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1. 发明专利

JP2017507986A ２，７−ジアザスピロ［３．５］ノナン化合物审中-公开
公开(公告)号：JP2017507986A
公开(公告)日：2017-03-23
申请号：JP2016557898
申请日：2015-03-17
申请人：リマインドエヌヴイRemynd Nv , リマインドエヌヴイRemynd Nv
发明人：グリフィウン，ジェラード , タイエ，バルトデ , タイエ，バルトデ , プリンセン，カトリーン , ヴィッテ，クーンデ , ヴィッテ，クーンデ , ブランシュ，エミリー , ラトニ，ハサン , ロジャース−エヴァンス，マーク
IPC分类号： C07D471/10 , A61K31/438 , A61K31/444 , A61K31/497 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/50 , A61P9/12 , A61P25/14 , A61P25/16 , A61P25/28
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要：本発明は、式(I)の化合物またはその立体異性体、鏡像異性体、ラセミ体、若しくは互変異性体に関し、式中、R1、R3、R4、L1、L2、L3、L4、及びnは、特許請求の範囲及び明細書に定義するのと同じ意味を有する。本発明は、このような化合物を含む組成物、特に医薬品、ならびに代謝性障害及び/または神経変性疾患、及び/またはタンパク質ミスフォールディング障害の予防及び/または治療のためのこのような化合物及び組成物の使用にも関する。【選択図】なし

2. 发明申请

US20170157137A1 2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS 审中-公开
公开(公告)号：US20170157137A1
公开(公告)日：2017-06-08
申请号：US15433164
申请日：2017-02-15
申请人： REMYND NV
发明人： Gerard Griffioen , Bart De Taeye , Katrien Princen , Koen De Witte , Emilie Blanche , Hasane Ratni , Mark Rogers-Evans
IPC分类号： A61K31/5377 , A61K31/444 , A61K31/435
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

3. 发明申请

US20170015665A1 2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS 有权
标题翻译： 2,7-DIAZASPIRO [3.5] NONANE化合物
公开(公告)号：US20170015665A1
公开(公告)日：2017-01-19
申请号：US15121790
申请日：2015-03-17
申请人： REMYND NV
发明人： Gerard Griffioen , Bart De Taeye , Katrien Princen , Koen De Witte , Emilie Blanche , Hasane Ratni , Mark Rogers-Evans
IPC分类号： C07D471/10
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
摘要翻译：本发明涉及式（I）化合物或式（I）的立体异构体，对映异构体，外消旋或互变异构体，其中R1，R3，R4，L1，L2，L3，L4和n具有相同意义如权利要求和说明书中所限定的那样。本发明还涉及包含这些化合物的组合物，特别是药物，以及这些化合物和组合物用于预防和/或治疗代谢紊乱和/或神经变性疾病和/或蛋白质错误折叠障碍的用途。

4. 发明授权

US09617264B2 2,7-diazaspiro[3.5]nonane compounds 有权
公开(公告)号：US09617264B2
公开(公告)日：2017-04-11
申请号：US15121790
申请日：2015-03-17
申请人： REMYND NV
发明人： Gerard Griffioen , Bart De Taeye , Katrien Princen , Koen De Witte , Emilie Blanche , Hasane Ratni , Mark Rogers-Evans
IPC分类号： C07D471/10
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

5. 发明专利

JP2019147834A 2,7−ジアザスピロ[3.5]ノナン化合物审中-公开
公开(公告)号：JP2019147834A
公开(公告)日：2019-09-05
申请号：JP2019094697
申请日：2019-05-20
申请人：リマインドエヌヴイ , REMYND NV
发明人：グリフィウン,ジェラード , デタイエ,バルト , プリンセン,カトリーン , デヴィッテ,クーン , ブランシュ,エミリー , ラトニ,ハサン , ロジャース−エヴァンス,マーク
IPC分类号： A61P3/00 , A61P25/28 , A61P43/00 , A61P25/16 , A61P3/10 , A61P21/00 , A61P25/02 , A61P25/00 , A61P25/14 , A61P3/08 , A61P3/04 , A61P3/06 , A61P9/00 , A61P9/12 , A61P1/16 , A61K31/438 , A61K31/444 , A61K31/497 , A61K31/5377 , C07D471/10
摘要：【課題】タンパク質ミスフォールディング障害(例:アミロイドーシス)に起因する疾患、例えば、代謝性障害(例:糖尿病)、神経変性疾患(例:アルツハイマー病、パーキンソン病等)等の予防及び/又は治療に有用な新規化合物の提供。【解決手段】下記式(I)で表される2,7−ジアザスピロ[3.5]ノナン化合物。 (nは0〜3の整数;R 1 はC 1〜6 アルキル等;R 3 及びR 4 は各々独立にC 6〜12 アリール、H、ヘテロアリール等;L 1 及びL 3 は各々独立に−SO 2 −、−CO−等;L 2 及びL 4 は各々独立に単結合、置換可C 1〜3 アルキレン等。) 【選択図】なし

7. 发明专利

JP2014518240A Useful 1,2,4-thiadiazol-5-yl piperazine derivatives for the treatment of neurodegenerative diseases 有权
公开(公告)号：JP2014518240A
公开(公告)日：2014-07-28
申请号：JP2014517749
申请日：2012-06-29
申请人：リマインド・ナムローゼ・フエンノートシャップRemynd Nv
发明人：グリフィオン，ジェラルド , ネッテコーフェン，マティアス , プリンセン，カトリーン , ラトニ，ハサネ , ビフィアン，ウォルター
IPC分类号： C07D285/08 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/28 , C07D417/04 , C07D417/12
CPC分类号： C07D285/135 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要：本発明は、構造式（ＩＡ）

の化合物に関する。本発明はまた、細胞毒性のＴＡＵミスフォールディングおよび／または凝集を特徴とする特定の神経変性障害を治療するための、構造式（ＩＡ）の化合物の使用に関する。

8. 发明授权

US09808456B2 Piperazine thiazole derivatives useful in the treatment of tauopathies such as Alzheimer's disease 有权
公开(公告)号：US09808456B2
公开(公告)日：2017-11-07
申请号：US14884689
申请日：2015-10-15
申请人： REMYND NV
发明人： Gerard Griffioen , Giuseppe Cecere , Matthias Nettekoven , Katrien Princen , Hasane Ratni , Mark Rogers-Evans , Walter Vifian
IPC分类号： A61K31/496 , C07D417/04 , C07D417/12 , C07D285/08 , C07D417/14
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2— or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.

9. 发明授权

US09750745B2 2,7-diazaspiro[3.5]nonane compounds 有权
公开(公告)号：US09750745B2
公开(公告)日：2017-09-05
申请号：US15433164
申请日：2017-02-15
申请人： REMYND NV
发明人： Gerard Griffioen , Bart De Taeye , Katrien Princen , Koen De Witte , Emilie Blanche , Hasane Ratni , Mark Rogers-Evans
IPC分类号： A61K31/5377 , A61K31/435 , A61K31/444
CPC分类号： A61K31/5377 , A61K31/435 , A61K31/444 , C07D471/10
摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

10. 发明申请

US20160101102A1 PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 有权
标题翻译：用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物
公开(公告)号：US20160101102A1
公开(公告)日：2016-04-14
申请号：US14884689
申请日：2015-10-15
申请人： REMYND NV
发明人： Gerard Griffioen , Giuseppe Cecere , Matthias Nettekoven , Katrien Princen , Hasane Ratni , Mark Rogers-Evans , Walter Vifian
IPC分类号： A61K31/496
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2— or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
摘要翻译：本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基四氢吡喃-4-基; 苯乙基被一个或多个卤素取代的苯乙基; 苯氧基甲基; 被一个或多个卤素取代的苯氧基甲基; 苄氧基乙基由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或者R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

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