Biogen Idec International Gmbh

Fumapharm Ag

Other

Biogen Idec International Ag

Rajendra Kumar Joshi

Hans-Peter Strebel

Peter P Speiser

Christian Zaugg

Jitka Ulrichová

Michael Tamm

Thomas J Schmidt

Hans Peter Strebel

According to a first aspect the invention relates to the use of fumaric acid derivatives selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoalkyl ester salts, fumaric acid monoamides, monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment or prevention of cardiac insufficiency, in particular left ventricular insufficiency, myocardial infarction and angina pectoris. According to a second aspect the invention relates to the use of fumaric acid derivatives, selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoalkyl ester salts, fumaric acid monoamides, monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment of asthma and chronic obstructive pulmonary diseases, especially asthma caused by allergies, infections, analgesics, job conditions or physical effort, mixed forms of asthma, or asthma cardiale.

Use of fumaric acid derivatives for treating cardiac insufficiency, and asthma

The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.

Utilization of dialkylfumarates

The present invention relates to compounds of the formula (I) wherein Xand Xindependently represent O, NH or S, Rand Rare independently selected from the group consisting of a C-Chydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue Xor Xin this case being NH, and hydrogen, both radicals Rand Rpreferably not being H, wherein Ris a residue selected from group consisting of &#x2014;S&#x2014;R, wherein Ris a C-Chydrocarbyl group, at least one of Rand Rnot being H when Xand Xare oxygen, &#x2014;S&#x2014;CH&#x2014;CH(NH)(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group, and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug and drugs containing the same. 

Thiosuccinic acid derivatives and the use thereof

The present invention relates to certain carbocyclic and oxacarbocyclic fumaric acid oligomers and the use thereof for preparing a pharmaceutical preparation as well of pharmaceutical preparations containing these compounds.

Carbocyclic and oxacarbocyclic fumaric acid oligomers

Fumaric acid amides of the general formula (I) wherein Rrepresents ORor a D- or L-amino acid radical &#x2014;NH&#x2014;CHR&#x2014;COOH bonded via an amide bond, wherein Ris hydrogen, a straight-chained or branched, optionally substituted Calkyl radical, a phenyl radical or Caralkyl radical and Ris a side chain of a natural or synthetic amino acid and Rrepresents a D- or L-amino acid radical &#x2014;NH&#x2014;CHR&#x2014;COOH bonded via an amide bond or a peptide radical comprising 2 to 100 amino acids bonded via an amide bond, wherein Ris a side chain of a natural or synthetic amino acid, are used for preparing a drug (1) for the therapy of an autoimmune disease; (2) for use in transplantation medicine; (3) for the therapy of mitochondrial diseases; or (4) for the therapy of NF-kappaB mediated diseases.

Fumaric acid amides

Dimethyl fumarate for the treatment of multiple sclerosis

The present invention relates to the use of individual fumaric acid derivatives or mixtures thereof for preparing a pharmaceutical composition for treating mitochondrial diseases, especially for treating Parkinson's syndrome, Alzheimer's disease, Chorea Huntington disease, retinopathia pigmentosa and mitochondrial encephalomyopathy. Preferably, the fumaric acid derivative(s) is/are those selected from the group consisting of fumaric acid dialkyl esters or fumaric acid monoalkyl esters in the form of the free acid or a salt thereof.

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Zurich, Switzerland

Rajendra Kumar Joshi