http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-070852-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5f1a30682c7f24ace5f2b16c6be633b6 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D237-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D237-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D473-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-501 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 |
| filingDate | 2009-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5d296c1493b91e0a96daa03684f3a625 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_78fd39f63a54eac7688d5658949be736 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2b6c894c5eda5bf616954a0597113061 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_be4d11c092e2af4aded9d65d8b78afe4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a3a81dbeb72e38337c3b4073e295893a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_51e8d7e51048790ab6d2f939f34a48c6 |
| publicationDate | 2010-05-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-070852-A1 |
| titleOfInvention | DERIVATIVES OF PIRIDAZINE AND ITS USE AS THERAPEUTIC AGENTS |
| abstract | Claim 1: A method for treating a skin disorder mediated by stearoyl-CoA desaturase (SCD) in a mammal, characterized in that the method comprises administering to the mammal in need thereof a therapeutically effective amount of a compound of the formula (1) where: x and y are each independently 1, 2 or 3; W is -C (O) N (R1) -; -C (O) N [C (O) R1a] -, -N (R1) C (O) N (R1) - or -N (R1) C (O) -; V is -C (O) -, -C (S) - or -C (R10) H; each R1 is independently selected from the group consisting of hydrogen; C1-6 alkyl optionally substituted with one or more substituents selected from the group consisting of halo, methyl or trifluoromethyl; and C2-6 alkyl optionally substituted with one or more substituents selected from the group consisting of methoxy and hydroxyl; R1a is selected from the group consisting of hydrogen, C1-6 alkyl and cycloalkyl; R2 is selected from the group consisting of C1-12 alkyl, C2-12 alkenyl, C2-12 hydroxyalkyl, C2-12 hydroxyalkenyl, C1-12 alkoxy, C2-12 alkoxyalkyl, C3-12 cycloalkyl, C4-12 cycloalkylalkyl, aryl, C7-12 aralkyl, C3-12 heterocyclyl, C3-12 heterocyclylalkyl, C1-12 heteroaryl and C3-12 heteroarylalkyl; or R2 is a multi-ring structure having 2 to 4 rings where the rings are independently selected from the group consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl and where some or all of the rings may be fused together; R3 is selected from the group consisting of C1-12 alkyl, C2-12 alkenyl, C2-12 hydroxyalkyl, C2-12 hydroxyalkenyl, C1-12 alkoxy, C2-12 alkoxyalkyl, C3-12 cycloalkyl, C4-12 cycloalkylalkyl, aryl, C7-12 aralkyl, C3-12 heterocyclyl, C3-12 heterocyclylalkyl, C1-12 heteroaryl and C3-12 heteroarylalkyl; or R3 is a multi-ring structure having 2 to 4 rings where the rings are independently selected from the group consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl and where some or all of the rings may be fused together; R4 and R5 are each independently selected from hydrogen, fluoro, chloro, methyl, methoxy, trifluoromethyl, cyano, nitro or -N (R12) 2; R6, R6a, R7, R7a, R8, R8a, R9 and R9a are each independently selected from hydrogen or C1-3 alkyl; or R6 and R6a together, or R7 and R7a together, or R8 and R8a together, or R9 and R9a together are an oxo group, with the proviso that when V is -C (O) -, R7 and R7a together, or R8 and R8a together, do not form an oxo group, while the remaining R6, R6a, R7, R7a, R8, R8a, R9 and R9a are each independently selected from hydrogen or C1-3 alkyl; or one of the R6, R6a, R7 and R7a together with one of the R8, R8a, R9 and R9a form an alkylene bridge, while the remaining R6, R6a, R7, R7a, R8, R8a, R9 and R9a are selected each one independently of hydrogen or C1-3 alkyl; R10 is hydrogen or C1-3 alkyl; and each R12 is independently selected from hydrogen or C1-6 alkyl; a stereoisomer, enantiomer or tautomer thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof. Claim 6: The method according to any one of claims 1 to 5, characterized in that the skin disorder is selected from the group consisting of acne, rosacea, seborrheic skin, oily skin (seborrhea syn) and seborrheic dermatitis, and any of the combinations of these. Claim 9: The method according to claim 1, characterized in that V is -C (O) - or -C (S) -; W is selected from -C (O) N (R1) - and -N (R1) C (O) -; R2 is selected from the group consisting of C1-12 alkyl, C2-12 alkenyl, C2-12 hydroxyalkyl, C2-12 hydroxyalkenyl, C1-6 alkoxy, C3-12 alkoxyalkyl, C3-12 cycloalkyl, C4-12 cycloalkylalkyl, aryl, C7-12 aralkyl, C3-12 heterocyclyl, C3-12 heterocyclylalkyl, C1-12 heteroaryl and C3-12 heteroarylalkyl; R3 is phenyl optionally substituted by one or more substituents selected from the group consisting of halo, cyano, nitro, hydroxy, C1-6 alkyl, trihaloalkyl C1-6, trihaloalkoxy C1-6, alkylsulfonyl C1-6, -N (R11) 2 , -OC (O) R11, -C (O) OR11, -S (O) 2N (R11) 2, cycloalkyl, heterocyclyl, heteroaryl and heteroarylcycloalkyl, with the proviso that R3 is not phenyl substituted with optionally substituted thienyl; R4 and R5 are each independently selected from hydrogen, fluoro, chloro, methyl, methoxy and trifluoromethyl; and R6, R6a, R7, R7a, R8, R8a, R9 and R9a are each independently selected from hydrogen or C1-3 alkyl. Claim 10: The method according to claim 1, characterized in that V is -C (O) -; W is selected from -C (O) N (R1) -, and -N (R1) C (O) -; R2 is selected from the group consisting of C7-12 alkyl, C3-12 alkenyl, C7-12 hydroxyalkyl, C2-12 alkoxyalkyl, C3-12 hydroxyalkenyl, C3-12 cycloalkyl, C4-12 cycloalkylalkyl, C13-19 aralkyl, C3-19 heterocyclyl alkyl -12, and C3-12 heteroarylalkyl; R3 is selected from the group consisting of C3-12 alkyl, C3-12 alkenyl, C3-12 hydroxyalkyl, C3-12 hydroxyalkenyl, C3-12 alkoxy, C3-12 alkoxyalkyl, C3-12 cycloalkyl, C4-12 cycloalkylalkyl, aryl, C7-12 aralkyl, C3-12 heterocyclyl, C3-12 heterocyclylalkyl, C5-12 heteroaryl and C3-12 heteroarylalkyl; R4 and R5 are each independently selected from hydrogen, fluoro, chloro, methyl, methoxy, trifluoromethyl; and R6, R6a, R7, R7a, R8, R8a, R9 and R9a are each independently selected from hydrogen or C1-3 alkyl. Claim 16: A formulation suitable for topical administration, characterized in that it includes a compound of the formula (1) as described in accordance with claim 1, and one or more penetration enhancers. Claim 17: A formulation suitable for topical administration in accordance with claim 16, characterized in that it includes: a) a compound of the formula (1) as described in accordance with claim 1; b) one or more penetration enhancers; c) optionally one or more antioxidants; d) optionally one or more solvents; e) optionally one or more co-solvents; f) optionally one or more surfactants; g) optionally one or more conservatives; and h) optionally one or more gelling agents. Claim 26: The formulation according to claim 18, characterized in that it includes: a) 6- [4- (5-Fluoro-2-trifluoromethyl-benzoyl) -piperazin-1- (2-cyclopropyl-ethyl) -amide il] pyridazin-3-carboxylic; b) diethylene glycol monoethyl ether or SEPA-9TM (2-n-nonyl-1,3-dioxolane); c) butylated hydroxytoluene, or a combination of butylated hydroxytoluene and butylated hydroxyanisole; d) benzyl alcohol; and e) optionally including sorbitan monolaureate. |
| priorityDate | 2008-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 73.