Abstract:
Compounds of general formula (I), wherein X is O, S or CR R ; each R and R is, independently, hydrogen or C1-C4 alkyl; Z is O, S or NR ; n is 0 or 1; Y is O, S, NR or CR R ; R is H, OH, CHO, NR R or C1-C10 hydrocarbyl, 0-(C1-C10 hydrocarbyl), either of which may be substituted with one orm ore substituents chosen from OR , COR , COOR , OCOR , CN, halogen, S(O)pR , NR R , NO2, NR COR , NR CONR R , CONR R or heterocyclyl; R , R and R are each, independently, hydrogen, C1-C6 hydrocarbyl or C1-C6 halohydrocarbyl; p is 0, 1 or 2; alternatively: when Y is NR or CR R , and: a) Z is NR ; or b) n is 0; the substituents of Y and Z or Y and R may together form a bridge represented by the formula -Q -Q - or -Q -Q -Q -, where Q , Q and Q each independently represent CR R , =CR , CO, NR , =N, O or S; each or R and R independently represents hydrogen, C1-C4 alkyl, OH or halogen; R represents hydrogen or C1-C4 alkyl; W is O or S; R is hydrogen or C1-C10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms; R and R are each independently hydrogen or C1-C4 alkyl; A is an aromatic or heteroaromatic ring system optionally substituted alternatively, two or more substituents of the group A may combine to form a fused 5- or 6-membered saturated or partially saturated carbocyclic or heterocyclic ring in which any carbon or quaternised nitrogen atom may be substituted with any of the groups mentioned above for A or in which a ring carbon atom may be part of a carbonyl group or a nitrogen atom may be oxidised.
Abstract translation:通式(I)的化合物,其中X是O,S或CR 4 R 5; 每个R 4和R 5独立地是氢或C 1 -C 4烷基; Z是O,S或NR 4; n为0或1; Y是O,S,NR 6或CR 4 R 5; R 6是H,OH,CHO,NR 16 R 17或C 1 -C 10烃基,O-(C 1 -C 10烃基),其中任一个可以被一个选自OR 16的取代基取代 ,COR 16,OCOR 16,CN,卤素,S(O)p R 16,NR 16 R 17,NO 2,NR 16 COR 17, NR 16 CONR 17 R 18,CONR 16 R 17或杂环基; R 16,R 17和R 18各自独立地为氢,C 1 -C 6烃基或C 1 -C 6卤代烃基; p为0,1或2; 或者:当Y是NR 6或CR 4 R 5时,和:a)Z是NR 4; 或b)n为0; Y和Z或Y和R 1的取代基可以一起形成由式-Q 1 -Q 2 - 或-Q 1 -Q 2 -Q 3 - 其中Q 1,Q 2和Q 3各自独立地表示CR 12 R 13,= CR 12,CO,NR 14,= N,O或S; 每个或R 12和R 13独立地表示氢,C 1 -C 4烷基,OH或卤素; R 14表示氢或C 1 -C 4烷基; W为O或S; R 1是氢或C 1 -C 10烃基或具有3至8个环原子的杂环基; R 2和R 3各自独立地为氢或C 1 -C 4烷基; A是任选地任选取代的芳族或杂芳族环系统,组A中的两个或多个取代基可以结合形成稠合的5或6元饱和或部分饱和的碳环或杂环,其中任何碳或季铵化氮原子可以是 被上述任何A取代或环碳原子可以是羰基或氮原子的一部分被氧化。
Abstract:
Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to Vl.
Abstract:
Novel compounds of general formula (I) wherein R1-R7 denote, in particular, a straight or branched hydrocarbon radical comprising 1-6 carbon atoms, Z is a straight or branched hydroxycarbon radical comprising 2-6 carbon atoms, a triple bond, a Z or E stereochemistry double bond (Z'CH=CHZ") in which Z' and Z", which are the same or different, are a hydrogen atom, a fluorine atom or a straight or branched hydrocarbon radical comprising 1-6 carbon atoms; n=0.1 or 2; X and X', which are the same or different, are O or NR'1, where R'1 is a hydrogen atom, a straight or branched hydroxycarbon radical comprising 1-5 carbon atoms, or a cycloalkyl radical comprising 3-7 carbon atoms; and Y = O,S.
Abstract:
The present invention relates to norketamine and ketamine/norketamine prodrugs, and methods of their use and analgesics. More particulary, the invention relates to norketamine and N-conjugated prodrugs of ketamine and norketamine, and methods of using these agents for the management of chronic pain without requiring administration of narcotics. The invemtion relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine and/or ketamine/norketamine prodrugs effective to alleviate pain to a subject suffering from pain.
Abstract:
The present invention relates to a polymerisable plasticiser formed by a hydrocarbon chain, one end of which bears more than one isocyanate function, said hydrocarbon chain comprising and/or being substituted by an aromatic ring and/or an aliphatic ring and/or said hydrocarbon chain is substituted by at least two hydrocarbon chains that can comprise an unsaturation, and the number of isocyanate functions being strictly greater than 1, preferably greater than 1.2, and, more preferably, grater than 1.5 but less than or equal to 2.2. The invention also relates to liquid polyurethane resin compositions and, in particular, stable, ready-to-use liquid polyurethane resin compositions comprising said plasticiser. The invention further relates to methods for replacing all or part of the exogenous plasticiser and/or solvent in a polyurethane resin by adding said polymerisable plasticiser.
Abstract:
La présente invention porte sur un plastifiant polymérisable constitué d'une chaîne hydrocarbonée dont une seule extrémité porte plus d'une fonction isocyanate, ladite chaîne hydrocarbonée comprenant et/ou étant substituée par un cycle aromatique et/ou un cycle aliphatique et/ou ladite chaîne hydrocarbonée est substituée par au moins deux chaînes hydrocarbonées pouvant comporter une insaturation, et le nombre de fonctions isocyanates étant strictement supérieur à 1, de préférence supérieur à 1,2, plus préférentiellement supérieur à 1,5 et inférieur ou égal à 2,2; sur des compositions de résine polyuréthane liquides, et notamment sur des compositions de résine polyuréthane liquides prêtes-à-l'emploi et stables, comprenant ledit plastifiant et sur des méthodes permettant de remplacer tout ou partie du solvant et/ou du plastifiant exogène d'une composition de résine polyuréthane par ajout dudit plastifiant polymérisable.
Abstract:
Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
Abstract:
There are provided according to the invention, novel compounds of formula (I) wherein R , R , R , R , R and R are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.