Abstract

The present invention relates to a pharmaceutical combination comprising (i) firibastat, (ii) a diuretic and (iii) a blocker of the systemic renin-angiotensin system selected from the group consisting of angiotensin I converting enzyme inhibitors (ACEIs) and angiotensin II receptor type 1 (AT1R) antagonists. Said composition is particularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N); Sulfinylamines (—N=SO); Sulfonylamines (—N=SO2)
• A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• A61K 38/55 - Protease inhibitors
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to compounds, to compositions comprising the same, to methods for preparing the compounds, and the use of these compounds in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• C07C 323/58 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
• A61P 9/12 - Antihypertensives
• A61K 31/10 - Sulfides; Sulfoxides; Sulfones
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)

Abstract

The present invention relates to a pharmaceutical combination comprising (i) firibastat, (ii) a diuretic and (iii) a blocker of the systemic renin-angiotensin system selected from the group consisting of angiotensin I converting enzyme inhibitors (ACEIs) and angiotensin II receptor type 1 (AT1R) antagonists. Said composition is particularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/12 - Aerosols; Foams
• A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/405 - Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
• A61K 35/74 - Bacteria
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 38/05 - Dipeptides
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 7/10 - Antioedematous agents; Diuretics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to a pharmaceutical combination comprising (i) firibastat, (ii) a diuretic and (iii) a blocker of the systemic renin-angiotensin system selected from the group consisting of angiotensin I converting enzyme inhibitors (ACEIs) and angiotensin II receptor type 1 (AT1R) antagonists. Said composition is particularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• A61P 7/10 - Antioedematous agents; Diuretics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/12 - Antihypertensives
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/12 - Aerosols; Foams
• A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/405 - Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
• A61K 35/74 - Bacteria
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 38/05 - Dipeptides
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• C07F 9/58 - Pyridine rings
• C07F 9/30 - Phosphinic acids (R2=P(:O)OH); Thiophosphinic acids
• C07F 9/653 - Five-membered rings
• C07F 9/6539 - Five-membered rings

Abstract

The present invention relates to compounds, to compositions comprising the same, to methods for preparing the compounds, and the use of these compounds in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
• A61K 33/04 - Sulfur, selenium or tellurium; Compounds thereof
• A61K 33/42 - Phosphorus; Compounds thereof
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/12 - Antihypertensives
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

The present invention relates to compounds, to compositions comprising the same, to methods for preparing the compounds, and the use of these compounds in therapy. In particular, the present invention relates to a compound of formula (I) that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• C07C 323/65 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfone or sulfoxide groups bound to the carbon skeleton
• A61K 9/12 - Aerosols; Foams
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61P 9/12 - Antihypertensives
• C07C 323/58 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton

Abstract

The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• C07F 9/572 - Five-membered rings
• C07F 9/653 - Five-membered rings
• C07F 9/6539 - Five-membered rings
• C07F 9/30 - Phosphinic acids (R2=P(:O)OH); Thiophosphinic acids
• C07F 9/32 - Esters thereof
• A61K 31/426 - 1,3-Thiazoles
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to compounds of one of the following formulas: to a composition comprising the same, to methods for preparing the compounds, and the use of these compounds in therapy. In particular, the present invention relates to compounds that are useful in the treatment and/or prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X or glaucoma.

IPC Classes  ?

• C07F 9/572 - Five-membered rings
• A61K 31/426 - 1,3-Thiazoles
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• C07F 9/30 - Phosphinic acids (R2=P(:O)OH); Thiophosphinic acids
• C07F 9/32 - Esters thereof
• C07F 9/653 - Five-membered rings
• C07F 9/6539 - Five-membered rings

Abstract

The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.

IPC Classes  ?

• C07F 9/30 - Phosphinic acids (R2=P(:O)OH); Thiophosphinic acids
• A61K 31/662 - Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to a new crystalline phase of (3S,3S′) 4,4′-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and its use, particularly in the pharmaceutical industry, and to processes for preparation thereof. The invention is also directed to pharmaceutical compositions containing at least one crystalline phase of (3S,3S′) 4,4′-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and to the therapeutic or prophylactic use of such crystalline phase and compositions comprising the same.

IPC Classes  ?

• C07C 323/66 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
• C07C 319/28 - Separation; Purification
• C07C 227/42 - Crystallisation

Abstract

The present invention relates to a pharmaceutical composition comprising, in at least one pharmaceutically acceptable support or vehicle, a combination of (3S,3S′)4,4′-disulfanediylbis(3-aminobutane 1-sulfonic acid) or a pharmaceutically acceptable salt or solvate thereof and a second active ingredient selected from the group consisting of angiotensin I converting enzyme inhibitors and angiotensin II receptor type I antagonists. Said composition is particularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
• A61P 9/12 - Antihypertensives
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 38/05 - Dipeptides
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 35/74 - Bacteria

Abstract

The present invention relates to a new crystalline phase of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and its use, particularly in the pharmaceutical industry, and to processes for preparation thereof. The invention is also directed to pharmaceutical compositions containing at least one crystalline phase of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and to the therapeutic or prophylactic use of such crystalline phase and compositions comprising the same.

IPC Classes  ?

• C07C 323/66 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
• A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N); Sulfinylamines (—N=SO); Sulfonylamines (—N=SO2)
• A61P 9/12 - Antihypertensives
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine

Abstract

The present invention relates to a new crystalline phase of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and its use, particularly in the pharmaceutical industry, and to processes for preparation thereof. The invention is also directed to pharmaceutical compositions containing at least one crystalline phase of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) (ABSD) with L-lysine and to the therapeutic or prophylactic use of such crystalline phase and compositions comprising the same.

IPC Classes  ?

• C07C 323/66 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
• A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N); Sulfinylamines (—N=SO); Sulfonylamines (—N=SO2)
• A61P 9/12 - Antihypertensives
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine

Abstract

The present invention relates to a new method for the preparation of (3S,3S′) 4,4′-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino)-4-(neopentyloxysulfonyl)butanoate A.

IPC Classes  ?

• C07C 319/24 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides by reactions involving the formation of sulfur-to-sulfur bonds
• C07C 303/22 - Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids by reactions not involving the formation of sulfo or halosulfonyl groups
• C07C 323/66 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton

Abstract

The present invention relates to a pharmaceutical composition comprising, in at least one pharmaceutically acceptable support or vehicle, a combination of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) or a pharmaceutically acceptable salt or solvate thereof and a second active ingredient selected from the group consisting of angiotensin I converting enzyme inhibitors and angiotensin II receptor type I antagonists. Said composition isparticularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to a pharmaceutical composition comprising, in at least one pharmaceutically acceptable support or vehicle, a combination of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) or a pharmaceutically acceptable salt or solvate thereof and a second active ingredient selected from the group consisting of angiotensin I converting enzyme inhibitors and angiotensin II receptor type I antagonists. Said composition isparticularly useful for the treatment of hypertension and related diseases and conditions.

IPC Classes  ?

• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/401 - Proline; Derivatives thereof, e.g. captopril
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61P 9/12 - Antihypertensives
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to a new method for the preparation of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino) -4-(neopentyloxysulfonyl)butanoate A. The present invention also relates to a crystalline (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid)trihydrate, which has a powder XRD diffractogram with characteristic peaks at approximately: 5.09; 14.30; 15.30; 18.32 degrees 2.theta. (K_alphal Cu anode); or 5.09; 14.30; 15.30; 18.32; 22.09; 22.79; 24.65; 25.60 and 25.83 degrees 2.theta. (K_alphal Cu anode).

IPC Classes  ?

• C07C 323/25 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated

Abstract

The present invention relates to a new method for the preparation of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino)-4-(neopentyloxysulfonyl)butanoate A.

IPC Classes  ?

• C07C 309/14 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton
• C07C 303/02 - Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof

Abstract

The present invention relates to a new method for the preparation of (3S,3S') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) in five steps from (S)-ethyl 2-(benzyloxycarbonylamino)-4-(neopentyloxysulfonyl)butanoate A.

IPC Classes  ?

• C07C 323/25 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07C 303/02 - Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
• C07C 309/14 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton