| JPWO2019228403A5 true JPWO2019228403A5 (https=) | 2022-05-27 |
Family
ID=68697812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020540731A Pending JP2021526123A (ja) | 2018-05-29 | 2019-05-29 | オートタキシン阻害剤とその使用 |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP3728257A4 (https=) |
| JP (1) | JP2021526123A (https=) |
| CN (1) | CN111801328B (https=) |
| CA (1) | CA3089527A1 (https=) |
| WO (1) | WO2019228403A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11591342B2 (en) * | 2018-02-14 | 2023-02-28 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | Heterocyclic compound, application thereof and pharmaceutical composition comprising same |
| CN113912600A (zh) * | 2020-07-09 | 2022-01-11 | 苏州爱科百发生物医药技术有限公司 | 一种atx抑制剂及其制备方法和应用 |
| CN115916777B (zh) * | 2020-07-09 | 2024-07-12 | 苏州爱科百发生物医药技术有限公司 | 一种atx抑制剂及其制备方法和应用 |
| JP2023536159A (ja) * | 2020-07-31 | 2023-08-23 | ジェネンテック, インコーポレイテッド | 炎症性呼吸器疾患の増悪を治療するための方法 |
| CN114315825A (zh) * | 2020-09-30 | 2022-04-12 | 江西济民可信集团有限公司 | 吡啶并咪唑衍生物及其制备方法和应用 |
| EP4225756A2 (en) | 2020-10-06 | 2023-08-16 | Ildong Pharmaceutical Co., Ltd. | Autotaxin inhibitor compounds |
| US20240317736A1 (en) * | 2020-11-04 | 2024-09-26 | Xizang Haisco Pharmaceutical Co., Ltd. | Deuterated derivative as atx inhibitor, and application thereof |
| CN112675308B (zh) * | 2020-12-09 | 2023-05-05 | 中国人民解放军军事科学院军事医学研究院 | 抑制enpp2基因和/或蛋白表达的物质在制备治疗多发性骨髓瘤的药物中的应用 |
| US20240327407A1 (en) | 2021-01-05 | 2024-10-03 | Cadila Heal Thcare Limited | Novel inhibitors of autotaxin |
| EP4323356A1 (en) | 2021-04-13 | 2024-02-21 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| TW202342138A (zh) * | 2022-03-31 | 2023-11-01 | 大陸商蘇州愛科百發生物醫藥技術有限公司 | Atx抑制劑或其鹽的結晶形式及其制備方法與應用 |
| JP2025525350A (ja) * | 2022-06-24 | 2025-08-05 | エフ. ホフマン-ラ ロシュ アーゲー | Magl阻害剤としての新規複素環-カルボニル-環式化合物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2970255T1 (sl) * | 2013-03-14 | 2017-12-29 | Galapagos Nv | Spojine in farmacevtski sestavki le-teh za zdravljenje vnetnih motenj |
| EP3010922B1 (en) * | 2013-06-19 | 2017-03-15 | Galapagos NV | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| TW201908293A (zh) * | 2017-07-12 | 2019-03-01 | 美商必治妥美雅史谷比公司 | 作為rock抑制劑之5員及雙環雜環醯胺 |
| US11591342B2 (en) * | 2018-02-14 | 2023-02-28 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | Heterocyclic compound, application thereof and pharmaceutical composition comprising same |
-
2019
- 2019-05-29 CN CN201980015925.4A patent/CN111801328B/zh active Active
- 2019-05-29 CA CA3089527A patent/CA3089527A1/en active Pending
- 2019-05-29 WO PCT/CN2019/089025 patent/WO2019228403A1/en not_active Ceased
- 2019-05-29 JP JP2020540731A patent/JP2021526123A/ja active Pending
- 2019-05-29 EP EP19810155.2A patent/EP3728257A4/en not_active Withdrawn
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