PE20020822A1 - UREA DERIVATIVES AS ANTAGONISTS OF INTEGRINANTAGONISTS OF HISTAMINE AS O4 RECEPTORS - Google Patents
UREA DERIVATIVES AS ANTAGONISTS OF INTEGRINANTAGONISTS OF HISTAMINE AS O4 RECEPTORSInfo
- Publication number
- PE20020822A1 PE20020822A1 PE20020000372002000023A PE2002000023A PE20020822A1 PE 20020822 A1 PE20020822 A1 PE 20020822A1 PE 20020000372002000023 A PE20020000372002000023 A PE 20020000372002000023A PE 2002000023 A PE2002000023 A PE 2002000023A PE 20020822 A1 PE20020822 A1 PE 20020822A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- histamine
- refers
- antagonists
- Prior art date
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
SE REFIERE A DERIVADOS DE UREA DE FORMULA I, DONDESE REFIERE A UNA COMBINACION SINERGICA DE UN ANTAG R1 ES ALQUILO C3-C10, ALQUENILO C3-C10, ALQUINILOONISTA DE RECEPTOR H1 DE HISTAMINA CON UN ANTAGONI C3-C10, CICLOALQUILO, CICLOALQUILO-ALQUILO C1-C10STA QUE ES AL MENOS 10 VECES MAS SELECTIVO PARA EL RECEPTOR H4 DE HISTAMINA EN COMPARACION CON EL RE, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ALQUILO C0-CEPTOR H3 DE HISTAMINA TAL COMO GPRv53 RECEPTOR ACC2-CICLOALQUILO, ENTRE OTROS; R3 Y R4 SON H, ALQUIOPLADO A PROTEINA G; PARA SER ADMINISTRADA SIMULTALO C1-C4, R2 Y R3 FORMAN UN ANILLO DE 4 A 8 MIEMBRNEAMENTE, SEPARADAMENTE O SECUENCIALMENTE. LA COMBOS; R5 ES ALQUILO C1-C6, CICLOALQUILO, CICLOALQUILO-ALQUILO C1-C4, HETEROCICLO, ENTRE OTROS; L1 ES SINACION PUEDE SER UTIL PARA EL TRATAMIENTO DE RINI, SO, SO2, CO, COO, CS, NRc, CH2, ENTRE OTROS; L2 TIS ALERGICA. LOS ANTAGONISTAS H4 INHIBEN LA INFILTRACION (QUIMIOTAXIS) DE EOSINOFILOS INDUCIDA POR ES UN ENLACE, O, S, SO, SO2, CO, COO, OCO, ENTRE OTROS; W ES O, S, NH, NRc, NCN, ENTRE OTROS; X ES CHISTAMINA EN LA NARIZ Y EN EL PULMON ALIVIANDO LA H2-ARILO, (CH2)n-HETEROARILO; Y ES ARILO MONOCICLOCONGESTION NASAL Y REDUCIENDO LA INFLAMACION ASOCI, HETEROARILO MONOCICLO; Z ES COORd, PO2Ord, SO2RdADA CON EL ASMA , SO2N(RD)(Rd), ENTRE OTROS; Rc ES H, ALQUILO C1-C10, CICLOALQUILO; Rd ES H, ALQUILO C1-C6, CICLOALQUILO, ENTRE OTROS; n ES 0-2; SON COMPUESTOS PREFERIDOS METIL ESTER DEL ACIDO (S)-2-{3-[2-(CICLOHEXILMETILCARBAMOIL)FENIL]UREIDO}-3-[4-(2,6-DICLOROBENZOILAMINO)FENIL]PROPIONICO, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON ANTAGONISTAS DEL INTEGRIN O4 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DESORDENES INMUNES E INFLAMATORIOSREFERS TO UREA DERIVATIVES OF FORMULA I, WHERE IT REFERS TO A SYNERGIC COMBINATION OF AN ANTAG R1 IS C3-C10 ALKYL, C3-C10 ALKYLONIST, HISTAMINE H1 RECEPTOR ALKINYLONIST WITH ANTAGONI C3-ALKYL CYL-CYL -C10STA WHICH IS AT LEAST 10 TIMES MORE SELECTIVE FOR THE HISTAMINE H4 RECEIVER IN COMPARISON WITH THE RE, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, C0-CEPTOR H3 ALKYL OF HISTAMINE SUCH AS GPRv53 ACC2-CYCLOALKYL RECEIVER, AMONG OTHERS; R3 AND R4 ARE H, ALKYOPLATE TO PROTEIN G; TO BE ADMINISTERED SIMULTANEOUSLY C1-C4, R2 AND R3 FORM A RING OF 4 TO 8 MEMBERS, SEPARATELY OR SEQUENTIALLY. THE COMBOS; R5 IS C1-C6 ALKYL, CYCLOALKYL, C1-C4 CYCLOALKYL-ALKYL, HETEROCYCLE, AMONG OTHERS; L1 ES SINACION MAY BE USEFUL FOR THE TREATMENT OF RINI, SO, SO2, CO, COO, CS, NRc, CH2, AMONG OTHERS; L2 TIS ALLERGIC. H4 ANTAGONISTS INHIBIT THE INFILTRATION (CHEMIOTAXIS) OF EOSINOPHILS INDUCED BY IS A LINK, O, S, SO, SO2, CO, COO, OCO, AMONG OTHERS; W IS O, S, NH, NRc, NCN, AMONG OTHERS; X IS CHISTAMINE IN THE NOSE AND IN THE LUNG, RELIEVING H2-ARYL, (CH2) n-HETEROARYL; AND IT IS ARYL MONOCYCLOCONGESTION NASAL AND REDUCING THE INFLAMMATION ASOCI, HETEROARYL MONOCYCLE; Z IS COORd, PO2Ord, SO2RdADA WITH ASTHMA, SO2N (RD) (Rd), AMONG OTHERS; Rc IS H, C1-C10 ALKYL, CYCLOALKYL; Rd IS H, C1-C6 ALKYL, CYCLOALKYL, AMONG OTHERS; n IS 0-2; PREFERRED COMPOUNDS METHYL ESTER OF ACID (S) -2- {3- [2- (CYCLOHEXYLMETILCARBAMOYL) PHENYL] UREIDE} -3- [4- (2,6-DICHLOROBENZOYLAMINO) PHENYL] PROPIONIC, AMONG OTHERS; IT ALSO REFERS TO A PROCEDURE FOR PREPARATION. THE COMPOUNDS ARE ANTAGONISTS OF INTEGRIN O4 AND MAY BE USEFUL FOR THE TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0101223.6A GB0101223D0 (en) | 2001-01-17 | 2001-01-17 | Histamine receptor antagonists |
| ES200100126A ES2200617B1 (en) | 2001-01-19 | 2001-01-19 | DERIVATIVES OF UREA AS ANTAGONISTS OF INTEGRINAS ALPHA 4. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20020822A1 true PE20020822A1 (en) | 2002-09-11 |
Family
ID=44359228
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE20020000372002000023A PE20020822A1 (en) | 2001-01-17 | 2002-01-15 | UREA DERIVATIVES AS ANTAGONISTS OF INTEGRINANTAGONISTS OF HISTAMINE AS O4 RECEPTORS |
Country Status (1)
| Country | Link |
|---|---|
| PE (1) | PE20020822A1 (en) |
-
2002
- 2002-01-15 PE PE20020000372002000023A patent/PE20020822A1/en not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |