AR075514A1 - DERIVATIVES OF THE PIPERIDIN-PYRIMIDINE ANTAGONISTS OF THE H4 RECEPTOR, PHARMACEUTICAL COMPOSITIONS AND THE SAME PREPARATION PROCESS - Google Patents
DERIVATIVES OF THE PIPERIDIN-PYRIMIDINE ANTAGONISTS OF THE H4 RECEPTOR, PHARMACEUTICAL COMPOSITIONS AND THE SAME PREPARATION PROCESSInfo
- Publication number
- AR075514A1 AR075514A1 ARP100100472A ARP100100472A AR075514A1 AR 075514 A1 AR075514 A1 AR 075514A1 AR P100100472 A ARP100100472 A AR P100100472A AR P100100472 A ARP100100472 A AR P100100472A AR 075514 A1 AR075514 A1 AR 075514A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- groups
- optionally substituted
- group
- haloc1
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
Abstract
Estos compuestos son utiles como antagonistas del receptor H4 de la histamina. Reivindicacion 1: Un compuesto caracterizado por la formula (1) donde: R1 y R2 forman, junto con el átomo de N al cual están unidos, un grupo heterocíclico saturado seleccionado de: (i) un grupo heterocíclico que contiene 2 átomos de N y no contiene ningun otro heteroátomo, donde dicho grupo heterocíclico puede estar opcionalmente sustituido por uno o más grupos C1-4 alquilo; y (ii) un grupo heterocíclico que contiene 1 átomo de N y no contiene ningun otro heteroátomo, donde dicho grupo heterocíclico está sustituido por un grupo -NRaRb y puede estar opcionalmente sustituido por uno o más grupos C1-4 alquilo; donde dichas grupos heterocíclicos (i) y (ii) pueden ser monocíclicos de 4 a 7 miembros, bicíclicos con puente de 7 a 8 miembros o bicíclicos fusionados de 8 a 12 miembros; o R1 representa H a C1-4 alquilo, y R2 representa azetidinilo, pirrolidinilo, piperidiniIo o azepanilo, donde R2 puede estar opcionalmente sustituida por uno o más grupos C1-4 alquilo; Ra representa H o C1-4 alquilo; Rb representa H o C1-4 alquilo; o Ra y Rb forman, junto con el átomo de N al que están unidos, un grupo azetidinilo, pirrolidinilo, piperidinilo o azepanilo que puede estar opcionalmente sustituido por uno o más grupos C1-4 alquilo; R3 representa -COR4, -CONR4R4', -CO2R4, -SO2R4 o -SO2NR4R4'; R4 representa C1-8 alquilo, R5-C1-8 alquilo o R6-C0-8 alquilo, donde en los grupos C1-8 alquilo, R5-C1-8, alquilo y R6-C0-8 alquilo cualquier grupo alquilo puede estar opcionalmente sustituido por uno a más grupos halogeno y un grupo metileno de la cadena de alquilo puede estar opcionalmente remplazado por -O-; R4 representa H o C1-8 alquilo; y opcionalmente R4 y R4' pueden estar unidos formando un grupo -C3-5 alquileno- que puede estar opcionalmente sustituido por uno o más grupos C1-8 alquilo; R5 representa -CONR4'R7, -NR4'COR7, -NR4'CO2R7, -NR4'SO2R7, -SO2NR4'R7, -NR4'CONR4'R7, -CONHSO2R7, -CO2R7, -OCOR7, -SO2R7, -NR4'R7, -OH o 1H-tetrazol-5-ilo; R6 representa C3-8cicloalquilo, heterocicloalquilo, arilo o heteroarilo, donde R6 puede estar opcionalmente sustituido por uno o más grupos seleccionados independientemente de C1-8 alquilo, haloC1-8 alquilo, halogeno, C1-8 alcoxi, haloC1-8 alcoxi, C1-8 alquiltio, -CN, C2-4 alquinilo, R5-C0-8 alquilo y R8-C0-8 alquilo; R7 representa H, C1-8 alquilo, C3-8 cicloalquil-C0-8 alquilo o aril-C0-8 alquilo, donde en los grupos C1-8 alquilo, C3-8 cicIoalquil-C0-8 alquilo y aril-C0-8 alquilo cualquier grupo alquilo puede estar opcionalmente sustituido por uno o más grupos halogeno, y cualquiera de los grupos C3-8 cicloalquilo y arilo puede estar opcionaImente sustituido por uno o más grupos seleccionados independientemente de C1-8 alquilo, haloC1-8alquilo, halogeno, C1-8alcoxi, haloC1-8 alcoxi, C1-8 alquiltio, -CN, C2-4 alquinilo y hidroxiC1-8 alquilo; y opcionalmente R4' y R7, en un grupo R5, pueden estar unidos formando un grupo -C3-5 alquileno- que puede estar opcionalmente sustituido por uno o más grupos C1-8 alquilo; y R8 representa C3-8cicloalquilo, heterocicloalquilo, arilo o heteroarilo, donde R8 puede estar opcionalmente sustituido por uno o más grupos seleccionados independientemente de C1-8 alquilo, haloC1-8 alquilo, halogeno, C1-8 alcoxi, haloC1-8 alcoxi, C1-8 alquiItio, -CN, C2-4 alquinilo y hidroxiC1-8 alquilo; o une sal del mismo.These compounds are useful as histamine H4 receptor antagonists. Claim 1: A compound characterized by the formula (1) wherein: R1 and R2 form, together with the N atom to which they are attached, a saturated heterocyclic group selected from: (i) a heterocyclic group containing 2 N atoms and it does not contain any other heteroatom, wherein said heterocyclic group may be optionally substituted by one or more C1-4 alkyl groups; and (ii) a heterocyclic group containing 1 N atom and not containing any other heteroatom, wherein said heterocyclic group is substituted by a -NRaRb group and may be optionally substituted by one or more C1-4 alkyl groups; wherein said heterocyclic groups (i) and (ii) may be monocyclics of 4 to 7 members, bicyclics with bridges of 7 to 8 members or bicyclics fused of 8 to 12 members; or R1 represents H to C1-4 alkyl, and R2 represents azetidinyl, pyrrolidinyl, piperidiniIo or azepanyl, where R2 may be optionally substituted by one or more C1-4 alkyl groups; Ra represents H or C1-4 alkyl; Rb represents H or C1-4 alkyl; or Ra and Rb form, together with the N atom to which they are attached, an azetidinyl, pyrrolidinyl, piperidinyl or azepanyl group which may be optionally substituted by one or more C1-4 alkyl groups; R3 represents -COR4, -CONR4R4 ', -CO2R4, -SO2R4 or -SO2NR4R4'; R4 represents C1-8 alkyl, R5-C1-8 alkyl or R6-C0-8 alkyl, where in the groups C1-8 alkyl, R5-C1-8, alkyl and R6-C0-8 alkyl any alkyl group may optionally be substituted by one to more halogen groups and a methylene group of the alkyl chain may be optionally replaced by -O-; R4 represents H or C1-8 alkyl; and optionally R4 and R4 'may be linked to form a -C3-5 alkylene group- which may be optionally substituted by one or more C1-8 alkyl groups; R5 represents -CONR4'R7, -NR4'COR7, -NR4'CO2R7, -NR4'SO2R7, -SO2NR4'R7, -NR4'CONR4'R7, -CONHSO2R7, -CO2R7, -OCOR7, -SO2R7, -NR4'R7 , -OH or 1H-tetrazol-5-yl; R6 represents C3-8cycloalkyl, heterocycloalkyl, aryl or heteroaryl, where R6 may be optionally substituted by one or more groups independently selected from C1-8 alkyl, haloC1-8 alkyl, halogen, C1-8 alkoxy, haloC1-8 alkoxy, C1- 8 alkylthio, -CN, C2-4 alkynyl, R5-C0-8 alkyl and R8-C0-8 alkyl; R7 represents H, C1-8 alkyl, C3-8 cycloalkyl-C0-8 alkyl or aryl-C0-8 alkyl, where in the groups C1-8 alkyl, C3-8 cycloalkyl-C0-8 alkyl and aryl-C0-8 alkyl any alkyl group may be optionally substituted by one or more halogen groups, and any of the C3-8 cycloalkyl and aryl groups may be optionally substituted by one or more groups independently selected from C1-8 alkyl, haloC1-8alkyl, halogen, C1 -8alkoxy, haloC1-8 alkoxy, C1-8 alkylthio, -CN, C2-4 alkynyl and hydroxyC1-8 alkyl; and optionally R4 'and R7, in a group R5, may be linked to form a group -C3-5 alkylene- which may be optionally substituted by one or more C1-8 alkyl groups; and R8 represents C3-8cycloalkyl, heterocycloalkyl, aryl or heteroaryl, where R8 may be optionally substituted by one or more groups independently selected from C1-8 alkyl, haloC1-8 alkyl, halogen, C1-8 alkoxy, haloC1-8 alkoxy, C1 -8 alkyl, -CN, C2-4 alkynyl and hydroxyC 1-8 alkyl; or unite salt from it.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382022 | 2009-02-18 | ||
| US17335409P | 2009-04-28 | 2009-04-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR075514A1 true AR075514A1 (en) | 2011-04-06 |
Family
ID=40912138
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100100472A AR075514A1 (en) | 2009-02-18 | 2010-02-17 | DERIVATIVES OF THE PIPERIDIN-PYRIMIDINE ANTAGONISTS OF THE H4 RECEPTOR, PHARMACEUTICAL COMPOSITIONS AND THE SAME PREPARATION PROCESS |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR075514A1 (en) |
| TW (1) | TW201041867A (en) |
| WO (1) | WO2010094721A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20131399A1 (en) * | 2010-10-07 | 2013-12-16 | Bayer Cropscience Ag | FUNGICIDAL COMPOSITION INCLUDING A TETRAZOLILOXIMA DERIVATIVE AND A THIAZOLYLPIPERIDINE DERIVATIVE |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7985745B2 (en) * | 2006-10-02 | 2011-07-26 | Abbott Laboratories | Method for pain treatment |
-
2010
- 2010-02-12 TW TW099104788A patent/TW201041867A/en unknown
- 2010-02-17 AR ARP100100472A patent/AR075514A1/en unknown
- 2010-02-17 WO PCT/EP2010/052006 patent/WO2010094721A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| TW201041867A (en) | 2010-12-01 |
| WO2010094721A1 (en) | 2010-08-26 |
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