Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).
The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.
Abstract: Human RelA-associated inhibitor (RAI) comprising 351 amino acid, process for producing it, cDNA encoding it, fragment capable of hybridizing selectively to the cDNA sequence, plasmid for expression and duplication comprising the cDNA, host cell transformed with the plasmid, antibody against the polypeptide, pharmaceutical composition comprising the polypeptide or the antibody against it and method for diagnosis of diseases using the antibody against the RAI.
Abstract: The invention discloses a useful and novel factor (polypeptide) which plays an important role for morbid vascular smooth muscle in restenosis after percutaneous transluminal coronany angioplasty (PTCA) and arterial sclerosis in the field of cardiovascular system.
Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I)
(wherein all symbols are as defined in the specification), or a salt thereof as active ingredient.
Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.
Abstract: A &ohgr;-substituted phenyl-prostaglandin of formula (I), a process for the preparation thereof, a mediciament comprising it as active ingredient (all symbols have the same meaning as described in the specification).
The compounds of the formula (I) bind strongly in PGE2 receptor (especially subtype EP4) and therefore are useful for the prophylaxis and/or treatment of immune diseases (autoimmune diseases (amyotrophic lateral sclerosis (ALS) etc.), post-transplantation graft rejection, etc.), asthma, abnormal bone formation, neurocyte death, pulmopathy, hepatopathy, etc. They are also related to sleeping disorders and platelet coagulations, and therefore they are also applicable to these diseases.
Abstract: Human ReIA-associated inhibitor (RAI) comprises 351 amino acids and is capable of binding to p65, a subunit of the transcription factor NF&kgr;B. A process for producing RAI, a cDNA encoding it, a fragment capable of hybridizing selectively to the cDNA sequence, a plasmid for expression and duplication comprising the cDNA, a host cell transformed with the plasmid, an antibody against the polypeptide, a pharmaceutical composition comprising the polypeptide or the antibody against it and a method for diagnosis of diseases using the antibody against the RAI are disclosed.
Abstract: Novel amidinophenol derivatives of formula (IB)
and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)
Abstract: A &ohgr;-cycloalkyl-prostaglandin E2 derivatives of the formula (I)
wherein R is carboxy or hydroxymethyl; R1 is oxo, methylene or halogen atom; R2 is H, OH or C1-4 alkoxy; R3 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkoxy, C3-7 cycloalkyl, phenyl, or phenyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkyl, C1-4 alkoxy, nitro, trifluoromethyl; n is 0-4;
and non-toxic salt thereof, prodrug thereof and cyclodextrin clathrate thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immune disease (autoimmune disease, organ transplantation, etc.), asthma, abnormal bone formation, neuron cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.
Abstract: Polymers derived from polymers represented by Formula (A) (d is 20˜500; and Rs, which may be the same or different, represent each H, alkyl or benzyl) by substituting a part or all of the consisting peptide bonds by (1) hydrazino-Glu (Formula B), and saccharide-modified Glu (Formula C) or by (2) hydorazino-Glu (Formula B), and saccharide-modified Glu (Formula C), and drug bonded Glu (Formula D). These polymers, which are carriers optionally bonded to drugs capable of migrating into target organs (cells), are useful as medicines.
Abstract: Aminobutylic acid derivatives of the formula (I)
wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.
Abstract: A novel monoclonal antibody against glyceraldehyde-3-phosphate dehydrogenase (GAPDH), its use and a hybridoma strain NCK-J24 which produces the antibody.
Abstract: The present invention relates to a fused thiophene derivative of the formula (I) (wherein all the symbols are defined as described in the specification) and an inhibitor of producing interleukin-6 and/or interleukin-12 comprising the said derivative as an active ingredient.
A fused thiophene derivative of the formula (I) is useful as an agent for the prevention and/or treatment of various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell carcinoma, Kaposi's sarcoma, rheumatoid arthritis, gammopathy, Castleman's disease, atrial myxoma, diabetes mellitus, autoimmune diseases, hepatitis, multiple sclerosis, colitis, graft versus host immune diseases, infectious diseases.
Abstract: A solution of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate (I) comprising at least one pH adjuster selected from tri-sodium phosphate, a hydrate thereof, sodium hydroxide or potassium hydroxide and a drug product using the solution. According to the invention, the solubility of the compound (I) increases and thereby it is possible to provide a solution thereof and a drug product using it. Moreover, by using a mixture of water and an organic solvent, greatly improved solubility makes it possible to manufacture a solution of higher concentration of the compound (I), and high-dosage drug products using it.
Abstract: Oxadiazole derivatives represented by formula (I):
(wherein R1 represents a hydrogen atom or an amino-protective group; R2, R3, and R4 each independently represents an alkyl group, a cycloalkyl group, a phenyl group which may be substituted, or a 3,4-methylenedioxyphenyl group, or R3 and R4 are taken together to represent a C2-6 alkylene group), a process of producing the same, and a process for producing oxadiazole derivatives represented by formula (II):
(wherein all symbols have the same meanings as described above) using the above derivative.
According to the invention, the compound represented by formula (II) is produced through fewer steps in a high yield.
Abstract: A novel monoclonal antibody against glyceraldehyde-3-phosphate dehydrogenase (GAPDH), its use and a hybridoma strain NCK-J24 which produces the antibody.
Since the monoclonal antibody produced by the hybridoma of the present invention recognizes GAPDH selectively and strongly, it can be used in screening and diagnosis of an apoptosis-concerning protein and prevention and/or treatment of neurodegenerative diseases (Alzheimer's disease, Parkinson's disease, Parkinson's syndrome, Huntington's disease, Machado-Joseph's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jacob's disease and the like) and GAPDH-concerning diseases (motor dysfunction and the like caused by spinal cord injury, spinal cord compression, cerebral ischemia, peripheral nerve injury and the like).
Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I)
(wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.
Abstract: Polymers derived from polymers represented by Formula (A) (d is 20˜500; and Rs, which may be the same or different, represent each H, alkyl or benzyl) by substituting a part or all of the consisting peptide bonds by (1) hydrazino-Glu (Formula B), and saccharide-modified Glu (Formula C) or by (2) hydorazino-Glu (Formula B), and saccharide-modified Glu (Formula C), and drug bonded Glu (Formula D).