Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-05-21
2004-02-03
Owen, Amelia (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S231500, C514S443000, C549S053000, C549S295000, C544S152000
Reexamination Certificate
active
06686390
ABSTRACT:
FIELD OF INVENTION
The present invention relates to novel anti-inflammatory compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
wherein R
1
represents amino or substituted or unsubstituted groups selected from alkyl, alkylamino, acylamino, cycloalkyl, cyclicamino, carboethoxycarbonylalkyl, hydrazino, hydrazido, aminoacid residue, aryl, heteroaryl or —N═CR(NR)
2
where R represents hydrogen or lower alkyl group; R
2
represents halogen, hydroxy, cyano, nitro, azido, formyl, oximealkyl, thio or substituted or unsubstituted groups selected from amino, alkyl, alkoxy, hydrazino, hydrazinoalkyl, hydrazido, hydrazidoalkyl, aminoacid residue, aminoacid residuealkyl, acyl, carbonyloxyalkyl, haloalkyl, aminoalkyl, haloalkoxy, hydroxyalkyl, alkoxyalkyl, thioalkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, aryl, aralkyl, aryloxy, aralkoxy, aryloxyalkyl, aralkoxyalkyl, carboxamidoalkyl, carbonylaminoalkyl groups or when the groups —S(═O)
m
—R
1
and R
2
are present on adjacent carbon atoms, R
1
and R
2
together with atoms to which they are attached may also form a substituted or unsubstituted 5-7 membered cyclic structure containing carbon atoms, a sulfur atom and may optionally contain one or two heteroatoms selected from O, S or N; R
3
represents hydrogen, halogen atom, hydroxy, nitro, cyano, azido or substituted or unsubstituted groups selected from hydrazino, hydrazinoalkyl, hydrazido, hydrazidoalkyl, aminoacid residues, alkyl, alkoxy, hydroxyalkyl, alkoxyalkyl, acylamino or amino groups; R
4
and R
5
may be same or different and independently represent hydrogen, halogen, hydroxy, cyano, nitro, thio, hydroxylamino, substituted or unsubstituted groups selected from alkyl, alkoxy, acyl, acyloxy, amino, hydrazino, hydrazinoalkyl, hydrazido, hydrazidoalkyl, aminoacid residues, aminoacyl, carboxyalkyl, carboxyalkenyl, aryl, aryloxy, aralkyl, aralkoxy, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, heteroaryl, heteroaryloxy, heteroaralkyl, heteroaralkoxy, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroaralkylcarbonyl, heteroaralkoxycarbonyl, heterocyclylcarbonyl, aminocarbonyl, aminocarbonylalkyl, carbonylamino, cycloalkylacylamino, alkylaminoalkoxy, alkylaminoacyl, carboxylic acid or its derivatives, saturated or partially saturated or aromatic single or fused 5 to 7 membered carbocycle ring or saturated or partially saturated or aromatic, single or fused 5 to 7 membered heterocycle ring; R
6
represents hydrogen, halogen, hydroxy, amino, cyano, nitro, thio, hydroxylamino or unsubstituted or substituted groups selected from alkyl, alkoxy, carboxyalkyl; the furanone ring may be fused with R
4
wherever possible; R
5
and R
6
together may represent ═C(R
a
)(R
b
), where R
a
and R
b
may be same or different and independently represent hydrogen, substituted or unsubstituted (C
1
-C
6
)alkyl or aryl; ═O or ═NR
7
where R
7
represents hydrogen, aryl or heteroaryl group; X represents oxygen or NR
8
, where R
8
represents hydrogen or substituted or unsubstituted groups selected from (C
1
-C
6
)alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, aralkenoyl, aralkanoyl and m is an integer in the range of 0-2.
The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
The present invention also relates to novel intermediates, process for their preparation and their use in the preparation of compounds of formula (I).
The compounds of general formula (I) are useful as antiinflammatory, analgesic, antipyretic, antiarthritic, antibacterial, anticancer agents or for treating Alzheimer diseases. The compounds of the present invention are also useful for the treatment of diseases of human or animals such as pain, fever or inflammation. Compounds of formula (I) also inhibit prostanoid-induced smooth muscle contraction by preventing the synthesis of contractile prostanoids and hence may be of use in the treatment of dysmenorrhea, premature labor and asthma. The compounds of the present invention are useful for treatment of pain, fever, and inflammation related to common cold, influenza, viral infections. The compounds of the present invention can be used for the treatment of arthritis such as rheumatoid arthritis, osteoarthritis, gouty arthritis, juvenile arthritis, spondylo arthritis; systemic lupus erythematosus, skin inflammation disorders such as eczema, burns, dermatitis, psoriasis; low back and neck pain, head ache, tooth ache, sprains, strains, myostis, neuralgia, synovitis, bursitis, tendinitis, injuries following surgical and dental procedures, post-operative inflammation including ophthalmic surgery such as cataract and refractive surgery.
The compounds of general formula (I) are also useful for the treatment of dysmenorrhoea, premature labour, asthma and bronchitis, gastrointestinal conditions such as inflammatory bowel disease, Crohn's disease, gastritis, irritable bowel syndrome, ulcerative colitis, diverticulitis, regional enteritis, peptic ulcers. These compounds may also be useful for treating inflammation in diseases such as vascular diseases, migraine head aches, periarteritis nodosa, thyroiditis, aplastic anemia, Behcat's syndrome, Hodgkin's diseases, scleroderma, myasthenia gravies, sarcoidosis, nephrotic syndrome, Type I diabetes, polymyositis, conjunctivitis, gingivitis, myocardial ischaemia, nephritis, swelling after injury, hypersensitivity and the like. The compounds of the present inventions are useful in the treatment of allergic rhinitis, respiratory distress syndrome, endotoxin shock syndrome, atherosclerosis, and central nervous system damage resulting from stroke, ischaemia and trauma; pulmonary inflammation such as in the case of viral infections and cystic fibrosis; ophthalmic diseases such as retinitis, retinopathy, uveitis, ocular photophobia and acute injury to eye tissues. The compounds of general formula (I) are also useful for treating central nervous system disorders such as cortical dementia (Alzheimer's diseases), useful for treatment of pain not limited to dental pain, muscular pain, pain from cancer, postoperative pain, and useful for the treatment of diseases where NSAIDS are used with the benefit of having significantly less side effects.
The compounds of general formula (I) are cyclooxygenase inhibitors and are therefore useful to treat the cyclooxygenase mediated diseases. The compounds of formula (I) are also useful for the treatment of mammals not limited to human beings such as horses, dogs, cats, sheep, pigs etc., and also for treating rats, mice, rabbits etc. The compounds of formula (I) may also be used in cotherapies for inflammation, Alzheimer's disease or cancer, in place of, or together with the conventional therapies.
The compounds of the general formula (I) are useful as partial or complete substitute for NSAIDS in compositions or preparations wherein they are presently coadministered with other agents or ingredients. The present invention also comprises pharmaceutical compositions for treating cyclooxygenase mediated diseases as defined earlier, comprising a non-toxic therapeutically effective amount of the compound of formula (I) as defined above and pharmaceutically acceptable carrier optionally containing one or more i
Casturi Seshagiri Rao
Mamnoor Prem Kumar
Misra Parimal
Pal Manojit
Ramanujam Rajagopalan
Dr. Reddy's Laboratories Limited
Ladas & Parry
Owen Amelia
LandOfFree
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