Abstract: The present invention relates generally to the use of compositions and methods for treating nociceptive events that occur on the ocular surface in association with dryness, injury, environmental pollutants, and infectious and non-infectious diseases. Specifically, the present invention is directed to the use of certain compounds for treating for treating ocular pain or ocular discomfort.

Abstract: The present invention concerns a pharmaceutical composition comprising an alpha-2 adrenergic receptor agonist for preventing or treating inflammatory pain and diseases in mucosa of oral cavity, pharynx and larynx. In another aspect the present invention provides mucosal bioadhesive slow release carriers for the extended and controlled release of alpha-2 adrenergic receptor agonists that can be used on mucosal surfaces for preventing or treating inflammatory pain and diseases in mucosa of oral cavity.

Abstract: Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.

Abstract: This invention relates to a new application of compound Clonidine Hydrochloride in a use of preparation of information intervention agent, a new preparation method of information intervention agent, and a product. The Clonidine Hydrochloride interacts with the human information receptor, therefore realizing the intervention through the Clonidine Hydrochloride information physical method, and treatment was not a chemical treatment. This invention comprises: putting the compound Clonidine Hydrochloride information package filler (3) into a container (4), closing the lid (7), sealing by a glue, attaching a hanging piece to the container (4) to form the Clonidine Hydrochloride information intervention agent (9) for clinical use. The usage of this invention is simple, convenient, safe, reliable and easy to accept. It is especially appropriate for use by senior people, unhealthy people, children, or people with disturbance of consciousness, mental retardation, and behavioral disorders.

Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.

Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.

Abstract: Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.

Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.

Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.

Abstract: A detergent dispersant contains a nitrogen-containing compound represented by the following formula (1). A lubricating oil composition contains the detergent dispersant. Each symbol in the formula means the same as described in the description.

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

Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.

Abstract: The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.

Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.

Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.

Abstract: A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a ?2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours (e.g., no more than once about every 24 hours) to a subject having a steady state plasma concentration of the ?2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.

Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression and schizophrenia.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.

Abstract: Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.

Abstract: An object of the present invention is to provide an angiogenesis inhibitor. The angiogenesis inhibitor according to the present invention contains a compound represented by the following general formula [I] or a salt thereof as an active ingredient. In the formula, the ring A represents a benzene ring or a naphthalene ring; X represents a single bond, an alkylene group or —CH2COOCH2—; Y represents an oxygen atom or N(R6); R1, R2 and R3 are the same or different and represent a hydrogen atom or an alkyl group, or R1 and R3 may be joined together to form a ring having one or more double bonds; R4 and R5 are the same or different and represent a hydrogen atom or an alkyl group; and R6 represents a hydrogen atom or an alkyl group.

Abstract: The present invention relates to alpha2-adrenergic receptor agonist nitrooxyderivatives having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of ocular diseases, in particular high intraocular pressure and glaucoma.

Abstract: The present invention comprises novel substituted 2-aminoimidazoles of formula I, processes for their preparation, pharmaceutical compositions thereof, and methods for their use in the treatment of disorders of the central nervous system, cardiovascular disorders, stroke and pulmonary disorders, urinary disorders such as acute or chronic renal failure, disorders of biliary function, respiratory disorders such as snoring or sleep apnea. wherein the substitutents R1-R8 are further defined herein.

Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.

Abstract: The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

Abstract: The invention relates to novel compounds of the type of the imidazolidines of the formula I in which R1 to R7 are as defined in the claims. They are used for preparing a medicament for the treatment or prophylaxis of the central nervous system, of lipid metabolism, of infection by ectoparasites, of disorders of gall function and for improving the respiratory drive and are therefore used for treating respiratory distress. Additionally, the compounds increase the muscle tone of the upper respiratory tract, thus suppressing snoring.

Abstract: A subject-matter of the disclosure is a novel composition for the dyeing of human keratinous fibres, for example, the hair, comprising a monocationic monoazo dye of formula (I) W1-N?N—W2-NW3-W4-W5, the dyeing processes employing it, the use of the dyes of formula (I) as direct dyes and the novel compounds of formula (I).

Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R2, A and X are as defined herein. Also disclosed are compounds and related compositions.

Abstract: The cationic dyes of formula (1) specified in claim 1 are suitable especially for colouring keratin-containing fibres, more especially for colouring hair.

Abstract: Compounds of the formula (II) wherein R1, R2, R3, R4, and R5 are as set forth herein, pharmaceutical compositions containing them, and their use in treating urinary incontinence.

Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered.

Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: The present invention relates to 2′-halo-3′,5′-dialkoxyphen-1′-yl-imino-2-imidazolidine, the tautomeric 2′-halo-3′,5′-dialkoxyanilino-2-imidazoline and/or the pharmacologically acceptable salts thereof and their use as pharmaceutical compositions.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: A compound of formula I or of formula II wherein: R1 is F, Cl, Br, CH2F, CF2H, or CF3; R2 is NR6R7, where R6 is Me, Et, Pr, or iPr, and R7 is Me, Et or Pr; and R3, R4, and R5 independently of one another each are H, Me, F, Cl, Br, CH2F, CF2H, or CF3, and if R4 is Me, F, Cl, Br, CH2F, CF2H, or CF3, then R1 is additionally H or Me, or a pharmacologically acceptable salt thereof. In addition, pharmaceutical compositions comprising an effective amount of these compounds, methods for the treatment or prophylaxis of urinary incontinence and diseases of the bladder using these compounds, and methods for making these compounds are disclosed.

Abstract: The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers.

Abstract: The invention relates to compounds of formula (I) in which the symbols have the meanings given in the claims. Said compounds are inhibitors of the sodium-dependent bicarbonate/chloride ion exchanger which can be used as medicines for the prophylaxis or treatment of a wide range of diseases, for example the treatment and/or prophylaxis of myocardial infarction, angina pectoris, diseases caused by ischaemia, impaired respiration, cardiac ischaemia, ischaemia of the peripheral and central nervous system and stroke, ischaemia of the peripheral organs and limbs and diseases in which cell proliferation is a primary or secondary cause, in the treatment of shock, during surgical interventions and organ transplants or for preserving and storing transplants to be used in surgical interventions.

Abstract: The invention relates to the use of guanidine compounds in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.

Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1

Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: wherein A, R1 and R2 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.

Abstract: The present invention relates to the use of &agr;1L-agonists for treating urinary incontinence.

Abstract: The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers.

Abstract: The present invention relates to the use of &agr;lL-agonists for treating urinary incontinence.

Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.