Amine salts of an integrin receptor antagonist
AssigneeMerck & Co., Inc.
InventorsGuy R. Humphrey, Marjorie See Waters, Wei Xu
Life of this patent
Estimating the term…
Loading patent…
AssigneeMerck & Co., Inc.
InventorsGuy R. Humphrey, Marjorie See Waters, Wei Xu
Estimating the term…
Amine salts of 3-(2-methyl-pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid are potent antagonists of the integrin αvβ3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts. Also disclosed are 3(R)- and 3(S)-(2-methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid in the form of a zwitterion trihydrate.
An amine salt of 3-(2-methyl-pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid of structural formula I:
A salt comprising the ions of 3-(2-methyl-pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid anion and protonated tris(hydroxymethyl)aminomethane cation.
A salt comprising the ions of 3-(2-methyl-pyrirmidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid anion and protonated 2-amino-2-methyl-1-propanol cation.
Dependencies are inferred from the claim text.