http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-060872-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d202e9e866984fe229f6facc38f1d740 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-403 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 |
| filingDate | 2007-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-07-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-060872-A1 |
| titleOfInvention | ANTAGONISTS OF REPLACED CGRP MONOCICLIC RECEIVERS |
| abstract | Claim 1: A compound of the formula (1) wherein A1 is selected from: -O-, -S (O) v-, -If (Ora) -C 1-4 alkyl-, wherein the alkyl is substituted or not substituted with 1-5 halo, -Si (C1-4 alkyl) 2, where each alkyl is independently unsubstituted or substituted with 1-5 halo-, -CR6R7-, -N (R8) -, - (C = O ) -, -C (R8) (Ra) -, -C (N (Rb) -SO2Rd (Ra) -, -C (N (Rb) (C = O) Ra) (Ra) -, -C (N (Rb) (C = O) ORa) (Ra) -, -CR10R11-, and -N (R11) -; A2 is selected from -CR6R7-, -CR10R11-, and - (C = O) -, A3 is selected from: -CR6R7-, -N (R8) -, -CR10R11-, and -N (R11) -; A4 is selected from: -CR6R7-, - (C = O) -, -N (R8 ) -, -CR10R11-, -N (R11) -, and a link between A2 and A3; Ea is selected from: -C (R5a) =, -N =, and - (N + -O -) =; Eb is selected from: -C (R5b) =, -N =, and - (N + -O -) =; Ec is selected from: -C (R5c) =, -N =, and - (N + -O- ) =; Q is selected from: - (C = O) -, -SO2-, -SO-, and -C (Ra) 2-; R4 is selected from: H, -C1-6 alkyl, which does not is substituted or substituted with 1-5 substituents that were selected onan each independently of between: halo, C3-6cycloalkyl, -CF3, and -O-Ra, C3-6cycloalkyl, benzyl, and phenyl; R5a, R5b and R5c are each independently selected from: H, -C1-6 alkyl, which is unsubstituted or substituted with 1-6 halo, halo, -ORa, and -CN; R6 and R7 are each independently selected from: H, -C1-6 alkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from: halo, -ORa, -C3-6 cycloalkyl , phenyl or heterocycle, said heterocycle being selected from: pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl, morpholinyl, thiazolyl, indolyl, indazolyl, benzimidazolyl and oxazolyl, said phenyl or substituted with 1 unsubstituted or substituted heterocycle -5 substituents each independently selected from: halo, -C 1-6 alkyl, which is unsubstituted or substituted with 1-5 halo, -ORa, -NRbRc, -CN, and oxo; -CO2Ra, -C (= O) NRbRc, -S (O) vRd, -CN, -NRbRc, -N (Rb) C (= O) Ra, -N (Rb) SO2Rd, -CF3, -O-CO2Rd , -O- (C = O) -NRbRc, -C (= O) Ra, -C3-8 cycloalkyl, which is unsubstituted or substituted with 1-5 substituents each selected independently from among: halo, - CN, -C 1-4 alkyl, which is unsubstituted or substituted with 1-3 halo, and -ORa, phenyl or heterocycle, said heterocycle being selected from: pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl , morpholinyl, thiazolyl and oxazolyl, said phenyl or heterocycle being unsubstituted or substituted with 1-5 substituents each independently selected from: halo, -ORa, C3-6cycloalkyl, phenyl, which is not substituted or substituted with 1- 5 substituents each independently selected from: halo, -C1-6 alkyl, which is not substituted or substituted with 1-6 halo, and -ORa, -CO2Ra, -C (= O) NRbRc, -S ( O) vRd, -CN, -NRbRc, - N (Rb) C (= O) Ra, -N (Rb) SO2Rd, -O-CO2Rd, -O (C = O) NRbRc, -NRb- (C = O) -NRbRc, -C (= O) Ra, -C1-6 alkyl, which is not substituted or substituted with 1-6 halo, and oxo; halo, -ORa, -CN, -CO2Ra, -N (Rb) C (= O) Ra, -NRbRc, -C (= O) NRbRc, and -O (C = O) Ra; or R6 and R7 and the carbon atom or atoms to which (to which they are attached) form a ring that is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cycloonyl, cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, dioxolanyl, dioxanil, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiapyranyl, oxetanyl, thiethanyl and tetrahydrothienyl, whereby the sulfur is not available is substituted or substituted with 1-5 substituents that are each independently selected from among: -C1-6 alkyl, which is not substituted or substituted with 1-3 substituents which are each independently selected from: halo, -ORa , -C3-6 cycloalkyl, -CO2Ra, -NRbRc, -S (O) vRd, -C (= O) NRbRc, phenyl, -C3-6 cycloalkyl, the C3-6 cycloalkyl group being opium nually condensed with the ring, and the C3-6 group being unsubstituted or substituted with 1-3 substituents each independently selected from: halo, -ORa, -C3-6cycloalkyl, -CO2Ra, -NRbRc, -S (O ) vRd, -C (= O) NRbRc, and phenyl, phenyl or heterocycle, said heterocycle being selected from: pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl, morpholinyl, imidazolyl, furanyl, tetrahydrofuranyl, tiazolhydrofuranyl, oxazolyl, the phenyl or heterocycle being optionally fused to the ring, and said phenyl or heterocycle is not substituted or substituted with 1-5 substituents each independently selected from: halo, -C 1-6 alkyl, which is unsubstituted or substituted with 1-5 halo, -ORa, -CO2Ra, -O (C = O) Ra, -CN, -NRbRc, oxo, -C (= O) NRbRc, -N (Rb) C (= O) Ra, - N (Rb) CO2Ra, -O (C = O) NRbRc, and -S (O) vRd, -ORa, -CO2Ra, -C (= O) NRbRc, -S (O) vRd, -CN, halo, - NRbRc, -N (Rb) C (= O) Ra, -N (Rb) SO2Rd, -O-CO2Rd, -O (C = O) - NRbRc, -NRb- (C = O) -NRbRc, -C (= O) Ra, and oxo; R8 is independently selected from: H, -C (= O) Ra, -CO2Ra, -S (= O) Rd, -SO2Rd, -C (= O) NRbRc, -C1-6 alkyl, which is not substituted or it is substituted with 1-5 substituents which are each independently selected from among: halo, -ORa, -C3-6cycloalkyl, phenyl or heterocycle, wherein said heterocycle selected from: pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl , pyrrolidinyl, thienyl, morpholinyl, thiazolyl and oxazolyl, said phenyl or heterocycle being unsubstituted or substituted with 1-5 substituents each independently selected from: halo, -C 1-6 alkyl, which is unsubstituted or substituted with 1-5 halo, and -ORa, -NRbRc, - C (= O) Ra, -CO2Ra, and oxo, -CO2Ra, -C (= O) NRbRc, -S (O) vRd, -CN, -NRbRc, -N ( Rb) C (= O) Ra, -N (Rb) SO2Rd, -CF3, -O-CO2Rd, -O (C = O) NRbRc, -NRb- (C = O) -NRbRc, and -C (= O ) Ra, C3-6cycloalkyl, which is unsubstituted or substituted with 1-6 substituents which are each independently selected from among: halo ; -CN, -ORa, and -C 1-6 alkyl, which is unsubstituted or substituted with 1-6 halo; or R7 and R8 and the atoms to which they are attached form a 4, 5, 6 or 7-membered alkyl or heteroalkyl ring that optionally contains an additional heteroatom that is selected from N, O, and S, in which the sulfur is optionally oxidized to the sulfone or sulfoxide, and said ring is unsubstituted or substituted with 1-4 substituents each independently selected from: halo, phenyl, which is unsubstituted or substituted with 1-3 substituents which are each independently selected from: halo, ORa, CN and -C (= O) ORa, -Ora, and -C 1-6 alkyl, which is not substituted or substituted with 1-6 halo; R10 is independently selected from: H, -C 1-6 alkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from: halo, -ORa, -CN, phenyl, and -C3 -cycloalkyl -6, which is unsubstituted or substituted with 1-6 halo, -C3-6cycloalkyl, which is unsubstituted or substituted with 1-6 halo; R11 is independently selected from the group consisting of phenyl, naphthyl, tetrahydronaphthyl, indanyl, biphenyl, phenanthryl, anthryl, azepinyl, azepanyl, azetidinyl, benzimidazolyl, benzisoxazolyl, benzofuranyl, benzofurazanyl, benzopyranyl, benzothiopyranyl, benzofuryl, 1,3-benzodioxolyl, benzothiazolyl , benzothienyl, benzoxazolyl, benzopyrazolyl, benzotriazolyl, chromanyl, cinnolinyl, dibenzofuranyl, dihydrobenzofuryl, dihydrobenzothienyl, dihydrobenzothiopyranyl, dihydrobenzothiopyranyl sulfone, furyl, furanyl, imidazolidinyl, imidazolinyl, imidazolyl, indolinyl, indolyl, isochromanyl, isoindolinyl, isoquinolinyl, isothiazolidinyl, isothiazolyl, morpholinyl, naphthyridinyl , oxadiazolyl, 2-oxoazepinyl, 4-oxonaftiridinilo, 2-oxopiperazinyl, 2- oxopiperidinyl, 2-oxopyrrolidinyl, 2-oxopyridyl, 2-oxoquinolinyl, piperidyl, piperazinyl, pyrazinyl, pyrazolidinyl, pyrazolyl, pyridazinyl, pyridinyl, pyridyl, pyrimidinyl, pyrimidyl pyrrolidinyl p irrolilo, quinazolinyl, quinolinyl, quinoxalinyl, tetrahydrofuranyl, tetrahydrofuryl, tetrahidroimidazopiridinilo, tetrahydroisoquinolinyl, tetrahydroquinolinyl, tetrazolyl, thiamorpholinyl, thiamorpholinyl sulfoxide, thiamorpholinyl sulfone, thiazolyl, thiazolinyl, thienofuryl, thienothienyl, thienyl, triazolyl, isoxazolyl, tetrahydrothienyl, tetrahydropyranyl, oxetanyl, tetrahidrotiapiranilo, and thietanyl , where R11 is not substituted or substituted with 1-5 substituents that are each independently selected from R12, R13, R14, R15a and R15b; R12, R13, R14, R15a and R15b are each independently selected from: -C1-6 alkyl, which is unsubstituted or substituted with 1-5 substituents which are each independently selected from: halo, -ORa, - C3-6 cycloalkyl, phenyl or heterocycle, said heterocycle being selected from: pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl, morpholinyl, thiazolyl and oxazolyl, said phenyl or heterocycle being unsubstituted or substituted with 1-5 substituents each independently selected from: halo, -C 1-6 alkyl, which is unsubstituted or substituted with 1-5 halo, and -ORa; -CO2Ra, - C (= O) NRbRc, -S (O) vRd, -CN, -NRbRc, -N (Rb) C (= O) Ra, -N (Rb) SO2Rd, -CF3, -O-CO2Rd , -O- (C = O) -NRbRc, -NRb- (C = O) -NRbRc, and -C (= O) Ra, -C1-6cycloalkyl, which is unsubstituted or substituted with 1-5 substituents which are each independently selected from: halo, -CN, -C1-6 alkyl, which is unsubstituted or substituted with 1-5 halo, -ORa, and phenyl, which is unsubstituted or substituted with 1-5 substituents where the substituents are selected |
| priorityDate | 2006-05-09-04:00^^<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: 96.