Abstract: Hydrates of N-[1-butyl-4-[3-[3-(hydroxy)propoxy]-phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N?-(2,6-diisopropyl-4-aminophenyl)urea hydrochloride of the formula: are quite excellent in stability than amorphous one and are more preferable for medicaments.

Abstract: It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III): (II) (III) (wherein m is 0 or 1; n is an integer of from 1 to 3; Y represents OH or NH2; and a dotted line shows a binding position), provided that when R2 is a group of the general formula (III), X represents NHCO or NHCH2; R3 and R4 independently represent each hydrogen or C1-6 alkyl; and Ar represents phenyl substituted by C1-6 alkyl at the o- and m-positions, optionally substituted heteroaryl or a bicyclic aromatic group; its pharmaceutically acceptable salt, and a remedy containing the above uracil derivative or its pharmaceutically acceptable salt as the active ingredient for, in particular, allergic diseases relating to a type IV allergic reaction, i.e.

Abstract: The present invention provides a lyophilized preparation of amrubicin, which contains L-cysteine or a salt thereof and has a water content of 0 to about 4% by weight within the preparation, and is stable even in a long-term storage, and further provides a method for production of said preparation. Said preparation is useful as a chemotherapeutic agent for cancers.

Abstract: Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2): (1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention can provide novel compounds useful as orally administrable growth hormone releaser, more specifically a benzimidazolidinone derivative of formula (1) or a pharmaceutically acceptable salt thereof: (1) wherein R1 is optionally substituted alkyl or the like; R2, R3 and R4 are each hydrogen, optionally substituted alkyl, or the like; R5 is optionally substituted aryl; q is 0 or 1; and W1 is a group represented by formula (2): (2) n is 1, 2 or 3; m is 0, 1, 2 or 3; R6 and R7 are each hydrogen, optionally substituted alkyl, or the like; and R8 and R9 are each hydrogen, optionally substituted alkyl, or the like.

Abstract: The present invention relates to a transdermal administration preparation for external application such as ointment, cream and the like, which contains SMP-114 or leflunomide or a pharmaceutically acceptable acid addition salt thereof as an active ingredient. The present invention further relates to a pharmaceutical composition for transdermal administration which contains, a) as an active ingredient, N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide or an active motabolite thereof or a pharmaceutically acceptable salt thereof; and B)(1) a carrier for transdermal administration which contains a base for dissolution in a proportion of not less than 40 w/w %, or (2) a carrier for transdermal administration which contains a hydrophobic base for suspension having no polar group in a molecule in a proportion of not less than 70 w/w %.

Abstract: The present invention provides an impaired glucose tolerance ameliorating drug and a therapeutic drug for lifestyle-related diseases, particular an antidiabetic drug, which contain a CXCR3 agonist as an active ingredient; a hypoglycemia ameliorating drug, a therapeutic drug for insulinoma or an anti-obesity drug containing a CXCR3 antagonist as an active ingredient; a method of screening for a new CXCR3 ligand using CXCR3 and a known CXCR3 ligand; a method of screening a CXCR3 ligand, which uses a co-expression system of CXCR3 and a coupling G protein; and a diagnostic method for type II diabetes, which includes detecting an amount of a CXCR3 ligand expressed in a biological sample.

Abstract: The invention presents a preparation for continuous intravenous administration containing hepatocyte growth factor (HGF) as an active ingredient. The preparation for continuous administration of the invention is effective at a lower dose as compared with single or frequent bolus administration of HGF, and therefore side effects can be reduced.

Abstract: Pyrrole derivatives represented by the following formula: 1

Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.

Abstract: Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof. These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.

Abstract: The present invention relates to a therapeutic agent for cartilaginous diseases, an accelerator for chondrocyte proliferation and an accelerator for proteoglycan production comprising HGF (hepatocyte growth factor) as an active component, and a treatment method for cartilaginous diseases of human or mammals comprising administering an effective amount of HGF. The active component HGF has an effect to promote the proliferation of chondrocytes and to promote the production of proteoglycan. Therefore, the therapeutic agent and accelerator of the present invention are useful for the prevention and treatment of various disorders caused by cartilaginous diseases.

Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.

Abstract: An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3 and R4 are independently hydrogen, optionally substituted alkyl etc; R5 is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1 and W2 is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1 and W2 is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3 alkylene; R6 and R7 are independently hydrogen, optionally substituted alkyl etc; R8 and R9 are independently hydrogen, optionally substituted alkyl etc; R10 and R11 are independently hydrogen, alkyl etc.

Abstract: L-ascorbic acid, L-ascorbic acid derivatives and salts thereof can reduce lactic acid levels in blood, and are useful for treating lactic acidosis and the like caused by administration of amoxapine, theophylline, metformin, phenformin, buformin, nalidixic acid, hopantenic acid, azidothymidine, dideoxycytidine, high caloric transfusion, propylene glycol, ethylene glycol, xylitol, lactose, sorbitol or the like.

Abstract: The present invention relates to a therapeutic agent for cartilaginous diseases, an accelerator for chondrocyte proliferation and an accelerator for proteoglycan production comprising HGF (hepatocyte growth factor) as an active component, and a treatment method for cartilaginous diseases of human or mammals comprising administering an effective amount of HGF. The active component HGF has an effect to promote the proliferation of chondrocytes and to promote the production of proteoglycan. Therefore, the therapeutic agent and accelerator of the present invention are useful for the prevention and treatment of various disorders caused by cartilaginous diseases.

Abstract: The present invention relates to a method for treating fibrosis caused by excessive collagen deposition. The method involves administering Hepatocyte Growth Factors (HGFs). The HGFs accelerate the decomposition of the collagen when administered in an effective amount.

Abstract: The invention provides methods and compositions relating to CPF proteins which regulate transcriptional activation, and related nucleic acids. The polypeptides may be produced recombinantly from transformed host cells from the disclosed CPF encoding nucleic acids or purified from human cells. The invention provides isolated CPF hybridization probes and primers capable of specifically hybridizing with the disclosed CPF genes, CPF-specific binding agents such as specific antibodies, and methods of making and using the subject compositions in diagnosis, therapy and in the biopharmaceutical industry.

Abstract: A &bgr;-lactam compound of the formula: wherein R1 is lower alkyl or OH-substituted lower alkyl, R2 is H or lower alkyl, X is O, S or NH, n is 1 to 3, R3 is —C(Ra)═NH (Ra is H, lower alkyl or substituted lower alkyl), or a salt thereof, or an ester thereof. These compounds show excellent antibacterial activity against Gram-positive bacteria, particularly against methicillin-resistant Staphylococci and methicillin-resistant and coagulase-negative Staphylococci.

Abstract: Novel indoloylguanidine derivatives shown by formula (1), wherein R1 represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: —OR3, —NR6R7, —SO2NR6R7 or —S(O)nR40; and R2 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: —CH2R20; and which inhibit the Na+/H+ exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na+/H+ exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caus