http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-040962-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-428 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P15-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-428 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 |
| filingDate | 2003-08-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-040962-A1 |
| titleOfInvention | COMPOUNDS DERIVED FROM TIAZOL 1,3-2-ONA, PHARMACEUTICAL COMPOSITION AND COMPOSITE PREPARATION PROCESS |
| abstract | The compounds of the formula (1), in free or salt or solvate form, are also useful for treating conditions that are prevented or relieved by activating the beta-2 adrenoceptor. Also described are pharmaceutical compositions containing the compounds, and processes for the preparation of the compounds, and use of these to prepare medicaments. The inflammatory and obstructive diseases in the respiratory tract to which these compounds are applicable, include asthma of any type or genesis, whether it be intrinsic (non-allergic) or extrinsic (allergic) asthma. Other inflammatory or obstructive diseases and conditions of the respiratory tract to which treatment with these compounds is applicable, include acute lung injury (ALI), adult / acute insufficiency syndrome (ARDS), chronic pulmonary obstructive disease, respiratory tract, or of the lung (COPD, COAD, or CLD), including chronic bronchitis, or dyspnea associated with it, emphysema, as well as exacerbation of hyperreactivity of the airways as a result of another drug therapy, in particular another inhaled drug therapy. They are also applicable to the treatment of bronchitis of any type or genesis, including, for example, acute, arachidic, catarrhal, croup, chronic, or ftinoid bronchitis. Other inflammatory or obstructive airway diseases to which this is applicable include pneumoconiosis (an inflammatory, commonly occupational, lung disease, frequently accompanied by airway obstruction, either chronic or acute, and caused by inhalation repeated powders) of any type or genesis, including, for example, aluminosis, anthracosis, asbestosis, calicosis, ptilosis, siderosis, silicosis, tabacosis, and bisinosis. Considering their beta2 agonist activity, the compounds herein are also useful in the treatment of a condition that requires relaxation of the smooth muscle of the uterus or vascular system. Therefore, they are useful for the prevention or relief of premature labor pains in pregnancy. They are also useful in the treatment of chronic and acute urticaria, psoriasis, rintitis, allergic conjunctivitis, actinitis, hay fever, and mastocytosis. Claim 1: a compound of the formula (1) in free or salt or solvate form, wherein: X is -R11-Ar-R2 or -Ra-Y; ar denotes a phenylene group optionally substituted by halogen, hydroxyl, C1-10 alkyl, (C1-10) alkoxy-(C1-10) alkyl, phenyl, C1-10 alkyl substituted by phenyl, C1-10 alkoxy substituted by phenyl, phenyl substituted by C1-10 alkyl, or phenyl substituted by C1-10 alkoxy; R1 and R2 are attached to the adjacent carbon atoms in Ar, and whether r1 is C1-10 alkylene and R2 is hydrogen, C1-10 alkyl, C1-10 alkoxy, or halogen, or R1 and R2, together with the carbon atoms in Ar with which they are attached, denote a 5, 6, or 7-membered cycloaliphatic ring; Ra is a C1-10 alkylene bond or optionally substituted by hydroxyl, C1-10 alkoxy, C6-10 aryl, or c7-14 aralkyl; and Y is C1-10 alkyl, C1-10 alkoxy, C2-10 alkenyl, or C2-10 alkynyl optionally substituted by halogen, cyano, hydroxyl, C1-10 alkyl C1-10 alkoxy, or C1-10 haloalkyl; C3-10 cycloalkyl optionally fused with one or more benzene rings, and optionally substituted by C1-10 alkyl, C1-10 alkoxy, C3-10 cycloalkyl, C7-14 aralkyl, C7-14 aralkyloxy, or C6-10 aryl, in wherein C3-10 cycloalkyl, C7-14 aralkyl, C7-14 aralkyloxy, or C6-10 aryl are optionally substituted by halogen, hydroxyl, C1-10 alkyl, C1-10 alkoxy, or C1-10 haloalkyl; C6-10 aryl optionally substituted by halogen, hydroxyl, C1-10 alkyl, C1-10 alkoxy, C1-10 haloalkyl, phenoxy, C1-10 thioalkyl, C6-10 aryl, a 4 to 10 membered heterocyclic ring having at least a nitrogen, oxygen or sulfur atom in the ring, or by NRbRc, wherein Rb and Rc are each independently C1-10 alkyl optionally substituted by hydroxyl, C1-10 alkoxy, or phenyl, or Rb may additionally be hydrogen; phenoxy optionally substituted by C1-10 alkyl, C1-10 alkoxy, or by phenyl optionally substituted by C1-10 alkyl or C1-10 alkoxy; a 4- to 10-membered heterocyclic ring having at least one nitrogen, oxygen or sulfur atom in the ring, this heterocyclic ring being optionally substituted by halogen, C1-10 alkyl, C1-10 alkoxy, C1-10 haloalkyl, C6 aryl -10, C7-14 aralkyl, C7-14 aralkyloxy, (C1-10) alkoxycarbonyl, or 4-10 membered heterocyclyl-(C1-10) alkyl; -NRdRe, where Rd is hydrogen or C1-10 alkyl, and Re is C1-10 alkyl optionally substituted by hydroxyl, or Re is C6-10 aryl optionally substituted by halogen, or Re is a 4 to 10 membered heterocyclic ring which it has at least one nitrogen, oxygen or sulfur atom in the ring, whose ring is optionally substituted by halogen-substituted phenyl, or Re is aryl (C6-10) -sulfonyl optionally substituted by (C1-10) -amino or di (C1-10 alkyl) amino; -SRf, wherein Rf is C6-10 aryl or C7-14 aralkyl optionally substituted by halogen, C1-10 alkyl, C1-10 alkoxy, or C1-10 haloalkyl; or -CONHRg, wherein Rg is C1-10 alkyl, C3-10 cycloalkyl, or C6-10 aryl. Claim 14: A process for the preparation of a compound of the formula (1) as claimed in claim 1, which comprises: (i) either (A) reacting a compound of the formula (2): wherein X is as defined in claim 1, and R7 denotes a protecting group, to replace R7 with hydrogen, or (B) reacting a compound of the formula (3): wherein X and R7 are as defined above in the present, and R8 and R9 each independently denote a protecting group, to convert the groups R7, R8, and R9 to hydrogen; and (ii) recovering the compound of the formula (1) in free or salt or solvate form. |
| priorityDate | 2002-08-09-04:00^^<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: 58.