http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-093763-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b7ac99f53337cf91bc276974e5f0f7c8 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B59-002 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B59-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-06 |
| filingDate | 2013-09-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2015-06-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-093763-A1 |
| titleOfInvention | ISOTOPICALLY ENRICHED ARILSULFONAMIDE CCR3 ANTAGONISTS |
| abstract | Isotopically enriched arylsulfonamides, for example, of the formula (1), which are useful for modulating the activity of CCR3 and its pharmaceutical compositions. Also, methods of use for treating, preventing or improving one or more symptoms of a disease, disorder or condition mediated by CCR3. Claim 1: An isotopically enriched compound characterized by the formula (1) or one of its enantiomers, a mixture of enantiomers, a mixture of two or more diastereomers, a tautomer or a mixture of two or more tautomers; or one of its pharmaceutically acceptable salts, solvates, hydrates or prodrugs; wherein: R¹, R², R³, R⁴, R⁵ and R⁸ are each, independently, (a) hydrogen, deuterium, halo, cyano, nitro or guanidine; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl or heterocyclyl; or (c) -C (O) R¹ᵃ, -C (O) OR¹ᵃ, -C (O) NR¹ᵇR¹ᶜ, -C (NR¹ᵃ) NR¹ᵇR¹ᶜ, -OR¹ᵃ, -OC (O) R¹ᵃ, -OC (O) OR¹ᵃ, - OC (O) NR¹ᵇR¹ᶜ, -OC (= NR¹ᵃ) NR¹ᵇR¹ᶜ, -OS (O) R¹ᵃ, -OS (O) ₂R¹ᵃ, -OS (O) NR¹ᵇR¹ᶜ, -OS (O) ₂NR¹ᵇR¹ᶜ, -NR¹ᵇR¹ᶜ, -NR¹ᵃC (O) R1ᵈ, -NR¹ᵃC (O) OR¹ᵈ, -NR¹ᵃC (O) NR¹ᵇR¹ᶜ, -NR¹ᵃC (= NR¹ᵈ) NR¹ᵇR¹ᶜ, -NR¹ᵃS (O) R¹ᵈ, -NR¹ᵃS (O) ₂R¹ᵈ, -NR¹ᵃS (O) NR¹ᵇR¹ᶜ, -NR¹ᵃS (O) ₂NR¹ᵇR¹ᶜ, -SR¹ᵃ, -S (O) R¹ᵃ, -S (O) ₂R¹ᵃ, -S (O) NR¹ᵇR¹ᶜ or -S (O) ₂NR¹ᵇR¹ᶜ; R⁶, R⁷ and R⁹ are each, independently, (a) hydrogen or deuterium; R¹⁰ is (a) hydrogen; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl or heterocyclyl; or (c) -C (O) R¹ᵃ, -C (O) OR¹ᵃ, -C (O) NR¹ᵇR¹ᶜ, -C (NR¹ᵃ) NR¹ᵇR¹ᶜ, -S (O) R¹ᵃ, -S (O) ₂R¹ᵃ, -S (O ) NR¹ᵇR¹ᶜ or S (O) ₂NR¹ᵇR¹ᶜ, R¹¹ is (a) deuterium, halo, cyano, nitro, oxo or guanidine; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl or heterocyclyl; or (c) -C (O) R¹ᵃ, -C (O) OR¹ᵃ, -C (O) NR¹ᵇR¹ᶜ, -C (NR¹ᵃ) NR¹ᵇR¹ᶜ, -OR¹ᵃ, -OC (O) R¹ᵃ, -OC (O) OR¹ᵃ, - OR¹ᵃ, -OC (O) R¹ᵃ, -OC (O) OR¹ᵃ, -OC (O) NR¹ᵇR¹ᶜ, -OC (= NR¹ᵃ) NR¹ᵇR¹ᶜ, -OS (O) R¹ᵃ, -OS (O) ₂R¹ᵃ, -OS (O) NR¹ᵇR¹ᶜ, -OS (O) ₂NR¹ᵇR¹ᶜ, -NR¹ᵇR¹ᶜ, -NR¹ᵃC (O) R¹d, -NR¹ᵃC (O) OR¹d, -NR¹ᵃC (O) NR¹ᵇR¹ᶜ, -NR¹ᵃC (= NR¹d) NR¹ᵇR¹ᶜ, -NR¹ᵃS (O) R¹d, -NR¹ᵃS (O) ₂R¹d, -NR¹ᵃS (O) NR¹ᵇR¹ᶜ, -NR¹ᵃS (O) ₂NR¹ᵇR¹ᶜ, -SR¹ᵃ, -S (O) R¹ᵃ, -S (O) ₂R¹ᵃ, -S (O) NR¹ᵇR¹ᶜ or -S (O) ₂NR¹ᵇR¹ᶜ; each R¹ᵃ, R¹ᵇ, R¹ᶜ and R¹d is, independently, hydrogen, deuterium, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, heteroaryl or heterocyclyl; or each pair of R¹ᵇ and R¹ᶜ together with the N atom to which they are attached, independently form heteroaryl or heterocyclyl; X is O or S; m is an integer of 0, 1, 2 or 3; n is an integer of 1, 2 or 3; and p is an integer of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13 or 14; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, heterocyclyl and heteroaryl optionally is substituted with one or more substituents Q, where each Q is independently selected from (a) deuterium, cyano, halo and nitro; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl and heterocyclyl, each of which is also optionally substituted with one or more , in one embodiment, one, two, three or four substituents Qᵃ; and (c) -C (O) Rᵃ, -C (O) ORᵃ, -C (O) NRᵇRᶜ, -C (NRᵃ) NRᵇRᶜ, -ORᵃ, -OC (O) Rᵃ, -OC (O) ORᵃ, - OC (O) NRᵇRᶜ, -OC (NRᵃ) NRᵇRᶜ, -OS (O) Rᵃ, -OS (O) ₂Rᵃ, -OS (O) NRᵇRᶜ, -OS (O) ₂NRᵇRᶜ, -NRᵇRᶜ, -NRᵃC (O) Rᵈ , -NRᵃC (O) ORᵈ, -NRᵃC (O) NRᵇRᶜ, -NRᵃC (NRᵈ) NRᵇRᶜ, -NRᵃS (O) Rᵈ, -NRᵃS (O) ₂Rᵈ, -NRᵃS (O) NRᵇRᶜ, -NRᵃS (O) ₂NRᵇRᶜ, -SRᵃ, -S (O) Rᵃ, -S (O) ₂Rᵃ, -S (O) NRᵇRᶜ and -S (O) ₂NRᵇRᶜ, where each Rᵃ, Rᵇ, Rᶜ and Rᵈ is, independently, (i) hydrogen or deuterium; (ii) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl or heterocyclyl, each optionally substituted with one or more, in a form of embodiment, one, two, three or four substituents Qᵃ; or (iii) each pair of Rᵇ and Rᶜ together with the N atom to which they are attached form heterocyclyl, optionally substituted with one or more, in one embodiment, one, two, three or four substituents Qᵃ; wherein each Qᵃ is independently selected from the group consisting of (a) deuterium, cyano, halo and nitro; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl and heterocyclyl; and (c) -C (O) Rᵉ, -C (O) ORᵉ, -C (O) NRᶠRᵍ, -C (NRᵉ) NRᶠRᵍ, -ORᵉ, -OC (O) Rᵉ, -OC (O) ORᵉ, - OC (O) NRᶠRᵍ, -OC (= NRᵉ) NRᶠRᵍ, -OS (O) Rᵉ, -OS (O) ₂Rᵉ, -OS (O) NRᶠRᵍ, -OS (O) ₂NRᶠRᵍ, -NRᶠRᵍ, -NRᵉC (O) Rʰ, -NRᵉC (O) ORʰ, -NRᵉC (O) NRᶠRᵍ, -NRᵉC (= NRʰ) NRᶠRᵍ, -NRᵉS (O) Rʰ, -NRᵉS (O) ₂Rʰ, -NRᵉS (O) NRᶠRᵍ, -NRᵉS (O) ₂NRᶠRᵍ, -SRᵉ, -S (O) Rᵉ, -S (O) ₂Rᵉ, -S (O) NRᶠRᵍ and -S (O) ₂NRᶠRᵍ; wherein each Rᵉ, Rᶠ, Rᵍ and Rʰ is, independently, (i) hydrogen or deuterium; (ii) C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₇ cycloalkyl, C₆₋₁₄ aryl, C₇₋₁₅ aralkyl, heteroaryl or heterocyclyl; or (iii) each pair of Rᶠ and Rᵍ together with the N atom to which they are attached form heterocyclyl. |
| priorityDate | 2012-09-07-04:00^^<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: 47.