http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-074387-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b735f147a8c094f1c87c78a18cd69428 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-422 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-20 |
| filingDate | 2009-11-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a72de13292aa90af99b92a40db77b7c7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b5d84e032ab29258a23403804b145fe8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_30f2b899b706a79c4c666c3c7c202326 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_23e63e167a0fce05ec03a597a2063df1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d8f9ffcaeb320e07f837a0db1af9de26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7f375af9338556cee53dfe619377f037 |
| publicationDate | 2011-01-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-074387-A1 |
| titleOfInvention | AN ANTIMICROBIAL COMPOUND, A PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUND, A METHOD FOR MANAGING SUCH COMPOUND AND ITS USES |
| abstract | Processes for the synthesis of compounds or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, their salts or solvates; Pharmaceutical compositions comprising compounds of the formula (1) and methods for their use. The compounds herein are useful as effective antimicrobial agents against a number of Gram-positive and / or Gram-negative aerobic and / or anaerobic pathogens, such as Streptococcus, Enterococcus, Bacterioid, Clostridium, H influenzae, Moraxella multi-resistant species drugs; acid resistant organisms such as Mycobacterium tuberculosis, as well as species of Staphylococcus and Enterococcus resistant to Linezolid. Claim 1: A compound of the formula (1) its pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including the R and S isomers, polymorphs, prodrugs, metabolites, their salts or solvates, wherein the dotted line is independently a single bond or is absent ; when the dotted line is a simple bond, "A" represents the carbon atom and when the dotted line is absent, "A" is CH or N; Y and Y1 are the same or different and independently represent O or S; R1 and R2 are the same or different and independently represent hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C1-12 alkoxy, haloalkoxy C1-12, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl, C3-20 cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, heteroaryl- (CH2) n-, - (CH2) nC (= Y) NR5R6, - (CH2) nC (= Y) OR5, - (CH2) n- NR5R6, - (CH2) n-OC (= Y) R5, - (CH2) n-OC (= Y) OR5, - (CH2) n-NOC (= Y) NR5R6, - (CH2) nN (R5) C (= Y) OR6, - (CH2) nN (R5) C (= Y) NR5R6, - (CH2) nN (R5) C (= Y) R6, - (CH2) nN (R5) C (= Y) R5 , - (CH2) n-YR5 (in which each methylene group can be substituted by one or more halogen atoms), -C (= Y) NR5R6, -OC (= Y) R5, -OC (= Y) NR5R6, -C (= Y) OR5, -OR5, -OC (= Y) OR5, -SR5, -NO2, -NR5R6, -N (R5) C (= Y) R6, -N (R5) -C ( = Y) OR5, or -N (R5) C (= Y) NR5R6, each of which may optionally be substituted in any available position by one or more Ra substituents; or R1 and R2 may together with the carbon atom to which they are attached form a 3- to 10-membered, partially unsaturated or saturated monocyclic ring that may contain one to three heteroatoms independently selected from O, S or N; the ring thus formed can be fused with one or two rings independently selected from the group comprising an aryl ring, a cycloalkyl ring, a heterocyclyl ring or a monocyclic heteroaryl ring, the ring so formed optionally can be substituted in any position available by one or more Ra substituents; R3 represents hydrogen, C1-12 alkyl, C1-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxy C1-6-C1-3 alkyl, C3-20 cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, heteroaryl- (CH2) n-, - (CH2) n-YR5, - (CH2) nC (= Y) R5, - (CH2) n-NR5R6, - (CH2) nC (= Y) NR5R6, - (CH2) nC (= Y) OR5, - (CH2) n-OC (= Y) R5, - (CH2) n-OC (= Y) OR5, - (CH2) nN (R5) C (= Y) R6, - (CH2) nN (R5 ) C (= Y) OR6, - (CH2) nN (R5) C (= Y) NR5R6, - (CH2) n-OC (= Y) NR5R6, - (CH2) nN (R5) C (= Y) R6 , (where each methylene group may be substituted by one or more halogen atoms), each of which may be optionally substituted at any available position by one or more Ra substituents; R4 represents hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C1-12 haloalkoxy, C1-6 alkoxy-C1-6 alkyl , C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl, C3-20 cycloalkyl, heterocyclyl, aryl, heteroaryl, -C (= Y) NR5R6, -C (= Y) OR5, -NR5R6, -NR5C (= Y) R6, -C (= Y) R5, -O (C = Y) R5, -OC (= Y) OR5, -OC (= Y) NR5R6, -OR5, - (CH2) n-OR5, -SR5 , -NO2, -N (R5) C (= Y) OR6, or -N (R5) C (= Y) NR5R6, each of which may optionally be substituted in any available position by one or more Ra substituents; Z represents C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C1-12 alkoxy, C1-12 haloalkoxy, C1-6 alkoxy-C1- 6, C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl ,, -C3-20 cycloalkyl, heterocyclyl, aryl, heteroaryl, n-cycloalkyl- (CH2) n-, n-heterocyclyl- (CH2) n-, n-aryl- (CH2) n-, n-heteroaryl- (CH2) n-, N3- (CH2) n-, n-NCS- (CH2) n-, -C (= Y) R5, -C (= Y) OR6, -C (= Y) NR5R6, -OC (= Y) OR5, - (CH2) n-YR5, - (CH2) n-OP (= O) R5R6, - (CH2) n-NHP (= O) R5R6, - (CH2) n-OC (= Y) R5, - (CH2) n-OC (= Y) OR5, - (CH2) nC (= Y) R5, - (CH2) nC (= Y) NR5R6, - (CH2) n-OC (= Y) NR5R6, - (CH2) nC (= Y) OR5, - (CH2) n-NR5R6, - (CH2) n-NR5C (= Y) R6, - (CH2 ) n-NR5C (= Y) OR6, - (CH2) n-NR5C (= Y) NR5R6, - (CH2) n-NR5S (O) dR6, (in which each methylene group can be replaced by one or more halogen atoms), each of which may optionally be substituted in any available position by one or more Ra substituents; T, U V and W are the same or different and independently represent hydrogen or halogen; R5 and R6 with the same or different and are independently selected from hydrogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C3-8 cycloalkyl, heterocyclyl , aryl, heteroaryl, aryloxy, cycloalkyl- (CH2) n-, n-heterocyclyl- (CH2) n-, n-aryl- (CH2) n-, n-heteroaryl- (CH2) n-, each of which it can optionally be substituted in any available position with halogen, hydroxyl, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 alkoxy, C1-12 alkylcarbonyl, C1-12 alkoxycarbonyl, C3-8 cycloalkyl, C1 haloalkyl -12, C1-12 haloalkoxy, C2-12 haloalkenyl, aryl, heterocyclyl, heteroaryl, aryl- (CH2) n-, heterocyclyl- (CH2) n-, heteroaryl- (CH2) n-, cycloalkyl- (CH2) n- , -CN, -OR7, -NO2, -NR7R8, -N (R7) C (= Y) R8, -N (R7) C (= Y) OR8, -N (R7) C (= Y) NR7R8, - C (= Y) R7, -C (= Y) NR7R8, -OC (= Y) R7, -OC (= Y) NR7R8, -C (= Y) OR7, -OC (= Y) OR7, -sR7, -S (O) dR7, -SO2NR7R8, -NR7SO2R8, -OP (= O) R7R8, -NHP (= O) R7R8, or -P (= O) R7R8, or R5 and R6 are p they can be joined together with the heteroatom to which they are attached to form a heterocyclic ring or a heteroaryl ring that can also contain one to three heteroatoms independently selected from O, S or N, the optionally formed ring can be substituted with one or more selected substituents hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C1-12 alkoxy, C1-12 haloalkoxy, C1-6 alkoxy C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl ,, C3-8 cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, heteroaryl- (CH2) n-, C1-12 alkylcarbonyl, C1-12 alkoxycarbonyl, -CN, -OR7, -CF3, -OCF3, -CH2CF3, -CF2CF3, -NO2, -NR7R8, -N (R7) C (= Y) R8, -N (R7) C (= Y) OR8, -N (R7) C (= Y) NR7R8, -C (= Y) R7, -C (= Y) NR7R8, -OC (= Y) R7, -OC (= Y) NR7R8, -OC (= Y) OR7, -C (= Y) OR7, -SR7, -S (O) dR7, -SO2NR7R8, -NR7SO2R8, -OP (= O) R7R8, -NHP (= O) R7R8, or -P (O) R7R8, the ring as formed can also be fused with saturated or unsaturated rings of 3 to 7 members, which can contain from one to three heteroatoms independently selected from O, S or N, the optionally formed ring can be substituted in any available position by one or more substituents Ra ; Ra is independently selected from hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, oxo, C1-12 alkoxy, C1 alkoxy -6-C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl ,, C1-12 haloalkoxy, C3-8 cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, heteroaryl- (CH2) n-, C1-12 alkylcarbonyl, C1-12 alkoxycarbonyl, -CN, -YR7, - (CH2) n-YR7, -NO2, = NOR7, -NR7R8, -N (R7) C (= Y) R8, -N (R7) C (= Y) OR8, -N (R7) C (= Y) NR7R8, -C (= Y) R7, - C (= Y) NR7R8, -OC (= Y) R7, -OC (= Y) NR7R8, -C (= Y) OR7, -OC (= Y) OR7, -SR7, -S (O) dR7, - SO2NR7R8, -OP (= O) R7R8, -NHP (= O) R7R8, - (CH2) n-CN, -YR7, - (CH2) n-YR7, -NO2, = NOR7, - (CH2) n-NR7R8 , - (CH2) n-NR7C (= Y) R8, - (CH2) n-NR7C (= Y) OR8, - (CH2) n-NR7C (= Y) NR7R8, - (CH2) nC (= Y) R7 , - (CH2) nC (= Y) NR7R8, - (CH2) n-OC (= Y) R7, - (CH2) n-OC (= Y) NR7R8, - (CH2) nC (= Y) OR7, - (CH2) n-OC (= Y) OR7, - (CH2) n-SR7, - (CH2) nS (O) dR7, - (CH2) n-SO2NR7R8, - (CH2) n-OP (= O) R7R8 , - (CH2) n-NHP (= O) R7R8, or - (CH2) n-P (O) R7R8; each of which may optionally be substituted in any available position by one or more substituents selected from hydrogen, halogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, haloalkynyl C2-12, oxo, C1-12 alkoxy, C1-12 haloalkoxy, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy-C1-3 alkyl ,, C3-8 cycloalkyl, heterocyclyl, aryl , heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, heteroaryl- (CH2) n-, C1-12 alkylcarbonyl, C1-12 alkoxycarbonyl, -CN, -OR9 , - (CH2) NOR9, -CF3, -NO2, -NR9R10, -N (R9) C (= Y) R10, -N (R9) C (= Y) OR10, -N (R9) C (= Y) NR9R10, -C (= Y) R9, -C (= Y) NR9R10, -OC (= Y) R9, -OC (= Y) NR9R10, -OC (= Y) OR9, -C (= Y) OR9, -SR9, -S (O) dR9, -SO2NR9R10, -NR9SO2R10, -OP (= O) R9R10, -NHP (= O) R9R10, -P (O) R9R10, - (CH2) n-CN, -OR9, - (CH2) n-OR9, -CF3, -NO2, - (CH2) n-NR9R10, - (CH2) n-NR9C (= Y) R10, - (CH2) n-NR9C (= Y) OR10, - ( CH2) n-NR9C (= Y) NR9R10, - (CH2) nC (= Y) R9, - (CH2) nC (= Y) NR9R10, - (CH2) n-OC (= Y) R9, - (CH2) n-OC (= Y) NR9R1 0, - (CH2) n-OC (= Y) OR9, - (CH2) nC (= Y) OR9, - (CH2) n-SR9, - (CH2) nS (O) dR9, - (CH2) n- SO2NR9R10, - (CH2) n-NR9S (O) 2R10, - (CH2) n-OP (= O) R9R10, - (CH2) n-NHP (= O) R9R10, or - (CH2) nP (O) R9R10 ; R7 and R8 are independently selected from hydrogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C1-12 haloalkyl, C2-12 haloalkenyl, C2-12 haloalkynyl, C3-8 cycloalkyl, heterocyclyl, aryl, heteroaryl, cycloalkyl- (CH2) n-, heterocyclyl- (CH2) n-, aryl- (CH2) n-, or heteroaryl- (CH2) n-, each of which can be optional |
| priorityDate | 2008-11-20-04:00^^<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: 33.