Abstract:
The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Abstract:
Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
Abstract:
This application provides for oxazolisoquinoline derivatives of the formula or a pharmaceutically acceptable salt of said compound wherein: B is —CH═CH—; M is —C(R1)(R2)—; and the remaining substituents are as defined in the specification as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. This application also provides for combination therapy with the compounds of Ib or pharmaceutically acceptable salts thereof with other cardiovascular agents.
Abstract:
Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
Abstract:
Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
Abstract:
Disclosed are compounds of the formula: or the pharmaceutically acceptable salts or solvates thereof, wherein: Ar1 is a chlorophenyl group, Ar2 is a dichlorophenyl group, R1 is a —(CH2)m—X—(CH2)n—R2 group, X is a —NH—, —O—, —C(O)— or —S(O)2— group, and R2 is a substituted phenyl group. These compounds are CB1 receptor modulators. Also disclosed are methods of treating CB1 modulated diseases or conditions such as the metabolic syndrome.
Abstract:
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
Abstract:
A computer finger mouse includes a concave structure for embrace the fingertips of a hand in a relaxed positions. The concave structure allows the mouse be held and manipulated by the fingertips of a hand only. A hand holding and manipulating the computer finger mouse is in a naturally relaxed and curled position, without requiring static twisting of the hand, wrist, or forearm. As a result, fatigue, discomfort, and pain are minimized or eliminated even after a long period of continuous use.
Abstract:
A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is —O— or —NR6— when the double-dashed line represents a single bond; X is H, —OH or —NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.
Abstract:
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.