CY1123797T1 - Αναστολεις kv1.3 και η ιατρικη εφαρμογη τους - Google Patents
Αναστολεις kv1.3 και η ιατρικη εφαρμογη τουςInfo
- Publication number
- CY1123797T1 CY1123797T1 CY20201100815T CY201100815T CY1123797T1 CY 1123797 T1 CY1123797 T1 CY 1123797T1 CY 20201100815 T CY20201100815 T CY 20201100815T CY 201100815 T CY201100815 T CY 201100815T CY 1123797 T1 CY1123797 T1 CY 1123797T1
- Authority
- CY
- Cyprus
- Prior art keywords
- group
- alkyl
- hydrogen
- nr4r5
- heterocycloalkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 6
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
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- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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Abstract
Η παρούσα εφεύρεση αφορά σε μια ένωση του γενικού τύπου (III) ή ένα άλας, ουσία διάλυσης ή προφάρμακό της, καθώς επίσης και στις ιατρικές χρήσεις στις οποίες αυτές συμμετέχουν, όπου (III) το Α1 επιλέγεται από την ομάδα που αποτελείται από Ν και C-R8, το Α2 επιλέγεται από την ομάδα που αποτελείται από Ν και C-R3, το Α3 επιλέγεται από την ομάδα που αποτελείται από Ν και C-R9, το Α4 και το Α5 και το Α6 επιλέγονται ανεξάρτητα από την ομάδα που αποτελείται από Ν και C-R1, το R1 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο, (C1-C3)αλκύλιο, αλογόνο, (C1-C3)αλκόξυ, και (C1-C3)αλοαλκύλιο, το R2 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο, αλογόνο, και (C1-C3)αλκύλιο, το R3 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο, (C1-C3)αλκύλιο, NR4R5, (C1-C3)αλκύλιο-NR4R5 και κύανο, όπου το R4 και το R5 επιλέγονται ανεξάρτητα από την ομάδα που αποτελείται από υδρογόνο, (C3-C5)κυκλοαλκύλιο, (C3-C5)ετεροκυκλοαλκύλιο, (C1-C3)αλκύλιο, ή το R4 και το R5 μαζί με το άτομο αζώτου στο οποίο είναι προσαρτημένα σχηματίζουν έναν ετεροκυκλικό δακτύλιο με 5 έως 7 μέλη, ο οποίος περιλαμβάνει προαιρετικά, εκτός από το προαναφερθέν άτομο αζώτου, μια περαιτέρω ομάδα ετεροατόμου που επιλέγεται από την ομάδα που αποτελείται από Ο and NR6, όπου το R6 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο, μεθύλιο, ακετύλιο και φορμύλιο, το Υ επιλέγεται από την ομάδα που αποτελείται από Ο and S, το R7 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο, και (C1-C3)αλκύλιο, τo R8 επιλέγεται από την ομάδα που αποτελείται από (C1-C4)αλκύλιο, (C3-C5)κυκλοαλκύλιο και (C3-C5)ετεροκυκλοαλκύλιο, το R9 επιλέγεται από την ομάδα που αποτελείται από υδρογόνο,(C1-C3)αλκύλιο και (C1-C3)αλκόξυ, καθώς και σε μεθόδους για παραγωγή αυτών των ενώσεων.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15159083 | 2015-03-13 | ||
PCT/EP2016/055441 WO2016146575A1 (en) | 2015-03-13 | 2016-03-14 | Kv1.3 inhibitors and their medical application |
Publications (1)
Publication Number | Publication Date |
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CY1123797T1 true CY1123797T1 (el) | 2022-03-24 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CY20201100815T CY1123797T1 (el) | 2015-03-13 | 2020-09-01 | Αναστολεις kv1.3 και η ιατρικη εφαρμογη τους |
Country Status (29)
Country | Link |
---|---|
US (2) | US10399991B2 (el) |
EP (1) | EP3268372B9 (el) |
JP (1) | JP6506410B2 (el) |
KR (1) | KR20170137055A (el) |
CN (1) | CN107548396B (el) |
AU (1) | AU2016232330B2 (el) |
BR (1) | BR112017019386A2 (el) |
CA (1) | CA2979501A1 (el) |
CY (1) | CY1123797T1 (el) |
DK (1) | DK3268372T3 (el) |
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MX2022004144A (es) * | 2019-10-07 | 2022-06-14 | De Shaw Res Llc | Compuestos heterobiciclicos de arilo como bloqueadores del canal de potasio tipo shaker kv1.3. |
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JPS5729765A (en) | 1980-10-08 | 1982-02-17 | Yuuichi Yanagi | Melting of snow on roof |
ID28959A (id) * | 1998-12-04 | 2001-07-19 | Bristol Myers Squibb Co | Turunan-turunan 3-tersubstitusi-4-arilkinolin-2-on sebagai modulator saluran kalium |
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 |
US20040171073A1 (en) | 2002-10-08 | 2004-09-02 | Massachusetts Institute Of Technology | Compounds for modulation of cholesterol transport |
ITPD20020325A1 (it) | 2002-12-18 | 2004-06-19 | Consorzio Interuniversitario Nazionale La Chimic | Sintesi di aniline funzionalizzate mono-n-sostituite. |
EP1743069A1 (de) | 2004-05-07 | 2007-01-17 | Voith Patent GmbH | Saugwalze in einer maschine zur herstellung einer faserstoffbahn |
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 |
RU2008109911A (ru) | 2005-08-17 | 2009-09-27 | Зольвай Фармасьютикалз Гмбх (De) | Способ применения соединений, ингибирующих калиевые каналы |
US20100239562A1 (en) | 2006-05-22 | 2010-09-23 | The Johns Hopkins University | Kv CHANNELS IN NEURODEGENERATION AND NEUROPROTECTION |
WO2008040058A1 (en) | 2006-10-04 | 2008-04-10 | Bionomics Limited | Novel chromenone potassium channel blockers and uses thereof |
NZ575685A (en) | 2006-10-04 | 2012-04-27 | Bionomics Ltd | Novel benzofuran 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 |
BRPI0817520A2 (pt) | 2007-10-04 | 2015-08-18 | Bionomics Ltd | Novos bloqueadores de canal de aril potássio e usos destes |
WO2009061770A2 (en) | 2007-11-07 | 2009-05-14 | 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 | NEW KALIUM CHANNEL BLOCKS AND APPLICATIONS THEREOF |
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 |
WO2011034834A2 (en) | 2009-09-15 | 2011-03-24 | 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 |
AU2012318736A1 (en) | 2011-10-03 | 2014-05-22 | The Regents Of The University Of California | Treatment of obesity and obesity-related disorders by pharmacological targeting of Kv1.3 potassium channels |
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- 2016-03-14 WO PCT/EP2016/055441 patent/WO2016146575A1/en active Application Filing
- 2016-03-14 AU AU2016232330A patent/AU2016232330B2/en not_active Ceased
- 2016-03-14 SM SM20200475T patent/SMT202000475T1/it unknown
- 2016-03-14 EP EP16709798.9A patent/EP3268372B9/en active Active
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- 2016-03-14 BR BR112017019386-8A patent/BR112017019386A2/pt not_active IP Right Cessation
- 2016-03-14 KR KR1020177025481A patent/KR20170137055A/ko not_active Application Discontinuation
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- 2016-03-14 CA CA2979501A patent/CA2979501A1/en not_active Abandoned
- 2016-03-14 HU HUE16709798A patent/HUE050606T2/hu unknown
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- 2017-09-11 PH PH12017501653A patent/PH12017501653B1/en unknown
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2018
- 2018-03-12 HK HK18103377.7A patent/HK1243998A1/zh unknown
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2019
- 2019-07-25 US US16/522,124 patent/US20190352308A1/en not_active Abandoned
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2020
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