http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046787-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 |
| filingDate | 2004-12-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9ff1c366b4564326966a28e5bb69772c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b6b0b1940844b58b18e5b4b0b1a688c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5353299f265f73c50a8245a056b7a922 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e78805a643c89cb7eec63d9a0d1e3010 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fcf8e437843e0467fb8f282154c94497 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e49c8a1473bbc3dacafad6a23feb9778 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_39a5758f9e5705e61bf7ea04f0c29943 |
| publicationDate | 2005-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-046787-A1 |
| titleOfInvention | HETEROCICLIC ANTIMIGRAN AGENTS |
| abstract | Peptide receptor antagonists related to calcitonin gene ("CGRP receptor"), pharmaceutical compositions comprising them, methods to identify them, methods of treatment using them and their use in therapy for the treatment of neurogenic vasodilation, neurogenic inflammation, migraine, and other headaches, thermal injury, circulatory shock, flushing associated with menopause, inflammatory airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions whose treatment can be carried out by the CGRP receptor antagonism. Claim 1: A compound characterized in that it has the formula (1) or a pharmaceutically acceptable salt or solvate thereof wherein V is a 5-membered ring selected from the group consisting of imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, furanyl, isoxazolyl , oxadiazolyl, triazolyl, thiadiazolyl and tetrazolyl, or a 6-membered ring selected from the group consisting of pyridyl, pyrimidinyl, triazinyl, pyrazinyl, pyridazinyl and tetrazinyl; or a fused bicyclic ring system selected from the group consisting of indolyl, isoindolyl, indazolyl, benzimidazolyl, benzithiazolyl, triazolopyridinyl, imidazopyridinyl, quinolinyl, isoquinolinyl, cinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, optionally substituted: 3 of the same or different substituents selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl, C (O) OC-C2-3 alkyl, C1-4 alkylcarbonyl, carboxy, C1-4 alkylcarboxy , trifluoromethyl, halo, cyano, amino, amido, nitro, carbamoyl, ureido, C1-4 alkylamino, C1-4 dialkylamino, C1-4 dialkylamino-C1-2 alkyl, sulfonamide and sulfonyl, and V optionally contains 1 or 2 carbonyls; provided that if t is 1, then V is optionally substituted with one of the substituents selected from the group consisting of halo, C1-4 alkyl, C1-4 alkylidino alkylidino of 4, C1-4 alkoxy, hydroxy C1-4 alkyl, C 1-4 alkylcarbonyl, trifluoromethyl, halo and cyano; and V optionally contains 1 or 2 carbonyls; (V´) t where t is 0 or 1; and V 'is selected from the group consisting of C3-7 cycloalkyl, phenyl, adamantyl, quinuclidyl, azabicyclo [2.2.1] heptyl, azetidinyl, tetrahydrofuranyl, furanyl, dioxolanyl, thienyl, tetrahydrothyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, imidazolyl, imidazolyl , imidazolidinyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyranyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, piperidinyl, piperazinyl, morpholino, thiomorpholino and dioxolanyl, and wherein V ´ is optionally substituted with 1 or 2 of the same or different substituents selected from the group consisting of halo, cyano, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, hydroxy, amino, C3-7 cycloalkyl, C1 alkylamino -4, C1-4 dialkylamino, (C1-3 alkyl) 0-2ureido, C (O) OC2-3alkyl, carboxy, amido, nitro, phenyl and benzyl; and wherein V 'optionally contains 1 or 2 carbonyls, and V and V' are optionally interrupted by C1-3 alkylene, O, (CH2) 0-2C (O) - (CH2) 0-2-, or N-alkyl C1-4, C1-3 alkylene being optionally interrupted by, or has O, N or S attached thereto; U is CH2, O or NH; Q is (Sy) sR3; wherein Sy is C1-3 alkylene or C1-3 alkylidene and s is 0 or 1, R3 is R3a or R3b where R3a is (i) a heterocycle having two fused rings with 5 to 7 members in each of the rings, the heterocycle contains 1 to 5 of the same or different heteroatoms selected from the group consisting of O, N and S and the heterocycle optionally contains 1 or 2 carbonyls, wherein the carbonyl C atom is a member of the fused rings; (ii) a 4- to 6-membered heterocycle containing 1 to 3 of the same or different heteroatoms selected from the group consisting of O, N and S that optionally contains 1 to 2 carbonyls, wherein the carbonyl C atom is a 4 to 6 member heterocycle member; (iii) C3-7 cycloalkyl; (iv) carbazolyl, fluorenyl, phenyl, -O-phenyl, -O-C 1-4 alkylene-phenyl, or naphthyl; or (v) C1-8 alkyl, C2-7 alkenyl, -C (O) R3´, CHC (O) O-R3´, CH (CH3) C (O) O-R3´, -C (O) O -R3 'or C2-7 alkynyl, and wherein R3a is optionally substituted with 1 to 3 of the same or different substituents selected from the group consisting of benzyl, phenyl, -O-phenyl, -O-C1-3 alkylenephenyl, - C1-3-alkylene (O) -phenyl, cyano, amino, nitro, halo, C1-6 alkyl, C1-3 mono-bi-tri-haloalkyl, C1-3 mono-bi-tri-haloalkyloxy, (C1 alkyl -3) 1-2amine, -OR3´, - C (O) R3´, -C (O) O-R3´, -OC (O) R3´, -N (R3´) 2, -C (O) N (R3´) 2, -N (R3´) C (O) (R3´) 2, -N (R3´) C (O) N (R3´) 2, -N (R3´) C (O) OR3´, OC (O) N (R3´) 2, -N (R3´) SO2R3´, -SO2N (R3´) 2 and -SO2R3´; R3´ is H or C1-6 alkyl; R3b is R3a but it is not phenyl or substituted phenyl; provided that if V and V 'together form substituted or unsubstituted imidazol-2-yl or a substituted or unsubstituted fused bicyclic system containing imidazol-2-yl, then R3 is R3b, D is O, NCN or NSO2 C1 alkyl -3; A is C, N or CH; m and n are independently 0, 1 or 2; as long as if m and n are 0, then A is not N; if m is 2, then n is not 2; or if n is 2, then m is not 2; E is N, CH or C; p is 0 or 1; if p is 1, then G, J and E together form Ax or Ay; Ax is a fused heterocycle that has two fused rings with 5 to 7 members in each of the rings, the heterocycle contains 1 to 4 of the same or different heteroatoms selected from the group consisting of O, N and S and optionally containing 1 or 2 carbonyls, wherein the carbonyl C atom is a member of the fused heterocycle; Ay is a 4- to 6-membered heterocycle containing 1 to 3 heteroatoms selected from the group consisting of O, N and S, and optionally containing 1 to 2 carbonyls, wherein the carbonyl C atom is a member of the heterocycle of 4 to 6 members; wherein Ax and Ay are optionally substituted with C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, cyano, C3-7 cycloalkyl, phenyl, halophenyl, halo, furanyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, imidazolyl, imidazolinyl, imidazolidinyl , pyrazolyl, pyrazolinyl, pyrazolidinyl, pyridyl, pyrimidinyl, piperidinyl, piperazinyl or morpholino; or if p is 0 such that G and J are each linked to A, then A is C, and G, J and A together form a spirocyclic ring system with the rings of the system containing A and where GJA is Ax o Ay. |
| priorityDate | 2003-12-05-04:00^^<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: 78.