HUP0201314A2 - Aril-szubsztituált pirazolok, imidazolok, oxazolok, tiazolok és pirrolok, valamint ezek alkalmazása és az ezeket tartalmazó gyógyászati készítmények - Google Patents
Aril-szubsztituált pirazolok, imidazolok, oxazolok, tiazolok és pirrolok, valamint ezek alkalmazása és az ezeket tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP0201314A2 HUP0201314A2 HU0201314A HUP0201314A HUP0201314A2 HU P0201314 A2 HUP0201314 A2 HU P0201314A2 HU 0201314 A HU0201314 A HU 0201314A HU P0201314 A HUP0201314 A HU P0201314A HU P0201314 A2 HUP0201314 A2 HU P0201314A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- oxazoles
- thiazoles
- pyrroles
- imidazoles
- Prior art date
Links
- 125000003118 aryl group Chemical group 0.000 title abstract 2
- 150000002460 imidazoles Chemical class 0.000 title abstract 2
- 150000002916 oxazoles Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000003217 pyrazoles Chemical class 0.000 title abstract 2
- 150000003233 pyrroles Chemical class 0.000 title abstract 2
- 150000003557 thiazoles Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000002193 Pain Diseases 0.000 abstract 3
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 108091006146 Channels Proteins 0.000 abstract 1
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 abstract 1
- 206010056677 Nerve degeneration Diseases 0.000 abstract 1
- 108010052164 Sodium Channels Proteins 0.000 abstract 1
- 102000018674 Sodium Channels Human genes 0.000 abstract 1
- 208000009205 Tinnitus Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 208000005298 acute pain Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000001773 anti-convulsant effect Effects 0.000 abstract 1
- 239000003416 antiarrhythmic agent Substances 0.000 abstract 1
- 208000028683 bipolar I disease Diseases 0.000 abstract 1
- 230000000903 blocking effect Effects 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 230000002920 convulsive effect Effects 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 239000003589 local anesthetic agent Substances 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 239000002287 radioligand Substances 0.000 abstract 1
- 239000011734 sodium Substances 0.000 abstract 1
- 229910052708 sodium Inorganic materials 0.000 abstract 1
- 231100000886 tinnitus Toxicity 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/416—2,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Anesthesiology (AREA)
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- Psychology (AREA)
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- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Pyrrole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
A találmány tárgyát az (I) általános képletű aril-szubsztituáltpirazolok, imidazolok, oxazolok, tiazolok és pirrolok képezik,melyekről felismerték, hogy görcsoldó hatásúak, és a nátrium (Na+)csatornák blokkolásával hatnak. Az (I) általános képletben Heetjelentése a fenti heterociklusos csoportok valamelyike adott esetbenhelyettesítve, R5-R13 jelentései egymástól függetlenül előnyösenhidrogén vagy halogénatom, alkil-, haloalkil-, cikloalkil-, aril- vagyheteroarilcsoport. A találmány további tárgya gyógyászati készítmény,amely hatásos mennyiségű (I) általános képletű vegyületet tartalmazegy vagy több gyógyászatilag elfogadható hordozóanyaggal vagyhígítóanyaggal együtt. A találmány tárgya ezen kívül tetszőleges, 3Hés 14C izotóppal jelölt fenti vegyület, valamint ezek alkalmazásaradioligandumként a nátriumcsatornák kötőhelyén. A találmány szerintivegyületek alkalmasak az alábbi rendellenességek kezelésére,megelőzésére vagy enyhítésére: globális és fokális ischaemiát követőidegi leépülés, fájdalom - beleértve az akut, krónikus és neuropátiásfájdalmat -, görcsös és neurodegeneratív állapot, mániás depresszió;valamint az (I) általános képletű vegyület alkalmazható helyiérzéstelenítőként, antiaritmiás szerként és fülzúgás kezelésére. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12655399P | 1999-03-26 | 1999-03-26 | |
PCT/US2000/007944 WO2000057877A1 (en) | 1999-03-26 | 2000-03-24 | Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0201314A2 true HUP0201314A2 (hu) | 2002-12-28 |
HUP0201314A3 HUP0201314A3 (en) | 2003-02-28 |
Family
ID=22425462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0201314A HUP0201314A3 (en) | 1999-03-26 | 2000-03-24 | Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof and pharmaceutical compositions containing them |
Country Status (29)
Country | Link |
---|---|
US (2) | US6414011B1 (hu) |
EP (2) | EP1173169B1 (hu) |
JP (2) | JP4832647B2 (hu) |
KR (1) | KR20020015308A (hu) |
CN (1) | CN1353605A (hu) |
AR (1) | AR023171A1 (hu) |
AT (1) | ATE467620T1 (hu) |
AU (1) | AU782353B2 (hu) |
BR (1) | BR0009322A (hu) |
CA (1) | CA2368631A1 (hu) |
CY (1) | CY1111163T1 (hu) |
CZ (1) | CZ20013435A3 (hu) |
DE (2) | DE60044395D1 (hu) |
DK (1) | DK1173169T3 (hu) |
ES (1) | ES2345921T3 (hu) |
HU (1) | HUP0201314A3 (hu) |
IL (1) | IL145508A0 (hu) |
MX (1) | MXPA01009655A (hu) |
NO (1) | NO20014659L (hu) |
NZ (2) | NZ514756A (hu) |
PL (1) | PL351439A1 (hu) |
PT (1) | PT1173169E (hu) |
RU (1) | RU2001129155A (hu) |
TR (1) | TR200102790T2 (hu) |
TW (1) | TW502019B (hu) |
UA (1) | UA72244C2 (hu) |
WO (1) | WO2000057877A1 (hu) |
YU (1) | YU68701A (hu) |
ZA (1) | ZA200108807B (hu) |
Families Citing this family (116)
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US7517880B2 (en) * | 1997-12-22 | 2009-04-14 | Bayer Pharmaceuticals Corporation | Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas |
US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
EP1158985B1 (en) | 1999-01-13 | 2011-12-28 | Bayer HealthCare LLC | OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS |
ATE303162T1 (de) * | 1999-04-09 | 2005-09-15 | Euro Celtique Sa | Natrium kanalblocker zusammensetzungen und deren verwendung |
TWI292316B (en) * | 1999-10-11 | 2008-01-11 | Sod Conseils Rech Applic | Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof |
AR029489A1 (es) | 2000-03-10 | 2003-07-02 | Euro Celtique Sa | Piridinas, pirimidinas, pirazinas, triazinas sustituidas por arilo, composiciones farmaceuticas y el uso de las mismas para la manufactura de un medicamento |
MXPA02009279A (es) | 2000-03-24 | 2004-09-10 | Euro Celtique Sa | Pirazoles, triazoles y tetrazoles sustituidos con arilo como bloqueadores del canal de sodio. |
AU2001249610B2 (en) | 2000-03-31 | 2005-03-24 | Euro-Celtique S.A. | Aminopyridines and their use as anticonvulsants and sodium channel blockers |
FR2818978B1 (fr) * | 2000-12-28 | 2003-02-28 | Sod Conseils Rech Applic | Modulateurs de canaux sodiques derives de 2-piperidylimidazoles |
TWI248438B (en) * | 2001-04-10 | 2006-02-01 | Sod Conseils Rech Applic | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
FR2825926A1 (fr) * | 2001-06-14 | 2002-12-20 | Sod Conseils Rech Applic | Derives d'imidazoles modulant les canaux sodiques |
MXPA04000411A (es) * | 2001-07-16 | 2004-03-18 | Euro Celtique Sa | Tiazolidinonas arilo sustituidas y uso de las mismas. |
AU2002333374B2 (en) | 2001-09-03 | 2007-03-22 | Newron Pharmaceuticals S.P.A. | Pharmaceutical composition comprising gabapentin or an analogue thereof and an (alpha)- aminoamide and its analgesic use |
AR036873A1 (es) * | 2001-09-07 | 2004-10-13 | Euro Celtique Sa | Piridinas aril sustituidas a, composiciones farmaceuticas y el uso de las mismas para la preparacion de un medicamento |
AR037233A1 (es) * | 2001-09-07 | 2004-11-03 | Euro Celtique Sa | Piridinas aril sustituidas, composiciones farmaceuticas y el uso de dichos compuestos para la elaboracion de un medicamento |
EP1478358B1 (en) | 2002-02-11 | 2013-07-03 | Bayer HealthCare LLC | Sorafenib tosylate for the treatment of diseases characterized by abnormal angiogenesis |
EP1483247B1 (en) * | 2002-03-13 | 2009-06-24 | Euro-Celtique S.A. | Aryl substituted pyrimidines and the use thereof |
AU2003257033A1 (en) * | 2002-07-31 | 2004-02-16 | Euro-Celtique S.A. | Aryl substituted benzimidazoles and their use as sodium channel blockers |
EP1438956A1 (en) * | 2003-01-16 | 2004-07-21 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful as antimigraine agents |
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