JP2011529500A5 - - Google Patents
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- JP2011529500A5 JP2011529500A5 JP2011521224A JP2011521224A JP2011529500A5 JP 2011529500 A5 JP2011529500 A5 JP 2011529500A5 JP 2011521224 A JP2011521224 A JP 2011521224A JP 2011521224 A JP2011521224 A JP 2011521224A JP 2011529500 A5 JP2011529500 A5 JP 2011529500A5
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- JP
- Japan
- Prior art keywords
- group
- haloalkyl
- alkyl
- halogen
- 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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- 229910052736 halogen Inorganic materials 0.000 claims 41
- 150000002367 halogens Chemical class 0.000 claims 41
- 125000001424 substituent group Chemical group 0.000 claims 35
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 33
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 27
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 26
- 125000001188 haloalkyl group Chemical group 0.000 claims 26
- -1 cyano, hydroxy Chemical group 0.000 claims 24
- 125000003545 alkoxy group Chemical group 0.000 claims 19
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 18
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 18
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims 17
- 125000004454 (C1-C6) alkoxycarbonyl 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 15
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 13
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000004663 dialkyl amino group Chemical group 0.000 claims 13
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 125000004438 haloalkoxy group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 7
- 125000001931 aliphatic group Chemical group 0.000 claims 7
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000002785 azepinyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 208000022461 Glomerular disease Diseases 0.000 claims 1
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 1
- 206010018378 Glomerulonephritis rapidly progressive Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003892 ceramide glucosyltransferase inhibitor Substances 0.000 claims 1
- 201000005637 crescentic glomerulonephritis Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000001434 glomerular Effects 0.000 claims 1
- 229940125921 glucosylceramide synthase inhibitor Drugs 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 231100000855 membranous nephropathy Toxicity 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 201000008171 proliferative glomerulonephritis Diseases 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13721408P | 2008-07-28 | 2008-07-28 | |
| US61/137,214 | 2008-07-28 | ||
| PCT/US2009/051864 WO2010014554A1 (en) | 2008-07-28 | 2009-07-27 | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015056011A Division JP6038213B2 (ja) | 2008-07-28 | 2015-03-19 | 虚脱性糸球体症および他の糸球体疾患の処置のためのグルコシルセラミドシンターゼ阻害 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529500A JP2011529500A (ja) | 2011-12-08 |
| JP2011529500A5 true JP2011529500A5 (https=) | 2012-07-19 |
Family
ID=41110511
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011521224A Pending JP2011529500A (ja) | 2008-07-28 | 2009-07-27 | 虚脱性糸球体症および他の糸球体疾患の処置のためのグルコシルセラミドシンターゼ阻害 |
| JP2015056011A Expired - Fee Related JP6038213B2 (ja) | 2008-07-28 | 2015-03-19 | 虚脱性糸球体症および他の糸球体疾患の処置のためのグルコシルセラミドシンターゼ阻害 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015056011A Expired - Fee Related JP6038213B2 (ja) | 2008-07-28 | 2015-03-19 | 虚脱性糸球体症および他の糸球体疾患の処置のためのグルコシルセラミドシンターゼ阻害 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US8389517B2 (https=) |
| EP (1) | EP2320886B1 (https=) |
| JP (2) | JP2011529500A (https=) |
| CA (1) | CA2731685A1 (https=) |
| WO (1) | WO2010014554A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1811991B1 (en) | 2004-11-10 | 2018-11-07 | Genzyme Corporation | Treatment of type 2 diabetes using inhibitors of glycosphingolipid synthesis |
| SI2032134T1 (sl) | 2006-05-09 | 2015-10-30 | Genzyme Corporation | Postopki zdravljenja bolezni zamaščenih jeter, ki obsegajo inhibicijo sintezo glukosfingolipida |
| EP2594564B1 (en) * | 2007-05-31 | 2016-09-28 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitors |
| CN101888840A (zh) | 2007-10-05 | 2010-11-17 | 简詹姆公司 | 使用脑酰胺衍生物治疗多囊性肾疾病的方法 |
| CA2731685A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| EP3078373A1 (en) | 2008-10-03 | 2016-10-12 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitor |
| KR101987736B1 (ko) | 2011-03-18 | 2019-06-11 | 젠자임 코포레이션 | 글루코실세라마이드 합성효소 억제제 |
| US8961959B2 (en) * | 2011-10-17 | 2015-02-24 | The Regents Of The University Of Michigan | Glucosylceramide synthase inhibitors and therapeutic methods using the same |
| AU2012326361B2 (en) | 2011-10-17 | 2017-08-03 | Biotheryx, Inc. | Substituted biaryl alkyl amides |
| MA37975B2 (fr) | 2012-09-11 | 2021-03-31 | Genzyme Corp | Inhibiteurs de synthase de glucosylcéramide |
| WO2014150043A1 (en) * | 2013-03-15 | 2014-09-25 | Concert Pharmaceuticals Inc. | Inhibitors of the enzyme udp-glucose: n-acyl-sphingosine glucosyltransferase |
| JP6537500B2 (ja) * | 2013-09-20 | 2019-07-03 | ビオマリン プハルマセウトイカル インコーポレイテッド | 疾患治療用のグルコシルセラミドシンターゼ阻害剤 |
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| CN107635980A (zh) | 2015-03-11 | 2018-01-26 | 生物马林药物股份有限公司 | 用于治疗疾病的葡糖神经酰胺合酶抑制剂 |
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| US12472144B2 (en) | 2017-08-08 | 2025-11-18 | Amneal Pharmaceuticals Llc | Pharmaceutical composition comprising eliglustat |
| JP2021506920A (ja) | 2017-12-21 | 2021-02-22 | リソソーマル・セラピューティクス・インコーポレイテッドＬｙｓｏｓｏｍａｌ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 結晶性の置換シクロヘキシルピラゾロ［１，５−ａ］ピリミジニルカルボキサミド化合物およびその治療的使用 |
| US11760741B2 (en) * | 2018-05-02 | 2023-09-19 | Kashiv Biosciences, Llc | Pro-drugs of eliglustat |
| CN114040762A (zh) | 2019-02-04 | 2022-02-11 | 建新公司 | 使用葡糖神经酰胺合酶(gcs)的抑制剂治疗纤毛疾病 |
| WO2020193746A1 (en) | 2019-03-28 | 2020-10-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting the survival of patients suffering from melanoma |
| EP4048397B1 (en) | 2019-10-23 | 2023-08-16 | The Regents Of The University Of Michigan | Glucosylceramide synthase inhibitors for therapeutic applications |
| AU2020384066B2 (en) | 2019-11-15 | 2025-10-30 | Green Cross Corporation | Novel derivatives having 2,3-dihydro-1H-indene or 2,3-dihydrobenzofuran moiety or pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising the same |
| US20230002380A1 (en) | 2019-11-15 | 2023-01-05 | Yuhan Corporation | Novel compounds having inhibitory activity against glucosylceramide synthase or pharmaceutically acceptable salt thereof, processes for preparing the same, and pharmaceutical compositions comprising the same |
| JP2023512366A (ja) | 2020-02-03 | 2023-03-27 | ジェンザイム・コーポレーション | リソソーム蓄積性疾患と関連する神経学的症状を処置するための方法 |
| EP4142878B1 (en) | 2020-04-28 | 2024-06-26 | The Regents of The University of Michigan | Pyridine inhibitors of glucosylceramide synthase and therapeutic methods using the same |
| AU2021311131B2 (en) | 2020-07-24 | 2026-02-19 | Genzyme Corporation | Pharmaceutical compositions comprising venglustat |
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| EP2594564B1 (en) * | 2007-05-31 | 2016-09-28 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitors |
| CN101888840A (zh) | 2007-10-05 | 2010-11-17 | 简詹姆公司 | 使用脑酰胺衍生物治疗多囊性肾疾病的方法 |
| WO2009117150A2 (en) | 2008-03-20 | 2009-09-24 | Genzyme Corporation | Method of treating lupus with ceramide derivatives |
| CA2731685A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| EP3078373A1 (en) | 2008-10-03 | 2016-10-12 | Genzyme Corporation | 2-acylaminopropanol-type glucosylceramide synthase inhibitor |
-
2009
- 2009-07-27 CA CA2731685A patent/CA2731685A1/en not_active Abandoned
- 2009-07-27 US US13/055,036 patent/US8389517B2/en not_active Expired - Fee Related
- 2009-07-27 WO PCT/US2009/051864 patent/WO2010014554A1/en not_active Ceased
- 2009-07-27 JP JP2011521224A patent/JP2011529500A/ja active Pending
- 2009-07-27 EP EP09790852.9A patent/EP2320886B1/en active Active
-
2013
- 2013-02-07 US US13/762,102 patent/US8729075B2/en not_active Expired - Fee Related
-
2014
- 2014-04-17 US US14/255,634 patent/US9481671B2/en not_active Expired - Fee Related
-
2015
- 2015-03-19 JP JP2015056011A patent/JP6038213B2/ja not_active Expired - Fee Related
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