Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein

Abstract: The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, 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 relates to compounds of Formula I, wherein R1, R2, R3, R4, and n are as defined, and to pharmaceutically acceptable salts of said compounds. Compounds of Formula I have activity in agonizing 5HT7 receptors and are useful in treating, for example, disorders that can be treated by modulating circadian rhythms.

Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers.

Abstract: Methods for detecting acetylcholinesterase in a brain of a patent, comprising administering to the patient a detectable amount of a radiolabeled compound of a class of benzisoxazoles or a pharmaceutically acceptable salt thereof, are disclosed herein. The methods are useful for diagnosing, estimating the severity of, or monitoring the progression of a dementia, such as Alzheimer's disease, in a patient.

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p 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: A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.

Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.

Abstract: The present invention relates to a process for the preparation of pesticidal compounds, and more particularly to the preparation of pyrazole compounds. In particular, the present invention relates to a process for preparing 1-arylpyrazoles and 1-pyridylpyrazoles which have pesticidal activity. More particularly, the present invention relates to a novel process by which 3,4,5-trisubstituted 1-arylpyrazoles may be produced directly in a reaction which involves coupling of an aryldiazonium species with an appropriately substituted precursor bearing a desired substituent.

Abstract: A pharmaceutical composition for treating a disorder that is treated by modulation of serotonergic neurotransmission comprising administering (7S,9aS)-cis-2-Benzo[d]isoxazol-3-yl-7-(3-pyrrolidin-1-ylmethyl-phenoxymethyl)-octahydro-pyrido-[1,2-a]pyrazine and sertraline is disclosed.

Abstract: The present invention is concerned with pharmaceutical compositions comprising a mixture of amlodipine enantiomers, which compositions have both anti-hypertensive and additional cardiovascular properties derived respectively from their calcium channel-blocking activity and their ability to release vascular nitric oxide (NO).

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: The present invention provides compositions and methods for the use of antigenic peptides derived from the Fc portion of the epsilon heavy chain of an IgE molecule as vaccines for the treatment and prevention of IgE-mediated allergic disorders. In particular, the invention provides compositions, methods for the treatment and prevention of IgE-mediated allergic disorders comprising an immunogenic amount of one or more antigenic peptides derived from the CH3 domain or junction of Ch-3/CH4 domain of an IgE molecule and methods for the evaluation of IgE mediated allergies in dogs.

Abstract: The invention provides non-human, genetically-modified mammals and genetically modified animals cells having a functionally disrupted P2×7 receptor gene. Also provided are methods for producing genetically modified mice in which one or both P2×7R alleles have been functionally inactivated.

Abstract: There is provided a compound of formula I, wherein A, D, R1, R2, R3, X and n have meanings given in the description, which are useful in the prophylaxis and in the treatment of diseases mediated by opiate receptors, such as pruritus.

Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant ?7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant ?7 nicotinic receptor agonist.

Abstract: The invention provides a compound of formula I: wherein G, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection using such compounds or salts.

Abstract: Polynucleotide and polypeptide sequences are described. The polypeptide sequences comprise one or more of: (a) a polypeptide having the deduced amino acid sequence translated from the polynucleotide sequence in SEQ ID NO: 1 or SEQ ID NO: 5 and variants, fragments, homologues, analogues and derivatives thereof; (b) a polypeptide of SEQ ID NO: 2 and variants, fragments, homologues, analogues and derivatives thereof (c) a polypeptide encoded by the cDNA of NCIMB 41110 and variants, fragments, homologues, analogues and derivatives thereof; or (d) a polypeptide which has at least 78% identity to (i) the polypeptide encoded by the polynucleotide of SEQ ID NO: 1 or SEQ ID NO: 5, (ii) the polypeptide of SEQ ID NO: 2, or (iii) the polypeptide encoded by the cDNA of NCIMB 41110. Such polypeptide sequences are, inter alia, useful in the prophylaxis and/or treatment of sexual dysfunction, in particular male erectile dysfunction (MED) or female sexual dysfunction (FSD), preferably female sexual arousal disorder (FSAD).

Abstract: A process for interconverting a mixture of cis-trans isomers of a compound of formula I into the substantially pure cis isomer. Cis isomers of formula I are useful intermediates in the synthesis of cis isomers of benzamide piperidine compounds which exhibit activity as NK-1 receptor antagonists.

Abstract: The present invention relates to the use of a resorcinol derivative, i.e., 4-(2,4-dihydroxyphenyl)cyclohexanol, or a pharmaceutically acceptable salt thereof, as a skin lightening agent.