Abstract: This invention relates to certain benzenesulfonamides and their use as PDE7 inhibitors

Abstract: Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows: 1

Abstract: A compound of the formula: 1

Abstract: Anesthetizing plastic or other drug delivery polymer system including a hydrophobic polymer and a drug that has an aromatic ring.

Abstract: The invention discloses stable diesters of chelating agents of divalent metal ions, processes for their preparation and pharmaceutical compositions thereof. Most preferred compounds according to the present invention are stable lipophilic diesters comprising a covalent conjugate of a BAPTA and a pharmaceutically acceptable alcohol. The diesters are useful in a method for treating a condition or disease related to an excess of divalent metal ions, and in particular for the treatment of a condition or disease related to elevated levels of intracellular calcium ions, such as in brain or cardiac ischemia, stroke, epilepsy, Alzheimer's disease or cardiac arrhythmia and in open heart surgery.

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of oxime derivatives represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Compound of formula (I): 1

Abstract: The present invention relates to the use of deprenyl compounds to rescue damaged nerve cells in a patient and to kits containing deprenyl compounds useful for rescuing damaged nerve cells in a patient.

Abstract: Novel amidinophenol derivatives of formula (IB) 1

Abstract: Non-nucleoside reverse transcriptase inhibitors of formula (P-1) wherein: Ar1 is an unsaturated, optionally substituted, mono or bicyclic ring structure comprising 0 to 3 hetero atoms selected from S, O and N; Ar2 is an aromatic, optionally substituted, monocyclic ring structure comprising at least one nitrogen hetero atom and zero to two further hetero atoms selected from S, O and N; R4 and R5 are independently H or C3-C8 cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C5 alkoxy, C1-C4 alkanoyloxy, C1-C4 alkylthio, amino, carboxy, carbamoyl, cyano, halo, hydroxy, aminomethyl, hydroxymethyl, carboxymethyl, or halo substituted C1-C6 alkyl mercapto, nitro; or R4 and RS join to form a 3-6 membered, optionally substituted ring structure; R6 is 0 or S; Rx is the residue of a natural or unnatural amino acid; and L* is a linker moiety which is ether-, carbonate- or ester-bound to the adjacent oxygen and ester linked to Rx; and pharmaceutically acceptable salts thereof are anti-HIV agents with favourable ph

Abstract: A non-invasive and non-systemic method for intradermal prevention OR amelioration of pain from a surgically closed wound is disclosed. The method comprises topical delivery of a local anesthetic to an exterior surface of a surgically closed wound.

Abstract: A new family of compounds, particularly aryl-indane compounds, is disclosed. The compounds may be used as inhibitors of P-glycoprotein-mediated transport. Use of the compounds to enhance bioavailability and to modulate multi-drug resistance to chemotherapeutic agents is disclosed.

Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: A fungicidal compound of formula (I) having a fluorovinyloxyphenyl moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein: X is CH or N; Y is O or S; Z is O or NH; R1 is hydrogen or CF3; and R2 is hydrogen, a C1-10 alkyl, naphthyl, thiophenyl or a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, phenoxy, halogen, and methylenedioxy radicals.

Abstract: Provided herein is a novel and useful device and method for locally delivering and controllably releasing oxybutynin in the cervical region of a female. A device of the invention comprises a ring comprising trifluoropropylmethyl/dimethyl siloxane elastomer. A pharmaceutical composition comprising oxybutynin and an excipient is placed within a bore located in the ring, wherein the bore runs from the surface of the ring into the ring. The ring has a sufficient size such that it can be inserted into the vaginal canal of a female. A cap comprising is placed over the bore at the surface of the ring in order to contain the pharmaceutical composition within the bore. When the ring is inserted into the vaginal canal, the trifluoropropylmethyl/dimethyl siloxane elastomer controllably releases and locally delivers a therapeutically effective amount of oxybutynin to the detrusor muscle to treat the female's urinary incontinence.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: Compound represented by the structural formula 1

Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.

Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.

Abstract: Substituted indenyl sulfonyl acetic acids are useful in the treatment of precancerous lesions.

Abstract: In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

Abstract: Disclosed are methods and compositions for the treatment of glaucoma and ocular hypertension, comprising the administration of a prostaglandin FP receptor agonist and a prostaglandin synthesis inhibitor.

Abstract: The present invention relates to the pesticidal use of 1-aryl-1-(substituted thio, sulfinyl and sulfonyl)-2-nitroethane compounds having the structural formula I 1

Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process for

Abstract: The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I 1

Abstract: Compounds of formula I 1

Abstract: Inhibitors of matrix metalloproteases such as collagenase are capable of inhibiting the release of human soluble CD23 and are therefore useful in the treatment and prophylaxis of conditions in which an excess of s-CD23 is implicated, such as allergy and autoimmune disease.

Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

Abstract: Use of amino-substituted hydroxybenzophenones of the formula I in which the variables have the meanings explained in the description, as photostable UV filters in cosmetic and pharmaceutical preparations for protecting human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.

Abstract: The compound of formula 1 1

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: Compounds of formula (I) 1

Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general Formula (I) and a pharmaceutically acceptable salt or an oxide or a hydrate thereof, that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

Abstract: The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus. Parkinson's Disease, neuronal and cardiac ischemia. Huntington's disease and stroke.

Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1

Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).

Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), 1

Abstract: The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat neurodegenerative retinal disorders is disclosed.

Abstract: Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.

Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.

Abstract: This invention relates to methods of using neurotrophic compounds having an affinity for FKBP-type immunophilins to stimulate or promote neuronal growth or regeneration and to prevent neuronal degeneration.

Abstract: The invention relates to novel compounds derived from pentaerythrite compounds of formula (XII) and (XVI), which can be used as pharmaceutically active substances, specially in the treatment of cardiac and circulatory diseases.

Abstract: The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat angiogenesis-related disorders, including ophthalmic angiogenesis-related disorders such as diabetic retinopathy and exudative macular degeneration, is disclosed.

Abstract: The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, &agr;-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.

Abstract: Compounds of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mannnalian hosts, and processes for their preparation, are also described.