http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-032134-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a2901e694724c2a759f619944cb7d2a4 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-424 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B53-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4162 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 |
| filingDate | 2000-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_db6d9b6c715c82cfcbe496ec374ef0a5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_34d7b6b0fb0d2a6325c2e5f2ca17f5b7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b54811629d82fc1ca66bb86a50698810 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8f173358ab3950cdbcb587d74b1d7a6b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_35c5fd40050cf0de91d1f759b02c480f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6adecfa1c5969dfb1c4d1d3810e667d8 |
| publicationDate | 2003-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-032134-A1 |
| titleOfInvention | COMPOUNDS DERIVED FROM TIENOISOXAZOLIL- AND TIENILPIRRAZOLIL-FENOXI-SUBSTITUTED PROPILES AS D4 ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS, PREPARATION PROCEDURES, INTERMEDIARY COMPOUNDS AND MANUFACTURING MANUFACTURING PRODUCTS |
| abstract | A compound of formula (1) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: X is N (CH3) or O; R1 is OH or C1-6 alkoxy; R2 is H or C1-6 alkyl; R3 is (CH2) nQ, CH2CH (OH) Q, CH (CH3) Q, 1,2,3,4-tetrahydronaphthyl, indanyl or adamantyl, where Q is thienyl, phenyl, furanyl, naphthyl, pyridyl, indolyl, indazolyl, cyclohexyl, 1,2-methylenedioxyphenyl, cyclohexenyl or 1 H -pyrazolo [4,3-c] pyridyl, and Q is optionally substituted with one or two moieties independently selected from halo, C 1-6 alkyl, C 1-6 alkoxy, hydroxy, S (O) 2NH2, trifluoromethyl or cyano and n is 2; R4 is H or C1-6 alkyl; or R3 and R4, together with the nitrogen atom to which R3 and R4 are attached, form 1,4-dioxa-8-azoespiro [4.5] decanyl, piperazinyl, morpholinyl, piperidinyl, pyrrolidinyl, azocanyl, 1,2,3, 4-tetrahydroisoquinolinyl, 1,2,3,4-tetrahydro-B-carbolinyl, 4,5,6,7-tetrahydrothienyl [3,2-c] pyridyl or 8-azabicyclo [3.2.1] octane, each which may be mono- or independently disubstituted with halo, C1-6 alkyl, C1-6 alkoxy, C (O) phenyl, OH, CN, O-phenyl or (CH2) mZ; Z is benzisoxazolyl, indazolyl, benzisothiazolyl, benzothienyl, pyrimidinyl, pyridyl, 1,2-methylenedioxyphenyl or phenyl; and Z, CH (OH) phenyl or O-phenyl are optionally substituted with one or two moieties independently selected from halo, C1-6 alkyl, C1-6 alkoxy; hydroxy, trifluoromethyl, S (O) 2NH2 or cyano, and m is 0 or 1; provided that, when R1 is OH, R2 is H: (a) when R4 is H and R3 is (CH2) nQ, where n is 1 or 2, then Q cannot be indolyl or phenyl; or (b) when R3 and R4 form piperazinyl substituted with (CH2) mZ, when m is 1 then it cannot be phenyl. A pharmaceutical composition that includes the compounds of formula (1) in admixture with a pharmaceutically acceptable carrier. Procedures for preparing said class of compounds and intermediates. Uses of the compounds of formula (1) for the manufacture of medicaments for the treatment of medical conditions mediated by the inhibition of the D4 receptor. These conditions include, for example, attention deficit hyperactivity disorder, obsessive-compulsive disorder, psychosis, substance abuse, substance dependence, Parkinson's disease, parkinsonism, tardive dyskinesia, syndrome Gilles de la Tourette, behavior disorder and oppositional provocation disorder. |
| priorityDate | 1999-09-14-04:00^^<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: 60.