AR048260A1 - Compuestos de heteroaril- y fenilsulfamoilo sustituidos - Google Patents
Compuestos de heteroaril- y fenilsulfamoilo sustituidosInfo
- Publication number
- AR048260A1 AR048260A1 ARP050100890A ARP050100890A AR048260A1 AR 048260 A1 AR048260 A1 AR 048260A1 AR P050100890 A ARP050100890 A AR P050100890A AR P050100890 A ARP050100890 A AR P050100890A AR 048260 A1 AR048260 A1 AR 048260A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- optionally substituted
- phenyl
- alkyl
- alkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 12
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 7
- -1 phenylsulfamoyl compounds Chemical class 0.000 abstract 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000002971 oxazolyl group Chemical group 0.000 abstract 3
- 125000000335 thiazolyl group Chemical group 0.000 abstract 3
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004011 3 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000001845 4 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 239000012190 activator Substances 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005366 cycloalkylthio group Chemical group 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000006503 p-nitrobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1[N+]([O-])=O)C([H])([H])* 0.000 abstract 1
- 239000003614 peroxisome proliferator Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
Classifications
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/44—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C323/46—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms
- C07C323/49—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
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- 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
- C07D263/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract
La presente se refiere a compuestos de heteroaril- y fenilsulfamoílo sustituidos, composiciones farmacéuticas que contienen tales compuestos y al uso de tales compuestos como agonistas del receptor activador del proliferador de peroxisoma (PPAR). Reivindicacion 1: Un compuesto que tiene formula (1) o un profármaco de dicho compuesto o una sal farmacéuticamente aceptable de dicho compuesto o profármaco, en el que Q es C: cada R1 es independientemente H, halo, alquilo C1-5, opcionalmente sustituido con uno o más halo o con alcoxi C1-3, alcoxi C1-5 opcionalmente sustituido con uno a once halo, alquiltio C1-5 opcionalmente sustituido con uno o más halo, o R1 junto con los dos átomos de C adyacentes forma un anillo carbocíclico 5-6 de cinco o seis miembros condensado, totalmente saturado, parcialmente insaturado o totalmente insaturado en el que cada C en la cadena de carbono puede reemplazarse opcionalmente por un heteroátomo seleccionado entre O y S; R2 es H o alquilo C1-5 opcionalmente sustituido con alcoxi C1-3; X es -COOR4, -O-(CR32)-COOR4, -S-(CR32)-COOR4, CH2-(CR5w)-COOR4, 1H-tetrazol-5-il-E- o tiazolidindiona-5-il-G-; donde w es 0, 1 o 2; E es (CH2)r y r es 0, 1, 2, o 3, y G es (CH2)s o metilideno y s es 0 o 1; cada R3 es independientemente H, alquilo C1-4 opcionalmente sustituido con uno a nueve halo o con alcoxi C1-3 opcionalmente sustituido con uno o más halo, o R3 y el C al que está unido forman un anillo carbocíclico de 3, 4, 5 o 6 miembros; R4 es H, alquilo C1-4; bencilo o p-nitrobencilo cada R5 es independientemente H, alquilo C1-4 opcionalmente sustituido con uno a mueve halo o con alcoxi C1-3, alcoxi C1-4 opcionalmente sustituido con uno a nueve halo, alquiltio C1-4 opcionalmente sustituido con uno a nueve halo, o con alcoxi C1-3, o R5 y el C al que está unido forman un anillo carbocíclico de 3, 4, 5 o 6 miembros en el que cualquier C de un anillo de 5 o 6 miembros puede reemplazarse por un átomo de O; Ar1 es fenilo o fenilo condensado a un miembro seleccionado entre tiazolilo, furanilo, oxazolilo, pirimidina, fenilo o tienilo, donde Ar1 está opcionalmente mono-, di- o tri-sustituido independientemente con: halo, alquilo C1-3 opcionalmente sustituido con uno a nueve halo o alcoxi C1-3 opcionalmente sustituido con uno a nueve halo o alquiltio C1-3 opcionalmente sustituido con uno a nueve halo; B es un enlace, CO, (CY2)n, CYOH, CY=CY, -L-(CY2)n-, -(CY2)n-L-, -L-(CY2)2-L-, NY-OC-CONY-, -SO2NY-, -NY-SO2- donde cada L es independientemente O, S, SO o SO2, cada Y es independientemente H o alquilo C1-3 y n es 0, 1, 2 o 3; Ar2 es un enlace, fenilo, fenoxibencilo, fenoxifenilo, benciloxifenilo, benciloxibencilo, pirimidilo, piridinilo, pirazolilo, imidazolilo, tiazolilo, tiadiazolilo, oxazolilo, oxadiazolilo o fenilo condensado a un anillo seleccionado entre el grupo compuesto por: fenilo, pirimidinilo, tienilo, furanilo, pirrolilo, tiazolilo, oxazolilo, pirazolilo e imidazolilo; cada J es independientemente H, hidroxi, halo, alquilo C1-8, opcionalmente sustituido con de uno a once halo, alcoxi C1-8 opcionalmente sustituido con uno a once halo, alquiltio C1-8 opcionalmente sustituido con uno a once halo, cicloalquilo C3-7, cicloalcoxi C3-7, cicloalquiltio C3-7 o fenilo opcionalmente sustituido con uno a cuatro sustituyentes seleccionados entre el grupo compuesto por: halo, alquilo C1-3 opcionalmente sustituido con uno a cinco halo, alcoxi C1-3 opcionalmente sustituido con uno a cinco halo, alquiltio C1-3 opcionalmente sustituido con uno a cinco halo; p y q son cada uno independientemente 0, 1, 2 o 3; y con las condiciones: a) si Ar1 es fenilo, B es un enlace, Ar2 es un enlace o fenilo y X es -COOH, entonces q es diferente de 0 y J es diferente de H, halo, alquilo C1-8 o fenilo no sustituido; b) si Ar1 es fenilo, B no es un enlace, Ar2 es fenilo y X es -COOR4 entonces B se une a Ar1 en posicion para a NR2; y c) si B es O, S, SO, NH, CO, CH2 o SO2 entonces R1 no es H.
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| US55211404P | 2004-03-10 | 2004-03-10 | |
| US11/012,139 US7262318B2 (en) | 2004-03-10 | 2004-12-16 | Substituted heteroaryl- and phenylsulfamoyl compounds |
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| Application Number | Title | Priority Date | Filing Date |
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| ARP050100890A AR048260A1 (es) | 2004-03-10 | 2005-03-08 | Compuestos de heteroaril- y fenilsulfamoilo sustituidos |
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| PE (1) | PE20051147A1 (es) |
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-
2004
- 2004-12-16 US US11/012,139 patent/US7262318B2/en not_active Expired - Fee Related
-
2005
- 2005-02-23 DO DO2005P000025A patent/DOP2005000025A/es unknown
- 2005-02-28 AP AP2006003714A patent/AP2006003714A0/xx unknown
- 2005-02-28 WO PCT/IB2005/000526 patent/WO2005092845A1/en not_active Ceased
- 2005-02-28 CA CA002559035A patent/CA2559035A1/en not_active Abandoned
- 2005-02-28 BR BRPI0508555-1A patent/BRPI0508555A/pt not_active IP Right Cessation
- 2005-02-28 JP JP2007502428A patent/JP2007528387A/ja not_active Withdrawn
- 2005-02-28 AU AU2005225628A patent/AU2005225628B2/en not_active Expired - Fee Related
- 2005-02-28 KR KR1020067018485A patent/KR20070001173A/ko not_active Abandoned
- 2005-02-28 EA EA200601442A patent/EA200601442A1/ru unknown
- 2005-02-28 EP EP05708637A patent/EP1725524A1/en not_active Withdrawn
- 2005-03-08 AR ARP050100890A patent/AR048260A1/es not_active Application Discontinuation
- 2005-03-08 PE PE2005000265A patent/PE20051147A1/es not_active Application Discontinuation
- 2005-03-09 DO DO2005000034A patent/DOP2005000034A/es unknown
- 2005-03-09 TW TW094107153A patent/TW200610525A/zh unknown
- 2005-03-09 PA PA20058625701A patent/PA8625701A1/es unknown
- 2005-03-10 UY UY28794A patent/UY28794A1/es not_active Application Discontinuation
- 2005-03-10 NL NL1028519A patent/NL1028519C2/nl not_active IP Right Cessation
- 2005-03-10 SV SV2005002047A patent/SV2005002047A/es not_active Application Discontinuation
-
2006
- 2006-06-16 US US11/424,626 patent/US20060258723A1/en not_active Abandoned
- 2006-08-22 IL IL177631A patent/IL177631A0/en unknown
- 2006-09-08 EC EC2006006834A patent/ECSP066834A/es unknown
- 2006-09-08 MA MA29311A patent/MA28461B1/fr unknown
- 2006-10-10 NO NO20064615A patent/NO20064615L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IL177631A0 (en) | 2006-12-31 |
| SV2005002047A (es) | 2005-12-13 |
| US20060258723A1 (en) | 2006-11-16 |
| AU2005225628A1 (en) | 2005-10-06 |
| AU2005225628B2 (en) | 2008-09-11 |
| NO20064615L (no) | 2006-12-07 |
| JP2007528387A (ja) | 2007-10-11 |
| CA2559035A1 (en) | 2005-10-06 |
| NL1028519A1 (nl) | 2005-09-13 |
| BRPI0508555A (pt) | 2007-08-07 |
| PE20051147A1 (es) | 2006-01-28 |
| ECSP066834A (es) | 2006-12-29 |
| US7262318B2 (en) | 2007-08-28 |
| KR20070001173A (ko) | 2007-01-03 |
| NL1028519C2 (nl) | 2006-06-22 |
| TW200610525A (en) | 2006-04-01 |
| EA200601442A1 (ru) | 2007-02-27 |
| EP1725524A1 (en) | 2006-11-29 |
| AP2006003714A0 (en) | 2006-08-31 |
| PA8625701A1 (es) | 2006-01-25 |
| DOP2005000025A (es) | 2006-11-15 |
| DOP2005000034A (es) | 2005-12-15 |
| US20050228015A1 (en) | 2005-10-13 |
| UY28794A1 (es) | 2005-10-31 |
| MA28461B1 (fr) | 2007-03-01 |
| WO2005092845A1 (en) | 2005-10-06 |
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