Choongwae Pharma Corporation

Myriad Genetics, Inc.

Molecumetics Ltd.

Institute for Chemical Genomics

Bryet Us, Inc.

Masakatsu Eguchi

Michael S Kahn

Jae Uk Chung

Sung Hwan Moon

Kwang Won Jeong

Sung Chan Lee

Cu Nguyen

Hwa-Ok Kim

Marcin Stasiak

Cyprian Okwara Ogbu

Soo Jin Lee

Patrick Douglas Boatman, Jr

Hiroshi Nakanishi

Jan Urban

Min Sang Lee

Jessymol Mathew

Vincent Huber

Kwang-Won Jeong

Sung-Hwan Moon

Sung-Chan Lee

The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Reverse-turn mimetics and method relating thereto

The invention provides &#x3b1;-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.

Alpha-helix mimetics and methods relating to the treatment of fibrosis

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility as diagnostic and therapeutic agents for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. In one embodiment, these reverse-term mimetics have a general structure of formula (VI): wherein R, R, R, X, Xand Xare defined as provided herein.

The invention provides &#x3b1;-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, Rand Ras set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis. 

Conformationally constrained compounds of structure: which mimic the secondary structure of &#x3b2;-strand regions of biologically active peptides and proteins are disclosed. Such &#x3b2;-strand mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents that inhibit protease, kinase and the like. Libraries containing the &#x3b2;-strand mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members.

Beta-strand mimetics and method relating thereto

Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

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Bellevue, WA, United States of America

Masakatsu Eguchi