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US 6,440,961 B1Granted
Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
AssigneesDr. Reddy's Research Foundation, Reddy-Cheminor, Inc.
InventorsBraj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Abstract
A compound of formula (1) it derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, processes for its preparation and methods of use thereof.
Claims78
A compound of formula (1)
- its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, wherein R1, R2, R3, and R4 may be same or different and represent hydrogen, halogen, hydroxy, nitro, cyano, formyl or unsubstituted or substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or its derivatives, or sulfonic acid or its derivatives;
- the ring A fused to the ring containing X and N represents a 5-6 membered cyclic structure containing carbon atoms, which optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms, which optionally may be substituted;
- the ring A is saturated or contains one or more double bonds or is an aromatic moiety;
- X represents a heteroatom selected from oxygen, or sulfur;
- Ar represents an unsubstituted or substituted divalent single or fused aromatic or heterocyclic group;
- R5 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl or unsubstituted or substituted aralkyl group or forms a bond together with the adjacent group R6;
- R6 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl group, acyl, or unsubstituted or substituted aralkyl or R6 forms a bond together with R5;
- R7 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- R8 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- Y represents oxygen or NR10, where R10 represents hydrogen, alkyl, aryl, hydroxyalkyl, aralkyl, heterocyclyl, heteroaryl or heteroaralkyl groups;
- R8 and R10 together form a 5 or 6 membered cyclic structure containing carbon atoms, which optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen;
- n is an integer ranging from 1-4 and m is an integer 0 or 1.
9 more elements
A compound which is selected from the group consisting of:
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid;
- Li Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxy2-methylpropanoic acid;
- Li Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2ethoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxy2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxy2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-phenoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[2-(Phenothiazin-10-yl)methylbenzofuran-5-yl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[2-(Phenothiazin-10-yl)methylbenzofuran-5-yl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[2-(Phenothiazin-10-yl)methylbenzofuran-5-yl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxy-2-methylpropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-butoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-butoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-butoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hexyloxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hexyloxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hexyloxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hydroxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hydroxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-hydroxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (±) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (+) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid;
- Li, Na, K, Mg, lysine, arginine, guanidine, diethanolamine, choline, ammonium, substituted ammonium salts or aluminium salts of (−) 3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-phenoxypropanoic acid.
36 more elements
(±)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof.
(+)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt polymorph or a solvate thereof.
(−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof.
(−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, arginine salt:
- and a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof.
(±)3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof.
A process for the preparation of compound of formula (III)
- its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, wherein R1, R2, R3, and R4 are same or different and represent hydrogen, halogen, hydroxy, nitro, cyano, formyl or unsubstituted or substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or its derivatives, or sulfonic acid or its derivatives;
- the ring A fused to the ring containing X and N represents a 5-6 membered cyclic structure containing carbon atoms, which optionally contains one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms, which optionally may be substituted;
- the ring A is saturated or contains one or more double bonds or is an aromatic moiety;
- X represents a heteroatom selected from oxygen, or sulfur;
- Ar represents an unsubstituted or substituted divalent single or fused aromatic or heterocyclic group;
- R7 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- R8 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- n is an integer ranging from 1-4 and m is an integer 0 or 1;
- which comprises:
- a) reacting a compound of the formula (IIIa)
- where all symbols are as defined above with a compound of formula (IIIb)
- where R7 and R8 are as defined above excluding hydrogen atom and R11 is a C1-C6)alkyl group to yield a compound of formula (III) defined above;
- or
- b) reacting a compound of the formula (IIIa)
- where all symbols are as defined above with Wittig reagents;
- or
- c) reacting a compound of the formula (IIIa)
- where all symbols are as defined above with a compound of formula (IIIc)
- where R6 represents hydrogen atom and R7, and R8 are as defined above to yield a compound of formula (III);
- or
- d) reacting a compound of formula (IIIe)
- where L1 represents a leaving group and all other symbols are as defined above with a compound of formula (IIId)
- where R7, R8 and Ar are as defined above to produce a compound of formula (III) where all symbols are as defined above;
- or
- e) reacting a compound of formula (IIIg)
- where all symbols are as defined above with a compound of formula (IIIf)
- where all symbols are as defined above and L1 is a leaving group to produce a compound of formula (III) defined above;
- or
- f) reacting a compound of formula (IIIh)
- where all symbols are as defined above with a compound of formula (IIId)
- where all symbols are as defined above to produce a compound of formula (III) defined above;
- or
- g) reacting a compound of formula (IIIi)
- where all symbols are as defined above with a compound of formula (IIIj)
- where R7=R8 and are as defined above excluding hydrogen to produce a compound of formula (III) and if desired converting the compounds of formula (III) obtained in any of the processes described above into a pharmaceutically acceptable salt, or pharmaceutically acceptable solvate.
32 more elements
A process for the preparation of compound of formula (I)
- its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, and its pharmaceutically acceptable solvates, wherein R1, R2, R3, and R4 are same or different and represent hydrogen, halogen, hydroxy, nitro, cyano, formyl or unsubstituted or substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or its derivatives, or sulfonic acid or its derivatives;
- the ring A fused to the ring containing X and N represents a 5-6 membered cyclic structure containing carbon atoms, which optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms, which optionally may be substituted;
- the ring A is saturated or contains one or more double bonds or is an aromatic moiety;
- X represents a heteroatom selected from oxygen, or sulfur;
- Ar represents an unsubstituted or substituted divalent single or fused aromatic or heterocyclic group;
- R5 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl or unsubstituted or substituted aralkyl group;
- R6 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl group, acyl, or unsubstituted or substituted aralkyl;
- R7 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- R8 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- Y represents oxygen;
- n is an integer ranging from 1-4 and m is an integer 0 or 1;
- which comprises:
- a) reducing a compound of formula (III)
- which represents a compound of formula (I) where R5 and R6 represent a bond and Y represents an oxygen atom and all other symbols are as defined above, to yield a compound of the formula (I) where R5 and R6 each represent hydrogen atom and all other symbols are as defined above;
- or
- b) reacting a compound of formula (Ia)
- where all symbols are as defined above, R8 is as defined above excluding hydrogen and L3 is a leaving group with an alcohol of formula (Ib)
- R7—OH (Ib)
- where R7 represents unsubstituted or substituted groups selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups to produce a compound of formula (I) where all symbols are as defined above;
- or
- c) reacting a compound of formula (IIe)
- wherein L1 is a leaving group and all other symbols are as defined above with a compound of formula (Ic)
- where all symbols are as defined above to produce a compound of formula (I) where all symbols are as defined above;
- or
- d) reacting a compound of formula (IIIh)
- where all symbols are defined above with a compound of formula (Ic)
- where all symbols are as defined above to produce a compound of formula (I) defined above;
- or
- e) reacting a compound of formula (Id)
- which represents a compound of formula (I), where R7 represents hydrogen atom and all other symbols are as defined above with a compound of formula (Ie)
- R7—Hal (Ie)
- where R7 represents unsubstituted or substituted groups selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups and Hal represents halogen atom to produce a compound of formula (I) where all symbols are as defined above;
- or
- f) reacting a compound of the formula (IIIa)
- where all symbols are as defined above with a compound of formula (IIIc)
- where R6 is hydrogen and R7, and R8 are as defined above to produce a compound of formula (I) where all symbols are as defined above;
- or
- g) reacting a compound of formula (IIIg)
- where all symbols are as defined above with a compound of formula (If)
- where L1 is a leaving group and all other symbols are as defined above to produce a compound of formula (I) where all symbols are as defined above;
- or
- h) converting a compound of formula of (Ig)
- where all symbols are defined above to a compound of formula (I) where all symbols are as defined above;
- or
- i) reacting a compound of formula (Ih)
- where R8 is as defined above excluding hydrogen and all other symbols are as defined above with a compound of formula (Ib)
- R7—OH (Ib)
- where R7 represents unsubstituted or substituted groups selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups to produce a compound of formula (I) where all symbols are as defined above and if desired converting a compound of formula (I) obtained in any of the processes described above into a pharmaceutically acceptable salt, or pharmaceutically acceptable solvate.
45 more elements
A process for the preparation of compound of formula (I)
- its derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, wherein R1, R2, R3, and R4 are same or different and represent hydrogen, halogen, hydroxy, nitro, cyano, formyl or unsubstituted or substituted groups selected from alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or its derivatives, or sulfonic acid or its derivatives;
- the ring A fused to the ring containing X and N represents a 5-6 membered cyclic structure containing carbon atoms, which optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms, which optionally may be substituted;
- the ring A is saturated or contains one or more double bonds or is an aromatic moiety;
- X represents a heteroatom selected from oxygen, or sulfur;
- Ar represents an unsubstituted or substituted divalent single or fused aromatic or heterocyclic group;
- R5 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl or unsubstituted or substituted aralkyl group or forms a bond together with the adjacent group R6;
- R6 represents hydrogen, hydroxy, alkoxy, halogen, lower alkyl group, acyl, or unsubstituted or substituted aralkyl or R6 forms a bond together with R5;
- R7 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- R8 represents hydrogen or unsubstituted or substituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups;
- Y represents NR10, where R10 represents hydrogen, alkyl, aryl, hydroxyalkyl, aralkyl, heterocyclyl, heteroaryl or heteroaralkyl groups;
- R8 and R10 together form a 5 or 6 membered cyclic structure containing carbon atoms, which optionally contain one or more heteroatoms selected from oxygen, sulfur or nitrogen;
- n is an integer ranging from 1-4 and m is an integer 0 or 1;
- which comprises reacting a compound of formula (I) where all the symbols are as defined above and Y represents oxygen, with appropriate amines of the formula NHR8R10, where R8 and R10 are as defined above and if needed converting the compound of formula (I) obtained above into a pharmaceutically acceptable salt, or a pharmaceutically acceptable solvate.
10 more elements
A pharmaceutical composition which comprises (±)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
A pharmaceutical composition which comprises (+)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
A pharmaceutical composition which comprises (−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
A pharmaceutical composition which comprises (−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, arginine salt:
- and a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
A pharmaceutical composition which comprises (±)3-[4-[2-(Phenothiazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid:
- or a tautomeric form, a stereoisomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof and a pharmaceutically acceptable carrier, diluent, excipient or solvate.
Dependencies are inferred from the claim text.