http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-082458-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-4858 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4168 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5513 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-421 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-422 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-1623 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2018 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5513 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-421 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-422 |
| filingDate | 2011-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6d9faf20d5ad3940f025a79d7d9f9964 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_44cb154ebc71eb9565cb225b883176f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_10bbdc7422b8f5664282f7d28cc996d4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4b40cce78a359647fe4c7d4e3e6f6ab9 |
| publicationDate | 2012-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-082458-A1 |
| titleOfInvention | COMBINATION INCLUDING AN ANTIPSYCHOTIC PHARMACO AND A TAAR AGONIST1 |
| abstract | Pharmaceutical combination for the treatment of schizophrenia and acute manic episodes associated with bipolar disorders, comprising a compound that is active on a receptor 1 associated with trace amines (TAAR1 agonist) and an antipsychotic drug. Pharmaceutical compositions comprising a combination of an atypical antipsychotic drug and a TAAR1 agonist as described in claim 2, 3 and 4. Claim 1: Combination comprising an atypical antipsychotic drug and a TAAR1 agonist. Claim 2: Combination according to claim 1, comprising olanzapine and a TAAR1 agonist of formula (1) wherein: R1 is hydrogen, deuterium, tritium, lower alkyl, hydroxy, lower alkoxy, lower alkyl with halogen, lower alkoxy substituted by halogen, halogen, phenyl optionally substituted by halogen, or is phenyloxy, benzyl, benzyloxy, -COO-lower alkyl, -O- (CH2) or O-lower alkyl, NH-cycloalkyl, cycloalkyl or tetrahydropyran-4-yloxy, in which substituents for n> 1 may be the same or different; X is a link, -CHR-, -CHRCHR'-, -OCH2-, -NRCHR ', -OCHRCHR', -CH2OCHR-, -CH2CH2CH2-, -SCH2-, -S (O) 2CH2-, -CH2SCH2-, -CH2N (R) CH2-, -cycloalkyl-CH2- or SiRR'-CH2-; R / R ’can be, independently of one another, hydrogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, phenyl or lower alkyl; Y is phenyl, naphthyl, thiophenyl, pyridinyl, cycloalkyl, 1,2,3,4-tetrahydronaphthalene-2-yl, 2,3-dihydrobenzo [1,4] dioxin-6-yl or benzo [1,3jioxol-5- ilo; n is 0, 1, 2 or 3; or is 2 or 3; or a pharmaceutically acceptable acid addition salt thereof, or a TAAR1 agonist of formula (2) in which R is hydrogen or lower alkyl; R1 is - (CH2) n- (O) o-heterocycloalkyl, optionally substituted with lower alkyl, hydroxy, halogen, or with - (CH2) p-aryl; n is 0, 1 or 2; o is 0 or 1; p is 0, 1 or 2; R2 is cycloalkyl, heterocycloalkyl, or is aryl or heteroaryl, in which the aromatic rings are optionally substituted with one or two substituents, selected from lower alkyl, halogen, heteroaryl, CF3, OCF3, OCH2CF3, lower alkoxy, CH2-lower alkoxy , lower alkynyl or cyano; X is a link, -NR’-, -CH2NH-, -CHR ’’ -, - (CH2) q-O- or - (CH2) 2-; R ’is hydrogen or lower alkyl; R 'is hydrogen, lower alkyl, lower alkoxy; q is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Claim 3: Combination according to claim 2, comprising olanzapine and a TAAR1 agonist of formula (3) wherein R1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkyl with halogen, lower alkoxy substituted with halogen or halogen , in which the substituents for n = 2 may be the same or different; X is a link, -NRCHR ’, -CHRCHR’ or -OCHRCHR ’; R / R ’can be, independently of one another, hydrogen, lower alkyl; n is 1 or 2; or a TAAR1 agonist of formula (2) in which R is hydrogen; R1 is pyrrolidinyl; R2 is aryl or heteroaryl, in which the aromatic rings are optionally substituted with halogen; X is a link or -NR’-; R ’is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. Claim 4: Combination according to claims 1 to 3, comprising olanzapine and a TAAR1 agonist, the TAAR1 agonists being: S1 = (S) -4 - ((S) -2-phenyl-butyl) -4.5- dihydro-oxazol-2-ylamine, S2 = (S) -4- (3-fluoro-2-methyl-phenyl) -4,5-dihydro-oxazol-2-ylamine, S3 = (S) -4- (4 -chloro-2-trifluoromethyl-phenyl) -4,5-dihydro-oxazol-2-ylamine, S4 = (S) -4 - [(ethyl-phenyl-amino) -methyl] -4,5-dihydro-oxazole- 2-ylamine, S5 = 3 - [(S) -1 - ((S) -2-amino-4,5-dihydro-oxazol-4-ylmethyl) -propoxy] -phenol, S6 = (4-pyrrolidin-3 -yl-phenyl) -amide of 5-chloro-pyridin-2-carboxylic acid, S7 = 4-chloro-N- (4-pyrrolidin-3-yl-phenyl) -benzamide, S8 = 1- (5-chloro- pyridin-2-yl) -3- (4-pyrrolidin-3-yl-phenyl) urea, S9 = (S) -4 - [(S) -1- (4-fluoro-phenyl) -ethoxymethyl] -4, 5-Dihydro-oxazol-2-ylamine, S10 = {4- [2 - ((S) -2-amino-4,5-dihydro-oxazol-4-yl) -ethyl] -phenyl} -amide of acid 5 -chloro-pyrimidin-2-carboxylic acid, S11 = N- {4- [2 - ((S) -2-amino-4,5-dihydro-oxazol-4-yl) -ethyl] -phenyl} -4-chloro -benzamide, S12 = (R) -2-chloro-6-methyl-N- (4- (morpholin-2- il) phenyl) isonicotinamide, S13 = (S) -N- (4- (morpholin-2-yl) phenyl) -6- (2,2,2-trifluoroethoxy) nicotinamide, S14 = (S) -N- (4 - (morpholin-2-yl) phenyl) -2- (trifluoromethyl) isonicotinamide, S15 = (S) -1- (4-fluorobenzyl) -3- (4- (morpholin-2-yl) phenyl) urea, S16 = (S) -1- (3-cyanophenyl) -3- (4- (morpholin-2-yl) phenyl) urea, and S17 = (S) -6-chloro-N- (4- (morpholin-2-yl ) phenyl) nicotinamide. Claim 5: Compound S2 = (S) -4- (3-fluoro-2-methyl-phenyl) -4,5-dihydro-oxazol-2-ylamine, comprised of formulas (1) or (3) according to the claims 2 and 3. Claim 6: Combination according to claims 1 to 4, comprising olanzapine and a TAAR1 agonist for the treatment of schizophrenia and manic episodes associated with bipolar disorder, with a reduced incidence of metabolic syndrome. Claim 7: Combination according to claim 6, comprising olanzapine and a TAAR1 agonist for the treatment of schizophrenia and manic episodes associated with bipolar disorder, with antidiabetic efficacy. Claim 9: Combination according to claim 8, comprising olanzapine and a TAAR1 agonist for the treatment of schizophrenia and manic episodes associated with bipolar disorder, with antidiabetic efficacy, resulting in the reduction of fat mass and weight bodily. Claim 16: Method for the treatment of schizophrenia and manic episodes associated with bipolar disorder according to claim 15, wherein the reduced incidence of metabolic syndrome results from antidiabetic efficacy with reduced excursions of blood glucose, fat mass and body weight, which comprises administering in an human being who needs an effective amount of a combination thereof comprising an atypical antipsychotic drug and a TAAR1 agonist. |
| priorityDate | 2010-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 91.