- COMPOSITIONS AND METHODS FOR THE TREATMENT OF MODERATE TO SEVERE PAIN
-
The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.
- -
-
-
- COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION
-
The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of inflammation may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of Type II diabetes, Type I diabetes, insulin resistance, cardiovascular disease, arrhythmia, atherosclerosis, coronary artery disease, hypertriglyceridemia, dyslipidemia, retinopathy, nephropathy, neuropathy, macular adema, arthritis, osteoarthritis, rheumatoid arthritis, inflammatory bowel syndrome, neudegeneration, Alzheimer's disease, Huntington's disease, Ulcerative colitis, Crohn's disease, Multiple Sclerosis, muscular dystropthy, metabolic syndrome, fatty liver, bone diseases, inflammatory diseases.
- -
-
Paragraph 0112; 0117; 0118
(2015/06/03)
-
- COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION
-
The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of inflammation may he formulated for oral buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of Type II diabetes, Type I diabetes, insulin resistance, cardiovascular disease, arrhythmia, atherosclerosis, coronary artery disease, hypertriglyceridemia, dyslipidemia, retinopathy, nephropathy, neuropathy, macular adema, arthritis, osteoarthritis, rheumatoid arthritis, inflammatory bowel syndrome, neudegeneration, Alzheimer's disease, Huntington's disease. Ulcerative colitis, Crohn's disease. Multiple Sclerosis, muscular dystropthy, metabolic syndrome, fatty liver, bone diseases, inflammatory diseases.
- -
-
-
- COMPOSITIONS AND METHODS FOR THE TREATMENT OF MODERATE TO SEVERE PAIN
-
The invention relates to the compounds of formula (I) and formula (II) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I) or formula (II), and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, severe pain, chronic pain, chemotherapy induced pain, epilepsy, glaucoma, arthritis, tooth aches, inflammation, musculoskeletal pain, sciatica, radiculopathy pain, migraine, neuropathic pain, post herpetic neuralgia, neuralgia pain, multiple sclerosis, multiple sclerosis, restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, amyotrophic lateral sclerosis (ALS), convulsions, partial seizures, mood-stabilizing agent and bipolar disorder.
- -
-
-
- 2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors
-
The CXC chemokine CXCL8/IL-8 plays a major role in the activation and recruitment of polymorphonuclear (PMN) cells at inflammatory sites. CXCL8 activates PMNs by binding the seven-transmembrane (7-TM) G-protein-coupled receptors CXC chemokine receptor 1 (CXCR1) and CXC chemokine receptor 2 (CXCR2). (R)-Ketoprofen (1) was previously reported to be a potent and specific noncompetitive inhibitor of CXCLS-induced human PMNs chemotaxis. We report here molecular modeling studies showing a putative interaction site of 1 in the TM region of CXCR1. The binding model was confirmed by alanine scanning mutagenesis and photoaffinity labeling experiments. The molecular model driven medicinal chemistry optimization of 1 led to a new class of potent and specific inhibitors of CXCL8 biological activity. Among these, repertaxin (13) was selected as a clinical candidate drug for prevention of post-ischemia reperfusion injury.
- Allegretti, Marcello,Bertini, Riccardo,Cesta, Maria Candida,Bizzarri, Cinzia,Di Bitondo, Rosa,Di Cioccio, Vito,Galliera, Emanuela,Berdini, Valerio,Topai, Alessandra,Zampella, Giuseppe,Russo, Vincenzo,Di Bello, Nicoletta,Nano, Giuseppe,Nicolini, Luca,Locati, Massimo,Fantucci, Piercarlo,Florio, Saverio,Colotta, Francesco
-
p. 4312 - 4331
(2007/10/03)
-
- Studies on anti-inflammatory drugs of 2-arylpropanoic acids: Part IX - A practical synthesis of ketoprofen by 1,2-aryl rearrangement
-
An efficient synthesis of ketoprofen via chloration, Friedel-Crafts acylation, reduction, coupling, ketalization, rearrangement, hydrolysis and oxidation from commercially available m-bromo-benzoic acid in overall yield of about 60% has been described.
- Chen, Fener,Liu, Jidong,Shao, Lanying,Yan, Qiongjiao
-
p. 989 - 992
(2007/10/03)
-
- Enantioselective syntheses of 2-arylpropanoic acid non-steroidal antiinflammatory drugs and related compounds
-
(S)-2-[4′-(2″-Methylpropyl)phenylpropanoic acid (ibuprofen) and (S)-2-(3′-benzoylphenyl)propanoic acid (ketoprofen) have been synthesised in high enantiomeric excess. Control of stereochemistry was achieved by a combination of Sharpless epoxidalion followed by catalytic hydrogenolysis of the introduced benzylic epoxide oxygen bond. Also, the coupling of organic compounds in the presence of palladium with enantiopure 2-(3-iodophenyl)propanoic and 2-(4-iodophenyl)propanoic acids, prepared by the methodology above, is a general method for the synthesis of optically active arylpropanoic acids.
- Hamon, David P.G.,Massy-Westropp, Ralph A.,Newton, Josephine L.
-
p. 12645 - 12660
(2007/10/02)
-
- Alternative syntheses of (S)-ketoprofen based on dimethyl L-tartrate
-
Two alternative asymmetric syntheses of (S)-ketoprofen, starting from 3-benzylpropiophenone or 3-propionylbenzophenone and dimethyl L-tartrate as chiral auxiliary, are described.
- Camps,Farres,Mauleon,Palomer,Carganico
-
p. 1739 - 1758
(2007/10/02)
-
- Synthesis of Arylpropanoic Acids From Optically Active 2-(Iodophenyl)propanoic Acids
-
The coupling of organozinc compounds with homochiral 2-(3-iodophenyl)propanoic and 2-(4-iodophenyl)propanoic acids in the presence of palladium is a general method for the synthesis of optically active arylpropanoic acids.
- Hamon, David P. G.,Massy-Westropp, Ralph A.,Newton, Josephine L.
-
p. 5333 - 5336
(2007/10/02)
-
- Process for preparing alpha-(3-benzylphenyl) propionic acid derivative
-
A process for preparing α-(3-benzylphenyl)-propionic acid or its derivative, a precursor of ketoprofen (trade name), which comprises dehydrogenating a by-product oil fraction formed in the production of ethylbenzene using synthetic zeolite as an alkylating catalyst, and carbonylating the product with carbon monoxide or the like. This precursor can be easily converted into ketoprofen, a useful medicine as an anti-inflammatory agent.
- -
-
-
- Method of preparing ketoprofen
-
A method of preparing ketoprofen by reacting aniline with a halide of an alpha-halogen propionic acid, benzylation of 3-methyl-2-indolinone, alkaline hydrolysis of 5-benzyl-3-methyl-2-indolinone, deamination of 2-(3-benzyl-6-aminophenyl)propionic acid and oxidation of 2-(3-benzylphenyl)propionic acid.
- -
-
-
- Process for preparing ketoprofen
-
A process for preparing ketoprofen by reacting aniline with a halide of an alpha-halogen propionic acid, benzylation of 3-methyl-2-indolinone, alkaline hydrolysis of 5-benzyl-3--methyl-2-indolinone, deamination of 2-(3-benzyl-6-aminophenyl)-propionic acid and oxidation of 2-(3-benzylphenyl)propionic acid.
- -
-
-
- ARENES FROM ALKANES OR CYCLOALKANES THROUGH DEHYDRATION OR REARRANGEMENT WITH PYRIDINIUM CHLORIDE
-
The preparations of various kinds of arylacetic acids both from the precursors and from the synthetic equivalents of (2-oxocyclohexenyl)acetic acids are reviewed.Particular attention is paid to the methods by which these intermediates can be obtained since the usefulness of the reaction is obviously bound to substrate availability.Further developments in the field of aromatic hydrocarbons and heterocyclic compounds are illustrated and a model for the reaction is proposed.In addition to the data already published in scientific journals and in the patent literature, several unpublished data are reported.
- Baiocchi, Leandro,Giannangeli, Marilena,Bonanomi, Michele,Picconi, Giuseppe,Ridolfi, Pietro
-
p. 199 - 216
(2007/10/02)
-
- alpha-Phenylpropionic Acid Derivatives. Synthesis and Dethiation of 5-Benzoylbenzothiophene-3-carboxylic Acid
-
The total synthesis of the title compound 8 started with p-thiocresol which was acylated with oxalyl chloride to give compound 1.This product underwent a condensation reaction with chloroacetic acid under basic conditions yielding compound 2.Two different synthetic pathways were used to convert compound 2 into the title compound 8.The first consisted in decarboxylation of 2 to 3, which was then converted to the ester 4, which was brominated and the product 5 was subjected to a Friedel-Craft's reaction with benzene.The resulting benzyl derivative 6 was oxidized to the benzoyl stage i.e. compound 7, which was finally hydrolyzed to 8.The second pathway was similar to the first one so that the steps of esterification, bromination, Friedel-Craft's alkylation and oxidation started with the dicarboxylic acid 2.Thus compounds 12-16 were obtained, and the last product was decarboxylated to 8.The yields in both procedures were similar.Finally, the dethiation of compound 8 with Raney nickel afforded compounds 18, 19 and 20.
- Hannoun, Mohammad,Blazevic, Nikola,Kolbah, Dragutin,Mihalic, Mladen,Kajfez, Franjo
-
p. 1131 - 1136
(2007/10/02)
-
- ENANTIOSELECTIVE SYNTHESIS AND ABSOLUTE CONFIGURATION OF (+)-α-(3-BENZOYLPHENYL)PROPIONIC ACID
-
Asymmetric homogeneous hydrogenation of α-(3-benzoylphenyl)acrylic acid (4), which is preparared in 90percent overall yield from (3-benzoylphenyl)acetic acid (1), affords (+)-α-(3-benzoylphenyl)propionic acid, (+)-5, in 93.7percent chemical and 67.4percent optical yield.The absolute configuration of (+)-5 is correlated with that of (+)-(S)-hydratropic acid via (+)-α-(3-benzylphenyl)propionic acid, (+)-6.The origin of the CD bands of (+)-6 is discussed and comparison of chiroptical data with those of (+)-(S)-hydratropic acid, reveals that (+)-6 has an S configuration.Since (+)-6 is chemically correlated with (+)-5, the absolute S configuration of this enantiomer is confirmed.
- Comisso, Giovanni,Mihalic, Mladen,Kajfez, Franjo,Sunjic, Vitomir,Snatzke, Guenther
-
p. 123 - 128
(2007/10/02)
-