Preventives/remedies for glaucoma
AssigneesSenju Pharmaceutical Co., Ltd., Mitsubishi Pharma Corporation
InventorsMitsuyoshi Azuma, Yukuo Yoshida, Mitsunori Waki, Masayoshi Uehata
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Abstract
An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.
Claims9
A method for the treatment of glaucoma, which comprises administering an effective amount of a compound having a Rho kinase inhibitory activity to a patient in need thereof, wherein the compound having the Rho kinase inhibitory activity is an amide compound of formula (I′):
- wherein
- Ra′ is a group of the formula
- wherein
- R′ is hydrogen, alkyl, or cycloalkyl, cycloalkylalkyl, phenyl or aralkyl, which optionally has a substitutent on the ring,
- R1 is hydrogen, alkyl, or cycloalkyl, cycloalkylalkyl, phenyl or aralkyl, which optionally has a substituent on the ring, or R′ and R1 in combination form, together with the adjacent nitrogen atom, a heterocycle optionally having, in the ring, oxygen atom, sulfur atom or optionally substituted nitrogen atom,
- R2 is hydrogen or alkyl,
- R3 and R4 are the same or different and each is hydrogen, alkyl, aralkyl, halogen, nitro, amino, alkylamino, acylamino, hydroxy, alkoxy, aralkyloxy, cyano, acyl, mercapto, alkylthio, aralkylthio, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl or azide, and
- A is a group of the formula
- wherein
- R10 and R11 are the same or different and each is hydrogen, alkyl, haloalkyl, aralkyl, hydroxyalkyl, carboxy or alkoxycarbonyl, or R10 and R11 in combination form, together with the adjacent carbon atom, a cycloalkyl, and l, m and n are each 0 or an integer of 1-3,
- Rb is hydrogen, an alky, an aralkyl, an aminoalkyl or a mono- or dialkylaminoalkyl;
- and
- Rc is an optionally substituted heterocycle containing nitrogen,
- an isomer thereof or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.