Abstract: To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

Abstract: A pyrazine derivative of the following formula (I): wherein R1 is hydrogen or optionally substituted lower alkyl; X is hydrogen, halogen, hydroxy, cyano, acyl, or amino, aryl, heterocyclic group or the like; Y is hydrogen, halogen, hydroxy, acyl, amino, or the like; Z is aryl or heteroaryl, each of which is optionally substituted; or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

Abstract: A pyrazine derivative of the following formula (I): wherein R1 is hydrogen or optionally substituted lower alkyl; X is hydrogen, halogen, hydroxy, cyano, acyl, or amino, aryl, heterocyclic group or the like; Y is hydrogen, halogen, hydroxy, acyl, amino, or the like; Z is aryl or heteroaryl, each of which is optionally substituted; or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

Abstract: An aminopyrimidine compound of the following formula (I) wherein Q is (a) or (b) in which R and R? are each optionally substituted aryl or heterocyclic group,R5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R1 is hydrogen, optionally substituted lower alkyl or cyclo(lower) alkyl which may be interrupted by an oxygen atom; R2 and R3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R2 and R3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g.

Abstract: A thiazole derivative of the formula (I): wherein R is a 1-optionally substituted-6-oxo-1,6-dihydro-3-pyridazinyl, R? is an optionally substituted phenyl, and R2 is hydrogen, a group of the formula (i): wherein R4 is hydrogen, lower alkyl or lower alkenyl, and R5 is hydrogen, optionally substituted lower alkyl, acyl, cyclo(lower)alkyl, lower alkenyl, optionally substituted aryl or heterocyclic, or a group of the formula (ii): wherein X is oxygen or sulfur, R8 is hydrogen or lower alkyl, R9 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, lower alkoxy or mono- or di-lower alkylamino or R8 and R9 may combine together to form optionally substituted saturated N-containing heterocyclic, or a salt thereof.

Abstract: The present invention relates to a linker shown by the following formula (I):

Abstract: The present invention relates to a linker shown by the following formula (I): X—SO2—R1—(A)m—R2  (I) wherein R1 is a group of the formula (A): [wherein R3, R4 and R5 are the same or different hydrogen, etc], etc, R2 is a group which can form a chemical bond to a resin which may be protected by a conventional protective group, A is lower alkylene, etc, X is a leaving group, and m is an integer of 0 or 1, with proviso that A is (C2-C6)alkylene, and m is an integer of 1, when R1 is a group of the formula (A).

Abstract: A compound of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is 1-hydroxyethyl,R.sup.3 is methyl,R.sup.4 is optionally substituted pyridyl(lower)alkyl, optionally N-substituted 2-oxopiperazin-1-yl-(lower)alkyl, optionally substituted imidazol-1-yl(C.sub.2 -C.sub.3)alkyl, optionally substituted imidazol-5-yl-(lower)alkyl, optionally substituted imidazol-2-yl-(lower)alkyl, optionally substituted pyrazol-4-(or 5-)yl(lower)alkyl, optionally substituted pyrazol-1-ylethyl, optionally substituted triazolyl(lower)alkyl, optionally substituted pyrimidinyl(lower)alkyl, optionally substituted dihydropyrimidinyl(lower)alkyl, or optionally substituted (2,3-dihydroimidazo-[1,2-b]pyrazol-1-yl)ethyl, andR.sup.5 is hydrogen or imino-protective group,and pharmaceutically acceptable salts thereof, which have antimicrobial activity.

Abstract: Novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and processes for their preparation are disclosed. These novel compounds have antimicrobial activity, and are useful as a medicament in the treatment of infectious diseases in human beings and animals.

Abstract: A compound represented by the following general formula: ##STR1## which is useful as an intermediate for production of a clinically excellent synthetic antibacterial, a salt thereof, and a process for producing the same.In said formula,R.sup.1 is a hydrogen atom or a carboxyl-protecting group;R.sup.2 is a hydrogen atom or a lower alkyl group;X.sup.1 is a hydrogen atom or a halogen atom;X.sup.2 is a halogen atom;X.sub.a.sup.5 is a hydrogen atom or a halogen atom;A is a methylene group; a group of >CH--COOR.sup.4, etc.,in which R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom or a carboxyl-protecting group;B is a methylene group or a carbonyl group;provided that both A and B must not be methylene groups at the same time.

Abstract: The invention relates to carbapenem derivatives useful as antimicrobial agents, more particularly to intermediate compounds for the preparations thereof of the formula ##STR1##

Abstract: 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds of the formula: ##STR1## in which R.sup.1 is carboxy, COO.sup.-- or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.8 is hydrogen or lower alkyl,Z is a group of the formula: ##STR2## wherein R.sup.3 is hydrogen; lower alkyl or lower alkenyl, each of which is optionally substituted by the group consisting of lower alkoxy, carbamoyl, hydroxy, halogen, mono(or di)(lower)alkylcarbamoyl, mono(or di)(lower)alkenylcarbamoyl, mono(or bis)[hydroxy(lower)alkyl]carbamoyl, optionally substituted cyclic-aminocarbonyl, acylamino, ureido, optionally substituted heterocyclic-carbonylamino, carbamoyloxy, mono(or di)(lower)alkylcarbamoyloxy, lower alkylthio, halo(lower)alkylthio, optionally substituted heterocyclicthio, optionally substituted heterocyclic group, optionally substituted aryl, and acyl;R.sup.9 is hydrogen or lower alkyl, andR.sup.

Abstract: Novel carbapenem compounds of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is unsaturated bicyclic heterocyclic group which may be substituted by suitable substituent(s),R.sup.5 is hydrogen or imino-protective group, andA is lower alkylene,or pharmaceutically acceptable salts thereof.Processes for their preparation and pharmaceutical compositions for the treatment of infectious diseases are also disclosed.

Abstract: The present invention concerns intermediates in the preparation of novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof. The novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof show antimicrobial activity.

Abstract: Novel 3-pyrrolidinylthio-1-azabiycyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof have antimicrobial activity and are useful as medicaments in the treatment of infectious diseases caused by pathogenic microorganisms.