Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Wajiha Khan

Waleed Danho

Joseph Swistok

Jefferson Wright Tilley

David Charles Fry

George Kenneth Ehrlich

Nader Fotouhi

Rebecca Taub

Anish A Konkar

Karin Conde-Knape

Cristina Martha Rondinone

Robert Alan Goodnow, Jr

Huifeng Niu

Francesca Milletti

Yi Han

David C Fry

Anish Konkar

Rebecca Anne Taub

George Ehrlich

The present invention provides compounds to disrupt the eIF4E-eIF4G interaction and pharmaceutically acceptable salts of such compounds. Generally, the compounds are cell-penetrating peptides which bind mammalian initiation factor eIF4E (CPP-eIF4E), wherein the peptide comprises an amino acid sequence selected from the group consisting of SEQ ID NOS: 7, 9-11, 12-26, 27-44 and 45-51. More preferably, the amino acid sequence comprises at least 9 to about 40 amino acids and the mammalian initiation factor eIF4E is human initiation factor eIF4E.

Cell penetrating peptides to target EIF4E

The present invention provides compounds which are analogs of glucose-dependent insulinotropic polypeptide (GIP) and pharmaceutically acceptable salts of such compounds. These compounds have activity as agonists of GIP receptor.

Glucose-dependent insulinotropic peptide analogs

Provided herein are neuropeptide-2 receptor agonists of the formula (I):Y&#x2014;R&#x2014;R&#x2014;X&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;NH&#x2003;&#x2003;(I) (SEQ ID NO: 1),as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.

Neuropeptide-2 receptor (Y-2R) agonists

Provided herein are neuropeptide-2 receptor agonists of the formula (I): as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. X is 4-oxo-6-(1-piperazinyl)-3(4H)-quinazoline-acetic acid (Pqa). These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.

Neuropeptide-2 receptor (Y-2R) agonists and uses thereof

Provided herein are neuropeptide-2 receptor agonists of the formula (I):Y&#x2014;R&#x2014;R&#x2014;X&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;NH, &#x2003;&#x2003;(I)as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.

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East Hanover, NJ, United States of America

Wajiha Khan