Abstract: This invention provides compounds of formula I having the structure 1

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: Disclosed are compounds which bind VAL-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: This invention provides compounds of the formula: 1

Abstract: This invention provides methods for treating, preventing or inhibiting anxiety, anxiety-related conditions and phobias in a mammal using compounds of the formula: 1

Abstract: This invention provides compounds of formula I having the structure 1

Abstract: Novel piperazine derivatives are provided having the formula 1

Abstract: This invention provides compounds of the formulae: 1

Abstract: The present invention relates to a novel lysyl oxidase genes, termed EER-7. The invention relates to the protein and nucleic acids encoding the protein. The invention further relates to an assay system to identify compounds that selectively modulate EER-7 protein activity by interaction with estrogen receptors.

Abstract: Regulatory elements responsible for tissue-specific transcriptional regulation of the human &bgr;3-adrenergic receptor (&bgr;3-AR) were identified. A region localized between −6.50 and −6.30 kb of the proximal promoter contained three sequences that act synergistically to achieve full transcriptional activity. One segment, termed segment A, contains an Sp1 binding site. Another of the sequences, termed segment B, is a binding site for a trans-acting factor present in cells that constitutively express &bgr;3-AR. In a specific embodiment, the trans-acting factor is expressed in neuroblastoma (SK-N-MC) and brown adipose tissue cells, but little or not at all in CV-1, HeLa, or white adipose tissue cells. The third segment, C, is an S1 nuclease-sensitive site having CCTT repeats.

Abstract: Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

Abstract: The invention relates to vaccines which are suitable for the prevention of clostridial diseases of sheep (and lambs), providing an effective immunity for up to a year or more following a single injection or dose.

Abstract: This invention provides aryloxy indole derivatives which are useful for the treatment of diseases affected by disorders of the serotonin-affected neurological systems, such as depression and anxiety, the compounds having the formula: 1

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alkynyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl C1 to C6 alkoxy, or C1 to C6 aminoalkyl gro

Abstract: Nucleic acids encoding the long form and shorter isoform of the neurotensin receptor subtype 2, referred to as HNT2R (long) and HNT2R (short), are described. Polypeptides having amino acid sequences of the HNT2R and HNT2RS isolated proteins are also provided. A method is also provided for isolating and cloning receptors expressed from the novel HNT2R and HNT2R cDNAs for use in development/implementation of high throughput screens to identify novel neurotensin agonists and antagonists. Methods are also provided for identifying compounds that bind to HNT2R.

Abstract: The present invention provides methods for synergistic control of ectoparasitic arthropods with a synergistically effective amount of a combination of the macrocyclic lactone moxidectin and an arylpyrrole compound. Also provided are methods of protecting animals from infestation and attack by ectoparasites with said combination. The present invention also provides synergistic insecticidal compositions comprising as essential active ingredients the macrocyclic lactone moxidectin and an arylpyrrole compound.

Abstract: This invention provides the use of CCl-779 in the treatment of neoplasms.

Abstract: This invention provides compounds useful in treating serotonin-related central nervous system disorders, including anxiety, generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, sleep disorders, sexual dysfunction, alcohol and drug addiction, Alzheimer's disease, Parkinson's disease, obesity and migraine, the compounds having the general formula: 1