Abstract: A topical gel composition comprising between about 0.005 and 1.0% ivermectin, between about 30 and 40% of a pharmaceutically acceptable alcohol, between about 30 and 40% of a pharmaceutically acceptable glycol, and a pharmaceutically acceptable carrier, useful for treating Pediculosis capitis infestation in a human patient.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C1–4 alkyl, 4) C3–7 cycloalkyl, 5) CF3, 6) OCF3, 7) C1–4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3 .

Abstract: The present invention concerns certain isoquinolinone compounds and their utility as inhibitors of voltage-dependent potassium channels or currents, such as Kv1.5 and IKur, that could serve as targets for the treatment of cardiac arrhythmias especially atrial arrhythmias. The present invention also provide a method for treating or preventing conditions which respond to the inhibition of potassium channels or currents, such as cardiac arrhythmias and more especially atrial arrhythmias. The present invention further includes pharmaceutical formulations and a process of making a pharmaceutical composition comprising a compound of certain isoquinolinone or its pharmaceutically acceptable salts, hydrates, solvates, crystal forms, and stereoisomers thereof, and a pharmaceutically acceptable carrier.

Abstract: The present invention is directed to the radioligand compound, [35S]-radiolabeled (+)-N-[1?-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4?-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the IKr channel, and may have antiarrhythmic activity.

Abstract: The invention includes mouse serotonin 5-HT2c receptor isoforms having amino acid replacements at one or more positions of the natural mouse serotonin 5-HT2c receptor polypeptide sequence, specifically at one or more of positions 157, 159 and 161. The polypeptides are useful for identifying ligands which bind with the serotonin 5-HT2c receptor and modulators of the serotonin 5-HT2c, and for identifying drugs with affinity for 5-HT2 receptors which are used to treat schizophrenia, Parkinsonism, and anxiety disorders.

Abstract: This invention provides a drug combination comprised of a thyroid hormone receptor beta agonist with a fibrate in therapeutically effective amounts, which is useful for reducing cholesterol synthesis, lowering plasma cholesterol levels and lowering plasma triglyceride levels.

Abstract: The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.

Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.

Abstract: The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:

Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.

Abstract: The present invention is a method for diagnosing a patient at risk to thrombocytopenia induced by administration of a GP IIb/IIIa receptor antagonist, which comprises combining i) a plasma sample of the patient; ii) detectable monoclonal antibody which recognizes induced binding sites formed on the GP IIb/IIIa receptor following association of a fibrinogen receptor antagonist with the GP IIb/IIIa receptor; and iii) GP IIb/IIIa receptor:GP IIb/III receptor antagonist complex, and determining association of the detectable monoclonal antibody with the complex in the presence of the plasma.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A is

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline Anhydrous Form B, 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type A Monohydrate, and 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type B monohydrate, or a pharmaceutically acceptable salt thereof.

Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.

Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.

Abstract: The invention includes mouse serotonin 5-HT2c receptor isoforms having amino acid replacements at one or more positions of the natural mouse serotonin 5-HT2c receptor polypeptide sequence, specifically at one or more of positions 157, 159 and 161. The polypeptides are useful for identifying ligands which bind with the serotonin 5-HT2c receptor and modulators of the serotonin 5-HT2c, and for identifying drugs with affinity for 5-HT2 receptors which are used to treat schizophrenia, Parkinsonism, and anxiety disorders.

Abstract: There is described antifungal combination therapy comprising the use of known antifungal agents such as the azoles or polyenes in combination with a pneumocandin derivative antifungal agent. More particularly, the invention relates to antifungal combination therapy comprising the use of azoles such as fluconazole, voriconazole, itraconazole, ketoconazole, miconazole, ER 30346, SCH 56592; polyenes such as amphotericin B, nystatin or liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or other chitin inhibitors, elongation factor inhibitors such as sordarin and analogs thereof, mannan inhibitors such as predamycin, bactericidal/permeability-inducing (BPI) protein products such as XMP.97 or XMP.127 or complex carbohydrate antifungal agents such as CAN-296 in combination with a pneumocandin derivative as described herein.