AR049024A1 - METHOD TO TREAT NEUROPATHIC PAIN WITH A CRTH2 RECEIVER ANTAGONIST - Google Patents
METHOD TO TREAT NEUROPATHIC PAIN WITH A CRTH2 RECEIVER ANTAGONISTInfo
- Publication number
- AR049024A1 AR049024A1 ARP050101515A AR049024A1 AR 049024 A1 AR049024 A1 AR 049024A1 AR P050101515 A ARP050101515 A AR P050101515A AR 049024 A1 AR049024 A1 AR 049024A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- nr9r10
- different
- same
- optionally substituted
- Prior art date
Links
- 102000009389 Prostaglandin D receptors Human genes 0.000 title abstract 6
- 108050000258 Prostaglandin D receptors Proteins 0.000 title abstract 6
- 208000004296 neuralgia Diseases 0.000 title abstract 3
- 208000021722 neuropathic pain Diseases 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 14
- 239000002464 receptor antagonist Substances 0.000 abstract 5
- 229940044551 receptor antagonist Drugs 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 102000040430 polynucleotide Human genes 0.000 abstract 1
- 108091033319 polynucleotide Proteins 0.000 abstract 1
- 239000002157 polynucleotide Substances 0.000 abstract 1
- -1 said het1 Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Uso de un antagonista del receptor CRTH2 en la fabricacion de un medicamento para el tratamiento del dolor neuropático y a un método para tratar el dolor neuropático usando un antagonista del receptor CRTH2. Reivindicacion 2: Uso de acuerdo con la reivindicacion 1, donde el antagonista del receptor CRTH2 es un compuesto de formula general (1) o una sal farmacéuticamente aceptable del mismo o solvato del mismo, donde: R1 es H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4 o (CH2)mRx; Rx es het1, fenilo o cicloalquilo C3-6, estando dicho het1, fenilo y cicloalquilo C3-6 opcionalmente sustituidos con uno o más grupos Q1 o alquilo C1-4, estando dicho alquilo C1-4 opcionalmente sustituido con uno o más grupos Q1; Q1 es halogeno, NO2, CN, SO2CH3, SO2NR9R10, CR9, COOR9, C(=O)NR9R10, NR9R10, NR9SO2R10, NR9C(=O)R10 o C(=O)R9 donde R9 y R10 son iguales o diferentes y se seleccionan entre H y alquilo C1-4; m es un numero entero seleccionado entre 0, 1 y 2; R2 es alquilo C1-4, donde el grupo alquilo puede estar sustituido con uno o más sustituyentes seleccionados entre halogeno, OR9, NR9R10, COOR9, C(=O)NR9R10, NHSO2R9 y C(=O)alquilo C1-4, donde R9 y R10 son iguales o diferentes y se seleccionan entre H y alquilo C1-4; R3 es cicloalquilo C3-6 o -A-Ry; A es un enlace, alquileno C1-3 lineal o ramificado, o alquenileno C2-3; Ry es arilo C6-12 o het2, donde los grupos arilo y het2 están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre: arilo C6-12, het1, Q2, y alquilo C1-4, estando dicho alquilo C1-4 opcionalmente sustituido con uno o más grupos Q2 que son iguales o diferentes; Q2 es halogeno, NO2, CN, SO2CH3, SO2NR9R10, OR9, SR9, OCH2CF3, COOR9, C(=O)NR9R10, NR9R10, NR9SO2R10, NR9C(=O)R10 o C(=O)R9 donde R9 y R10 son iguales o diferentes y se seleccionan entre H y alquilo C1-4; R4 es H o alquilo C1-4; R5, R6, R7 y R8 son iguales o diferentes y se seleccionan entre H, Q3, y alquilo C1-4, estando dicho alquilo C1-4 opcionalmente sustituido con uno o más grupos Q3 que son iguales o diferentes; Q3 es halogeno, NO2, CN, SO2CH3, SO2NR9R10, OR9, SR9, COOR9, C(=O)NR9R10, NR9R10, NR9SO2R10, NR9C(=O)R10 o C(=O)R9 donde R9 y R10 son iguales o diferentes y se seleccionan entre H y alquilo C1-4; het1 es un heterociclo aromático de 5 a 10 miembros que tiene de 1 a 4 heteroátomos seleccionados entre oxígeno, azufre y nitrogeno; y het2 es un grupo heterocíclico de 5 a 10 miembros saturado, insaturado o parcialmente saturado que tiene de 1 a 4 heteroátomos seleccionados entre oxígeno, azufre y nitrogeno. Reivindicacion 4: Uso de acuerdo con la reivindicacion 1, donde el antagonista del receptor CRTH2 es un anticuerpo, dominio de union a un ligando de anticuerpo o un polinucleotido. Reivindicacion 5: Uso de acuerdo con la reivindicacion 1, donde el antagonista del receptor CRTH2 se usa de forma separada, secuencial o simultánea en combinacion con un segundo compuesto farmacologicamente activo.Use of a CRTH2 receptor antagonist in the manufacture of a medicament for the treatment of neuropathic pain and a method for treating neuropathic pain using a CRTH2 receptor antagonist. Claim 2: Use according to claim 1, wherein the CRTH2 receptor antagonist is a compound of general formula (1) or a pharmaceutically acceptable salt thereof or solvate thereof, wherein: R1 is H, C1-4 alkyl, alkenyl C2-4, C2-4 alkynyl or (CH2) mRx; Rx is het1, phenyl or C3-6 cycloalkyl, said het1, phenyl and C3-6 cycloalkyl being optionally substituted with one or more groups Q1 or C1-4 alkyl, said C1-4 alkyl being optionally substituted with one or more groups Q1; Q1 is halogen, NO2, CN, SO2CH3, SO2NR9R10, CR9, COOR9, C (= O) NR9R10, NR9R10, NR9SO2R10, NR9C (= O) R10 or C (= O) R9 where R9 and R10 are the same or different and are select between H and C1-4 alkyl; m is an integer selected from 0, 1 and 2; R2 is C1-4 alkyl, where the alkyl group may be substituted with one or more substituents selected from halogen, OR9, NR9R10, COOR9, C (= O) NR9R10, NHSO2R9 and C (= O) C1-4 alkyl, where R9 and R10 are the same or different and are selected from H and C1-4 alkyl; R3 is C3-6 cycloalkyl or -A-Ry; A is a bond, linear or branched C1-3 alkylene, or C2-3 alkenylene; Ry is C6-12 aryl or het2, where the aryl and het2 groups are optionally substituted with one or more substituents selected from: C6-12 aryl, het1, Q2, and C1-4 alkyl, said C1-4 alkyl being optionally substituted with one or more Q2 groups that are the same or different; Q2 is halogen, NO2, CN, SO2CH3, SO2NR9R10, OR9, SR9, OCH2CF3, COOR9, C (= O) NR9R10, NR9R10, NR9SO2R10, NR9C (= O) R10 or C (= O) R9 where R9 and R10 are equal or different and are selected from H and C1-4 alkyl; R4 is H or C1-4 alkyl; R5, R6, R7 and R8 are the same or different and are selected from H, Q3, and C1-4 alkyl, said C1-4 alkyl being optionally substituted with one or more Q3 groups that are the same or different; Q3 is halogen, NO2, CN, SO2CH3, SO2NR9R10, OR9, SR9, COOR9, C (= O) NR9R10, NR9R10, NR9SO2R10, NR9C (= O) R10 or C (= O) R9 where R9 and R10 are the same or different and are selected from H and C1-4 alkyl; het1 is a 5-10 membered aromatic heterocycle having 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen; and het2 is a saturated, unsaturated or partially saturated 5 to 10 membered heterocyclic group having 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen. Claim 4: Use according to claim 1, wherein the CRTH2 receptor antagonist is an antibody, binding domain to an antibody ligand or a polynucleotide. Claim 5: Use according to claim 1, wherein the CRTH2 receptor antagonist is used separately, sequentially or simultaneously in combination with a second pharmacologically active compound.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0408799A GB0408799D0 (en) | 2004-04-20 | 2004-04-20 | Method of treating pain |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049024A1 true AR049024A1 (en) | 2006-06-21 |
Family
ID=32344079
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050101515 AR049024A1 (en) | 2004-04-20 | 2005-04-18 | METHOD TO TREAT NEUROPATHIC PAIN WITH A CRTH2 RECEIVER ANTAGONIST |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR049024A1 (en) |
| GB (1) | GB0408799D0 (en) |
| TW (1) | TW200603802A (en) |
-
2004
- 2004-04-20 GB GB0408799A patent/GB0408799D0/en not_active Ceased
-
2005
- 2005-04-15 TW TW094112108A patent/TW200603802A/en unknown
- 2005-04-18 AR ARP050101515 patent/AR049024A1/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW200603802A (en) | 2006-02-01 |
| GB0408799D0 (en) | 2004-05-26 |
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| FA | Abandonment or withdrawal |