http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-068700-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_938a6d7a15cbc93a74abe1953eb25d47 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 |
| filingDate | 2007-12-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_df6f5f2196b90184f099597f2603f4c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1345f8ec5d99512587be79ab69367bd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5bb7b4802d232af69a3173214d22a033 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_529d4a080173d1977d7deff7b6b98ab7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5c9910e530e02b5e095640d1ed0310c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_82f543a2a25525c2a9337dcf11750c06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb4d67e6d399d32ef6d36c1231b1ff73 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_92ed311674554b1f83f71909a55ee004 |
| publicationDate | 2009-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-068700-A1 |
| titleOfInvention | ANTIGONISTS OF CGRP RECEPTORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND USES OF THE SAME FOR THE TREATMENT OF PAIN, INFLAMMATORY PROCESSES AND VASCULAR DISORDERS, AND OTHER DISEASES |
| abstract | Pharmaceutical compositions thereof and uses to treat diseases and conditions measured by the CGRP receptor. Claim 1: CGRP receptor antagonists, characterized in that they consist of compounds of the formula (1), wherein: X is S, SO, or SO2; Z1 is a bond or NR7, O, S, CH2, C (O), NR7C (O) NR7, where R7 is hydrogen, C1-4 aliphatic or C1-4 aliphatic C (O); Z2 is a bond, O, CH2O, or C (O); the A ring is phenyl or a 4-7 membered heterocyclic or heteroaryl ring or a 10-14 membered heteroaryl or heterocyclic bicyclic ring wherein said heterocyclic or heteroaryl ring has 1-4 heteroatoms selected from O, N, or S; where ring A is optionally substituted with up to 5 R1 substituents; where: Z2 is a link, Z1 is a link, NR7, O, S, CH2, C (O), NR7C (O) NR7; or where: Z1, Z2, and R6 are absent, ring A is not aromatic, and ring A together with ring B form a spirocyclic ring system; R6 is hydrogen or a C1-4 aliphatic; m is 1-3; n is 1-3; with the proviso that m + n is less than or equal 4; RY is aryl, heteroaryl, cycloaliphatic, C1-6 aliphatic, C1-6 aryl-aliphatic, C1-6 heteroaryl-aliphatic, C1-6 heterocyclyl-aliphatic or C1-6 cycloaliphatic-aliphatic; where RY is optionally substituted with up to 5 R2 substituents; RX is hydrogen, aryl, heteroaryl, C1-6 aliphatic, C1-6 aryl-aliphatic, C1-6 heteroaryl-aliphatic, where RX is optionally substituted with up to 5 R3 substituents; or two RXs, taken together with the carbon atom to which they are attached, form a 3-9 membered monocyclic, aryl, heteroaryl or heterocyclic ring system, 9-14 member bicyclic or 12-14 member tricyclic where each heteroaryl ring or heterocyclic has up to 3 heteroatoms selected from O, S and N; wherein said annular system formed by two RXs is optionally substituted with up to 5 R4 substituents; RZ is absent, is hydrogen, CN, aliphatic C1-6, halo-aliphatic C1-6, O-aliphatic C1-6, O- (halo-aliphatic C1-6), halo, aryl-aliphatic C1-6, or heteroaryl C1-6 aliphatic; the dotted line is a single or double bond; with the proviso that, when it is a double bond, then RZ and one of RW is absent; Each RW is independently absent, it is hydrogen, halo, oxo, C1-6 aliphatic, C1-6 halo-aliphatic, C1-6 -O-aliphatic, -O- (C1-6 halo-aliphatic), aryl, aryl-aliphatic C1-6, C3-7 cycloaliphatic; or two RWs taken together form an optionally substituted C3-7 cycloaliphatic or heterocyclic ring, wherein said heterocyclic ring has up to 3 heteroatoms selected from O, S and N; wherein said ring formed by two RWs is optionally substituted with up to 5 R5 substituents; where each occurrence of R1, R2, R3, R4, and R5 is independently Q-RM; where Q is a link or is a C1-6 aliphatic chain where up to two non-adjacent methylene units of Q are optionally and independently replaced by CO, CO2, COCO, CONR, OCONR, NRNR, NRNRCO, NRCO, NRCO2, NRCONR, SO, SO2, NRSO2, SO2NR, NRSO2NR, O, S, or NR; where each occurrence of MRI is independently selected from R ', halogen, NO2, CN, OR', SR ', N (R') 2, NR'C (O) R ', NR'C (O) N (R' ) 2, NR'CO2R ', C (O) R', CO2R ', OC (O) R', C (O) N (R ') 2, OC (O) N (R') 2, SOR ', SO2R ', SO2N (R') 2, NR'SO2R ', NR'SO2N (R') 2, C (O) C (O) R ', or C (O) CH2C (O) R'; where each occurrence of R is independently selected from hydrogen or a C1-6 aliphatic group optionally substituted with 0-5 occurrences of RK; and each occurrence of RK is independently selected from -RV, halogen, -NO2, -CN, -ORV, -SRV, -N (RV) 2, - NRVCORV, -NRVCON (RV) 2, -NRVCO2RV, -CORV, - CO2RV, -OCORV, -CON (RV) 2, -C (= N-CN), -OCON (RV) 2, -SORV, -SO2RV, -SO2N (RV) 2, -NRVSO2RV, NRVSO2N (RV) 2, -COCORV, -COCH2CORV, -OP (O) (ORV) 2, -P (O) (ORV) 2, -OP (O) 2ORV, -P (O) 2ORV, or -OPO (RV) 2, where RV it is hydrogen or an unsubstituted C1-6 aliphatic; and where each occurrence of R 'is independently hydrogen, a C1-6 aliphatic group optionally substituted with 0-5 occurrences of RM1; and each occurrence of RM1 is independently selected from RT, halogen, -NO2, -CN, -ORT, -SRT, -N (RT) 2, -NRTCORT, -NRTCON (RT) 2, -NRTCO2RT, -CORT, -CO2RT , -OCORT, -CON (RT) 2, -C (= N-CN), -OCON (RT) 2, -SORT, -SO2RT, -SO2N (RT) 2, -NRTSO2RT, -NRTSO2N (RT) 2, -COCORT, -COCH2CORT, -OP (O) (ORT) 2, -P (O) (ORT) 2, -OP (O) 2ORT, -P (O) 2ORT, -PO (RT) 2, or -OPO (RT) 2, where RT is hydrogen or an unsubstituted C1-6 aliphatic; or R 'is a 3-8 membered, saturated, partially unsaturated or completely unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, or a saturated, partially unsaturated 8-12 bicyclic ring system completely unsaturated having 0-5 heteroatoms independently selected from nitrogen, oxygen or sulfur where said monocyclic or bicyclic ring is optionally substituted with 0-5 occurrences of RU; and each occurrence of RU is independently selected from a saturated 3-8 membered monocyclic ring, partially unsaturated or completely unsaturated optionally substituted with 0-3 occurrences of -RQ1 and having 0-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, or RU is -RQ, halogen, = O, = NRQ, -NO2, -CN, -ORQ, -SRQ, -N (RQ) 2, -NRQCORQ, -NRQCON (RQ) 2, -NRQCO2RQ, -CORQ, - CO2RQ, -OCORQ, -CON (RQ) 2, -C (= N-CN), -OCON (RQ) 2, -SORQ, -SO2RQ, -SO2N (RQ) 2, -NRQSO2RQ, -NRQSO2N (RQ) 2 , -COCORQ, -COCH2CORQ, -OP (O) (ORQ) 2, -P (O) (ORQ) 2, -OP (O) 2ORQ, -P (O) 2ORQ, -PO (RQ) 2, or - OPO (RQ) 2, where RQ and RQ1 are hydrogen or an unsubstituted C1-6 aliphatic; or R and R ', two occurrences of R, or two occurrences of R', are taken together with the atom (s) that are joined to form a 3-12 membered monocyclic or bicyclic ring, saturated, partially unsaturated or completely unsaturated having 0-4 heteroatoms independently selected from nitrogen, oxygen or sulfur where said monocyclic or bicyclic ring is optionally substituted with 0-5 occurrences of RT1; and each occurrence of RT1 is independently selected from -RS, halogen, = O, = NRS, -NO2, -CN, -ORS, -SRS, -N (RS) 2, -NRSCORS, -NRSCON (RS) 2, - NRSCO2RS, -CORS, -CO2RS, -OCORS, -CON (RS) 2, -C (= N-CN), -OCON (RS) 2, -SORS, -SO2RS, -SO2N (RS) 2, -NRSSO2RS, -NRSSO2N (RS) 2, -COCORS, -COCH2CORS, -OP (O) (ORS) 2, -P (O) (ORS) 2, -OP (O) 2ORS, -P (O) 2ORS, -PO ( RS) 2, or -OPO (RS) 2, where RS is hydrogen or an unsubstituted C1-6 aliphatic; said compounds being selected from Table (2). |
| priorityDate | 2007-06-13-04:00^^<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: 45.