AR027032A1 - DERIVATIVES OF BENZIMIDAZOL REPLACED SUBSTITUTES OF HOMOPIPERIDINIL - Google Patents
DERIVATIVES OF BENZIMIDAZOL REPLACED SUBSTITUTES OF HOMOPIPERIDINILInfo
- Publication number
- AR027032A1 AR027032A1 ARP000106788A ARP000106788A AR027032A1 AR 027032 A1 AR027032 A1 AR 027032A1 AR P000106788 A ARP000106788 A AR P000106788A AR P000106788 A ARP000106788 A AR P000106788A AR 027032 A1 AR027032 A1 AR 027032A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- hydrogen
- aryl1
- trifluoromethanesulfonyl
- Prior art date
Links
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical class C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- -1 homopiperidinyl Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 5
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 3
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 3
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 230000002040 relaxant effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invencion se relaciona con compuestos de formula (1) sus profármacos, N-oxidos, sales de adicion, aminas cuaternarias y formasestereoquímicamente isoméricas, en donde el radical bivalente representa un homopiperidinilo saturado o insatura do que tiene un enlace doble, y en donde dichoradical bivalente es sustituido por R2 siendo R2 hidrogeno, hidroxi, alquilo C1-4 o alquiloxi C-4; -a1=a2-a3=a4- representa un radical bivalente opocionalmentesustituido; R1 es hidrogeno, alquilo C1-6, ar ilo1, alquilo C1-6 sustituido con arilo1, alquiloxicarbonilo C1-4, aril1carbonilo, aril1alquilcaaarbonilo C1-6,alquilcarbonilo C1-4, trifluorometilo, trifluorometilcaarbonilo, alquisulfonilo C1-6 aril1sulfonilo, metanosulfonilo, bencenosulfonilo, tri fluormetanosulfonilodimetilsulfamoílo; X representa O, S, o NR3, en donde R3 es hidrogeno; alquilo C1-6; metanosulfonilo; bencenosulfonilo; trifluorometanosulfonil,dimetilsulfamoílo; X representa O, S, o NR3, en donde R3 es hidrogeno; alquilo C1-6; m etanosulfonilo; bencenosulfonilo; trifluorometanosulfonilo;dimetilsulamoílo; X representa O, S o NR3, en donde R3 es hidrogeno; alquilo C1-6; metanosulfonilo; bencenosulfonilo; trifluorometanosulfonilo;dimetilsulfamoílo; alquilo C1-4 sustituido con a rilo 2, y opcionalmente con hidroxi; alquilcarbonil C1-4 alquilo C1-4 sustituido con arilo2; arilo1 es feniloopcionalmente sustituido, pirimidilo opcionalmente sustituido, naftilo, quinolinilo; o 1,3-benzodioxolilo; arilo2 es fenilo opcionalmente sus tituido, actividadrelajante fundica. Se describen procesos para la preparacion de dichos productos, formulaciones que comprende dichos productos y su uso como una medicina enparticular para el tratamiento de síntomas dispépticos, síndrome de intestin o irritable y otras condiciones relacionadas con una relajacion deteriorada uobstaculizada del fondo.The present invention relates to compounds of formula (1) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical represents a saturated or unsaturated homopiperidinyl having a double bond, and wherein bivalent radical is substituted by R2 being R2 hydrogen, hydroxy, C1-4 alkyl or C-4 alkyloxy; -a1 = a2-a3 = a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1alkylcarbarylcarbonyl, C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcaarbonyl, C1-6 alkylsulfonyl, methanesulfonyl, sulfonyl , tri fluoromethanesulfonylodimethylsulfamoyl; X represents O, S, or NR3, where R3 is hydrogen; C1-6 alkyl; methanesulfonyl; benzenesulfonyl; trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S, or NR3, where R3 is hydrogen; C1-6 alkyl; m ethanesulfonyl; benzenesulfonyl; trifluoromethanesulfonyl; dimethylsulamoyl; X represents O, S or NR3, where R3 is hydrogen; C1-6 alkyl; methanesulfonyl; benzenesulfonyl; trifluoromethanesulfonyl; dimethylsulfamoyl; C1-4 alkyl substituted with a ryl 2, and optionally with hydroxy; C 1-4 alkylcarbonylC 1-4 alkyl substituted with aryl2; aryl1 is phenyl optionally substituted, optionally substituted pyrimidyl, naphthyl, quinolinyl; or 1,3-benzodioxolyl; aryl2 is optionally its substituted phenyl, ironic relaxing activity. Processes for the preparation of said products are described, formulations comprising said products and their use as a particular medicine for the treatment of dyspeptic symptoms, bowel or irritable syndrome and other conditions related to a deteriorated or obstacized fundus relaxation.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP6246660A JPH0873461A (en) | 1994-09-06 | 1994-09-06 | Novel camptothecin derivative, its production method and antitumor agent |
EP99204441 | 1999-12-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR027032A1 true AR027032A1 (en) | 2003-03-12 |
Family
ID=37515280
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP000106788A AR027032A1 (en) | 1994-09-06 | 2000-12-20 | DERIVATIVES OF BENZIMIDAZOL REPLACED SUBSTITUTES OF HOMOPIPERIDINIL |
Country Status (1)
Country | Link |
---|---|
AR (1) | AR027032A1 (en) |
-
2000
- 2000-12-20 AR ARP000106788A patent/AR027032A1/en not_active Application Discontinuation
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant, registration | ||
FD | Application declared void or lapsed, e.g., due to non-payment of fee |