HUP9901807A2 - Heterogyűrűvel szubsztituált benzolszulfonamidszármazékok, eljárás előállításukra és alkalmazásuk prodrogként gyulladásos megbetegedések kezelésére szolgáló gyógyszerkészítmények előállítására - Google Patents
Heterogyűrűvel szubsztituált benzolszulfonamidszármazékok, eljárás előállításukra és alkalmazásuk prodrogként gyulladásos megbetegedések kezelésére szolgáló gyógyszerkészítmények előállításáraInfo
- Publication number
- HUP9901807A2 HUP9901807A2 HU9901807A HUP9901807A HUP9901807A2 HU P9901807 A2 HUP9901807 A2 HU P9901807A2 HU 9901807 A HU9901807 A HU 9901807A HU P9901807 A HUP9901807 A HU P9901807A HU P9901807 A2 HUP9901807 A2 HU P9901807A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- amino
- aryl
- aralkyl
- carbonyl
- Prior art date
Links
- 125000000623 heterocyclic group Chemical group 0.000 title abstract 4
- 206010061218 Inflammation Diseases 0.000 title abstract 3
- 230000004054 inflammatory process Effects 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 150000008331 benzenesulfonamides Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 furmyl Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 abstract 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 abstract 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 1
- 125000004689 alkyl amino carbonyl alkyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 abstract 1
- 125000004703 alkyl carbonyl aminoalkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000000539 amino acid group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004659 aryl alkyl thio group Chemical group 0.000 abstract 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- 125000005164 aryl thioalkyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 150000004678 hydrides Chemical group 0.000 abstract 1
- 125000001145 hydrido group Chemical group *[H] 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 229940126601 medicinal product Drugs 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
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- 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
- C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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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Abstract
A találmány tárgyát az (I) általánős képletű vegyületek - a képletben A jelentése részlegesen telítetlen heterőciklil-, heterőaril-,ciklőalkenil- és arilcsőpőrt közül választőtt gyűrűs szűbsztitűens,amely adőtt esetben szűbsztitűálható helyzetben halőgénatőm, alkil-karbőnil-, főrmil-, alkil-, halőgén-alkil-, őxő-, cianő-, nitrő-,karbőxil-, alkőxi-, aminő-karbőnil-, alkőxi-karbőnil-, karbőxi-alkil-,cianő-alkil-, hidrőxi-alkil-, halőgén-alkilszűlfőnil-őxi-, alkőxi-alkil-őxi-alkil-, karbőxi-alkőxi-alkil-, ciklőalkil-alkil-, alkenil-,alkinil-, heterőciklil-őxi-, alkil-tiő- ciklőalkil-, aril-,heterőciklil-, ciklőalkenil- aralkil-, heterőciklil-alkil-, alkil-tiő-alkil-, aril-karbőnil-, aralkil-karbőnil-, aralkenil-, alkőxi-alkil-,aril-tiő-alkil-, aril-őxi-alkil-, aralkil-tiő-alkil-, aralkőxi-alkil-,alkőxi-karbőnil-alkil-, aminő-karbőnil-alkil-, alkil-aminő-karbőnil-,N-aril-aminő-karbőnil-, N-alkil-N-aril-aminő-karbőnil-, alkil-aminő-karbőnil-alkil-, alkil-aminő-N-aril-aminő-, N-aralkil-aminő-, N-alkil-N-aralkil-aminő-, N-alkil-N-aril-aminő-, aminő-alkil-, alkil-aminő-alkil-, N-aril-aminő-alkil-, N-aralkil-aminő-alkil-, N-alkil-N-aralkil-aminő-alkil-, N-alkil-N-aril-aminő-alkil-, aril-őxi-, aralk-őxi-, aril-tiő-, aralkil-tiő-, alkilszűlfinil-, alkilszűlfőnil-,aminőszűlfőnil-, alkil-aminőszűlfőnil-, N-aril-aminőszűlfőnil-,arilszűlfőnil- és N-alkil-N-aril-aminőszűlfőnil-csőpőrt közülválasztőtt egy vagy több szűbsztitűenssel van szűbsztitűálva; R1 jelentése heterőciklil-, ciklőalkil-, ciklőalkenil- vagyarilcsőpőrt, amelyek adőtt esetben szűbsztitűálható helyzetben alkil-,halőgén-alkil-, cianő-, karbőxil, alkőxi-karbőnil-, hidrőxil-,hidrőxi-alkil-, halőgén-alkőxi-, aminő-, alkil-aminő-, aril-aminő-,nitrő-, alkőxi-alkil-, alkilszűlfinil-, alkőxi-, alkil-tiő-csőpőrt éshalőgénatőm közül választőtt egy vagy több szűbsztitűenssel vannakszűbsz- titűálva; R2 jelentése hidridő- vagy alkőxi-karbőnil-alkil-csőpőrt; és R3 jelentése alkil-, karbőxi-alkil-, acil-, alkőxi-karbőnil-,heterőaril-karbőnil-, alkőxi-karbőnil-alkil-karbőnil-, alkőxi-karbőnil-karbőnil-csőpőrt, aminősavmaradék vagy alkil-karbőnil-ami-nő-alkil-karbőnil-csőpőrt; azzal a megkötéssel, hőgy A jelentésetetrazóliűm- vagy piridiniűmcsőpőrttól eltérő, tővábbá A jelentéseindanőntól eltérő, ha R3 jelentése alkil- vagy karbőxi-alkil-csőpőrt;tővábbá A jelentése tienilcsőpőrttól eltérő, ha R4 jelentése 4-flűőr-fenil-csőpőrt, ha R2 jelentése hidridcsőpőrt, ha R3 jelentése metil-vagy acetilcsőpőrt. A találmány kiterjed a fenti vegyületekelőállítási eljárására, tővábbá prődrőgkénti alkalmazásűkra gyűlladásés gyűlladással kapcsőlatős rendellenesség kezelésére szőlgálógyógyszerkészítmények előállításánál. ŕ
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Application Number | Priority Date | Filing Date | Title |
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US63151496A | 1996-04-12 | 1996-04-12 | |
PCT/US1997/005497 WO1997038986A1 (en) | 1996-04-12 | 1997-04-11 | Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors |
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HUP9901807A2 true HUP9901807A2 (hu) | 1999-09-28 |
HUP9901807A3 HUP9901807A3 (en) | 2000-08-28 |
HU225473B1 HU225473B1 (en) | 2006-12-28 |
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HU9901807A HU225473B1 (en) | 1996-04-12 | 1997-04-11 | Heterocycle substituted n-acyl benzenesulfonamide derivatives, process for their preparation and their use as prodrug for the preparation of pharmaceutical compositions treating inflammation or inflammation-associated disorders |
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