Genzyme Corporation

Merck Serono S. A.

Laboratoires Serono S.a.

Applied Research Systems Ars Holding N.v.

Zhong Zhao

Gian Luca Araldi

Yihua Liao

Yibin Xiang

Adulla P Reddy

Seng H Cheng

Andrew Charles Good

John Marshall

Bradford Hirth

Cassandra Celatka

Ronald K Scheule

Markus Metz

Elyse Bourque

Thomas A Natoli

Elina Makino

Oxana Beskrovnaya

Mario A Cabrera-Salazar

Katherine Jancsics

Herve Husson

Matthias Schwarz

Renato Skerlj

Nadia Brugger

Srinivasa R Karra

Sean D McKenna

John P Leonard

Amanda E Sutton

Renato Tony Skerlj

Bagna Bao

Christopher Yee

Andrew T Papoulis

Alexandra Joseph

Paul Mason

Jill Gregory

John Leonard

Mohamud Mohamud

Brian Healey

Yinyin Huang

Sanjay Danthi

Yiding Hu

Kara Carter

Katherine Jancisics

Ronald Scheule

Mario Cabrera-Salazar

Andrew Papoulis

The invention relates to inhibitors of glucosylceramide synthase (GCS) of the Formula I: represented by the following structural formula or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein, useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.

Glucosylceramide synthase inhibitors

The invention relates to inhibitors of glucosylceramide synthase (GCS), such as Compound of Formula I, shown below, as defined herein, useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer. 

The invention features compounds of Formula (I), Formula (I)-A and Formula (I)-B as disclosed herein, as well as methods of synthesis, therapy, diagnostics, and assays. 

NAMPT inhibitors and methods

The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.

Antiproliferative pyrimidyl, fused pyrimidyl and pyrimidyl hydrazones

Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.

Pyrrolidine derivatives as prostaglandin modulators

The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.

Pyrazolidinone compounds as ligands of the prostaglandin EP2 and/or EP4 receptors

1,2-substituted 5-pyrrolidinone compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, renal dysfunction, an immune deficiency disorder, dry eye, ichthyosis, elevated intraocular pressure, sleep disorder, or gastric ulcer, inflammatory disorders and other diseases and disorders associated with the prostaglandin family of compounds.

Gamma lactams as prostaglandin agonists and use thereof

The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.

Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.

A gamma-lactam diene of Formula I: which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders.

G-lactam derivatives as prostaglandin agonists

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Wayland, MA, United States of America

Zhong Zhao