http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-093797-A1

Outgoing Links

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filingDate 2013-12-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6e696c056e82eb550b229c61f24cfd03
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_16c4629e95fdcc82efee28ac246f2fe2
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publicationDate 2015-06-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-093797-A1
titleOfInvention Phenylethylpyridine derivatives PDE-4 INHIBITORS
abstract Claim 1: A compound characterized in that it is of the general formula (1), wherein R¹ is selected from hydrogen, C₁₋₄ alkyl, and -SO₂-C₁₋₄ alkyl; R² is selected from aryl and a 5- to 11-membered heteroaryl, wherein said aryl or heteroaryl is optionally substituted with 1 to 3 groups independently selected in each case from the list consisting of: halogen, C₁₋₄ haloalkyl, hydroxy , -SO₂NR⁸R⁹, -CN, -NR¹⁰SO₂R¹¹, C₁₋₄ alkyl and C alco alkoxy, where the C₁₋₄ alkyl or C₁₋₄ alkoxy groups are optionally substituted with a C₃₋₇ cycloalkyl group, and where R⁸ is hydrogen or alkyl C₁₋₆; R⁹ is hydrogen or C₁₋₆ alkyl; R¹⁰ is hydrogen or C₁₋₆ alkyl; R¹¹ is hydrogen or C₁₋₆ alkyl; Z is a diradical selected from the list consisting of: a union, - (CH₂) ₘ-, -S-, -S (O) -, -S (O₂) -, a group -C (O) -, and a group [1] - (CH₂) ₘ-OC (O) - [2] where [1] and [2] represent, respectively, the point of attachment of the group Z to the phenyl ring and the nitrogen atom and m is an integer in the range between 1 and 4; L¹ is a diradical selected from the list consisting of: a link, - (CH₂) ₚ-, [3] - (CH₂) ₚ-O- [4], [3] - (CH₂) ₚ-NR¹⁰- (CH₂ ) ₜ- [4], [3] - (CH₂) ₚ-OC (O) - [4], [3] - (CH₂) ₚ-NR¹⁰C (O) - [4], [3] - (CH₂) ₚ-NR¹⁰S (O₂) - [4], [3] - (CH₂) ₚ-S (O₂) -N (R¹⁰) - [4] where [3] and [4] respectively represent the junction point of the group L¹ to the carbonyl group and the phenyl ring, and where R¹⁰ is as described above, p is an integer in the range between 1 and 4 and t is an integer in the range between 1 and 4; R³ is hydrogen or is selected from the group consisting of: halogen, haloalkyl C₁₋₄, hydroxy, aminocarbonyl, di-C₁₋₄-aminocarbonyl alkyl, -SO₂NR¹²R¹³, -CN, -NR¹⁴SO₂R¹⁵, - (CH₂) ₘ-NR¹⁴SO₂R¹⁵-, alkyl C₁₋₄ and C alco alkoxy, where the C₁₋₄ alkyl or C₁₋₄ alkoxy groups are optionally substituted with a C₃₋₇ cycloalkyl group, ₘ ₑₛ ᶜₒₘₒ ₛₑ ᵈₑₛᶜʳⁱᵇₑ ₚʳₑᶜₑᵈₑₙₜₑₘₑₙₜₑ, ʸ R¹² is hydrogen or C₁₋₆ alkyl; R¹³ is hydrogen or C₁₋₆ alkyl; R¹⁴ is hydrogen or C₁₋₆ alkyl; R¹⁵ is hydrogen or C₁₋₆ alkyl; q is an integer in the range between 1 and 3; R⁴ and R⁵ are different or equal and are independently selected from the group consisting of: H; C₃₋₇carbonyl cycloalkyl; C₁₋₆ alkyl, optionally substituted with one or more substituents selected from C₃₋₇ cycloalkyl or C₅₋₇ cycloalkenyl; C₁₋₆ haloalkyl; C₃₋₇ cycloalkyl; C₅₋₇ cycloalkenyl; C₂₋₆ alkenyl; and C₂₋₆ alkynyl; or R⁴ and R⁵, together with the atoms that interconnect them, form a 2,2-difluoro-1,3-dioxolane ring of formula (2) fused to the phenyl unit that joins the -OR⁴ and -OR⁵ groups, where asterisks indicate carbon atoms shared with said phenyl ring; R⁶ is selected from the group consisting of: CN, NO₂, CF₃ and halogen atoms; n is 0 or an integer in the range between 1 and 3; A is a nitrogen-containing group that can be selected from: a group (a) that is - (CH₂) ₛ-NR¹⁶R¹⁷ where s is an integer in the range between 1 and 4 and R¹⁶ and R¹⁷ are independently hydrogen or C₁ alkyl ₋₄; and a group (b) which is a monocyclic, bicyclic or tricyclic saturated heterocyclic ring system optionally substituted with one or two R¹⁸ groups that are independently selected in each case from C₁₋₄ alkyl and benzyl; N-oxides in the pyridine ring, deuterated derivatives and pharmaceutically acceptable salts or solvates thereof.
priorityDate 2012-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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