摘要:
New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meanings as given above, to the reaction with N,N-dimethylethylenediamine without solvent to open the E-lactone ring followed by acylation of 17-hydroxyl group with corresponding acylating agents and an antitumor agent containing the same as an active ingredient.
摘要:
New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R.sup.4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R.sup.5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 substituents should not be a hydrogen atom and also that if any one of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.
摘要:
A thrombolytic peptide composed of 136 amino acids residues, which has little problems of antigenicity and is efficacious in only small doses as compared with staphylokinase (SAK). This peptide is obtained by cleaving amino acids or peptides which do not affect the activity of SAK by using a trypsin protease. In particular, SAK-11, which is obtained by cleaving a peptide composed of ten amino acid residues at the N-terminal of SAK, is superior to SAK in the fibrinolysis, plasminogen activation, and fibrin specificity.
摘要:
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.
摘要:
An antiulcer agent effective on prevention of ulceration and acceleration of healing of ulcers and processes for preparing the same are disclosed. The antiulcer agent comprises rhamnan (a homopolysaccharide), rhamnose or a rhamnose oligomer as an active ingredient. Rhamnan is prepared by separating rhamnan sulfate from rhamnan sulfate-containing algae and desulfurating the rhamnan sulfate. Rhamnan oligomers are prepared by hydrolyzing rhamnan obtained by desulfuration of rhamnan sulfate or by hydrolyzing microbial cells of a Bifidobacterium or polysaccharides separated therefrom.
摘要:
An antitumor agent is provided by including, as an active ingredient, a polysaccharide-glycan complex obtained by treating a Gram-positive bacteria such as lactic acid bacteria and Bifidobacterium strains with a cell wall lytic enzyme produced by a bacterium belonging to the genus Achromobacter.The polysaccharide-glycan complex has no toxicity and causes no side effect. Being water-soluble, it is easily formulated into any arbitrary dose form, such as an injectable solution. It can easily be prepared from an easily available starting material.
摘要:
The present invention relates to antihypertensives and food and drinks, containing as effective component polysaccharideglycopeptide complexes derived from cell wall of Gram positive bacteria (also referred to as peptidoglycan). The present invention provides extremely strong and safe antihypertensives and food and drinks, which may exert hypotensive effects if administered orally to spontaneous hypertensive rats and renal hypertensive rats at a single dose as low as 1 mg/kg.
摘要:
New peptides represented by the following general formula (wherein X is OH or NH2, R is an amino acid residue selected from Arg, His, Lys, Methyl-Arg or Methyl-Tyr, n is an integer of 1-4, and in the case that n is 2-4, R may be identical with or different from each other) and an anti-dementia drug which contains one or more of these new peptides and has a high blood brain barrier (BBB) permeability and furthermore is low in a side effect.
摘要:
A diarylheptanoide derivative of the following formula (1), ##STR1## and a drug composition comprising this compound, such as a 5-lipoxygenase inhibitor, an antiinflammatory agent, and the like. The diarylheptanoide derivative (1) is effective for treating and preventing various inflammatory diseases due to its strong 5-lipoxygenase inhibiting effect.