Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is  wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.

Abstract: A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, 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, 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, wherein b is N Y1 or O; c is CY2 or N; d is CY2; e is CY1 or N; f is CY1 or N; g is CY1 or N; Y1 is hydrogen, C1-4 alkyl, or halogen; Y2 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy; A is  and W, X, Z, R3, R4 and R5 are defined in the specification.

Abstract: The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with an oral composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis and sarcoidosis.

Abstract: Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, wherein A is wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.

Abstract: A method for eliciting an &agr;v&bgr;5 or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of the formula which are useful for inhibiting restenosis, angiogenesis, atherosclerosis, diabetic retinopathy, macular degeneration, inflammation or tumor growth.

Abstract: A method for treating Pediculosis capitis infestation in a human patient which comprises orally administering to the human a total amount of ivermectin of between about 400 ug/kg and about 1200 ug/kg over a period of time of about one week, wherein equal portions of the total amount are administered according to an administration sequence selected from the group consisting of c) a first day and a second day, and d) a first day, a second day and a third day, during the one week time period. The invention is also a method for treating Pediculosis capitis infestation in a human patient which comprises orally administering to the human a total amount of ivermectin of between about 6 mg and 135 mg over a period of time of about one week, wherein equal portions of the total amount are administered according to an administration sequence selected from the group consisting of e) a first day and a second day, and f) a first day, a second day and a third day, during the one week time period.

Abstract: Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, wherein A is

Abstract: The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof. The invention is also a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor and an NSAID, e.g., a COX-2 inhibitor.

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: The invention concerns recombinant human adenosine receptors A1, A2a, A2b and A3 which have been prepared by cDNA cloning and polymerase chain reaction techniques. The invention also concerns expression systems for these receptors and an assay using the expression systems. The recombinant adenosine receptors comprising the invention can be utililized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein ##STR2##

Abstract: A method for inhibiting platelet aggregation in a mammal comprising administering to the mammal a safe and therapeutically effective amount of a GPIIb/IIIa receptor antagonist or a pharmaceutically acceptable salt thereof and a safe and therapeutically effective amount of low molecular weight heparin. A method for inhibiting platelet aggregation in a mammal comprising administering to the mammal a safe and therapeutically effective amount of (2-S-(n-butylsulfonylamino)-3[4-(piperidin-4-yl)butyloxyphenyl]-propionic acid or a pharmaceutically acceptable salt thereof and a safe and therapeutically effective amount of low molecular weight heparin.

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: A compound which inhibits human thrombin and which has the general structure ##STR1## such as ##STR2##

Abstract: The invention is a pharmaceutical composition for oral administration to a patient comprising pharmaceutically effective amount of [3(R)-[2-Piperidin-4-yl)ethyl]-2-piperidone-1]acetyl-3(R)-methyl-.beta.-al anine, or a pharmaceutically acceptable salt thereof; pharmaceutically acceptable amounts of a polymeric binder; and pharmaceutically acceptable amounts of pharmaceutically acceptable excipients.The invention is also a process for making a pharmaceutical composition comprising [3(R)-[2-Piperidin-4-yl)ethyl]-2-piperidone-1]acetyl-3(R)-methyl-.beta.-al anine, which comprises the steps ofa) mixing, in a vessel suitable for granulation, a pharmaceutically acceptable amount of [3(R)-[2-Piperidin-4-yl)ethyl]-2-piperidone-1]acetyl-3(R)-methyl-.beta.

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: