Abstract: The present invention relates to compounds of the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X and Y are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S?O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S?O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C?O)—, R5—(NR6)—(C?O)—, R5—(C?O)—NR6—, R5—O—(C?O)—, R5—(C?O)—O—, R5—CR7?CR8— or R5—C?C_; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use.

Abstract: The present invention provides compounds of formula I: wherein R1, R2, X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I).

Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.

Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).

Abstract: This invention relates to therapeutic methods for treatment or prevention of tissue damage resulting from ischemia in mammals.

Abstract: A compound of the formula: or a pharmaceutically acceptable salt, ester or ether thereof, wherein R1 through R12 are independently hydrogen or the like; X1 and X2 are independently CH2 or the like; R13 is hydrogen or the like; or R12 and R13 taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R14 and R15 are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.

Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.

Abstract: The invention provides compounds of Formula I: wherein m1 is 0 or 1; m2 is 1 or 2; R1 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl; R2 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl, provided that when m1 is 1 at least one of R1 and R2 is —H; or a pharmaceutically acceptable salt, pharmaceutical composition, a pure enantiomer or racemic mixture thereof. The invention also provides a method for treating a disease or condition in a mammal, wherein the ?7 nicotinic acetylcholine receptor is implicated and for treating diseases where there is a sensory-gating deficit in a mammal comprising administering to a mammal a therapeutically effective amount of a compound of Formula I. These compounds may be in the form of pharmaceutical salts or compositions, and may be in pure enantiomeric form or may be racemic mixtures.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems re

Abstract: A pharmaceutical knowledge base is provided that contains multiple information items stored in at least one computer. Pharmaceutical knowledge is represented in a multi-dimensional coordinate space having at least first, second and third axes, where the first axis pertains to diseases, the second axis pertains to targets, and the third axis pertains to drug compounds. Pharmaceutical knowledge may be mapped into the multi-dimensional coordinate space by assigning each information item one or more locations in the space, dependent upon the data contained within the information item. This mapping may then be used to reveal hitherto unappreciated connections between the axes, such as the potential use of a particular compound or target for treating a certain disease.

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract: The present invention provides methods of treating diabetic cardiomyopathy, the methods comprising administering to a patient having or at risk of having diabetic cardiomyopathy a therapeutically effective amount of a glycogen phosphorylase inhibitor.

Abstract: This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: The present invention provides ?3-adrenergic receptor agonists of structural Formula (I) as well as pharmaceutical formulations thereof and methods for treating ?3-adrenergic receptor-mediated diseases, conditions, or disorders using such compounds.

Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5)alkenyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C?O), or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, M is a covalent bond O, S, NH or the like, Y is 4- to 12-membered bicyclic-carbocyclic rings or 4- to 12-membered bicyclic-heterocyclic rings, or 5- to 17 membered spirocarbocyclic rings or 5- to 17-membered spiroheterocyclic rings or the like, Z1, Z2, Z3 and Z4 are hydrogen or the like, is disclosed. These compounds have ORL1-receptor agonist activity, and are thus useful as analgesics or the like in mammalian subjects.

Abstract: The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives.

Abstract: This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-o-methyl-4-C-[(propylamino)methyl]-?-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-?-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.