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:
A compound of the formula (I): wherein: for example, a compound below: wherein: R1 is CH3, H or Na; and X1—X2—X3 is: or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
摘要:
An inhibitor for an inflammatory cell infiltration in the respiratory tract, an inhibitor for hyperirritability in the respiratory tract, a muciparous inhibitor, or a bronchodilator which contains as an active ingredient a compound represented by the formula (I) or (II): wherein R1 is the group represented by the formula: —C(=Z)-W—R4 wherein Z is an oxygen atom or the like; W is an oxygen atom or the like; R4 is optionally substituted alkyl or the like; R2 and R3 are independently optionally substituted alkyl or the like; or R2 and R3 are taken together to form optionally substituted alkylene which may contain a heteroatom(s); m is an integer of 0 to 2; A is optionally substituted aryl or optionally substituted heteroaryl; wherein R5 is the group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 and Y3 are each independently a bond or the like; Y2 is —C(═O)—NRb— or the like; Ra is optionally substituted alkyl, or the like; Rb is a hydrogen atom or the like; R6 is a hydrogen atom or the like; R7 and R8 are each independently optionally substituted alkyl or the like; or R7 and R8 are taken together with the adjacent carbon atoms to form a 5 to 8 membered ring which may contain a heteroatom(s) and/or an unsaturated bond(s); R9 is optionally substituted alkyl which may contain a heteroatom(s) and/or an unsaturated bond(s), or the like; X is a oxygen atom or the like.
摘要翻译:用于呼吸道炎症细胞浸润的抑制剂,呼吸道中的高刺激性抑制剂,粘液抑制剂或支气管扩张剂,其含有由式(I)或(II)表示的化合物作为活性成分:其中R 其中Z为氧原子等;其中Z为氧原子等;其中Z为氧原子等;其中Z为氧原子等; W是氧原子等; R 4是任选取代的烷基等; R 2和R 3独立地是任选取代的烷基等; 或R 2和R 3一起形成任选取代的可含有杂原子的亚烷基; m为0〜2的整数; A是任选取代的芳基或任选取代的杂芳基; 其中R 5为由下式表示的基团:-Y 1 -Y 2 -Y 3 -R 其中Y 1和Y 3各自独立地为键或类似物; Y 2是-C(-O)-NR B 2 - 等; R a是任选取代的烷基等; R b是氢原子等; R 6是氢原子等; R 7和R 8各自独立地是任选取代的烷基等; 或R 7和R 8与相邻的碳原子一起形成可含有杂原子和/或不饱和键的5至8元环 (s); R 9是可以含有杂原子和/或不饱和键的任选取代的烷基等; X是氧原子等。
摘要:
The present invention provides a pharmaceutical composition for use as a Th2 differentiation inhibitor comprising a compound represented by Formula (I): wherein each of ring A, ring B and ring C is an aromatic carbocyclic ring, a heterocyclic ring and the like, X is a single bond, —O—, —CH2—, —NH—, —SO— and the like, Y is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl and the like, each of V1 and V2 is a single bond, —O—, —NH—, —OCH2— and the like, a prodrug, pharmaceutically acceptable salt or solvate thereof.
摘要:
A compound of the formula (I): wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1—X2—X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
摘要:
A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(═O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(═O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.
摘要翻译:式(I)的化合物:其中A是任选具有不饱和键的亚烷基; R是-C(-O)-R 1; R 1是羟基等; m为0或1; p为0或1; X 1和X 3各自独立地是任选取代的芳基或任选取代的杂芳基等; X 2是一个键,-CH 2 - , - S - , - SO 2 - , - CH 2 ,-O-CH 2 - , - CH 2 -S-,-S-CH 2 - 等 ; X 4是-CH 2 - , - CH 2 -CH 2 - , - C( - O) 发现具有针对血栓素A 2 O 2受体和前列腺素D 2受体的双重拮抗活性的 - 等等。
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:
A compound, pharmaceutically acceptable salt thereof, or hydrate thereof having a PGD.sub.2 -antagonistic activity, and an inhibitory activity against infiltration of eosinophils, useful for treating mast cell dysfunction-associated diseases, such as systemic mastocytosis and disorder of systemic mast cell activation, as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, inflammation and atopic dermatitis, which is shown by the formula (I): ##STR1## is provided.
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 present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them.A compound of the formula (I): wherein R1 is —CH2—CH═CH—CH2—CH2—CH2—COOR2 or —CH═CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(═O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.