Abstract: The present invention provides a pigment/additive comprising discrete multivalent oxidation state (DiMVO) phenothiazine compounds having corrosion inhibiting properties. These novel DiMVO phenothiazines are useful in preparing waterborne primer coating formulations for application to metals and metal alloys and demonstrating corrosion inhibiting properties. Furthermore, such formulations are chromate-free and have reduced VOC content. Methods of preparing and using such compounds and waterborne formulations also are described.

Abstract: The present invention encompasses phenoxazine derivatives and methods of use thereof.

Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.

Abstract: Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as ?-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.

Abstract: A rechargeable metal ion cell comprising: an anode comprising at least one metal; a charge-carrying electrolyte comprising a charge carrying medium and at least one metal salt; and an organic polymer cathode, wherein such cathode comprises at least one N-substituted polyphenothiazine polymer [polymer (P)], such polymer (P) comprising at least one N-substituted phenothiazine recurring unit of formula: wherein R? is an electron-withdrawing group comprising at least one heteroatom selected from the group consisting of O, S, P, and N.

Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.

Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.

Abstract: A compound for use in electrochromic devices. The compound includes (1) ?-(10-phenothiazyl)propoxy phosphonic acid; (2) ?-(10-phenothiazyl)propyl-phosphonic acid; and (3) ?-(10-phenothiazyl)propionate phosphonic acid.

Abstract: The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula in which A, X, Y, R1, R2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

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: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C═O or CH2; and R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C12)alkyl, (C3-C8)cycloalkyl and (C1-C12)alkyl (C6-C14)aryl; or R7 and R8 when taken together form a (C2-C7)alkylene group; or —NR7R8 together forms a (C2-C14)heterocyclic or substituted (C2-C14)heterocyclic. Such compounds modulate the activity of serine hydrolases and can be used in pharmaceutical compositions for the treatment of Alzheimer's disease.

Abstract: The invention relates to the use of N-substituted phenothiazines for the production of medicaments for the treatment of cerebral disorders. The invention likewise relates to novel active compounds which are prepared by reaction of phenothiazine with the appropriate acids, esters or amides or by reaction of the phenothiazinecarbonyl halides with amines. The active compounds are particularly suitable for the treatment of dementias and age-related leaning and memory disorders and depressions.

Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), ##STR1## [wherein R.sup.1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R.sup.2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R.sup.3 represents a group of the formula, ##STR2## (R.sup.4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group. m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.

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: Processes are provided for preparing crystalline moricizine hydrochloride from moricizine using hydrochloric acid, wherein the crystalline moricizine hydrochloride so obtained is substantially free of occluded water.

Abstract: An ultraviolet light-absorbing polymer which comprises a homopolymer of a polymerizable monomer having the structure: ##STR1## wherein: Z is N or --CH--,R is H or CH.sub.3,R.sub.1 and R.sub.2 may be the same or different and are H, alkyl or alkyloxy having from 1 to 20 carbon atoms, alkylcarboxy having from 2 to 20 carbon atoms, arylcarboxy having from 7 to 25 carbon atoms or hydroxyl;R.sub.3 is H, hydroxyl, hydroxyalkyl having from 1 to 20 carbon atoms or siloxy;R.sub.4, R.sub.5, R.sub.6 and R.sub.7 may be the same or different and are H or halogen;x is an integer from 1 to 20; ora copolymer thereof with an ethylenically unsaturated comonomer, the copolymer comprising an ultraviolet light-absorbing effective amount of the ultraviolet light-absorbing polymerizable monomer.

Abstract: Preparation of 2-alkylthio-phenothiazines by direct functionalization of phenothiazine by reaction of the phenothiazine, N-protected by an acryl group, with a sulfonating agent such as sulfuric acid, sulfuric anhydride, chlorosulfonic acid, or oleum, in order to obtain, after work-up of the reaction mixture, phenothiazine-2-sulfonic acid, followed by the reduction of this or, optionally, of its acyl chloride derivative, to obtain 2-mercapto-phenothiazine which subsequently is subjected to S-alkylation to thereby obtain the desired target compound.

Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: An ultraviolet light-absorbing, polymerizable monomer having the structure ##STR1## wherein: Z is N or --CH--,R is H or CH.sub.3,R.sub.1 and R.sub.2 may be the same or different and are H, alkyl or alkyloxy having from 1 to 20 carbon atoms, alkylcarboxy having from 2 to 20 carbon atoms, arylcarboxy having from 7 to 25 carbon atoms or hydroxyl;R.sub.3 is H, hydroxyl, hydroxyalkyl having from 1 to 20 carbon atoms or siloxy;R.sub.4, R.sub.5, R.sub.6 and R.sub.7 may be the same or different and is H or halogen; andx is an integer from 1 to 20.

Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.

Abstract: Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.

Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.

Abstract: Permeability characterized in that the carboxy group at 1-position of the prostaglandin is combined with a cell membrane permeable substance having hydroxy group or amino group through the intermediation of an ester bond to the hydroxy group or an amide bond to the amino group are novel and have improved cell membrane permeability.

Abstract: Oxazine, thiazine and diazine leuco dyes are synthesized through a reaction using a dicyclohexylcarbodiimide adduct. The adducts are themselves novel compounds.

Abstract: Phenothiazine derivatives and analogs thereof having the Formula I are useful as inhibitors of the biosynthesis of mammalian leukotrienes. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation, and are useful as cytoprotective agents.

Abstract: The present invention refers to novel anellated 4H-1,4-benzothiazines, several processes for the synthesis thereof, their use as pharmaceutical agents, in particular their use as lipoxygenase-inhibiting agents, pharmaceutical compositions containing the novel benzothiazines and a process for their manufacture.

Abstract: The invention is directed to N,N' and N,N',N'-substituted silylureas and a process for their production in which in a single step process there are reacted a halogenoalkylsilane or a halogenbenzylsilane with a primary or secondary amine and an alkali cyanate in equimolar amounts.

Abstract: A series of organic diamine base compounds derived from either an aromatic, alicyclic or heterocyclic ring and possessing, for the most part, an intervening methylene group between the ring and the aforesaid basic moiety have been prepared, including their pharmaceutically acceptable acid addition salts as well as oral pharmaceutical compositions containing same. These particular compounds are found to be useful in therapy as oral hypoglycemic agents. Preferred member compounds include 1,1'-[1,2-phenylenebis(methylene)]bispiperidine, 2,3-dihydro-2-[2-(1-piperidinomethyl)phenylmethyl]-1H-isoindole and 2,3-dihydro-2-[2-(4-morpholinomethyl)phenylmethyl]-1H-isoindole. Alternate methods of preparation are provided and the two principal synthetic routes leading to these compounds are described in some detail.

Abstract: Phenothiazine derivatives of the formula ##STR1## wherein R is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, CN, CH.sub.3 O or CH.sub.3 CO; Y is S, SO, or SO.sub.2 ; Z is imidazol-1-yl, 2-methyl-imidazol-1-yl, pyrazol-1-yl or benzimidazol-1-yl; and n is 1, 2 or 3; or the physiologically acceptable acid addition salts thereof; are useful as antihypertensive agents, for example.

Abstract: Soft quaternary surface active agents having the formula: ##STR1## wherein >N represents a tertiary open chain or cyclic aliphatic amine; wherein >N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.20 open chain or cyclo alkyl group, a C.sub.1 -C.sub.20 alkoxyalkyl group, a C.sub.1 -C.sub.20 acyloxyalkyl group, a C.sub.1 -C.sub.20 haloalkyl group, a C.sub.1 -C.sub.20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C.sub.1 -C.sub.4 alkyl group, an O--C.sub.1 -C.sub.8 acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 represents a C.sub.9 -C.sub.22 straight or branched alkyl group, a --(CH.sub.2).sub.n -- ##STR2## group, wherein R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C.sub.0 -C.sub.

Abstract: New chemical compounds, which are pyrrolidinoethylamine amides, in the form of free bases and salts thereof, which are useful as antitussives, pharmaceutical compositions thereof, and method of treating therewith.In the form of their salts, the compounds have the formula: ##STR1## wherein ##STR2## is an acyl radical of a phenylacetic, 60 -phenyl-.alpha.-(1 to 5 C atoms) acetic, (1 to 5 C atoms) diphenylacetic, benzilic, diphenyl-.alpha.-chloroacetic, .alpha.-lower-alkoxy-.alpha.,.alpha.-diphenylacetic, 3-coumarincarboxylic, 9-xanthenecarboxylic, phenoxyacetic, phenoxyisobutyric, halophenoxyisobutyric, or 9-flourene carboxylic acid, and wherein R'H represents an inorganic or organic acid.Medicaments containing these active principles may be used, inter alia, in the treatment of coughs and respiratory complaints.

Abstract: The invention provides new acetohydroxamic acid derivatives, having interesting properties on the central nervous system, of the formula: R.sub.1 R.sub.2 R.sub.3 C-CO-NHOH, in which R.sub.2 and R.sub.3 are each hydrogen or C.sub.1-6 alkyl, and R.sub.1 is C.sub.1-6 alkyl Z.sub.1 Z.sub.2 N (where Z.sub.1 and Z.sub.2 are each phenyl, substituted phenyl, or cycloalkyl), substituted hydantoinyl, benzhydroxylcarboxamido, Z.sub.3 CH.sub.2 -- (where Z.sub.3 = optionally substituted aryl), Z.sub.4 -A- (where Z.sub.4 is optionally substituted phenyl or naphthyl, and A is --NH--, --N(C.sub.1-4 alkyl)--, --N(C.sub.5-6 cycloalkyl)--, --NHCO--, --N(C.sub.1-4 alkyl)CO--, --N(C.sub.5-6 cycloalkyl)CO--, --CONH--, --CON(C.sub.1-4 alkyl)--, --CON(C.sub.5-6 cycloalkyl)--, --NHCONH--, --N(C.sub.5 H.sub.6)CONH--, or --N(substituted phenyl)CONH--, optionally substituted benzimidazolyl, or an optionally substituted tricyclic radical, and their metal and acid addition salts.

Abstract: New pyridine compounds of the general formula I ##STR1## wherein R denotes an optionally substituted cycloaliphatic hydrocarbon radical, Ph denotes an ortho-phenylene radical or especially a para-phenylene radical, A denotes a lower alkylene radical or a direct bond, X denotes an optionally functionally modified oxo group and Py denotes a pyridine radical, are useful as fibrinolytics, thrombolytics, antiphlogistics and as mild analgesics.

Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group, m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.