Abstract: Provided herein are methods, compositions, and kits for the treatment of an enteric nervous system disorder. Such methods may comprise administering to a subject an effective amount of a phenothiazine compound, a peripherally restricted dopamine decarboxylase inhibitor, and/or a peripherally restricted dopamine D2 receptor antagonist that does not substantially inhibit hERG channels.

Abstract: The invention disclosed herein is direct to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in treating neurodegenerative diseases and promoting the generation or survival of neurons in the mammalian brain. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to a method of promoting the generation or survival of neurons in a patient in need thereof in neurodegenerative and related diseases.

Abstract: A compound for an organic optoelectronic device is represented by the following Chemical Formula 1:

Abstract: The invention includes compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, treating diseases associated with activated lymphocytes, or treating PAH.

Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

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

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-14 or encompassed by formulas I-XII) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract: Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR1R2 ??(y1) -L-Z-R3 ??(y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR1R2; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO3M; —PO3M2; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR5]4+; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R1, R2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R3 is optionally substituted alkyl, (het)aryl; R? is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4,

Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: A compound of Formula (Ih) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.

Abstract: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like.

Abstract: A compound of Formula (Ig) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.

Abstract: According to the method of the present invention, an alkali metal compound, dimethyl sulfoxide, trimethyloxosulfonium halide and 3-quinuclidinone are added in a specific order to give the following compound [II]. This compound is, without treatment or isolation, directly reacted with an alkali metal salt of phenothiazine to give the following compound [III], from which the following compound [I] is obtained. During the production of compound [I], a by-produced acidic gas is removed and water is added to ensure industrial, safe and efficient production of compound [I] at a constantly high yield. Inasmuch as the present invention enables production of the following highly pure compound [A] by eliminating hydrogen halide of compound [I] in glyme in the presence of at least one kind of a base selected from potassium hydroxide and potassium alkoxide, compound [A] having a high purity of not less than 85 mol % can be provided.

Abstract: A compound of formula (I) ##STR1## its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates, wherein R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different; R.sup.1 and R.sup.2 together represent along with carbon atoms to which they are attached an aromatic cyclic structure containing 5-6 ring atoms which may optionally be substituted; X represents a heteroatom selected from oxygen or sulfur; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.

Abstract: The present invention relates to a novel brain cell protective agent having for its active ingredient a morphinan derivative represented with Compound 1 ##STR1## or pharmacologically acceptable acid addition salt thereof. The compounds used in the present invention were found to have excellent defensive effects against brain nerve cell necrosis in both in vitro and in vivo pharmacological evaluations, and can be used as useful preventive and therapeutic agents of ischemic brain disorders, brain nerve cell disorders and dementia.

Abstract: Novel .beta.-aryl-.alpha.-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. ##STR1## The compounds have hypolipidemic, antihyperglycemic uses.

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 carboxcylic acids of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the 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 the secretion and circulation of insulin antagonising peptides.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain 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: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.

Abstract: Disclosed is a novel oxazinone derivative represented by formula (I) given below or a pharmaceutically acceptable acid-addition salt thereof, which is useful as an anti-inflammatory agent, an agent for suppressing neutrophil infiltration and as a serine protease inhibitor: ##STR1## where A includes, for example, ##STR2## in which W is --O--, --S--, --CH.dbd.CH-- or --NR.sup.9 -- or means that (CH.sub.2).sub.n is directly bonded to (CH.sub.2).sub.n,V.sup.2 is .dbd.CR.sup.12 -- or .dbd.N--, andD is 5 to 7-membered carbon ring or hetero ring;X is --O--, --S--, --CO--, or --NR.sup.15 or means that A is directly bonded to (CH.sub.2).sub.l ;Y is --O--, --CH.dbd.CH-- or --NR.sup.16 -- or means that (CH.sub.2).sub.l is directly bonded to Z;Z is --CH.sub.2 -- or --CO--; andl is an integer of 0 to 4.Further, R and R.sup.1 to R.sup.16 are hydrogen atom, lower alkyl group, etc.

Abstract: New phenothiazine derivatives of general formula (I) in whichR represents 4- to 6-membered cycloalkyl, or represents --CH.sub.2 R" in which R" is hydrogen, alkyl containing 1 to 5 carbon atoms, alkenyl or alkynyl containing 2 to 4 carbon atoms, cycloalkyl (3- to 6-membered), phenyl, optionally substituted (with 1 or 2 halogen atoms or with a hydroxyl, alkyl, alkyloxy, trifluoromethyl or nitro radical) or heterocyclic selected from furyl, thienyl or pyridyl, andR' either represents a radical of general formula (IIa) in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, cycloalkylalkyl, hydroxyalkyl or acetyloxyalkyl or, together with the nitrogen atom to which they are attached, form a saturated or partially unsaturated 4- to 7-membered heterocycle optionally substituted with 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, andR.sub.

Abstract: This invention describes compositions containing nitrogen, sulfur and optionally oxygen which are useful as antioxidants for lubricants.

Abstract: 1-[(phenothiazin-10-yl)alkyl]-.alpha.-phenyl-4-piperidinemethanols and methods for treating pain or psychosis utilizing compounds or compositions thereof are disclosed.

Abstract: This invention relates to 1-[n-(2-alkylthio-10H-phenothiazin-10-yl)alkyl]-4-benzoylpiperidines and methods for treating pain or psychosis utilizing compounds or compositions thereof.

Abstract: Alkoxyalkyl and alkylmercaptoalkyl substituted bridged benzofuroisoquinolines have opioid antagonist, and/or appetite-controlling properties. Preferred compounds are kappa receptor selective antagonists. Examples of such preferred compounds are 5-Methoxymethyl-3-n-propyl- 1,2,3,4,5,6,7,7a-octahydro-4a,7-ethanobenzofuro[3,2-e]isoquinolin-9-ol and 3-Cyclopropylmethyl-5-methoxymethyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano benzofuro[3,2-e]isoquinoline-9-ol.

Abstract: The present invention relates to compounds of the formula (I): ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is a C.sub.1-7 bivalent aliphatic hydrocarbon group or a single bond;R.sub.2 and R.sub.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members;R.sup.4 is hydrogen, halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl optionally substituted by one to three halogen atoms; or a group R.sub.1 CO.sub.2 H as hereinbefore defined; andA is C.sub.1-4 alkylene or ANR.sub.2 R.sub.3 forms a group --CH.sub.2 --(CH.sub.2).sub.2 or CH.sub.2 --(CH.sub.2).sub.2B is an acidic group other than a mono-carboxylic acid group of comparable or greater acid strength than a carboxylic acid group in a similar chemical environment, provided that any sulphonamide group contains at least one N-H bond.

Abstract: New phenothiazine derivatives having the general formula: ##STR1## wherein R represents a straight or branched alkyl group or alkenyl group having 5-15 carbon atoms, their acid addition salts and anti-psychotic drugs containing such new compounds.

Abstract: Unsaturated heterocyclic dihydropyridines of the formula: ##STR1## wherein the substituents defined herein have been found to have useful antihypertensive activity.

Abstract: New phenothiazine derivatives having the general formula: ##STR1## wherein R represents hydrogen atom or a lower alkyl group, and A represents a lower alkylene group, and process for the production thereof. The phenothiazine derivatives have remarkable activities against the central nervous system, and are useful as psychotropic drugs.

Abstract: N-(4-Amino-2-butynyl)imides are prepared from N-propargylimides, paraformaldehyde and the appropriate secondary amine. The compounds are useful as stimulants or depressants of the central nervous system.