Asahi Kasei Pharma Corporation

Rintaro Yamada

Minoru Seto

Kenichiro Sato

Koki Matsubara

Shunsuke Kaneko

Daisuke Shikanai

Akifumi Oomura

Koh Kawasaki

Katsuhiko Sakurada

Atsushi Iesato

A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; Grepresents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; Grepresents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; Grepresents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; Grepresents hydroxyl group, or &#x2014;N(R)(R) (Rand Rrepresent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, or a saturated heterocyclic group); Gis a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase. 

Sulfonamide compound

The present invention relates to a compound represented by the following formula (1): wherein D, A, D, R, D, and Reach have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK&#x3b2; inhibiting activity and the like and is useful for the prevention and/or treatment of IKK&#x3b2;-associated diseases or symptoms and the like.

8-substituted isoquinoline derivative and the use thereof

A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; Grepresents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; Grepresents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Grepresents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or &#x2014;C(R)(R)&#x2014; (Rand Rrepresent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); Grepresents hydroxyl group (Y is a single group), or &#x2014;N(R)(R) (Rand Rrepresent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, a saturated heterocyclic group, an alkylsulfonyl group, an acyl group, or an amidino group); Gis a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase. 

A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; Grepresents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; Grepresents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; Grepresents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; Grepresents hydroxyl group, or &#x2014;N(R)(R) (Rand Rrepresent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, or a saturated heterocyclic group); Gis a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits phosphorylation of the myosin regulatory light chain. 

A novel compound represented by the formula (1): [Rrepresents hydrogen atom, chlorine atom, or hydroxyl group; X. . . Xrepresents&#x2014;CH(R)&#x2014;CH(R)&#x2014;, &#x2014;CH(R)&#x2014;CH(R)&#x2014;CH(R)&#x2014;, etc.; Rto Rrepresent hydrogen atom, or an alkyl group; A, A, A, and Arepresent hydrogen atom, or an alkyl group; Y represents &#x2014;CH(A)&#x2014;, &#x2014;CH(A)&#x2014;C(A)(A)&#x2014;, &#x2014;CH(A)&#x2014;C(A)(A)&#x2014;C(A)(A)&#x2014;, or a single bond; A, A, A, A, and Arepresent hydrogen atom, or an alkyl group; Z represents hydroxyl group, or &#x2014;N(A)(A); Arepresents hydrogen atom, or an alkyl group, Arepresents hydrogen atom, an alkyl group, an aralkyl group, etc.; and groups in each of one or more combinations selected from the group consisting of combinations of Aand A, Aand A, Aand A, Aand A, Aand A, Aand A, Aand A, Aand A, and Aand Amay bind to each other to form a 5- or 6-membered ring], or a salt thereof, which potently inhibits the phosphorylation of myosin regulatory light chain.

Tricyclic compound

A compound represented by the following formula (1) or a salt thereof: wherein Rrepresents hydrogen atom, a halogen atom and the like; Rrepresents hydrogen atom, a halogen atom, a Calkyl group and the like; and Rrepresents &#x2014;O&#x2014;X&#x2014;C(A)(A)-C(A)(A)-N(A)(A) (X represents propylene group etc., Aand Arepresent hydrogen atom, or a Calkyl group, Arepresents a Calkyl group substituted with hydroxyl group, or hydrogen atom, and A, A, and Arepresent hydrogen atom, a Calkyl group and the like) and the like, which has an inhibitory activity on the phosphorylation of myosin regulatory light chain, and is useful for treatment of diseases relating to contraction of various cells and the like.

Growing community of inventors

Tokyo, Japan

Rintaro Yamada