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Valsartan saltsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Five-membered Hetero Ring Containing At Least One Nitrogen Ring Atom (e.g., 1,2,3-triazoles, Etc.), Tetrazoles (including Hydrogenated)Valsartan salts description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070149587, Valsartan salts. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This application is a continuation application of Ser. No. 10/333,100, filed Feb. 24, 2003, which is a 371 of International Application number PCT/EP01/08253, filed Jul. 17, 2001. [0002] The invention relates to new salts of the AT.sub.1 receptor antagonist (S)--N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5-yl- )-biphenyl-4-yl-methyl]-amine (valsartan) of formula [0003] The active ingredient valsartan is the free acid which is described specifically in EP 0443983, especially in example 16; it has two acidic hydrogen atoms: (i) the hydrogen atom (H atom) of the carboxyl group, and (ii) that of the tetrazole ring. Accordingly, one acidic H atom (primarily the carboxyl H atom) or both acidic H atoms may be replaced by a monovalent or higher valent, e.g. divalent, cation. Mixed salts may also be formed. [0004] EP 443983 does not disclose any specific salts of valsartan. Also, it does not mention any special properties of salts. Meanwhile, the active ingredient valsartan has been introduced as an anti-hypertensive agent in a series of countries under the trade name DIOVAN. [0005] The free acid valsartan has a melting point in a closed crucible of 80 to 95.degree. C. and in an open crucible of 105 to 110.degree. C. and a melting enthalpy of 12 kJ/mol. The optical rotation is [.alpha.].sup.20.sub.D=(-70.+-.2).degree. for a concentration of c=1% in methanol. [0006] The density of the valsartan crystals and of the salt hydrates was determined by a helium pycnometer (Accupyc 1330 of Micromeritics, Norcross, Ga., USA). The density for the crystals of the free acid valsartan is 1.20.+-.0.02. [0007] The X-ray diffraction diagram consists essentially of a very broad, diffuse Xray reflection; the free acid is therefore characterised as almost amorphous under X-ray. The melting point linked with the measured melting enthalpy of 12 kJ/mol unequivocally confirm the existence of a considerable residual arrangement in the particles or structural domains for the free acid valsartan. [0008] There is a need for more stable, e.g. crystalline forms of valsartan, which are even easier to manage in the drying or grinding processes following the final stage of the chemical preparation process and also in the steps for preparing the pharmaceutical formulations. Many futile attempts have been made to find improved forms through salt formation, the forms ideally being as crystalline as possible, as well as physically and chemically stable. Only the salts according to the invention, their solvates and polymorphous forms thereof exhibit the desired improved properties. [0009] The formation of salts of valsartan with the desired advantageous properties has proved to be difficult. In the majority of cases, for example, amorphous salts with little stability are obtained (such as hard foams, waxes or oils). Extensive research has shown that the salts of valsartan according to the invention have proved to be particularly advantageous compared with the free acid valsartan. [0010] The objects of the present invention are salts of valsartan which are selected from the group consisting of the monosodium salt, the monopotassium salt, the dipotassium salt, the magnesium salt, the calcium salt, the bis-diethylammonium salt, the bis-dipropylammonium salt, the bis-dibutylammonium salt, the mono-L-arginine salt, the bis-L-arginine salt, the mono-L-lysine salt and the bis-L-lysine salt, as well as salt mixtures, or respectively, an amorphous form, a solvate, especially hydrate, as well as a polymorphous form thereof, the respective production and usage, and pharmaceutical preparations containing such salts. [0011] The objects of the present invention are salts of valsartan which are selected from the group consisting of the monosodium salt, the monopotassium salt, the dipotassium salt, the magnesium salt, the calcium salt, the bis-diethylammonium salt, the bis-dipropylammonium salt, the bis-dibutylammoniumsalt, the mono-L-arginine salt, the bis-L-arginine salt, the mono-L-lysine salt and the bis-L-lysine salt, or respectively, an amorphous form, a solvate, especially hydrate, as well as a polymorphous form thereof. [0012] Salt mixtures are (i) single salt forms from different cations selected from the above group or (ii) mixtures of those single salt forms which exist for example in the form of conglomerates. [0013] Preferred salts are for example selected from the [0014] mono-sodium salt in amorphous form; [0015] di-sodium salt of valsartan in amorphous or crystalline form, especially in hydrate form, thereof. [0016] Mono-potassium salt of valsartan in amorphous form; [0017] di-potassium salt of valsartan in amorphous or crystalline form, especially in hydrate form, thereof. [0018] calcium salt of valsartan in crystalline form, especially in hydrate form, primarily the tetrahydrate thereof; [0019] magnesium salt of valsartan in crystalline form, especially in hydrate form, primarily the hexahydrate thereof; [0020] calcium/magnesium mixed salt of valsartan in crystalline form, especially in hydrate form; [0021] bis-diethylammonium salt of valsartan in crystalline form, especially in hydrate form; [0022] bis-dipropylammonium salt of valsartan in crystalline form, especially in hydrate form; [0023] bis-dibutylammonium salt of valsartan in crystalline form, especially in hydrate form, primarily the hemihydrate thereof; [0024] mono-L-arginine salt of valsartan in amorphous form; Continue reading about Valsartan salts... Full patent description for Valsartan salts Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Valsartan salts patent application. ###
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