Remedies for cirrhosis
AssigneeShionogi & Co., Ltd.
InventorsKohji Hanasaki, Minoru Ikeda, Takashi Ono
Life of this patent
Estimating the term…
Abstract
It is provided that type-X sPLA2 inhibitors are useful in preventing or treating hepatocirrhosis.
Claims15
A composition for prevention or treatment of hepatocirrhosis which contains a type-X sPLA2 inhibitor as an active ingredient.
A composition for prevention or treatment of hepatocirrhosis which contains as an active ingredient a compound represented by the formula (I):
- 21
- wherein ring a is represented by the formula (a) to (d):
- 22
- wherein R1 and R2 are each independently hydrogen atom, non-interfering substituent, or -(L1)-(acidic group) wherein L1 is an acid linker having an acid linker length of 1 to 5, provided that one of the R1 and R2 is -(L1)-(acidic group);
- R3 and R4 are each independently hydrogen atom, non-interfering substituent, carbocyclic group, carbocyclic group substituted with a non-interfering substituent(s), heterocyclic group, or heterocyclic group substituted by a non-interfering substituent(s);
- and
- —B— is represented by the formula (e) to (h):
- 23
- wherein R5 is (j) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic group, or heterocyclic group, (k) the group represented by (j) each substituted independently with at least one group selected from non-interfering substituents, or -(L2)-R8 wherein L2 is a divalent linking group of 1 to 18 atom(s) selected from hydrogen atom(s), nitrogen atom(s), carbon atom(s), oxygen atom(s), and sulfur atom(s), and
- R8 is a group selected from the groups (j) and (k);
- R6 is hydrogen atom, halogen, C1 to C3 alkyl, C3 to C4 cycloalkyl, C3 to C4 cycloalkenyl, C1 to C3 alkyloxy, or C1 to C3 alkylthio;
- R7 is hydrogen atom or non-interfering substituent;
- RA is represented by the formula:
- 24
- wherein R9 and R10 are each independently hydrogen atom, C1 to C3 alkyl, or halogen;
- X and Y are each independently oxygen atom or sulfur atom;
- and
- Z is —NH2 or —NHNH2;
- RB is —CONH2 or —CONHNH2;
- and,
- Ring D is cyclohexene ring or benzene ring;
- provided that Ring A is (b), (c), or (d) when —B— is (e) or (f),
- a prodrug thereof, its pharmaceutically acceptable salt, or its solvate.
A composition for prevention or treatment of hepatocirrhosis which contains a compound as an active ingredient represented by the formula:
- 28 29 30 31 32
- a prodrug thereof, its pharmaceutically acceptable salt, or its solvate.
Use of a type-X sPLA2 inhibitor for the preparation of a medicament for the treatment of hepatocirrhosis.
A method of treating a mammal, including a human, to alleviate the pathological effects of hepatocirrhosis, which comprises administration to said mammal of a type-X sPLA2 inhibitor in a pharmaceutically effective amount.
Dependencies are inferred from the claim text.