HRP20141113T1 - Sredstva za lijeäśenje poremeä†aja koji ukljuäśuju modulaciju receptora rijanodina - Google Patents
Sredstva za lijeäśenje poremeä†aja koji ukljuäśuju modulaciju receptora rijanodina Download PDFInfo
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Claims (23)
1. Spoj, naznačen time, da je predstavljen strukturom Formule (I):
[image]
pri čemu R je COOH;
i njihove farmaceutski prihvatljive soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je u obliku soli s farmaceutski prihvatljivom kiselinom ili lužinom.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time, da je sol odabrana iz skupine koja se sastoji od natrija, kalija, magnezija, hemifumarata, hidroklorida i hidrobromida.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je odabran iz skupine koja se sastoji od:
[image]
[image]
[image]
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen strukturnom Formulom (1):
[image]
ili njihovom farmaceutski prihvatljivom soli.
6. Spoj u skladu s patentnim zahtjevom 5, naznačen time, da je u obliku soli s farmaceutski prihvatljivom kiselinom ili lužinom.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time, da je sol odabrana iz skupine koja se sastoji od natrija, kalija, magnezija, hemifumarata, hidroklorida i hidrobromida.
8. Spoj u skladu s patentnim zahtjevom 7, naznačen time, da je sol natrijeva sol.
9. Spoj u skladu s patentnim zahtjevom 7, naznačen time, da je sol hemifumaratna sol.
10. Farmaceutski pripravak koji sadrži spoj u skladu s patentnim zahtjevima 1-9, naznačena time, da je u kombinaciji s jednim ili više farmaceutski prihvatljivih ekscipijensa ili nosača.
11. Farmaceutski pripravak u skladu s patentnim zahtjevom 10, naznačen time, da se koristi u liječenju ili prevenciji stanja odabranih is skupine koja se sastoji od srčanih poremećaja i oboljenja, mišićnog umora, poremećaja i bolesti muskuloskeletalnog sustava, poremećaja i bolesti središnjeg živčanog sustava (CNS), kognitivne disfunkcije, nervno-mišićnih poremećaja i oboljenja, poremećaja i bolesti kostiju, tumorske kaheksije, maligne hipertermije, dijabetesa, iznenadne srčane smrti i sindroma iznenadne dječje smrti ili za poboljšanje kognitivne funkcije.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 10, za uporabu u liječenju ili prevenciji stanja u skladu s patentnim zahtjevom 11, naznačen time, da su srčani poremećaji ili oboljenja odabrani iz skupine koja se sastoji od poremećaja ili bolesti nepravilnog rada srca poput primjerice atrijske i ventrikularne aritmije, atrijske i ventrikularne fibrilacije, atrijske i ventrikularne tahiaritmije, atrijske i ventrikularne tahikardije, kateholaminergičke polimorfne ventrikularne tahikardije (CPVT) te njihovih varijanti izazvanih uslijed tjelovježbe; poremećaja i bolesti nepravilnog rada srca izazvanog uslijed tjelovježbe; srčanog zatajenja; kongestivnog zatajenja srca; kroničnog zatajenja srca; akutnog zatajenja srca; sistoličkog zatajenja srca; dijastoličkog zatajenja srca; akutne dekompenzacije srca; srčane ishemije/reperfuzijska ozljeda (I/R); kronične opstruktivne plućne bolesti; I/R ozljede uslijed srčane angioplastije ili uslijed trombolize za liječenje infarkta miokarda (MI); te visokog krvnog tlaka.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 10 za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11, naznačen time, da je mišićni zamor uzrokovan bolešću, poremećajem ili stanjem skeletnih mišića.
14. Farmaceutski pripravak u skladu s patentnim zahtjevom 10 za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11, naznačen time, da je muskuloskeletalni poremećaj, bolest ili stanje odabrano iz skupine koja se sastoji zamora skeletnih mišića izazvanog uslijed tjelovježbe; zamora mišića izazvanog uslijed produljene ili intenzivne tjelovježbe; kongenitalne miopatije; mišićne distrofije poput primjerice Duchenne-ove distrofije mišića (DMD), Becker-ove distrofije mišića (BMD), Limb-Girdle distrofije mišića (LGMD), facioskapulohumeralne mišićne distrofije, miotonične mišične distrofije, kongenitalne mišićne distrofije (CMD), distalne mišične distrofije, Emery- Dreifuss-ove mišićne distrofije i okulofaringealne mišićne distrofije; spinalne mišićne atrofije (SMA), spinalne i bulbarne mišićne atrofije (SBMA), zamora mišića povezanog sa starosnom dobi; sarkopenije, bolesti središnje jezgre; tumorske kaheksije; poremećaje mjehura i inkontinencije.
15. Farmaceutski pripravak u skladu s patentnim zahtjevom 10 za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11, naznačen time, da su poremećaj ili bolesti središnjeg živčanog sustava (CNS) odabrani iz skupine koja se sastoji od Alzheimer-ove bolesti (AD), neuropatije, napadaja, Parkinson-ove bolesti (PD) i Huntington-ove bolesti (HD); i nervno-mišićnih poremećaja i bolesti koje su odabrane iz skupine koja se sastoji od spinocerebelarne ataksije (SCA) i amiotrofna lateralna skleroza (ALS, Lou Gehrig-ova bolest).
16. Farmaceutski pripravak u skladu s patentnim zahtjevom za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11, naznačen time, da je kognitivna disfunkcija povezana sa stresom ili sa starosnom dobi, ili gdje kognitivna funkcija treba biti poboljšana zbog kratkog pamćenja, dugotrajnog pamćenja, pažnje ili učenja, ili gdje je kognitivna disfunkcija povezana s bolesti ili poremećajem koji je odabran iz skupine koja se sastoji od Alzheimer-ove bolesti (AD), poremećaja pažnje uzrokovanog hiperaktivnošću (ADHD), poremećaja autističnog spektra (ASD), generaliziranog anksioznog poremećaja (GAD), opsesivno-kompulzivnog poremećaja (OCD), Parkinson- ove bolesti (PD), post-traumatskog stresnog poremećaja (PTSD), Schizophrenije, bipolarnog poremećaja i unipolarne velike depresije.
17. Farmaceutski pripravak u skladu s patentnim zahtjevom 10 za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11, naznačen time, da je stanje tumorska kaheksija.
18. Farmaceutski pripravak u skladu s patentnim zahtjevom 17, naznačen time, da je tumorska kaheksija uzrokovana uslijed metastaziranja tumora kosti.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-9, ili njihove soli, naznačen time, da se koristi za liječenje ili prevenciju stanja odabranih iz skupine koja se sastoji od srčanih poremećaja ili oboljenja, zamora mišića, poremećaja muskuloskeletalnog sustava, poremećaja i bolesti središnjeg živčanog sustava (CNS), kognitivne disfunkcije, nervno-mišićnih poremećaja i bolesti, poremećaja i bolesti kosti, tumorske kaheksije, maligne hipertermije, dijabetesa, iznenadne srčane smrti i sindroma iznenadne dječje smrti ili za poboljšanje kognitivne funkcije.
20. Farmaceutski pripravak u skladu s patentnim zahtjevom 10 u kombinaciji s antisens-oligonukleotidom (AO) koji je specifičan za upletanje odsječka u ciljanoj mRNK za bolje preskakanje egzona u rečenoj ciljanoj mRNK, naznačen time, da se koristi za uporabu u liječenju ili prevenciji u skladu s patentnim zahtjevom 11.
21. Farmaceutski pripravak u skladu s patentnim zahtjevom 20, naznačen time, da se koristi u liječenju Duchenne-ove mišićne distrofije (DMD), pri čemu je antisens-oligonukleotid (AO) specifičan za upletanje odsječka od najmanje jednog od egzona DMD gena.
22. Farmaceutski pripravak u skladu s patentnim zahtjevom 21, naznačen time, da je antisens-oligonukleotid specifičan za upletanje odsječka egzona 23, 45, 44, 50, 51, 52 i /ili 53 DMD gena.
23. Postupak priprave u skladu s bilo kojim od patentnih zahtjeva 1-9, naznačen time, da se sastoji od koraka reakcije spojeva formule
[image]
sa spojem formule
[image]
pri čemu Ra je COOR1 ili CN; R1 je C1-C4 alkil, a L je odlazeća skupina kako bi se dobio spoj formule:
[image]
i
pretvaranjem skupine Ra u skupinu R kako bi se dobio spoj formule (I).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261625890P | 2012-04-18 | 2012-04-18 | |
| EP12167732.2A EP2708535A1 (en) | 2012-05-11 | 2012-05-11 | Agents for treating disorders involving modulation of ryanodine receptors |
| EP20130164051 EP2653466B1 (en) | 2012-04-18 | 2013-04-17 | Agents for treating disorders involving modulation of ryanodine receptors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20141113T1 true HRP20141113T1 (hr) | 2015-01-02 |
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| US9102645B2 (en) | 2013-03-15 | 2015-08-11 | Rosalind Franklin University Of Medicine And Science | Compounds for stabilizing ryanodine receptors from aberrant levels of calcium release |
| EP3021841B1 (en) | 2013-07-18 | 2022-11-16 | Baylor College Of Medicine | Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia |
| WO2015197562A1 (en) * | 2014-06-23 | 2015-12-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of disorders or diseases associated with ryanodine receptor dysfunction |
| US10071996B2 (en) | 2014-07-30 | 2018-09-11 | Aetas Pharma Co., Ltd. | Optical isomer of 1,4-benzothiazepine-1-oxide derivative, and pharmaceutical composition prepared using same |
| AU2015374155A1 (en) * | 2014-12-30 | 2017-07-20 | Myotherix, Inc. | Novel calcium modulators |
| ES2643856B1 (es) | 2016-05-24 | 2018-08-03 | Universidad Del Pais Vasco / Euskal Herriko Unibertsitatea | Triazoles para la regulación de la homeostasis de calcio intracelular |
| US11426415B2 (en) | 2017-03-06 | 2022-08-30 | Washington University | Treatment for Wolfram syndrome and other endoplasmic reticulum stress disorders |
| WO2019082940A1 (ja) * | 2017-10-25 | 2019-05-02 | 学校法人順天堂 | リアノジン受容体阻害薬 |
| US11026905B2 (en) | 2018-04-19 | 2021-06-08 | Tvardi Therapeutics, Inc. | STAT3 inhibitors |
| CN112367984B (zh) | 2018-04-19 | 2024-05-10 | 特维迪疗法公司 | Stat3抑制剂 |
| MX2022008914A (es) | 2020-01-24 | 2022-08-16 | Tvardi Therapeutics Inc | Compuestos terapeuticos, formulaciones y usos de los mismos. |
| CN116635378A (zh) | 2020-11-06 | 2023-08-22 | 赛特凯恩蒂克公司 | 二环1,4-二氮杂环庚酮和其治疗用途 |
| WO2022150603A1 (en) * | 2021-01-08 | 2022-07-14 | Armgo Pharma, Inc. | Crystalline forms of a ryanodine receptor modulator and uses thereof |
| WO2022246114A2 (en) * | 2021-05-20 | 2022-11-24 | Armgo Pharma, Inc. | Pharmaceutical compositions comprising a ryanodine receptor modulator and uses thereof |
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| US20230302013A1 (en) * | 2022-02-09 | 2023-09-28 | The Trustees Of Columbia University In The City Of New York | METHOD OF TREATING VIRAL-INDUCED COGNITIVE DYSFUNCTION BY TARGETING LEAKY RyR2 CHANNELS |
| EP4230196A1 (en) | 2022-02-21 | 2023-08-23 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of dystrophinopathies |
| WO2023244946A1 (en) | 2022-06-15 | 2023-12-21 | Tvardi Therapeutics, Inc. | Prodrugs of stat3 inhibitors |
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| US20020183307A1 (en) | 2000-07-26 | 2002-12-05 | Tremont Samuel J. | Novel 1,4-benzothiazephine and 1,5-benzothiazepine compounds as inhibitors of apical sodium co-dependent bile acid transport and taurocholate uptake |
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| DE112005003511T5 (de) | 2005-03-23 | 2008-04-17 | Battelle Memorial Institute, Richland | RFID-System mit verbesserter Leistungsfähigkeit |
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| KR101260859B1 (ko) | 2008-03-03 | 2013-05-06 | 르 라보레또레 쎄르비에르 | 감마-아미노알킬벤젠으로부터 벤조티아제핀을 제조하는 방법 |
| CN101891706B (zh) * | 2010-04-09 | 2013-05-29 | 复旦大学 | 3,4-二氢苯并[f][1,4]噻氮杂*类化合物或其盐及其药物用途 |
| WO2012019071A1 (en) | 2010-08-06 | 2012-02-09 | The Trustees Of Columbia University In The City Of New York | Methods of preventing and treating sarcopenia |
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| WO2012037105A1 (en) | 2010-09-14 | 2012-03-22 | The Trustees Of Columbia University In The City Of New York | Methods of treating, ameliorating or preventing stress-induced neuronal disorders and diseases |
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