摘要:
A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.
摘要:
The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
摘要:
A compound of the present invention is a compound represented by a general formula (A-1) [wherein, R′ represents a hydrogen atom or an acid-dissociable, dissolution-inhibiting group, provided that at least one R′ group is an acid-dissociable, dissolution-inhibiting group, R11 to R17 each represent an alkyl group of 1 to 10 carbon atoms or an aromatic hydrocarbon group, which may include a hetero atom within the structure; g and j each represent an integer of 1 or greater, and k and q each represent an integer of 0 or greater, provided that g+j+k+q is not greater than 5; a represents an integer from 1 to 3; b represents an integer of 1 or greater, and l and m each represent an integer of 0 or greater, provided that b+l+m is not greater than 4; c represents an integer of 1 or greater, and n and o each represent an integer of 0 or greater, provided that c+n+o is not greater than 4; and A represents a group represented by a general formula (Ia) shown below, a group represented by a general formula (Ib) shown below, or an aliphatic cyclic group].
摘要:
This invention is directed to the crystalline potassium salt of a lipoxin A4 analog of Formula (I): processes for preparing the crystalline potassium salts, methods for using them to treat disease-states characterized by inflammation, and pharmaceutical compositions comprising such crystalline potassium salts.
摘要:
The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
摘要:
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
摘要:
This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.
摘要:
The naphthyloxyacetic acid derivatives of the formula (I) 1 wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is nullSnull, nullSOnull, nullSO2null, nullOnull or nullNR4null; L is alkylene, null(CH2)mnullCHnullCHnull(CH2)nnull or null(CH2)xnullCH(OH)null(CH2)ynull; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.
摘要:
An industrially advantageous process for producing an aryloxyacetic acid represented by the formula (2): wherein m represents an integer of 1 or 2, n represents an integer from 0 to 4, Ar represents a aromatic hydrocarbon ring, each Rs independently represents an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, a cycloalkoxy group, an aryloxy group, a halogen atom, an alkylcarbonyl group, an arylcarbonyl group, a carboxyl group or a nitro group, comprising a step in which an oxygen-containing gas is made act on an aryloxyethanol represented by the formula (1): (R)n-Ar&Parenopenst;O—CH2.CH2.OH)m (1) wherein m, n, Ar, and R, respectively, have the same meanings as defined above, under conditions of using a catalyst comprising palladium and an indium compound and/or a copper compound in an aqueous medium and in the presence of 0.5 m or more equivalent of alkali per one mole of the aryloxyethanol represented by the formula (1); or under conditions of using a platinum catalyst, in an aqueous medium and in the absence of alkali or in the presence of less than 0.5 m equivalent of alkali per one mole of the aryloxyethanol represented by the formula (1).
摘要:
The invention relates to a polymeric optical amplifier doped with lanthanide ions, which are present in the amplifier in the form of a complex.The invention also relates to novel electrically neutral lanthanide complexes which can be applied with advantage in the above-described polymeric optical amplifiers. These complexes comprise host molecules which readily complex with the lanthanide and fully encapsulate it.