Abstract: The present Invention relates to pharmaceutical compositions of (3S, 11aR)-N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

Abstract: The present invention is in relation to preparation of Imipramine Pamoate by a simple two-step process. The process provides new form of Imipramine Pamoate. The present invention is cost effective, involves mild conditions to beget said compound.

Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

Abstract: The present invention relates to a pharmaceutical composition for treating, preventing or improving premature ejaculation, which is taken on demand prior to sexual activity, the composition comprising clomipramine hydrochloride in an amount of 14 to 16 mg, preferably about 15 mg, as an active ingredient. More preferably, the composition of the present invention further comprises pregelatinized starch and sodium starch glycolate. The pharmaceutical composition of the present invention can provide rapid onset of efficacy, reduce a dissolution (absorption) deviation according to the patient's gastrointestinal pH conditions and minimize side effects.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, and parasitic infections. The compounds are triphenyl methane analogs of imipramine blue and analogs thereof, as defined herein. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.

Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumours. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumours presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumour glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.

Abstract: An amorphous form of imipramine pamoate, morphologically pure forms, and mixtures of amorphous and morphologically pure imipramine pamoate characterized by differential scanning calorimetry, fourier transform infrared, and powder x-ray diffraction, and pharmaceutical compositions formed therefrom.

Abstract: The disclosure provides an antigenic composition useful for immunization against P. acnes, K. pneumoniae, S. aureus, or Streptococcus pyogenes. The disclosure provides a method for producing a vaccine for preventing infection and screening agents useful for preventing infection.

Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, h) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.

Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.

Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.

Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.

Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, and parasitic infections. The compounds are triphenyl methane analogs of imipramine blue and analogs thereof, as defined herein. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: Methods and small molecule compounds for stem cell differentiation are provided.

Abstract: An amorphous form of imipramine pamoate, morphologically pure forms, and mixtures of amorphous and morphologically pure imipramine pamoate characterized by differential scanning calorimetry, fourier transform infrared, and powder x-ray diffraction, and pharmaceutical compositions formed therefrom.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: The invention relates to pharmaceutically active compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention and particularly useful for the treatment or prophylaxis of diseases associated with parasitic infection such as pneumocystis pneumonia, toxoplasmosis, cryptosporidiosis, leischmaniasis and malaria.

Abstract: A compound having a general formula (II) wherein R1 is saturated or unsaturated alkyl, amino-alcohol, diamino, cycloalkyl, and C(?O)(CH2)nNR?R?, (CH2)nCHOHCH2NR?R?, wherein n is an integer, RQ, RT, R?, and R? are each independently a hydrogen, halogen, hydroxyl, saturated, unsaturated, aliphatic, or branched alkyl, substituted or unsubstituted (CH2)m-(hetero)aryl, and sulfonylamide; q and r are each an integer independently selected from 1-4; and pharmaceutically acceptable salts thereof, and the new therapeutic uses thereof and similar compounds as defibrillating, and/or anti-fibrillatory, and/or anti-arrhythmic and/or anti-ischemic drugs.

Abstract: Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.

Abstract: 5-Cyano-10-Hydroxy-10,11-Dihydro-5H-Dibenzi[b,f]azepine and the process for its preparation.

Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt th

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids andy esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: An aromatic tertiary amine compound of formula (I): ##STR1## wherein (A) and (B) are each a substituted or unsubstituted vinylene or o-arylene group; R.sup.1 to R.sup.4 are each a halogen atom, or a substituted or unsubstituted alkyl, aryl, alkoxy, aryloxy, dialkylamino, N-alkyl-N-arylamino or diarylamino group; R.sup.5 is a halogen atom, or a substituted or unsubstituted alkyl, alkoxy or dialkylamino group; h, i, j, k and l are each an integer of 0-4; and m is an integer of 1-6.

Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: The instant invention is directed to compounds, compositions and antipsychotic methods of use wherein the compounds are of formula I: ##STR1## wherein Y is an imide or benzoyl alkyl group and X is a cycloalkyl, phenyl or dibenzoazepinyl group.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: There are provided a hydrazone compound represented by formula (I), an electrophotographic photoreceptor which has a photosensitive layer containing the compound on an electrically conductive support, and an organic electroluminescent element containing the compound as a charge transporting material: ##STR1## wherein Ar.sub.1 represents a substituted or unsubstituted phenylene group, a substitued or unsubstituted naphthylene group, a substitued or unsubstituted biphenylene group, or a substituted or unsubstituted anthrylene group, Ar.sub.2 represents a substituted or unsubstituted aryl group, R.sub.1 and R.sub.2 each independently represents a hydrogen atom, a halogen atom, an unsubstituted alkyl group, or an unsubstituted alkoxy group, R.sub.3 represents an unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, Z represents an ethylene group or a vinylene group, and n is 0 or 1.

Abstract: Immunoassay methods and reagents for the specific quantification of amitriptyline or nortriptyline in a test sample are disclosed employing antibodies prepared with amitriptyline or nortriptyline derivatives of the Formula III: ##STR1## wherein for amitriptyline, R is CH.sub.3, and for nortriptyline, R is H. The present invention also describes the synthesis of unique fluorescein tracers of the structure of Formula IV and Formula V: ##STR2## wherein for a specific amitriptyline immunoassay, W.sub.1 is a heteroatom linked to the aromatic ring at the 2 or 3 position, and for a specific nortriptyline immunoassay, W.sub.2 is two heteroatoms linked together and attached to the aromatic ring at the 2 or 3 position, and wherein Q is a detectable moiety, preferably fluorescein or a fluorescein derivative.

Abstract: An improved method for preparing opipramol (I) is disclosed, wherein iminostilbene (II) is reacted with 1-bromo-3-chloropropane in the presence of a weak base selected from a hydrogen phosphate salt and an acetate salt and in the presence of a phase transfer agent to produce N-(3-halopropyl)iminostilbene (III), which is mixture of N-(3-chloropropyl)iminostilbene and N-(3-bromopropyl)iminostilbene, and then N-(3-halopropyl)iminostilbene is reacted with N-(2-hydroxyethyl)piperazine to form opipramol, as shown in the following equations, where X is chlorine or bromine.

Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Immunoassay methods and reagents for the specific quantification of imipramine or desipramine in a test sample are disclosed. The measurement of imipramine or desipramine is accomplished in a specific immunoassay employing antibodies prepared with imipramine or desipramine derivatives of the Formula III: ##STR1## wherein P is an immunogenic carrier material, X is two heteroatoms, Y is a linking group comprising from 1 to 6 carbon atoms and P is an immunogenic carrier material, and wherein for imipramine, R is CH.sub.3, and for desipramine, R is H.The present invention also describes the synthesis of unique labeled reagents of the structure of the Formula IV: ##STR2## wherein Z is a linking group comprising 1 to 4 carbon atoms and 0 to 2 heteroatoms and Q is a detectable moiety, preferably fluorescein or a fluorescein derivative, and wherein for imipramine, R.sub.1 is CH.sub.3, and for desipramine, R.sub.1 is H.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.

Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

Abstract: Novel bis-dibenzoazepine compounds useful in the treatment of malaria and drug-resistant malaria.

Abstract: N,N-(dibenzohexatrienylene)urea medicaments can be manufactured in a smooth one-step reaction by reacting a corresponding N,N-(dibenzohexatrienylene)amine with cyanic acid.

Abstract: Tricyclic antidepressant functionalized compounds are provided for conjugation through a side chain to antigenic compounds, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies and together with the enzyme conjugates find particular use in immunoassays for the determination or detection of the total amount of tricyclic antidepressants present in a sample.