Endogena Therapeutics, Inc.

Hoffmann-La Roche Inc.

Matthias Steger

Alex Mueller

Daphna Mokady

Mauro Marigo

Bernhard Fasching

Jens-Uwe Peters

Markus Boehringer

Bernd Michael Loeffler

Peter Weiss

Compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is selected from 5-oxazolyl, pyridine-4-yl, triazolyl, oxadiazolyl, imidazolyl and 2-methyloxazol-5-yl residue, R, and Rare independently selected from hydrogen, fluoro, chloro, methoxy, trifluoromethyl, methyl and difluoromethoxy, B is selected from a residue of formulae (II)-(IX) wherein,'*' denotes the point of attachment to the remainder of the molecule, andR, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, and Rare independently selected from hydrogen, linear or branched alkyl having 1-3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, 2,2,2-trifluoromethyl and difluoromethoxy.

N-(4-(oxazol-5-yl)phenyl) chromane-3-carboxamide derivatives and related compounds as stimulators of the production of retinal precursor cells for the treatment of neuroretinal diseases

A method of treating and/or preventing disease wherein retinal pigment epithelium, including administering compound of formula (I) or pharmaceutically acceptable salt, racemic mixture, corresponding enantiomer or, if applicable, corresponding diastereomer, wherein: X is either NH or O, R, Rand Rare independently selected from consisting hydrogen group, fluoro, chloro, trifluoromethyl, methyl and difluoromethoxy, A is selected from consisting residue group of formula (II)-(VII) or (VIII) '*' denotes point of attachment to molecule remainder, and R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare independently selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl, 2,2,2-trifluoroethyl and difluoromethoxy and Ris selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, trifluoromethyl, and 2,2,2-trifluoroethyl.

Compounds and their use as therapeutically active substances in the treatment and/or reducing signs or symptoms of diseases involving the retinal pigment epithelium

New compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, Ris selected from the group consisting of fluoro, chloro and methoxy; B is selected from the group consisting of a residue of formula (II), (III) and (IV) wherein, '*' denotes the point of attachment to the remainder of the molecule, and R, R', R&#x2033;, R, R&#x2032;, R&#x2033;, R, R&#x2032;, R&#x2033;, R, R&#x2032; and R&#x2033; are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino.

Compounds for use as therapeutically active substances in the treatment of retinal diseases

A method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, includes administering a compound of formula (Ia) or a pharmaceutically acceptable salt thereof to a patient having the retinal disease so as to be delivered to an eye of the patient in an amount effective to treat the retinal disease: wherein A is an 5-oxazolyl residue or a pyridine-4-yl residue, Ris selected from the group consisting of methoxy, fluoro and chloro; R, R, R, Rand Rof the phenyl ring B are independently from each other selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino; and at least two of R, R, R, Rand Rare hydrogens.

The present invention provides compounds of formula (I)wherein R, R, R, Rand X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

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Zurich, Switzerland

Matthias Steger