JP2018529648A5 - - Google Patents
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- Publication number
- JP2018529648A5 JP2018529648A5 JP2018506914A JP2018506914A JP2018529648A5 JP 2018529648 A5 JP2018529648 A5 JP 2018529648A5 JP 2018506914 A JP2018506914 A JP 2018506914A JP 2018506914 A JP2018506914 A JP 2018506914A JP 2018529648 A5 JP2018529648 A5 JP 2018529648A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- hydrogen
- alkyl
- amino
- 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
- -1 carboxy, amino Chemical group 0.000 claims description 84
- 150000001875 compounds Chemical class 0.000 claims description 64
- 229910052739 hydrogen Inorganic materials 0.000 claims description 39
- 239000001257 hydrogen Substances 0.000 claims description 39
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 150000002431 hydrogen Chemical group 0.000 claims description 14
- 150000001413 amino acids Chemical class 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 108010016626 Dipeptides Proteins 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 125000003282 alkyl amino group Chemical group 0.000 claims description 6
- 125000004414 alkyl thio group Chemical group 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 229910052805 deuterium Inorganic materials 0.000 claims description 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000004193 piperazinyl group Chemical group 0.000 claims description 6
- 125000003386 piperidinyl group Chemical group 0.000 claims description 6
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 6
- 125000003107 substituted aryl group Chemical group 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 4
- 108010060159 Apolipoprotein E4 Proteins 0.000 claims description 4
- 125000003277 amino group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 150000007942 carboxylates Chemical class 0.000 claims description 2
- 230000003920 cognitive function Effects 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000902 placebo Substances 0.000 claims description 2
- 229940068196 placebo Drugs 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000003287 1H-imidazol-4-ylmethyl group Chemical group [H]N1C([H])=NC(C([H])([H])[*])=C1[H] 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 description 6
- 0 *C(*)(C(C(*)(*)C1(*)N)N*)C1S(O)(=O)=O Chemical compound *C(*)(C(C(*)(*)C1(*)N)N*)C1S(O)(=O)=O 0.000 description 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 235000008206 alpha-amino acids Nutrition 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562203256P | 2015-08-10 | 2015-08-10 | |
| US62/203,256 | 2015-08-10 | ||
| PCT/US2016/046336 WO2017027582A1 (en) | 2015-08-10 | 2016-08-10 | Compositions and methods for treating and preventing neurodegenerative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018529648A JP2018529648A (ja) | 2018-10-11 |
| JP2018529648A5 true JP2018529648A5 (enExample) | 2019-09-26 |
| JP6928385B2 JP6928385B2 (ja) | 2021-09-01 |
Family
ID=57983633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506914A Active JP6928385B2 (ja) | 2015-08-10 | 2016-08-10 | 神経変性疾患を治療および予防するための組成物および方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US10590070B2 (enExample) |
| EP (1) | EP3334710B1 (enExample) |
| JP (1) | JP6928385B2 (enExample) |
| KR (1) | KR102657460B1 (enExample) |
| CN (1) | CN108026049B (enExample) |
| AU (1) | AU2016304862B2 (enExample) |
| CA (1) | CA2995093A1 (enExample) |
| EA (1) | EA035650B1 (enExample) |
| ES (1) | ES2965867T3 (enExample) |
| IL (1) | IL257332B (enExample) |
| MX (1) | MX380290B (enExample) |
| WO (1) | WO2017027582A1 (enExample) |
| ZA (1) | ZA201800831B (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3334710B1 (en) | 2015-08-10 | 2023-10-04 | Alzheon, Inc. | Compositions and methods for treating and preventing neurodegenerative disorders |
| CN114805211B (zh) | 2017-03-21 | 2024-08-23 | 润佳（苏州）医药科技有限公司 | 同位素富集3-氨基-1-丙磺酸衍生物、药物组合物及其用途 |
| US11198699B2 (en) | 2019-04-02 | 2021-12-14 | Aligos Therapeutics, Inc. | Compounds targeting PRMT5 |
| CN114269949A (zh) * | 2019-06-17 | 2022-04-01 | 阿尔泽恩股份有限公司 | 用于治疗神经变性病症的方法 |
| CN112791078B (zh) | 2019-11-13 | 2022-12-06 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| US20250345298A1 (en) | 2022-04-28 | 2025-11-13 | Alzheon, Inc. | Apoe4 correctors and methods of use |
| CN120641092A (zh) | 2022-12-02 | 2025-09-12 | 阿尔泽恩股份有限公司 | 用于用曲米沙特治疗神经变性病症的方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0407701A3 (en) * | 1989-05-15 | 1992-04-22 | Fujisawa Pharmaceutical Co., Ltd. | Antiretroviral pyrroline and pyrrolidine sulfonic acid derivatives |
| US5698155A (en) | 1991-05-31 | 1997-12-16 | Gs Technologies, Inc. | Method for the manufacture of pharmaceutical cellulose capsules |
| ZA9811595B (en) * | 1997-12-17 | 2000-06-19 | Biocryst Pharm Inc | Substituted cyclopentane and cyclopentene compounds useful as neuraminidase inhibitors. |
| BR0010099A (pt) * | 1999-04-28 | 2002-06-04 | Univ Kingston | Métodos para modular a agregação de amilóides em um indivìduo, para o tratamento de um estado doentio associado com amiloidose, composição para modular amiloidose, e, métodos para inibir os depósitos de amilóide associados com iapp em um indivìduo, para inibir fibrilogenese iapp em um indivìduo, para reduzir os agregados de amilóides associados com iapp em um indivìduo, para modular dano associado com amilóides em células, e para modular amiloidose in vivo ou ex vivo |
| KR20050101537A (ko) * | 2002-12-24 | 2005-10-24 | 뉴로켐 (인터내셔널) 리미티드 | 베타-아밀로이드 관련 질환의 치료를 위한 치료 제제 |
| US20070010573A1 (en) * | 2003-06-23 | 2007-01-11 | Xianqi Kong | Methods and compositions for treating amyloid-related diseases |
| CN100528840C (zh) * | 2003-06-23 | 2009-08-19 | 贝卢斯健康(国际）有限公司 | 改进的候选药物及其制备方法 |
| US7244764B2 (en) * | 2003-06-23 | 2007-07-17 | Neurochem (International) Limited | Methods and compositions for treating amyloid-related diseases |
| BRPI0411743A (pt) * | 2003-06-23 | 2006-08-08 | Neurochem Int Ltd | método e composições para tratar doenças relacionadas a amilóides |
| EP2862581B1 (en) | 2006-10-12 | 2021-08-11 | BHI Limited Partnership | Methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid |
| WO2009003009A1 (en) * | 2007-06-26 | 2008-12-31 | Enanta Pharmaceuticals, Inc. | Substituted pyrrolidine as anti-infectives |
| KR101173677B1 (ko) * | 2009-12-11 | 2012-08-13 | 한국과학기술연구원 | Ｅｐｐｓ를 유효성분으로 함유하는 베타아밀로이드 집적 관련 질환의 예방 또는 치료용 약학적 조성물 |
| EP3334710B1 (en) | 2015-08-10 | 2023-10-04 | Alzheon, Inc. | Compositions and methods for treating and preventing neurodegenerative disorders |
-
2016
- 2016-08-10 EP EP16835830.7A patent/EP3334710B1/en active Active
- 2016-08-10 KR KR1020187006588A patent/KR102657460B1/ko active Active
- 2016-08-10 ES ES16835830T patent/ES2965867T3/es active Active
- 2016-08-10 JP JP2018506914A patent/JP6928385B2/ja active Active
- 2016-08-10 CN CN201680053914.1A patent/CN108026049B/zh active Active
- 2016-08-10 AU AU2016304862A patent/AU2016304862B2/en active Active
- 2016-08-10 WO PCT/US2016/046336 patent/WO2017027582A1/en not_active Ceased
- 2016-08-10 MX MX2018001592A patent/MX380290B/es unknown
- 2016-08-10 CA CA2995093A patent/CA2995093A1/en active Pending
- 2016-08-10 EA EA201890460A patent/EA035650B1/ru unknown
- 2016-08-10 US US15/751,547 patent/US10590070B2/en active Active
-
2018
- 2018-02-04 IL IL257332A patent/IL257332B/en active IP Right Grant
- 2018-02-08 ZA ZA2018/00831A patent/ZA201800831B/en unknown
-
2020
- 2020-03-03 US US16/807,747 patent/US11053192B2/en active Active
-
2022
- 2022-02-16 US US17/673,269 patent/US12187668B2/en active Active
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