Abstract: HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(?O)rR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(?O)—, CH2, —CHOH—, —S—, —S(?O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally subs

Abstract: HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —O— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.

Abstract: The present invention relates to piperazine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.

Abstract: There is provided a novel use for vascular endothelial growth factor, herein designated VEGF-X, and a CUB domain present in the sequence of VEGF-X, which enhance smooth muscle cell proliferation and can be used to treat diseases associated with reduced smooth muscle cell proliferation. VEGF-X, and a CUB domain can also be used in tissue engineering applications to increase the number of smooth muscle cells within specific tissue to restore that tissue function or architecture. Screening methods for identifying inhibitors of VEGF-X biological activity are also disclosed and these inhibitors include neutralizing VEGF-X antibodies, antisense VEGF-X sequences or non-protein antagonists competing with VEGF-X biological activity. Also provided are therapeutic methods for treating disorders associated with smooth muscle cells hyperproliferation and methods of diagnosis a pathological condition or susceptibility to a pathological condition associated with smooth muscle cell hyperproliferation.

Abstract: The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.

Abstract: A novel human cDNA, termed PRSS11-L, was isolated which encodes a polypeptide that belongs to the S2/HtrA serine protease family. The PRSS11-L mRNA is widely expressed in several tissues throughout the body by multi-tissue Northern blotting. The full-length PRSS11-L cDNA, was cloned, expressed and purified. Proteolytic activity was demonstrated using the protein substrate casein. The isolated nucleic acid or polypeptide molecule of the invention can be used in detection assays, gene therapy, and screening assays.

Abstract: The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.

Abstract: The present invention provides nucleic acids. Polypeptides, antibodies and cells related to MAIL (Molecule possessing Ankyrin repeats Induced by LPS; or I?B-?), a novel member of the I?B family, expressed in LPS stimulated monocytes and uses thereof. The isolated nucleic acids, polypeptides, antibodies and cells of the invention can be used in detection assays, screening methods and drug discovery assays.

Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) ?in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) ?with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

Abstract: The present invention provides nucleic acid and polypeptide sequences describing a novel canine cold- and menthol-sensitive receptor, herein named as canine CMR1 (cCMR1). The isolated nucleic acid or polypeptide molecule of the invention can be used in detection assays and screening assays.

Abstract: A tool for the isolation of c-kit expressing cells is provided. This tool consists of a c-kit plasmid targeting vector which is capable of integrating into the wild type c-kit allele and encodes a chimeric fluorescent protein comprising a nucleolar localization signal such as, TCOF-12, RLP313, RPS254 or Fxr2h5. The construct generates a condensed, bright, fluorescent signal that can be localized in living tissue and after dissociation. The construct allows visualization using confocal microscopy and allows automated cell sorting of the dissociated cells using amongst others flow cytometry.

Abstract: The invention provides a compound of formula (I) and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides substituted 1,3,5-triazine compounds as kinase inhibitors and a method for treating or ameliorating a kinase mediated disorder.

Abstract: This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing ?a1=a2?a3=a4—and ?b1=b2?b3=b4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH?2?, —NHC(?O)R6, —C(?NH)R6 or a 5-membered hetrocycl; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl, —CHOH—, —S—, —S(?O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13, NR13R14; —

Abstract: The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.

Abstract: The use of nucleic acids and polypeptides which are involved in a pathway eventually leading to programmed cell death of yeast or fungi for the preparation of a medicament for treating diseases associated with yeast or fungi or for the treatment of prolifeative disorders or for preventing apoptosis in certain diseases is disclosed. Methods are provided to identify compounds which selectively modulate the expression or functionality of said polypeptides in the same or a parallel pathway. Also provided are compounds as well as pharmaceutical compositions, medicaments and vaccines. New nucleic acid sequences, probes and primers derived thereof, expression vectors and host cells transformed with said vectors, polypeptides and antibodies raised against said polypeptides are also disclosed.

Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.

Abstract: DNAs encoding human voltage gated sodium channel ?1A subunit have been cloned and characterized. The recombinant protein is capable of forming biologically active protein. The cDNA's have been expressed in recombinant host cells that produce active recombinant protein. The recombinant protein is also purified from the recombinant host cells. In addition, the recombinant host cells are utilized to establish a method for identifying modulators of the receptor activity, and receptor modulators are identified.

Abstract: The present invention provides methods for identifying test substances that bind to the ?2? subunit of a calcium channel.

Abstract: The present invention is directed to reporter molecules and tags that may be used to monitor a target substance in a biological system. More particularly, the present invention relates to the use of an apo metal binding protein as a reporter molecule or tag. An apo metal binding protein may be bound to a protein or tissue or introduced into a cell. The invention also relates to methods of utilizing the apo metal binding protein for detecting a cell expressing a protein of interest, localizing a protein in a cell, and designing a therapeutic agent for treating a disease or infection.