LPA receptor agonists and antagonists and methods of use
OwnerDuane D. Miller, Gabor Tigyi +4inventors
InventorsDuane D. Miller, Gabor Tigyi, Gangadhar G. Durgam, Tamas Virag, Michelle D. Walker, Ryoko Tsukahara
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Abstract
Disclosed are compounds according to formula (I) as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.
Claims7
A method for protecting intestinal and hematopoietic cells of a mammalian subject from apoptosis caused by radiation exposure or chemotherapy, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of formula (I)
- wherein,
- X1 is R1—Y1-A-;
- X2 is —Z1—P(S)(OH)2;
- X3 is hydrogen;
- A is a direct link or (CH2)l with l being an integer from 1-30;
- Y1 is (CH2)l with l being an integer from 1-30;
- Z1 is oxygen;
- Q1 and Q2 are independently selected from the group consisting of two hydrogens, ═NR4, ═O, and a combination of H and —NR5R6;
- R1 is independently a straight or branched-chain C1 to C30 alkyl, a straight or branched-chain C2 to C30 alkenyl, an aromatic or heteroaromatic ring (optionally substituted), an acyl, an arylalkyl, an aryloxyalkyl,
- R4, R5, R6, R7, and R8 are independently hydrogen, a straight or branched-chain C1 to C30 alkyl, a straight or branched-chain C2 to C30 alkenyl, an aromatic or heteroaromatic ring with or without mono-, di-, or tri-substitutions of the ring, an acyl, an arylalkyl, or an aryloxyalkyl including straight or branched-chain C1 to C30 alkyl.
A method for treating chemotherapy-induced tissue damage in the intestine of a mammalian subject, the method comprising administering to the subject a composition comprising a compound of formula (I)
- wherein,
- X1 is R1—Y1-A-;
- X2 is —Z1—P(S)(OH)2;
- X3 is hydrogen;
- A is a direct link or (CH2)l with l being an integer from 1-30;
- Y1 is (CH2)l with l being an integer from 1-30;
- Z1 is oxygen;
- Q1 and Q2 are independently selected from the group consisting of two hydrogens, ═NR4, ═O, and a combination of H and —NR5R6;
- R1 is independently a straight or branched-chain C1 to C30 alkyl, a straight or branched-chain C2 to C30 alkenyl, an aromatic or heteroaromatic ring (optionally substituted), an acyl, an arylalkyl an aryloxyalkyl,
- R4, R5, R6, R7, and R8 are independently hydrogen, a straight or branched-chain C1 to C30 alkyl, a straight or branched-chain C2 to C30 alkenyl, an aromatic or heteroaromatic ring with or without mono-, di-, or tri-substitutions of the ring, an acyl, an arylalkyl including straight or branched-chain C1 to C30 alky, or an aryloxyalkyl.
Dependencies are inferred from the claim text.