JPWO2020115683A5 - - Google Patents
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- Publication number
- JPWO2020115683A5 JPWO2020115683A5 JP2021525229A JP2021525229A JPWO2020115683A5 JP WO2020115683 A5 JPWO2020115683 A5 JP WO2020115683A5 JP 2021525229 A JP2021525229 A JP 2021525229A JP 2021525229 A JP2021525229 A JP 2021525229A JP WO2020115683 A5 JPWO2020115683 A5 JP WO2020115683A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- enantiomer
- pharmaceutically acceptable
- acceptable salt
- enantiomeric mixture
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 60
- 150000003839 salts Chemical class 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 39
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 10
- 206010060820 Joint injury Diseases 0.000 claims description 8
- 206010003246 arthritis Diseases 0.000 claims description 8
- 210000000845 cartilage Anatomy 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- -1 chloro, methyl Chemical group 0.000 claims description 6
- 230000001939 inductive effect Effects 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 210000004027 cell Anatomy 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 241000124008 Mammalia Species 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 210000003035 hyaline cartilage Anatomy 0.000 claims description 4
- 238000001727 in vivo Methods 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- VDFWWPFSYMHWLF-UHFFFAOYSA-N 2-oxabicyclo[2.2.1]heptane-3-carboxamide Chemical group C1CC2C(C(=O)N)OC1C2 VDFWWPFSYMHWLF-UHFFFAOYSA-N 0.000 claims description 2
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims description 2
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims description 2
- 210000001612 chondrocyte Anatomy 0.000 claims description 2
- 230000004069 differentiation Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 210000002744 extracellular matrix Anatomy 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims 1
- 230000002648 chondrogenic effect Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000000130 stem cell Anatomy 0.000 claims 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862776267P | 2018-12-06 | 2018-12-06 | |
| US62/776,267 | 2018-12-06 | ||
| PCT/IB2019/060454 WO2020115683A1 (en) | 2018-12-06 | 2019-12-04 | 5-hydroxy-7-oxabicyclo[2.2.1]heptane-2-carboxamide derivatives for inducing chondrogenesis for treating joint damage |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022509765A JP2022509765A (ja) | 2022-01-24 |
| JP2022509765A5 JP2022509765A5 (https=) | 2022-12-12 |
| JPWO2020115683A5 true JPWO2020115683A5 (https=) | 2022-12-12 |
| JP7471291B2 JP7471291B2 (ja) | 2024-04-19 |
Family
ID=68916501
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021525229A Active JP7471291B2 (ja) | 2018-12-06 | 2019-12-04 | 関節損傷を治療するための軟骨形成を誘導するための５－ヒドロキシ－７－オキサビシクロ［２．２．１］ヘプタン－２－カルボキサミド誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US12257243B2 (https=) |
| EP (1) | EP3891154B1 (https=) |
| JP (1) | JP7471291B2 (https=) |
| CN (1) | CN113015735B (https=) |
| ES (1) | ES2963508T3 (https=) |
| WO (1) | WO2020115683A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113015735B (zh) | 2018-12-06 | 2024-06-21 | 诺华股份有限公司 | 用于诱导软骨发生以治疗关节损害的5-羟基-7-氧杂双环[2.2.1]庚烷-2-甲酰胺衍生物 |
| ES2965684T3 (es) | 2018-12-06 | 2024-04-16 | Novartis Ag | Derivados de 6-hidroxi-8-oxatriciclo[3.2.1.02,4]octano-2-carboxamida para inducir condrogénesis para el tratamiento del daño articular |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7732484B2 (en) | 2000-08-01 | 2010-06-08 | University Of Virginia Patent Foundation | Use of selective adenosine A1 receptor allosteric enhancers to manipulate angiogenesis |
| WO2007130353A2 (en) | 2006-05-01 | 2007-11-15 | Johns Hopkins University | Phase 2 inducers, ppar-alpha agonists and related signalling pathways protect cartilage against inflammation, apoptosis and stress |
| AU2010273570B2 (en) | 2009-07-14 | 2014-07-03 | Novartis Ag | Mesenchymal stem cell differentiation |
| WO2012129562A2 (en) | 2011-03-24 | 2012-09-27 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| EP3143026B1 (en) * | 2014-05-13 | 2024-07-10 | Novartis AG | Compounds and compositions for inducing chondrogenesis |
| US9745253B2 (en) | 2015-03-13 | 2017-08-29 | Forma Therapeutics, Inc. | Alpha-cinnamide compounds and compositions as HDAC8 inhibitors |
| UY37759A (es) | 2017-06-09 | 2019-01-31 | Novartis Ag | Compuestos y composiciones para inducir condrogénesis |
| EP3706710B1 (en) | 2017-11-10 | 2024-04-10 | Novartis AG | Extended release formulations for intra-articular applications |
| CN113015735B (zh) | 2018-12-06 | 2024-06-21 | 诺华股份有限公司 | 用于诱导软骨发生以治疗关节损害的5-羟基-7-氧杂双环[2.2.1]庚烷-2-甲酰胺衍生物 |
-
2019
- 2019-12-04 CN CN201980073992.1A patent/CN113015735B/zh active Active
- 2019-12-04 JP JP2021525229A patent/JP7471291B2/ja active Active
- 2019-12-04 US US17/299,189 patent/US12257243B2/en active Active
- 2019-12-04 EP EP19821288.8A patent/EP3891154B1/en active Active
- 2019-12-04 WO PCT/IB2019/060454 patent/WO2020115683A1/en not_active Ceased
- 2019-12-04 ES ES19821288T patent/ES2963508T3/es active Active
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