CY1122470T1 - Αναστολεις kv1.3 και η ιατρικη εφαρμογη αυτων - Google Patents

Αναστολεις kv1.3 και η ιατρικη εφαρμογη αυτων

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CY1122470T1
CY1122470T1 CY20191101312T CY191101312T CY1122470T1 CY 1122470 T1 CY1122470 T1 CY 1122470T1 CY 20191101312 T CY20191101312 T CY 20191101312T CY 191101312 T CY191101312 T CY 191101312T CY 1122470 T1 CY1122470 T1 CY 1122470T1
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group
alkyl
hydrogen
nr4r5
heterocycloalkyl
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CY20191101312T
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English (en)
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Stefan Tasler
Ilga KRIMMELBEIN
Jürgen Kraus
Mirko Zaja
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4Sc Ag
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Publication of CY1122470T1 publication Critical patent/CY1122470T1/el

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Abstract

Η παρούσα εφεύρεση σχετίζεται με μια ένωση του γενικού χημικού τύπου (II) ή ένα άλας ή επιδιαλυτωμένο άλας εξ αυτής, ως επίσης και ιατρικές χρήσεις ενέχοντας αυτές, όπου το Α1 επιλέγεται από την ομάδα συνιστάμενη από Ν και C-R8˙ το Α2 επιλέγεται από την ομάδα συνιστάμενη από Ν και C-R3˙ το Α3 επιλέγεται από την ομάδα συνιστάμενη από Ν και C-R9˙ τα Α4 και Α5 και Α6 επιλέγονται ανεξαρτήτως από την ομάδα συνιστάμενη από Ν και C-R1˙ το R1 επιλέγεται από την ομάδα συνιστάμενη από υδρογόνο, (C1-C3)αλκύλιο, αλογόνο, (C1-C3)αλκοξυομάδα, και (C1-C3)αλοαλκύλιο˙ το R2 επιλέγεται από την ομάδα συνιστάμενη από υδρογόνο, αλογόνο, και (C1-C3)αλκύλιο˙ το R3 επιλέγεται από την ομάδα συνιστάμενη από υδρογόνο, (C1-C3)αλκύλιο, NR4R5, (C1-C3)αλκυλ-NR4R5, και κυανομάδα, όπου τα R4 και R5 επιλέγονται ανεξαρτήτως από την ομάδα συνιστάμενη από υδρογόνο, (C3-C5)κυκλοαλκύλιο, (C3-C5)ετεροκυκλοαλκύλιο και (C1-C3)αλκύλιο, ή τα R4 και R5 μαζί με το άτομο αζώτου στο οποίο αυτά προσαρτώνται σχηματίζουν έναν 5- έως 7-μελή ετεροκυκλικό δακτύλιο περιλαμβάνοντας προαιρετικώς επιπλέον στο προαναφερθέν άτομο αζώτου μια περαιτέρω ομάδα ετεροατόμου που επιλέγεται από την ομάδα συνιστάμενη από Ο και NR6, όπου το R6 επιλέγεται από την ομάδα συνιστάμενη από υδρογόνο, μεθύλιο, ακετύλιο και φορμύλιο˙ το Υ επιλέγεται από την ομάδα συνιστάμενη από Ο και S˙ το R8 επιλέγεται από την ομάδα συνιστάμενη από (C1-C4)αλκύλιο, (C3-C5)κυκλοαλκύλιο και (C3-C5)ετεροκυκλοαλκύλιο˙ και το R9 επιλέγεται από την ομάδα συνιστάμενη από υδρογόνο, (C1-C3)αλκύλιο και (C1-C3)αλκυξυομάδα˙ όπου ορισμένες ειδικότερες ενώσεις αποκλείονται από παραδοχή, και μεθόδους για παραγωγή τέτοιων ενώσεων.
CY20191101312T 2015-03-13 2019-12-13 Αναστολεις kv1.3 και η ιατρικη εφαρμογη αυτων CY1122470T1 (el)

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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
EP3133065A1 (en) 2015-08-21 2017-02-22 Merck Patent GmbH Compounds for optically active devices
EP3363793A1 (en) 2017-02-15 2018-08-22 Merck Patent GmbH Hydrophobic compounds for optically active devices
EP3363786A1 (en) 2017-02-15 2018-08-22 Merck Patent GmbH Compounds for optically active devices
WO2019057821A1 (en) 2017-09-20 2019-03-28 Lead Discovery Center Gmbh COUMARIN DERIVATIVES, PROCESSES FOR PREPARING THEM AND USES THEREOF IN THE TREATMENT OF CANCER
US10703735B2 (en) 2018-07-25 2020-07-07 Lead Discovery Center Gmbh 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof for the treatment of cancer
US20220119376A1 (en) * 2018-09-07 2022-04-21 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tricyclic compounds acting on crbn proteins
WO2020188049A1 (en) 2019-03-20 2020-09-24 Lead Discovery Center Gmbh Quinoline derivatives, processes for their preparation and uses thereof for the treatment of cancer
MX2022011615A (es) 2020-05-20 2022-12-15 AMO Ireland Derivados de azacoumarina y azatiocumarina para uso en dispositivos ópticamente activos.
CN115960112B (zh) * 2023-02-03 2024-02-20 北京大学深圳医院(北京大学深圳临床医学院) 一种花椒毒醇衍生物及其制备方法和应用

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5729765A (en) 1980-10-08 1982-02-17 Yuuichi Yanagi Melting of snow on roof
US6861405B2 (en) 2001-06-12 2005-03-01 Yale University Compositions and methods relating to glucose metabolism, weight control, and food intake
AUPS127202A0 (en) 2002-03-20 2002-04-18 Walter And Eliza Hall Institute Of Medical Research, The Therapeutic ion channel blocking agents and methods of use thereof
US7772408B1 (en) 2002-08-29 2010-08-10 The Regents Of The University Of California Substituted 5-alkoxypsoralens as inhibitors of potassium channel activity in lymphocytes and other cells
JP2006515274A (ja) 2002-10-08 2006-05-25 マサチューセッツ・インスティテュート・オブ・テクノロジー コレステロール輸送の調節のための化合物
ITPD20020325A1 (it) 2002-12-18 2004-06-19 Consorzio Interuniversitario Nazionale La Chimic Sintesi di aniline funzionalizzate mono-n-sostituite.
CN100486245C (zh) 2003-07-31 2009-05-06 中兴通讯股份有限公司 一种支持多媒体消息版权保护的多媒体消息业务实现方法
US7557138B2 (en) 2004-10-04 2009-07-07 The Regents Of The University Of California 5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel
WO2006096911A1 (en) 2005-03-15 2006-09-21 Harvey Andrew J Novel potassium channel blockers and uses thereof
CN101232886A (zh) 2005-08-17 2008-07-30 索尔瓦药物有限公司 使用钾通道抑制性化合物的方法
WO2007139771A1 (en) 2006-05-22 2007-12-06 The Johns Hopkins University Kv channels in neurodegeneration and neuroprotection
US8309545B2 (en) 2006-10-04 2012-11-13 Bionomics Limited Benzofuran potassium channel blockers and uses thereof
US8217189B2 (en) 2006-10-04 2012-07-10 Bionomics Limited Chromenone potassium channel blockers and uses thereof
CN101307056B (zh) * 2007-05-16 2011-04-27 中国科学院上海药物研究所 线型呋喃香豆素衍生物、其制备方法和用途、以及包含该衍生物的药物组合物
CA2701579A1 (en) 2007-10-04 2009-04-09 Bionomics Ltd. Novel aryl potassium channel blockers and uses thereof
US9114102B2 (en) 2007-11-07 2015-08-25 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Method of inhibiting ABCG2 and related treatments
EP2303850A4 (en) 2008-06-13 2012-10-31 Bionomics Ltd NOVEL BLOCKERS OF THE POTASSIUM CHANNEL AND THEIR USES
GB0815782D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
ES2345527B1 (es) 2008-10-08 2011-09-08 Hospital Clinic I Provincial De Barcelona Sustancias bloqueadoras de los canales kv 1.3 para el tratamiento de enfermedades asociadas a hiperplasia de la intima.
AR074558A1 (es) 2008-12-12 2011-01-26 Solvay Pharm Bv Espiro azepan oxazolidinonas como bloqueadores del canal de potasio kv1.3
WO2010130638A1 (en) 2009-05-14 2010-11-18 Evotec Ag Sulfonamide compounds, pharmaceutical compositions and uses thereof
US8859207B2 (en) 2009-09-15 2014-10-14 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Pharmaceutical compositions which inhibit FKBP52-mediated regulation of androgen receptor function and methods of using same
CN102091067B (zh) * 2009-12-09 2013-04-10 中国科学院上海药物研究所 呋喃香豆素类化合物在制备药物中的新用途
WO2011073273A1 (en) 2009-12-16 2011-06-23 Evotec Ag Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators
WO2011073269A1 (en) 2009-12-16 2011-06-23 Evotec Ag Piperidine aryl sulfonamide derivatives as kv1.3 modulators
WO2011073277A1 (en) 2009-12-16 2011-06-23 Evotec Ag PIPERIDINE ARYL SULFONAMIDE DERIVATIVES AS Kv1.3 MODULATORS
US9737585B2 (en) 2011-03-02 2017-08-22 Bioincept, Llc Compositions and methods for treatment of intracellular damage and bacterial infection
US20140171455A1 (en) * 2011-06-09 2014-06-19 The Regents Of The University Of California Reduction of Microglia-Mediated Neurotoxicity by Kv1.3 Inhibition
RU2014117558A (ru) 2011-10-03 2015-11-10 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Лечение ожирения и нарушений, связанных с ожирением, путем нацеливания фармакологических агентов на калиевые каналы
BR112018069854A2 (pt) * 2016-03-31 2019-01-29 Toray Industries métodos para produzir proteína, xilo-oligossacarídeos e glicose, método para suprimir a diminuição na saturação de oxigênio dissolvido ao cultivar um fungo e composição de celulase

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