JPWO2019178191A5 - - Google Patents
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- Publication number
- JPWO2019178191A5 JPWO2019178191A5 JP2020548963A JP2020548963A JPWO2019178191A5 JP WO2019178191 A5 JPWO2019178191 A5 JP WO2019178191A5 JP 2020548963 A JP2020548963 A JP 2020548963A JP 2020548963 A JP2020548963 A JP 2020548963A JP WO2019178191 A5 JPWO2019178191 A5 JP WO2019178191A5
- Authority
- JP
- Japan
- Prior art keywords
- acceptable salt
- pharmaceutically acceptable
- alkyl
- halo
- compound
- 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 160
- 150000003839 salts Chemical class 0.000 claims description 151
- 125000005843 halogen group Chemical group 0.000 claims description 78
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 39
- 125000000217 alkyl group Chemical group 0.000 claims description 37
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 25
- -1 C 1 -C 4 alkyl Chemical group 0.000 claims description 22
- 229910052799 carbon Inorganic materials 0.000 claims description 22
- 125000004970 halomethyl group Chemical group 0.000 claims description 22
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 12
- 125000001424 substituent group Chemical group 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 11
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- 125000000335 thiazolyl group Chemical group 0.000 claims description 6
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 5
- 125000004429 atom Chemical group 0.000 claims description 5
- 125000005347 halocycloalkyl group Chemical group 0.000 claims description 5
- 125000000623 heterocyclic group Chemical group 0.000 claims description 5
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 5
- 102100030122 Protein O-GlcNAcase Human genes 0.000 claims description 4
- 108010045982 hexosaminidase C Proteins 0.000 claims description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 3
- 210000004556 brain Anatomy 0.000 claims description 3
- 230000004770 neurodegeneration Effects 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 125000004076 pyridyl group Chemical group 0.000 claims description 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000034799 Tauopathies Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 230000006951 hyperphosphorylation Effects 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 description 10
- 208000032382 Ischaemic stroke Diseases 0.000 description 6
- 208000010877 cognitive disease Diseases 0.000 description 6
- 208000024827 Alzheimer disease Diseases 0.000 description 4
- 208000027061 mild cognitive impairment Diseases 0.000 description 4
- 208000018737 Parkinson disease Diseases 0.000 description 3
- 208000027089 Parkinsonian disease Diseases 0.000 description 3
- 206010034010 Parkinsonism Diseases 0.000 description 3
- 201000002212 progressive supranuclear palsy Diseases 0.000 description 3
- 208000028698 Cognitive impairment Diseases 0.000 description 2
- 201000011240 Frontotemporal dementia Diseases 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 2
- 206010015037 epilepsy Diseases 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- 201000010901 lateral sclerosis Diseases 0.000 description 2
- 208000005264 motor neuron disease Diseases 0.000 description 2
- 230000003387 muscular Effects 0.000 description 2
- 230000001568 sexual effect Effects 0.000 description 2
- 208000023697 ABri amyloidosis Diseases 0.000 description 1
- 206010003694 Atrophy Diseases 0.000 description 1
- 201000010374 Down Syndrome Diseases 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- 201000000162 ITM2B-related cerebral amyloid angiopathy 1 Diseases 0.000 description 1
- 208000003351 Melanosis Diseases 0.000 description 1
- 206010068871 Myotonic dystrophy Diseases 0.000 description 1
- 208000024777 Prion disease Diseases 0.000 description 1
- 206010039966 Senile dementia Diseases 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 208000037065 Subacute sclerosing leukoencephalitis Diseases 0.000 description 1
- 206010042297 Subacute sclerosing panencephalitis Diseases 0.000 description 1
- 208000018756 Variant Creutzfeldt-Jakob disease Diseases 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 230000033558 biomineral tissue development Effects 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- 230000001054 cortical effect Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 206010014599 encephalitis Diseases 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 231100000518 lethal Toxicity 0.000 description 1
- 230000001665 lethal effect Effects 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862642932P | 2018-03-14 | 2018-03-14 | |
| US62/642,932 | 2018-03-14 | ||
| US201862690536P | 2018-06-27 | 2018-06-27 | |
| US62/690,536 | 2018-06-27 | ||
| US201862699443P | 2018-07-17 | 2018-07-17 | |
| US62/699,443 | 2018-07-17 | ||
| PCT/US2019/021995 WO2019178191A1 (en) | 2018-03-14 | 2019-03-13 | O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021518340A JP2021518340A (ja) | 2021-08-02 |
| JPWO2019178191A5 true JPWO2019178191A5 (https=) | 2022-03-22 |
| JP2021518340A5 JP2021518340A5 (https=) | 2022-03-22 |
| JP7453916B2 JP7453916B2 (ja) | 2024-03-21 |
Family
ID=65952097
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020548963A Active JP7453916B2 (ja) | 2018-03-14 | 2019-03-13 | Ｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グリコピラノシダーゼ阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230117898A1 (https=) |
| EP (2) | EP3765458B1 (https=) |
| JP (1) | JP7453916B2 (https=) |
| CN (2) | CN112218863B (https=) |
| AU (1) | AU2019234759C1 (https=) |
| CA (1) | CA3093315A1 (https=) |
| ES (1) | ES2942211T3 (https=) |
| MA (1) | MA52004A (https=) |
| MX (1) | MX2020009530A (https=) |
| WO (1) | WO2019178191A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018154133A1 (en) * | 2017-02-27 | 2018-08-30 | Janssen Pharmaceutica Nv | [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors |
| PE20211591A1 (es) * | 2018-09-19 | 2021-08-18 | Biogen Ma Inc | Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| WO2021094312A1 (en) | 2019-11-11 | 2021-05-20 | Janssen Pharmaceutica Nv | Pyrrolidine and bicycloheteroaryl containing oga inhibitor compounds |
| WO2021110656A1 (en) | 2019-12-02 | 2021-06-10 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| WO2021123291A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
| AU2020409728A1 (en) | 2019-12-18 | 2022-08-11 | Janssen Pharmaceutica Nv | OGA inhibitor compounds |
| CN114929337A (zh) | 2019-12-18 | 2022-08-19 | 詹森药业有限公司 | Oga抑制剂化合物 |
| KR102533471B1 (ko) * | 2020-11-23 | 2023-05-19 | (주) 메디프론디비티 | O-GlcNAcase 저해 활성을 갖는 화합물 및 이의 용도 |
| CN114213315A (zh) * | 2021-12-31 | 2022-03-22 | 上海陶术生物科技有限公司 | 含氮杂环类化合物及其中间体的合成方法 |
| CN114560805B (zh) * | 2022-01-20 | 2024-11-29 | 上海陶术生物科技有限公司 | 含氮杂环化合物及其中间体的合成方法 |
| CN121405694A (zh) * | 2024-07-26 | 2026-01-27 | 浙江同源康医药股份有限公司 | Oga抑制剂及其应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| EP2780014A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| WO2013078320A1 (en) | 2011-11-21 | 2013-05-30 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| SI2953941T1 (sl) | 2013-02-11 | 2017-08-31 | Constellation Pharmaceuticals, Inc. | Modulatorji metil-modificirajočih encimov, sestavki in uporabe le-teh |
| RS58768B1 (sr) * | 2013-03-14 | 2019-06-28 | Merck Patent Gmbh | Inhibitori glikozidaze |
| WO2014151142A1 (en) | 2013-03-15 | 2014-09-25 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3033334A1 (en) | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3389658B1 (en) * | 2015-12-18 | 2020-11-25 | Merck Sharp & Dohme Corp. | Glycosidase inhibitors and uses thereof |
| CA3045957A1 (en) * | 2016-12-16 | 2018-06-21 | Janssen Pharmaceutica Nv | Monocyclic oga inhibitor compounds |
| US20190359609A1 (en) * | 2016-12-16 | 2019-11-28 | Janssen Pharmaceutica Nv | Bicyclic oga inhibitor compounds |
| WO2018154133A1 (en) * | 2017-02-27 | 2018-08-30 | Janssen Pharmaceutica Nv | [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors |
-
2019
- 2019-03-13 AU AU2019234759A patent/AU2019234759C1/en active Active
- 2019-03-13 EP EP19713945.4A patent/EP3765458B1/en active Active
- 2019-03-13 CN CN201980019170.5A patent/CN112218863B/zh active Active
- 2019-03-13 JP JP2020548963A patent/JP7453916B2/ja active Active
- 2019-03-13 MX MX2020009530A patent/MX2020009530A/es unknown
- 2019-03-13 CA CA3093315A patent/CA3093315A1/en active Pending
- 2019-03-13 EP EP23151036.3A patent/EP4186899A1/en active Pending
- 2019-03-13 MA MA052004A patent/MA52004A/fr unknown
- 2019-03-13 CN CN202410813893.5A patent/CN118955490A/zh active Pending
- 2019-03-13 WO PCT/US2019/021995 patent/WO2019178191A1/en not_active Ceased
- 2019-03-13 ES ES19713945T patent/ES2942211T3/es active Active
-
2022
- 2022-08-24 US US17/894,461 patent/US20230117898A1/en active Pending
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