Epis S.a.

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Syndromex Ltd.

Jacob Bar-Tana

Johannes Pill

Ernst-Christian Witte

Karlheinz Stegmeier

Bernd Hagenbruch

Jochanan Blum

Bruno Dreckmann

Yoelit Migron

Disclosed are methods of treating of type 2 diabetes mellitus and associated conditions in humans by administering an &#x3b1;,&#x3b1;-substituted long-chain dicarboxylic acid. In some of the disclosed methods the &#x3b1;,&#x3b1;-substituted long-chain dicarboxylic acid is administered as add-on therapy to anti-diabetic Standard-of-Care treatment.

Diabetes treatment regimens using alpha, alpha-substituted long-chain amphipathic carboxylates

Disclosed are methods of treatment of type 1 diabetes (T1D) in subjects under standard-of-care T1D treatment, by administration of substituted long-chain amphipathic dicarboxylic acids. Also disclosed are methods of reducing standard-of-care administered dose of insulin or an insulin analogue and/or obviating the need for administration of insulin or an insulin analogue in a T1D subject by administration of substituted long-chain amphipathic dicarboxylic acids.

Long-chain amphipathic dicarboxylic acids for treatment of diabetes type-1

This invention relates to deuterated tetramethyl dioic acids, compositions comprising them and uses thereof in the treatment of Metabolic Syndrome and any diseases, disorders or symptoms associated therewith.

Deuterated tetramethyl dioic acids, compositions comprising them and uses thereof

The invention relates to carboxylic acids and derivatives thereof and pharmaceutical compound containing them. The active compounds are represented by the formula compound represented by formula I, wherin R -R each independently represents an unsubstituted or substituted hydrocarbyl or heterocyclyl radical, Q represents a diradical consisting of a linear chain of 11 to 18 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteroatom chain members optionally forming part of a ring structure, and where one or both of de carboxyl groups can be substituted by an in vitro hydrolyzable physiologically acceptable substituent; with the proviso that: compounds wherein R -R each represents CH and Q represents a linear chain of 14 carbons, are excluded; and compounds wherein Q represents a linear chain of carbon atoms one of which is replaced by oxygen or sulfur, are excluded.

Carboxylic acids and derivatives thereof and pharmaceutical compositions containing them

In accordance with the present invention, there are provided therapeutically effective compounds comprising an amphipathic carboxylate of the formula R&mdash;COOH, or a salt or an ester or amide of such compound, where R designates a saturated or unsaturated alkyl chain of 10-24 carbon atoms, one or more of which may be replaced by heteroatoms, where one or more of said carbon or heteroatom chain members optionally forms part of a ring, and where said chain is optionally substituted by a hydrocarbyl radical, heterocyclyl radical, lower alkoxy, hydroxyl-substituted lower alkyl, hydroxyl, carboxyl, halogen, phenyl or (hydroxy-, lower alkyl-, lower alkoxy-, lower alkenyl- or lower alkinyl)-substituted phenyl, C,-C,cycloalkyl or (hydroxy-, lower alkyl-, lower alkoxy-, lower alkenyl- or lower alkinyl)-substituted C,-C,cycloalkyl wherein said amphipathic carboxylate is capable of being endogenously converted to its respective coenzyme A thioester.

The present invention relates to a novel class of compounds for treating hyperlipidemia, obesity and impaired glucose tolerance/noninsulin dependent diabetes mellitus without adversely affecting energy metabolism, and pharmaceutical compositions comprising the aforementioned compounds for the treatment of obesity, hyperlipidemia and maturity-onset diabetes.

The present invention provides pharmaceutical compositions containing at least one .alpha.-halogenated dicarboxylic acid of the general formula: ##STR1## wherein Hal is a chlorine, bromine or fluorine atom, R is a hydrogen atom or Hal and m is a number of from 4 to 16, and/or at least one pharmacologically acceptable salt, ester or amide thereof. The present invention also provides new compounds of general formula (I) but in which m is a number of from 8 to 16 and processes for the preparation thereof.

.alpha.-halogenated dicarboxylic acids, pharmaceutical compositions and

##STR1## .alpha., .omega.-dicarboxylic acids having the general formula (I') in which: R.sub.1 and R.sub.2, which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C.sub.3 -C.sub.7 -cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R.sub.1 and R.sub.2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R.sub.1 and R.sub.2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.

.alpha., .omega.-dicarboxylic acids and medicaments which contain these

A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof, wherein

Long-chain .alpha.,.omega.-dicarboxylic acids and derivatives thereof

A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism. The active compounds have the general formula ##STR1## or in-vivo hydrolysable functional derivatives of the carboxylic groups thereof, wherein

Growing community of inventors

Jerusalem, Israel

Jacob Bar-Tana