Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Disclosed therein is a method for preparing a polyacrylonitrile-based polymer for preparation of carbon fiber having a melting point controlled by selecting an optimal energy of microwave, and a method for preparing a carbon fiber through melt spinning using the preparation method for polyacrylonitrile-based polymer. The present invention uses microwave to control the properties of the polyacrylonitrile-based polymer in a simplified way and prepare the polymer optimized for preparation of carbon fiber precursor through melt spinning for a short polymerization time, and provides a means for mass production of the polyacrylonitrile-based polymer being suitable for melt spinning at a temperature lower than the stabilization temperature and acquiring properties adequate to preparation of carbon fiber through stabilization. Hence, the present invention is expected to contribute to mass production of high-performance carbon fibers at reduced cost.

Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.

Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.

Abstract: The invention provides compounds of formula I F-L-Q (I) where F comprises a fluorophore capable of absorbing energy at an excitation wavelength and, in the absence of a quencher, emitting energy at an emission wavelength, which is different than the excitation wavelength; Q comprises a quencher; L comprises a linker moiety having two ends, one end being covalently bound to F and the other end being covalently bound to Q. The compounds are capable of undergoing a reversible reaction (1), provided below: (1) where Q+ is an oxidized form of Q representing the absence of a quencher, Ox comprises an oxidizing agent, which is capable of oxidizing Q to its oxidized form Q, and Red comprises a reducing agent, which is capable of converting Q back to its reduced form Q. The compounds can undergo photo-induced electron transfer when irradiated with energy and when Q exists in its oxidized form, Q+.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.

Abstract: There is disclosed a method for using 123I to radiolabel SnADAM become an serotonin transporter radiotracer(123I -ADAM). At first, there is provided SnADAM solution via mixing SnADAM with ethanol. The SnADAM solution is shaken and further mixed with thin KI solution. The SnADAM solution is mixed with 123I-NH4I solution and H2O2 solution. The SnADAM-123I-NH4I—H2O2 mixture is kept still. Later, the SnADAM solution is mixed with NaHSO3 solution, and the mixture is shaken and further mixed with buffer solution of saturated Na2HPO4. The SnADAM solution is filled in an Accubond C8 column. The Accubond C8 column is washed with sterile water for injection to isolate non-reacting 123I ions. The Accubond C8 column is washed with ethanol, thus providing 123I-ADAM. The 123I-ADAM is blended in normal saline mixture. Millipore Millex GV is used to filter impurities and bacteria from the 123I-ADAM solution.

Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.

Abstract: To provide a medicament which efficiently expresses an immunosuppressive agent or an anti-inflammatory agent and reduces expression of side effect. A medicament includes diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, in combination with an immunosuppressive agent and/or an anti-inflammatory agent.

Abstract: A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or a hydrate thereof includes the steps of reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate; reducing the resulting ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene; forming 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol using a formaldehyde solution; and reducing the resulting 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol to form the desired product.

Abstract: A medicine which effectively functions as an immunosuppressant or anti-inflammatory agent and is effective in diminishing the occurrence of side effects. The medicine comprises a combination of: a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure and having the function of diminishing lymphocytes circulating through the periphery; and an immunosuppressant and/or an anti-inflammatory agent.

Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .

Abstract: The present invention provides novel diazonaphthoquinonesulfonic acid bisphenol derivatives. More particularly, the present invention relates to photo restive coating comprising alkali-soluble resin, a photoactive compound and a surfactant. The photoresist film prepared has less then one micron. The photoactive compound is soluble or swellable in aqueous alkaline solutions and is diazonaphthoquinonesulfonic bisphenol esters of the general formula (A), wherein DNQ represents a 2-Diazo-1-naphthoquinone-4-sulfonyl, 2-Diazo-1-naphthoquinone-5-sulfonyl, 1-Diazo-2-naphthoquinone-4-sulfonyl groups and R1 R1 represents an alkyl, aryl and substituted aryl groups. The invention also provides a process for coating and imaging the light-sensitive composition.

Abstract: The present invention relates to a bridge compound with an N,N-dialkylamino group, represented by the following formula (I), wherein, R, R?, R?, R1, R2, B, B?, i, j, m, and n are defined the same as the specification. The novel bridge compound of the present invention is suitable for being used as a bridge group between dyestuffs, ultraviolet absorbers, or one dyestuff and one ultraviolet absorber. In addition, the present invention further provides a dyestuff compound provided from the aforementioned bridge compound.

Abstract: The present invention relates to a novel reactive dyestuff with an N,N-dialkylamino bridge group, represented by the following formula (I): wherein R, B, B?, E1, E2, Z, Z?, i, j, R1, R2, m and n are defined the same as the specification. The reactive dyestuff of the present invention is suitable for exhaust dyeing, cold batch-up dyeing, continuous dyeing, printing and digital spray printing materials that contain hydroxyl group or polyamine fibers.

Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: The invention relates, in general, to the preparation of (R)(?)tamsulosin free base by reaction of (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide or an addition salt thereof with 1-(2-bromoethoxy)-2-ethoxybenzene in a polar aprotic solvent in the presence of an organic base. More particularly, the invention relates to a process for preparing pure solid crystalline (R)(?)tamsulosin in its free base form as a precursor for the production of (R)(?)tamsulosin hydrochloride.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:

Abstract: The invention disclosed a new process of asymmetric alkynylation of ketone or ketimine, involving the chiral ligand-mediated asymmetric addition of zinc or copper acetylide to a trifluoromethyl ketone or ketimine intermediate to give a chiral tertiary proparglic alcohols or amines. The adduct compounds include the key precursors to the potent HIV reverse transcriptase inhibitor Efavirenz (DMP 266), DPC 961 and DPC 083. The invention also disclosed a novel chiral amino alcohol ligand.

Abstract: The present invention relates to a novel process for the preparation of compounds of the formula (I) by reacting in a first step amino alcohols of the formula (II) with oleum to give sulphuric acid esters of the general formula (III) and by reacting these sulphuric acid esters in a second step with mercaptans or salts thereof of the general formula (IV) RSM ??(IV) wherein in each formula, where applicable, R1, R2, R3, R4, R5, R6, R, n and M have the meanings given in the disclosure, in the presence of a diluent and in the presence of a base.

Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.

Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

Abstract: Conjugates of a hydrophobic moiety, such as a lipid, linked through a cleavable dithiobenzyl linkage to a therapeutic agent are described. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of the therapeutic agent in its original form. The linkage is stable under nonreducing conditions. The conjugate can be incorporated into liposomes for administration in vivo and release of the therapeutic agent in response to endogeneous in vivo reducing conditions or in response to administration of an exogeneous reducing agent.

Abstract: The present invention provides diaryl sulfide derivatives that exhibit significant immunosuppressive effects with less side effects. The diaryl derivatives of the present invention are represented by the following general formula (1): One example is 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]propyl-1,3-propanediol.

Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.

Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.

Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

Abstract: Compounds of formula I: wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound of Formula I in admixture with at least one agriculturally acceptable extender or adjuvant and methods of controlling insects comprising applying said compositions to locus on crops where control is desired are disclosed. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims (see 37 C.F.R. 1.72(b)).

Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.

Abstract: The invention provides for a non-steroidal compound having the formula 1

Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN  (VIIIA) and processes for production of pharmacologically useful oxazolidinones.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ones and to their physiologically acceptable salts and physiologically functional derivatives.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN  (VIIIA) and processes for production of pharmacologically useful oxazolidinones.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]P—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.

Abstract: Described are fiber-reactive water-soluble azo compounds which contain a group of the general formula (2) as diazo component where R21 is hydrogen, methyl, ethyl, methoxy, ethoxy or sulfo, R22 is hydrogen, methyl, ethyl, methoxy, ethoxy or sulfo, R23 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl, n is 2 or 3 and the group —SO2—Y is a fiber-reactive group of the vinyl sulfone series, and which are capable of dyeing hydroxy- and/or carboxamido-containing material, especially fiber material, such as cellulose fibers, for example cotton, or regenerated cellulose fibers and also wool and synthetic polyamide fibers in high color strength and good fastnesses.

Abstract: The invention relates to novel bis-o-aminophenols, and bis-o-aminothiophenols of the following structure: ##STR1## where A.sup.1 to A.sup.6 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.6 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.

Abstract: The present invention has for its object to provide a commercially useful, expedient and efficient method for purification and isolation of an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1) or its enantiomer, which is capable of removing the various contaminants, particularly said byproducts, whereby the problem of instability of the compound (1) or its enantiomer can be overcome and a high product yield can be insured.The present invention relates to a method of purifying and isolating an N-protected (2S,3R)-1-halo-2-hydroxy-3-amino-4-phenylthiobutane (1): ##STR1## (wherein X represents a halogen atom; one of P.sup.1 and P.sup.2 represents a hydrogen atom and the other represents an amino-protecting group, or P.sup.1 and P.sup.

Abstract: Novel amine derivatives of the following general formula (I): ##STR1## (wherein) A may denote --(CH.sub.2)--O--, --(CH.sub.2).sub.2 --O--, or --(CH.sub.2).sub.2 --NH--;B may denote --(CH.sub.2).sub.2 --;R.sub.1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group;R.sub.2 may denote a hydrogen atom or a nitro group;R.sub.3 and R.sub.4 may denote a hydrogen atom;R.sub.8a and R.sub.8b which are the same may denote a chlorine atom or a methoxy group;R.sub.9 may denote a hydrogen atom or an amino group;R may denote a methyl group; andX may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: Compounds useful in radioimaging and radiochemotherapy as it particularly relates to the treatment and location of malignant melanomas and other pigmenting disorders, as well as novel acyl derivatives of phenolic thioester amines and their use in compositions for blocking melanin synthesis in human or animal melanocyte cells.

Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.

Abstract: Novel nitrobenzene compounds of the nitroparaphenylene-diamine type substituted by sulphur in the 5-position are disclosed. These compounds are intended especially for the dyeing of keratin fibers and in particular human hair. A process for their preparation, dyeing compositions in which these compounds are present and a dyeing process in which these compositions are used are also disclosed.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.