Abstract: The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.

Abstract: The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.

Abstract: This invention relates to a monolayer sugar-coated tablet which is coated with a sugar-coating liquid containing 30–54% by weight of saccharide, 2–10% by weight of polyethylene glycol and 0.2–2% by weight of polyvinylpyrrolidone, and a process for preparing the same. According to the invention, a monolayer sugar-coated tablet and a process for preparation thereof are provided with very great economical advantages that the skill required for conventional sugar-coating processing is unnecessary and furthermore consumption of sugar-coating material can be reduced and the processing time can be shortened.

Abstract: Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, —OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula —X—NR4R5, or the like.

Abstract: Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)—(A)n—Y, —CH2—CH(R4)—(A)n—Y, —CO—B1—A—Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.

Abstract: The present invention relates to a simple immunochemical semi-quantitative assay method according to chromatography, which comprises trapping a certain amount of an analyte in a sample with a predetermined amount of a fixed antibody for the analyte before qualitative analysis of the analyte, the certain amount corresponding to the amount of the fixed antibody, and thereby decreasing a concentration of the analyte to be subjected to subsequent immunochemical qualitative determination, and an apparatus therefor.

Abstract: Aminopyrazole derivatives represented by formula (I), or salts thereof, wherein X1 and X2 are each a hydrogen atom or a halogen atom, or X1 and X2 may be united together to form a lower alkylenedioxy group, Q is a pyridyl group or a quinolyl group, R1 is a hydrogen atom, a substituted or unsubstituted lower alkyl or aryl group, R2 is a hydrogen atom, a lower alkyl group, or an aralkyl group, and R3 represents a hydrogen atom, an organic sulfonyl group, or —C(═Y)—R4 in which R4 is a hydrogen atom or an organic residue and Y is an oxygen or sulfur atom, provided that, when R3 is a hydrogen atom, R1 is a group other than a hydrogen atom and R2 is a hydrogen atom. These amimopyrazole derivatives or their salts have excellent p38MAP kinase inhibiting activities and are hence useful in the prevention or treatment of diseases associated with tumor necrosis sis factor &agr;, interleukin 1, interleukin 6 or cyclooxygenase II.

Abstract: 4,5-Dihydro-[1H]-benz[g]indazole-3-carboxylic acid derivatives represented by the following formula, or their salts, have excellent antagonism to endothelin receptors and are useful as preventives or remedies for diseases such as hypertension, angina pectoris, myocardial infarction, brain infarction, cerebrovascular contraction, renal insufficiency, hepatic dysfunction, arteriosclerosis and post-PTCA restenosis. wherein Ar represents an optionally substituted aryl group, and R1 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted aryl group, an optionally substituted cycloalkyl group or an optionally substituted heterocyclic group.

Abstract: The present invention relates to a simple immunochemical semi-quantitative assay method according to chromatography, which comprises trapping a certain amount of an analyte in a sample with a predetermined amount of a fixed antibody for the analyte before qualitative analysis of the analyte, the certain amount corresponding to the amount of the fixed antibody, and thereby decreasing a concentration of the analyte to be subjected to subsequent immunochemical qualitative determination, and an apparatus therefor.

Abstract: A peptide derivative represented by the following formula or a salt thereof ##STR1## wherein A represents a hydrogen atom, and B represents a phenyl group substituted with a hydroxyl group;said derivative has an antitumor activity stronger than that of dolastatin 10, and is useful as an anticancer or antitumor agent.

Abstract: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.

Abstract: A benzothiophene compound represented by a formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, and R.sup.2 represents a halogen atom; a lower alkyl group; or a cycloalkyl group or cycloalkenyl group which may optionally be substituted with a lower alkyl group, a hydroxy group, an acyloxy group or an oxo group,which is a useful intermediate for synthesizing a 2-sub-stituted-3-(4-substituted benzoyl)-6-hydroxybenzo[b]-thiophene derivative having an antiestrogenic activity can be produced in an industrially advantageous manner by subjecting a compound represented by a formula: ##STR2## to a ring-closing reaction. Further, the novel compound of the formula (II) described above is a useful intermediate in the process of the present invention.

Abstract: A tetrapeptide derivative represented by the following formula or a salt thereof has a higher cytostatic activity than dolastatin 10, and is useful as an antitumor agent: ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represent a hydrogen atom, a lower alkyl group or an aralkyl group;Q represents ##STR2## or a group of -A.sub.2 -R.sub.7, wherein, A.sub.1 represents a direct bond or ##STR3## Y represents a hydrogen atom or --COR.sub.6, R.sub.5 represents a hydrogen atom, a lower alkyl group or an aralkyl group,R.sub.6 represents a hydroxyl group, a lower alkoxy group, an aralkyloxy group or ##STR4## wherein, R.sub.8 and R.sub.9 are the same or different and each represent a hydrogen atom, a lower alkyl group, a phenyl group or a 4- to 7-membered heterocyclic group containing one or two hetero atoms selected from S, O and N, or alternativelyR.sub.8 and R.sub.

Abstract: The invention relates to a specific cyclooxygenase 2 inhibitor which comprises, as an active ingredient, 2-(2,6-dichloro-4-hydroxyanilino)phenylacetic acid represented by the following formula (1): ##STR1## or a salt thereof, as an anti-inflammatory agent. The compound specifically inhibits cyclooxygenase 2 without inhibiting cyclooxygenase 1 activity and thus it is low in toxicity and safe.

Abstract: A plane heater is mounted on the lower surface of an air mat having a function of preventing bedsore, and the temperature of a patient is maintained via an air layer of the air mat. A time delay caused by heating via the air layer is adjusted through prediction control.

Abstract: In pharmaceutics for mucosal administration containing pharmacologically active peptides or proteins and tolmetin or salts thereof exhibited very excellent effect as mucosal absorption enhancers.Furthermore, when the pharmaceutics for mucosal administration are for rectal administration, the suppository in which at least either the active ingredient, peptide or protein, or the mucosal absorption enhancer is converted to a complex with a high molecular compound dissolving in water at pH 5 or higher and together uniformly dispersed in a fatty suppository base exhibited markedly improved rectal absorbability compared with that of conventional pharmaceutics for rectal administration and at the same time increased stability of the peptide or protein which is the active ingredient.

Abstract: This invention relates to peptide derivatives of the formula ##STR1## or salts thereof, wherein: (a) Q.sub.1 represents a 1-dimethylamino-2-methylpropyl group and Q.sub.2 represents an (R)- or (S)-2-hydroxy-2-phenylethylamino group, a 2-phenylcyclopropylamino group or a 1,2,3,4-tetrahydroisoquinolin-2-yl group, or(b) Q.sub.1 represents a 1-methyl-2-pyrrolidinyl group and Q.sub.

Abstract: An interface is formed by incorporating (1) a mixture comprising a water-soluble protein and a drug into a matrix, or preferably (2) a mixture comprising a water-soluble protein and a drug to a porous matrix coated with a cationic surfactant or other ionic surfactant. The coating amount of the ionic surfactant is about 0.1 to 50 .mu.g, and the content of the water-soluble protein is about 0.1 to 1,500 .mu.g, each per 1 cm.sup.2 of the matrix. The water-soluble protein includes an albumin and the drug includes a physiologically active peptide or protein, for example. The use of the stabilized interface inhibits decrease of the drug retaining amount, and insures an effective transdermal drug delivery with a high repeatability and accuracy.

Abstract: A peptide derivative represented by the following formula or a salt thereof ##STR1## wherein A and B each represent either of the following (a) and (b), (a) A represents a hydrogen atom, and B represents a phenyl group substituted with a halogen atom, hydroxyl group, lower alkyl group or lower alkoxy group, or a heteroaryl group,(b) A represents --CONH--R.sup.1, --CSNH--R.sup.1, a hydroxymethyl group, a lower alkoxycarbonyl group or a carboxyl group, wherein, R.sup.1 represents a lower alkyl group or a heteroaryl group, and B represents a phenyl group optionally substituted with a halogen atom, hydroxyl group, lower alkyl group or lower alkoxy group,has an antitumor activity stronger than that of dolastatin 10, and is useful as an anticancer or antitumor agent.

Abstract: A calcitonin, its derivative or a salt thereof is transdermally delivered by iontophoresis in which a substantially constant voltage in the range of 3 to 20 V is applied at an electric current of 0.05 to 0.5 mA/cm.sup.2. In this process, the calcitonin can be delivered transdermally with a higher absorptivity by applying a higher voltage for a short period (at a voltage of about 6 to 14 V for about 5 to 15 minutes) in the initial stage of the voltage application, and then applying a lower voltage for a long period (at a voltage of about 3 to 9 V for about 30 to 40 minutes).