Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing th

Abstract: A therapeutic composition for inhibiting the function of a target polynucleotide sequence in a mammalian cell includes an agent that provides to a mammalian cell an at least partially double-stranded RNA molecule comprising a polynucleotide sequence of at least about 200 nucleotides in length, said polynucleotide sequence being substantially homologous to a target polynucleotide sequence. This RNA molecule desirably does not produce a functional protein. The agents useful in the composition can be RNA molecules made by enzymatic synthetic methods or chemical synthetic methods in vitro; or made in recombinant cultures of microorganisms and isolated therefrom, or alternatively, can be capable of generating the desired RNA molecule in vivo after delivery to the mammalian cell.

Abstract: The present application provides human antibodies and antigen binding fragments thereof that specifically bind to the human interleukin-21 receptor (IL-21R). The antibodies can act as antagonists of IL-21R activity, thereby modulating immune responses in general, and those mediated by IL-21R in particular. The disclosed compositions and methods may be used for example, in diagnosing, treating or preventing inflammatory disorders, autoimmune diseases, allergies, transplant rejection, cancer, and other immune system disorders.

Abstract: A therapeutic composition for inhibiting the function of a target polynucleotide sequence in a mammalian cell includes an agent that provides to a mammalian cell an at least partially double-stranded RNA molecule comprising a polynucleotide sequence of at least about 200 nucleotides in length, said polynucleotide sequence being substantially homologous to a target polynucleotide sequence. This RNA molecule desirably does not produce a functional protein. The agents useful in the composition can be RNA molecules made by enzymatic synthetic methods or chemical synthetic methodsin vitro; or made in recombinant cultures of microorganisms and isolated therefrom, or alternatively, can be capable of generating the desired RNA molecule in vivo after delivery to the mammalian cell.

Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: 1

Abstract: A tumor necrosis factor-&agr; converting enzyme (TACE) is produced, purified, and crystallized. The three-dimensional coordinates of the crystal are obtained by X-ray diffraction. The coordinates can be recorded on a computer readable medium, or are part of a video memory, where they can be used as part of a system for studying for studying TACE. The coordinates are also used in designing, screening, and developing compounds that associate with TACE.

Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit 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 estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to C(CH3)2, C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt t

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in lowering cholesterol levels.

Abstract: This invention provides the use of a combination of CCI-779 and interferon alfa (&agr;) in the treatment of neoplasms.

Abstract: A vaccine against Newcastle Disease contains one or more mutant immunogens of the NDW strain. The mutant immunogen lacks the antigenic binding site on the F glycoprotein which is recognized by the monoclonal antibody mAb 54. Reagent kits and assay methods help to distinguish vaccinated members of a poultry flock from those that may have been infected with wild-type Newcastle Disease virus.

Abstract: The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.

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

Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection, the compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.

Abstract: The present invention addresses a need in the art for methods of identifying apoptotic proteins and methods for screening compounds which inhibit an apoptotic protein. More particularly, in certain embodiments, the invention relates to increased expression levels of a NALP1 gene and/or a NALP5 gene following neuron injury. In other embodiments, the present invention demonstrates that the recombinant expression of NALP1 and/or NALP5 polynucleotides stimulates apoptosis in cultured neurons, HeLa cells and NIH-3T3 cells. In yet other embodiments, the invention relates to mutations in the nucleotide binding sequence (NBS) of a NALP1 or a NALP5 polypeptide, wherein these NBS mutations inhibit purine nucleotide binding and reduce caspase activation.

Abstract: This invention provides combinations of an ER&bgr; selective ligand with an anti-arthritis agent, which are useful in the treatment or inhibition of arthritis.

Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection. The compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to methods and materials used to express the HBM protein in animal cells and transgenic animals. The present invention also relates to transgenic animals expressing the high bone mass gene, the corresponding wild-type gene, and mutants thereof. The invention provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in bone development, and methods of diagnosing and treating diseases involved in bone development. In preferred embodiments, the present invention is directed to methods for treating, diagnosing and preventing osteoporosis.

Abstract: The present invention relates generally to the fields of neuroscience, proteomics and mood disorders. More particularly, the present invention relates to the identification of a group of proteins modulated in subjects with a mood disorder; methods for detecting or screening mRNA encoding these proteins and methods for diagnosing mood disorders.