Abstract: A novel monoclonal antibody that specifically recognizes phosphatidylinositol-3,4,5-triphosphate (PIP3) but does not cross-react with structurally similar phospholipid antigens is advantageous for PIP3-specific immunoassay. The gene in the variable regions of the monoclonal antibody has been identified, which enables producing recombinant antibodies.

Abstract: The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.

Abstract: The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.

Abstract: The present invention relates to novel secretory polypeptides and precursor proteins thereof, which show a high homology to MIA (melanoma inhibitor activity)/CD-RAP (bovine cartilage-derived retinoic acid-sensitive protein); are specifically expressed in the cartilage tissue; and have an effect on the cartilage differentiation. The polypeptides and the DNAs encoding the same can be used for the diagnosis, treatment, or prevention of bone and joint diseases or pathological angiogenesis. As well, the polypeptides are useful as a reagent for screening a compound that promotes or inhibits the activity of the polypeptides. The antibody to the polypeptides can be used for the detection, quantification, or neutralization of the polypeptide in a test sample fluid. Further by using the promoter of the present invention, a therapeutic protein can be expressed predominantly in the cartilage tissue for a gene therapy.

Abstract: The invention provides compounds or salts thereof of the general formula (I): wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; X represents OCH2 or a group CR3R4; wherein each of R3 or R4 independently represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy or C3-6 cycloalkyl group. The compounds or salts thereof are useful for treatment of respiratory disorders such as asthma.

Abstract: A heat shrinkable multilayer film including a thermoplastic heat sealable inner layer, an abuse layer of a thermo-plastic polymer blend having a higher average melting point than said inner layer, and a thermoplastic, optically clear outer layer adjacent said abuse layer, wherein said outer layer has a lower Vicat softening point than said abuse layer. A film in accordance with the invention has high hot water seal strength, high burn-through resistance and superior optical properties without the need for irradiation.

Abstract: The invention relates to a transdermal therapeutic system (TTS) for transcutaneously administering tolterodine over a period of several days and to a method for producing the same. The TTS contains a self-adhesive layer-shaped matrix composition which contains a (meth)acrylate copolymer comprising ammonium groups. The TTS also contains at least one plasticizer and up to 25 wt, % of tolterodine.

Abstract: The invention provides methods for the one sided printing and manufacture of a Möbius strip. The invention includes a method comprising providing an image (30); aligning three substantially identical copies of the image (30) such that a first copy is juxtaposed to a second copy, and a third copy is centered beneath and adjacent to the first and second copies; setting a die layout in a desired configuration; die cutting the Möbius strip using a die (29); and assembling the Möbius strip. Using methods of the invention, relatively seamless Möbius strips may be constructed for use in a wide variety of retail items, such as gift and other novelty items and as a marketing tool for organization wishing to promote cyclical concepts.

Abstract: The present invention relates to devices for efficient transport, transfer and movement of fluids. In particular, the invention provides fluidic micro-structures for controlled transport and movement of liquids in devices for analytical and other purposes. Devices of the invention include one or more features that can enhance performance of the fluid transfer, referred to as a pre-shooter stop, a butterfly structure, a cascade structure, a waste chamber inlet, a capillary driven sample inlet chamber, a capillary stop structure, a bifurcation flow-through structure, and a hydrophobic vent.

Abstract: A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated.

Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

Abstract: Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B—L—A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.

Abstract: The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance), to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a pKa value below about 5, such as in a range of from about 4 to about 5.

Abstract: A novel monoclonal antibody that specifically recognizes phosphatidylinositol-3,4-biphosphate (PI-3,4-P2) but does not cross-react with structurally similar phospholipid antigens is advantageous for PI-3,4-P2-specific immunoassay. The gene in the variable regions of the monoclonal antibody has been identified, which enables producing recombinant antibodies.

Abstract: A novel organic anion transporter gene participating in organic anion transport in the placenta; and an organic anion transporter which is a polypeptide encoded by the gene. A placental organic anion transporter OAT4, more particularly, a placental organic anion transporter OAT4 having the amino acid sequence represented by SEQ ID NO:2 or an amino acid sequence derived therefrom by deletion, substitution or addition of a part of the amino acids thereof. A nucleic acid (preferably DNA) having a base sequence encoding the placental organic anion transporter OAT4 or a base sequence hybridizable therewith under stringent conditions.

Abstract: The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.

Abstract: The present invention provides improved medical introducer devices which incorporate a single or multi-layer PTFE peelable sheath. Devices of the present invention are suitable for use in inserting an ancilliary medical device, e.g., a catheter, guide wire and the like, into a patient. Methods of the present invention also are disclosed which employ a precision sintering process in order to produce sheaths having excellent tear properties and optimal peelability.

Abstract: The present invention relates to the use of a dibenzocyclooctane lignan derivative of the following general formula (I) for treatment of neurodegenerative disorders: wherein R1 is H or C1-4 lower alkyl; R2, R3, R4 and R5 are respectively H, OH, C1-4 lower alkyl, C1-4 lower alkoxy, or R2 and R3 or R4 and R5 are respectively combined to form the group of —OCH2O—. Pharmaceutical preparations containing the dibenzocyclooctane lignan derivative as the active ingredient also are disclosed.

Abstract: A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5′-sulfonated ring-closed intermediate also allows for synthesis of 5′-amino- and thio-LNAs.