http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-055630-A1

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filingDate 2006-09-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_80cf4625fcb0c0bcc500d584389691ee
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publicationDate 2007-08-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-055630-A1
titleOfInvention DERIVATIVES OF DIAZASPIRO AS ANTAGONISTS OF THE CCR8 RECEPTOR, A PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THE MANUFACTURE OF MEDICINES FOR THE TREATMENT OF RESPIRATORY DISEASES.
abstract Processes for its preparation, pharmaceutical compositions containing them and their therapeutic use, in medicines for the treatment of respiratory diseases. Claim 1: A compound characterized in that it responds to the general formula (1) wherein B represents the group of formula (2); Ring D, together with the two C atoms of benzene to which it is fused, is a 5 or 6-membered non-aromatic ring containing one or two O atoms in the ring, and optionally containing a double CC bond between the two ring C atoms other than said benzene C atoms, the D ring being optionally substituted with one or more substituents independently selected from C1-6 alkyl, cycloalkyl, or phenyl (said phenyl being optionally substituted with one or more substituents independently selected from halogen, hydroxyl or C1-4 alkoxy), and also where when the D-ring is a non-aromatic 5-membered ring containing two O atoms in the ring that are arranged in 1, 3 , the D ring may be optionally substituted with the E group, wherein the group E together with a single C atom in the D ring represents a 4 to 8 membered cycloalkyl ring, such that the E group forms a str uctura spiro with ring D; w, x, y and z are independently 1, 2 or 3; each R represents a group independently selected from halogen or C1-4 alkyl; n is 0, 1 or 2; A represents a group selected from phenyl, a 5- or 6-membered heteroaromatic ring containing at least one heteroatom in the ring independently selected from N, O or S, or pyridine-N-oxide, each group being optionally substituted with one or more substituents independently selected from hydroxyl, -CN, halogen, oxo (= O), C1-6 aminoalkyl, C1-6 alkylamino-C1-6 alkyl, N, Ndi (C1-6) alkylamino-C1-6 alkyl , C1-6 alkoxy, C1-6 alkylcarbonyl, -NR1R2, -C (O) -NR3R4, -C1-6 alkenyl-C (O) -NR3R4, -C1-4 alkyl-C (O) -NR5R6, -NHSO2 -R7, -NHC (O) R8, -SO2NH2, carboxyl, carboxy-C1-6 alkyl, C1-6 alkoxycarbonyl, C1-4 alkoxycarbonyl-C1-4 alkyl, C3-6 cycloalkylamino, phenyl, pyridyl (said phenyl being and pyridyl also substituted with one or more groups independently selected from halogen, hydroxyl, carboxy or C1-4 alkyl), C1-6 alkyl or C3-6 cycloalkyl (said two substituents being C1-6 alkyl and C3-6 cycloalkyl also their optionally substituted with one or more substituents independently selected from halogen, hydroxyl, or -CN); or A represents a 9 to 10-membered bicyclic ring system that contains one or more ring heteroatoms independently selected from N, O or S and that is optionally substituted with one or more substituents independently selected from hydroxyl, - CN, halogen, oxo, C1-6 alkoxy, -NR9R10, carboxyl, or C1-6 alkyl; p is 0, 1 or 2; R1 and R2 each independently represent an atom of H, a C1-6 alkyl, C3-6 cycloalkyl or R1 and R2 together with the N atom to which they are attached form a hydantoin group or form a saturated heterocycle of 4 to 7 members, said heterocycle being optionally substituted with hydroxyl, C1-4 alkoxy, or C1-4 alkoxy-C1-4 alkyl; R3 and R4 each independently represents an atom of H, C1-6 alkyl, or C3-6 cycloalkyl, or R3 and R together with the N atom to which they are attached form a saturated heterocycle of 4 to 7 members, being said heterocycle optionally substituted with aminocarbonyl; R5 and R6 each independently represents an atom of H, C1-6 alkyl, or C3-6 cycloalkyl, or R5 and R6 together with the N atom to which they are attached form a saturated heterocycle of 4 to 7 members, being said heterocycle optionally substituted with aminocarbonyl; R7 represents C1-6 alkyl, or a saturated or unsaturated 6-membered ring, where the ring contains at least one N atom, the ring being optionally substituted with one or more substituents independently selected from halogen, oxo, C1-6 alkoxy, or C1-6 alkyl; R8 represents pyridine-N-oxide optionally substituted with one or more substituents independently selected from halogen, or C1-6 alkyl, or R8 represents C1-6 alkyl, C1-6 hydroxyalkyl, or a saturated 5- or 6-membered heterocyclic ring containing at least one heteroatom independently selected from N and O, said ring being optionally substituted with one or more substituents independently selected from halogen, C1-6 alkoxy, oxo, or C1-6 alkyl; R9 and R10 each independently represents an H or C1-6 alkyl atom; or a salt acceptable for pharmaceutical use thereof. Claim 28: A process for the preparation of a compound according to claim 1 or salt acceptable for pharmaceutical use thereof characterized in that it comprises: (a) the reaction of a compound of formula (3) wherein w, x, y, zy B have the values defined in claim 1, with a compound of formula (4), wherein p is in accordance with claim 1 and A is in accordance with claim 1 or a protected derivative thereof, and LG is a leaving group, or (b) the reaction of a compound of formula (5) wherein p, w, x, y, and Z have the values defined in claim 1 and A is in accordance with claim 1 or a protected derivative thereof, with an aldehyde compound of formula (6) wherein D, n, and R have the values defined in claim 1, or (c) the reaction of a compound of the preceding formula (5) with a compound of formula (7) wherein D, n and R have the values defined in claim 1, and LG is a suitable leaving group and optionally following (a), (b) or (c): converting a compound of formula (1) into another compound of formula (1); remove the protective group (s), if any, and / or form a salt acceptable for pharmaceutical use.
priorityDate 2005-09-06-04:00^^<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: 37.