DK2844637T5 - Substituerede 3-haloallylamin-inhibitorer af ssao samt anvendelser deraf - Google Patents
Substituerede 3-haloallylamin-inhibitorer af ssao samt anvendelser deraf Download PDFInfo
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- DK2844637T5 DK2844637T5 DK13784562.4T DK13784562T DK2844637T5 DK 2844637 T5 DK2844637 T5 DK 2844637T5 DK 13784562 T DK13784562 T DK 13784562T DK 2844637 T5 DK2844637 T5 DK 2844637T5
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Claims (18)
1
1. Forbindelse med formel II:
Formel II eller et farmaceutisk acceptabelt salt, solvat eller polymorf form deraf; hvor: 5 R5 er en usubstitueret phenylengruppe eller en phenylengruppe substitueret med én eller flere grupper uafhængigt valgt blandt alkyl, halogen, alkoxy og halogenalkyl; R5 er valgt fra
R7 og R8 er uafhængigt valgt fra gruppen bestående af hydrogen, eventuelt substitute) eret Ci ealkyl og eventuelt substitueret C3-7cycloalkyl; og X er oxygen; hvor udtrykket "alkyl" henviser til monovalente ligekædede eller forgrenede mættede carbonhydridradikaler med fra 1 til 6 carbonatomer, og hvor udtrykket "halo" henviser til fluor, chlor, brom og iod og 15 hvor udtrykket "alkoxy" henviser til ligekædede eller forgrenede alkyloxygrupper, hvor alkyl er som defineret ovenfor, og hvor udtrykket "eventuelt substitueret" betyder den gruppe, som dette udtryk angår, kan være usubstitueret eller kan være substitueret med én eller flere grupper uafhængigt valgt blandt halogen, Ci-C5alkyl, C2-C5alkenyl, Ci-C6halogenalkyl, Ci-C6alkoxy, 20 hydroxy(Ci-5)alkyl, C3-C5cycloalkyl, C(0)H, C(0)0H, NHC(0)H, NHC(0)Ci-C4alkyl, C(0)Ci-C4alkyl, NH2, NHCi-C4alkyl , N(Ci-C4alkyl)2, N02, OH og CN.
2. Forbindelse ifølge krav 1, hvor R5 er en usubstitueret phenylengruppe eller en phenylengruppe substitueret med én eller flere grupper uafhængigt valgt blandt methyl, fluor, chlor, brom, OCH3 og CF3.
3. Forbindelse ifølge et hvilket som helst af kravene 1 eller 2, hvor R7 og R8 begge er hydrogen, R7 og R8 begge er Ci-5alkyl, eller R7 er hydrogen, og R8 er Ci-5alkyl.
4. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor R5 er
hvori R7 og R8 er defineret i krav 1 eller 3.
5. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor R6 er
hvori R7 og R8 er defineret i krav 1 eller 3.
6. Forbindelse ifølge krav 1, hvor forbindelsen er valgt fra gruppen bestående af:
eller et farmaceutisk acceptabelt salt eller solvat deraf.
7. Forbindelse ifølge krav 1, hvor forbindelsen er (E)-4-(2-(aminomethyl)-3-fluorallyloxy)-/V-tert-butylbenzamid, eller et farmaceutisk acceptabelt salt eller solvat deraf.
8. Farmaceutisk acceptabelt salt af en forbindelse ifølge et hvilket som helst af kravene 1 til 7.
9. Farmaceutisk acceptabelt salt ifølge krav 8, kendetegnet ved, at det er et syreadditionssalt.
10. Farmaceutisk acceptabelt salt ifølge krav 9, kendetegnet ved, at syreadditionssaltet er valgt fra gruppen bestående af hydrochlorider, hydrobromider, sulfater, formater, acetater, lactater, malater, tartrater, citrater, ascorbater, succinater, maleater, butyrater, valerater og fumarater.
11. Farmaceutisk acceptabelt salt ifølge krav 10, kendetegnet ved, at syreadditionssaltet er et hydrochloridsalt.
12. Farmaceutisk acceptabelt salt ifølge krav 11, hvor det farmaceutisk acceptable salt er (E)-4-(2-(aminomethyl)-3-fluorallyloxy)-/V-tert'-butylbenzamidhydrochlorid.
13. Sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 7 eller et farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 8 til 12 eller et solvat deraf og mindst et farmaceutisk acceptabelt excipiens, bærer eller fortyndingsmiddel.
14. Forbindelse ifølge et hvilket som helst af kravene 1 til 7 eller et farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 8 til 12 eller et solvat deraf til anvendelse i en fremgangsmåde til behandling af en sygdom forbundet med eller moduleret af SSAO/VAP-l-protein, omfattende indgivelse til et individ med behov derfor af en terapeutisk virkningsfuld mængde af forbindelsen eller det farmaceutisk acceptable salt eller solvat deraf, hvor sygdommen er inflammation, fibrose, en diabetesfremkaldt sygdom, en neuro-inflammatorisk sygdom eller en cancer.
15. Forbindelse eller farmaceutisk acceptabelt salt eller solvat til anvendelse ifølge krav 14, hvor inflammationen er forbundet med leversygdom, respiratorisk sygdom, cystisk fibrose, astma eller kronisk obstruktiv lungesygdom eller okulær sygdom.
16. Forbindelse eller farmaceutisk acceptabelt salt eller solvat til anvendelse ifølge krav 14, hvor sygdommen er en diabetesfremkaldt sygdom udvalgt fra gruppen bestående af diabetisk nefropati, glomerulosclerose, diabetisk retinopati, ikke-alkoholisk fedtleversygdom og choroidal neovaskularisering.
17. Forbindelse eller farmaceutisk acceptabelt salt eller solvat til anvendelse ifølge krav 14, hvor sygdommen er valgt fra gruppen bestående af cystisk fibrose, leverfibrose, levercirrhose, nyrefibrose, sclerodermi, idiopatisk lungefibrose og strålingsinduceret fibrose.
18. Forbindelse eller farmaceutisk acceptabelt salt eller solvat til anvendelse ifølge krav 17, kendetegnet ved, at sygdommen er en ikke-alkoholisk fedtleversygdom, ikke-alkoholisk steatohepatitis (NASFI) eller alkoholinduceret fibrose, der fører til levercirrhose.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261641814P | 2012-05-02 | 2012-05-02 | |
PCT/AU2013/000356 WO2013163675A1 (en) | 2012-05-02 | 2013-04-05 | Substituted 3-haloallylamine inhibitors of ssao and uses thereof |
Publications (2)
Publication Number | Publication Date |
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DK2844637T3 DK2844637T3 (da) | 2018-04-23 |
DK2844637T5 true DK2844637T5 (da) | 2018-08-13 |
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DK13784562.4T DK2844637T5 (da) | 2012-05-02 | 2013-04-05 | Substituerede 3-haloallylamin-inhibitorer af ssao samt anvendelser deraf |
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Country | Link |
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US (4) | US9302986B2 (da) |
EP (2) | EP2844637B1 (da) |
JP (3) | JP6182595B2 (da) |
KR (2) | KR20200030126A (da) |
CN (2) | CN107266332B (da) |
AU (2) | AU2013255103B2 (da) |
BR (1) | BR112014027406B1 (da) |
CA (2) | CA3086105A1 (da) |
CY (1) | CY1120334T1 (da) |
DK (1) | DK2844637T5 (da) |
ES (1) | ES2668300T3 (da) |
HK (2) | HK1203477A1 (da) |
HR (1) | HRP20180953T1 (da) |
HU (1) | HUE038437T2 (da) |
LT (1) | LT2844637T (da) |
ME (1) | ME03063B (da) |
MX (1) | MX360634B (da) |
NO (1) | NO2842608T3 (da) |
PL (1) | PL2844637T3 (da) |
PT (1) | PT2844637T (da) |
RS (1) | RS57086B1 (da) |
SG (2) | SG10201707020TA (da) |
SI (1) | SI2844637T1 (da) |
TR (1) | TR201807453T4 (da) |
WO (1) | WO2013163675A1 (da) |
Families Citing this family (51)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS57086B1 (sr) * | 2012-05-02 | 2018-06-29 | Boehringer Ingelheim Int | Supstituisani 3-haloalilamin inhibitori ssao i njihova primena |
GB201304526D0 (en) | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
WO2015189534A1 (en) | 2014-06-12 | 2015-12-17 | Proximagen Limited | Vap-1 inhibitors for treating muscular dystrophy |
JP2018076236A (ja) * | 2015-06-05 | 2018-05-17 | 株式会社アールテック・ウエノ | がんを処置するための医薬組成物 |
JP2019502672A (ja) | 2015-12-07 | 2019-01-31 | ベネボレンタイ ケンブリッジ リミティド | 疼痛の治療のためのvap−1阻害剤 |
JP6843888B2 (ja) * | 2016-02-12 | 2021-03-17 | ファーマクシス リミテッド | リジルオキシダーゼのハロアリルアミンインドールおよびアザインドール誘導体阻害剤およびその使用 |
WO2018027892A1 (en) * | 2016-08-12 | 2018-02-15 | Eli Lilly And Company | Amino pyrimidine ssao inhibitors |
MX2019004549A (es) * | 2016-10-19 | 2019-06-12 | Boehringer Ingelheim Int | Combinaciones que comprenden un inhibidor ssao/vap-1 y un inhibidor sglt2 y usos de los mismos. |
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