http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-055831-A1
Outgoing Links
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| filingDate | 2005-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2007-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-055831-A1 |
| titleOfInvention | PEPIRAZINILUREAS AND PIPERIDINILUREAS AS AMID HYDROLASSES MODULATORS OF FATTY ACIDS |
| abstract | Certain piperazinylurea and piperidinylurea compounds are useful FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by the activity of fatty acid amide hydrolase (FAAH). Consequently, the compounds to be treated can be administered, e.g. eg, anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis). Claim 1: A compound of the formula (1) wherein: Z is -N- or> CH; R1 is -H or -C 1-4 alkyl; Ar1 is 2-thiazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidinyl, 4-pyrimidinyl, 5- pyrimidinyl, or phenyl, each unsubstituted or substituted on a C ring member with 1 or 2 Ra remains; wherein each residue Ra is independently selected from the group consisting of -C1-4 alkyl, -C2-4 alkenyl, -OH, -C1-4 alkyl, halo, -CF3, -OCF3, -SCF3, - SH, -S (O) 0-2 C1-4alkyl, -OSO2 C1-4alkyl, -CO2H1-4alkyl, -CO2H, -C1-4alkyl, -N (Rb) Rc, -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are each, independently of each other, -H or -C 1-4 alkyl; and Ar2 is: (a) unsubstituted 1-naphthyl; or a phenanthrenyl, pyrenyl, fluorenyl, 2-naphthyl, or -NRd-9H-carbazolyl moiety, wherein Rd is selected from the group consisting of -H, -C 1-4 alkyl, and phenyl, each of said moieties is not substituted or substituted with one, two or three Re substituents; wherein each substituent Re is independently selected from the group consisting of -C1-4alkyl, -C2-4alkenyl, -OH, -C1-4alkyl, halo, -CF3, - OCF3, -SCF3 , -SH, -S (O) 0-2 C1-4alkyl, -OSO2 C1-4alkyl, -CO2C1-4alkyl, -CO2H, -COC1-4alkyl, -N (Rb) Rc, -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are as defined above; (b) phenyl fused in two adjacent C atoms of the ring with a group selected from the group consisting of - (CH2) 3-5- with 0 or 1 double bond, - (CH2) 2-3O-, -OCH2CH2O-, and -OCF2O- to form a fused ring structure; or phenyl substituted on adjacent C atoms of the ring with -OCH2O- to form 4-benzo [1,3] dioxolyl; each phenyl moiety also not substituted or substituted with one, two or three Re substituents as previously defined; (c) Ar6, wherein Ar6 is a 6-membered monocyclic heteroaryl having C as the point of attachment, with one or two N heteroatoms, unsubstituted or substituted with one, two or three Re substituents as defined previously; (d) Ar5, where Ar5 is a 5-membered monocyclic heteroaryl having C as the point of attachment, with a heteroatom selected from the group consisting of O, S,> NH, and> NRf, where Rf is C1 alkyl -8 or C0-3 phenyl alkyl, with 0, 1, 2 or 3 additional N heteroatoms, unsubstituted or substituted with 1, 2 or 3 Re substituents as previously defined; (e) a fused bicyclic heteroaryl of 9 or 10 members with a heteroatom selected from the group consisting of N, O and S, with an atom of C as the point of union of the ring, and optionally having up to four ring atoms of C additional replaced with N, said fused bicyclic heteroaryl has no more than five heteroatoms, and are not substituted or substituted with 1, 2 or 3 Re substituents as defined previously; (f) phenyl substituted in the 3 or 4 position with Rg, and optionally also substituted with 1, 2 or 3 Rh substituents, wherein each Rg is independently selected from the group consisting of -C2-8 alkyl , -C2-8 alkenyl, -C3-8cycloalkyl, -C3-8 heterocycloalkyl, and -O-C2-10 alkyl optionally substituted with -NRiRj, where Ri and Rj are each, independently of each other, -H or -C 1-8 alkyl, or Ri and Rj are taken together with the bonding N atom to form a 5, 6 or 7 membered heterocycloalkyl ring that optionally has an additional C ring atom replaced with O, S,> NH, or> C1-4alkyl; and each Rh substituent is independently selected from the group consisting of -C 1-4 alkyl, -C2-4 alkenyl., -OH, -C 1-4 alkyl, halo, -CF3, -OCF3, -SCF3 , -SH, -S (O) 0-2 C1-4alkyl, -OSO2 C1-4alkyl, -CO2C1-4alkyl, -CO2H, -COC1-4alkyl, -N (Rb) Rc, -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are as defined above; (g) phenyl substituted at position 3 or 4 with -L-Ar3, where: o L is a linker selected from the group consisting of - (CH2) 1-3-, -CH = CH-, -O-, -OCH2-, -CH2O-, -NH-,> C1-4alkyl,> S (= O) 0-2, -OSO2-, -C ::: C-, -C (= O) -, and a covalent bond; and o Ar3 is a moiety selected from the group consisting of: (1) phenyl, naphthyl, and phenanthrenyl; (2) Ar6 ', where Ar6' is a 6-membered monocyclic heteroaryl having the C as the point of attachment, with 1 or 2 heteroatoms of N; (3) Ar5 ', where Ar5' is a 5-membered monocyclic heteroaryl having C as the junction point, with a heteroatom selected from the group consisting of O, S,> NH, and> NRf, where Rf is -C 1-8 alkyl or -C 0-3 phenyl alkyl, and with additional 0, 1, 2 or 3 heteroatoms of N, and (4) a fused bicyclic heteroaryl of 9 or 10 members, having a heteroatom selected from the group consisting of N, O and S, with a C as the ring junction point, and which optionally has up to 4 additional C ring atoms replaced with N, said fused bicyclic heteroaryl has no more than 5 heteroatoms; wherein each of the moieties (1) to (4) is optionally disubstituted in adjacent carbons with - C1-4-O- alkylene, - (CH2) 2-3NH-, - (CH2) 1-2NH (CH2) - , - (CH2) 2-3N (C1-4 alkyl) -, or - (CH2) 1-2N (C1-4 alkyl) - (CH2) - to form a fused ring structure, and is also optionally substituted with 1 , 2 or 3 Rk substituents, wherein each Rk substituent is independently selected from the group consisting of -C1-4alkyl, -C2-4alkenyl, -OH, -C1-4alkyl, halo, - CF3, -OCF3, -SCF3, -SH, -S (O) 0-2 C1-4alkyl, -OSO2 C1-4alkyl, -CO2C1-4alkyl, -CO2H, -C1-4alkyl, - N (Rb) Rc , -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are as defined above; (h) 2-hydroxyphenyl or 2-methoxyphenyl, unsubstituted or substituted with 1, 2 or 3 Rl substituents, wherein each Rl substituent is independently selected from each other, from the group consisting of -CH3, 6-C2 alkyl- 4,6-C2-4 alkenyl, -OH, -OCH3, 6-C2-6alkyl, halo, -CF3, -OCF3, -SCF3, -SH, -C1-4 alkyl, -SO2 C1-4 alkyl, -CO2alkyl C1-4, -CO2H, -CO4-4alkyl, - N (Rb) Rc, -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are as defined previously; (i) 4-Halophenyl, unsubstituted or substituted with 1, 2 or 3 Rm substituents, wherein each Rm substituent is independently selected from the group consisting of -CH3, 2-C2-4 alkyl -C2-4alkenyl, 3-hydroxy, 4-hydroxy, -OCH3, 2-C2-6alkyl, halo, -CF3, -OCF3, -SCF3, -SH, -C1-4 alkyl, -SO2 C1-4alkyl, -CO2C1-4alkyl, -CO2H, -C1-4alkyl, - N (Rb) Rc, -SO2NRbRc, -NRbSO2Rc, -C (= O) NRbRc, -NO2, and -CN, where Rb and Rc are as were defined previously; or (j) 2-bromophenyl, 3-methylphenyl, 3-methoxyphenyl, 4-methoxyphenyl, or 3,4-dimethoxyphenyl; wherein, when Ar2 is 4-fluorophenyl, 3,4-difluorophenyl, 4-chlorophenyl or 3-methoxyphenyl, Ar1 is not unsubstituted phenyl or phenyl substituted with 4-Cl, -NO2, -CF3, or 4-CO2Et, and wherein, when Ar2 is 3,4-dichlorophenyl, Ar1 is not phenyl substituted with 4-Cl, -NO2, -CF3, or 4-CO2Et; a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug or a pharmaceutically acceptable metabolite of said compound. |
| priorityDate | 2004-12-30-04:00^^<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: 117.