http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1828119-A1

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0d269c8e41f178194d858c230c9f85e3
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40
filingDate 2005-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e9ad01c153cb99dd545bcf29066c730b
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc6e8b0660920a212d18ae036a47df1c
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publicationDate 2007-09-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1828119-A1
titleOfInvention N-pyrrolidin-3-yl-amide derivatives as serotonin and noradrenalin re-uptake inhibitors
abstract A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, - C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; aryl represents phenyl, naphthyl, anthracyl or phenanthryl; het represents an aromatic or non-aromatic 4-, 5­-or 6- membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6- membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R2 is aryl1 or het1, each optionally substituted; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is (CH2)aE, wherein a is 0, 1 or 2 and E is a group selected from: Formula (i) wherein: X is O, S, NR12, (CH2)v or a bond; b is 1, 2, 3 or 4; c is 1, 2 or 3; v is 1 or 2; R10 and 11 are each independently H or C1-4 alkyl; and R12 is H, 1-6 alkyl, C(O)C1-6 alkyl, SO2-C1-6alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula (iii) wherein: d is 1, 2, 3 or 4; a is 1, 2 or 3; f is 1 or 2; and R30 is H or C14 alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: g is 0, 1, 2 or 3; J is NR40; and R40 is C(O)C1-6 alkyl, S02-C1-6 alkyl; Formula (v) wherein: h is 0, 1, 2 or 3; and R50 is H, C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S-C1-4alkyl; Formula (vi) -CH(cyclopropane)2; Formula (vii) C1-6alkyl, substituted by at least one substituent; and Formula (viii) C3-8cycloalkyl-C1-6alkyl; wherein the C1-6alkyl moiety is substituted at any point other than at the junction with the C3-8cycloalkyl moiety, by at least one substituent. The compounds exhibit activity as both serotonin and/or noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
priorityDate 2004-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 1783.