- COMPOSITIONS AND METHODS FOR THE TREATMENT OF SEVERE PAIN
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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 severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic pain, generalized pain disorders, leukemia, cancer, chronic pain, chemotherapy induced pain, epilepsy, migraine, neuropathic pain, post herpetic neuralgia, neuralgia, pain, drug addiction, detoxification of drugs, Alzheimer's disease, 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.
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Paragraph 00104
(2013/12/03)
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- Considerations to the synthesis of methadone-nitrile as well as isomethadone-nitrile, and related compounds
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The 2-chloro-1-dialkylamino-propanes 4a-d are reacted with diphenylacetonitrile under phase transfer conditions to give a mixture of the nitriles la-d and 2a-d. Both chloro-dialkylamino-1-phenyl-ethanes 7a-d and 8a-d lead to 4-dialkylamino-2,2,3-triphenyl-butyronitriles 6a-d.
- Unterhalt,Coesfeld
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p. 229 - 234
(2007/10/03)
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- Aminoalkyl substituted urea derivatives and method of treatment
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The present invention relates to novel amino alkyl substituted urea derivatives as well as their acid addition salts with pharmaceutically acceptable acids, to methods for the preparation of said derivatives and pharmaceutical compositions containing same, and a method for the treatment of tumors therewith. The novel urea derivatives have shown pronounced anti-neoplastic activity when tested against various tumor models in animals. The novel compounds of the present invention may be represented by the following formula: STR1 wherein X and Y are the same or different and are selected from the group consisting of a phenyl group, each of said phenyl groups being optionally substituted with one or two groups selected from halogen, CF3, OH, or alkoxy (1-4 C-atoms); and R1 and R2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring; R3 and R4 are each selected from hydrogen, lower alkyl or alkenyl groups with from 1-6 carbon atoms inclusive, cyclopentyl or cyclohexyl; and n is 0 or 1, as well as pharmaceutically acceptable acid addition salts thereof. When X is different from Y and/or R3 is different from R4 the compounds of Formula I exist as optical isomers, which may be separated in the individual enantiomers, which often show the activity in different degree. These individual isomers as well as their isolation fall within the scope of the present invention.
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- Synthesis and anticonvulsant screening of 3,3-diphenyl-2-pyrrolidone derivatives
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Six derivatives of 3,3-diphenyl-2-pyrrolidone were synthesized and screened for anticonvulsant activity. The synthetic route involved a mono-N-demethylation of an intermediate N,N-dimethylaminonitrile with methyl chloroformate followed by cleavage of the carbamate group. Of the six derivatives, (±)-2-imino-1,5-dimethyl-3,3-diphenylpyrrolidine hydrochloride was effective in protecting mice against maximal electroshock (MES)-induced seizures at a 30-mg/kg dose level.
- Brine,Boldt
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p. 700 - 702
(2007/10/02)
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- Process for the preparation of 2,2-diphenyl-4-(dimethylamino)-pentane nitrile
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A process for the preparation of 2,2-diphenyl-4-(dimethylamino)-pentane nitrile. A charge mixture is prepared comprising diphenylacetonitrile, 1-(dimethylamino)-2-halopropane, a base, water, a water-immiscible organic solvent, and a quaternary salt selected from a group consisting of tetrabutylammonium halides, tetrabutylammonium hydrogen sulfate, cetyltrimethylammonium halides, benzyltriphenylphosphonium halides, and methyltrialkyl (C8 -C10) ammonium halides. The mixture is heated under an inert atmosphere to effect formation of 2,2-diphenyl-4-(dimethylamino)-pentane nitrile by reaction of diphenylacetonitrile, 1-(dimethylamino)-2-halopropane and a base.
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- Modification of methadone synthesis process step
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Alkylation of diphenylacetonitrile in methadone synthesis is carried out in presence of sodium hydroxide and DMF.
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