Columbia University

Sloan-kettering Institute for Cancer Research

Other

Research Foundation for Mental Hygiene, Inc.

Dalibor Sames

Andrew Carry Kruegel

Jonathan A Javitch

Madalee G Wulf

Samuel J Danishefsky

Philip O Livingston

Peter W Glunz

Govindaswami Ragupathi

Samuel Hintermann

Scott D Kuduk

Lawrence Williams

David Sulzer

Niko Gert Gubernator

Ting-Chao Chou

Kenneth O Lloyd

Xiao-Tao Chen

Heedong Yun

John Hartung

Xiao Tao Chen

Fay Ng

Marie-Laure Rives

Jacob Bradely Schwarz

Juraj Galeta

Vaclav Havel

Srijita Bhowmik

Susruta Majumdar

Minhee Lee

Xiaoguang Li

Xiaoguang Lei

Souvik Rakshit

Madalee M Gassaway

Shu Li

Paul Vadola

Richard Karpowicz

Valery Kudryashov

Adam Henke

Ignacio Carrera

Jacob B Schwartz

Andrew C Kruegel

Marie-Laure Rivers

The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.

Opioid receptor modulators

The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.

Mitragynine alkaloids as opioid receptor modulators

The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.

The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with a pain, a depressive disorder, a mood disorder, an anxiety disorder, borderline personality disorder, opioid addiction, or opioid withdrawal symptoms by administering the compound to the subject.

Carboxylic diarythiazepineamines as mixed mu- and delta-opioid receptor agonists

Mitragynine analogs for the treatment of pain, mood disorders and substance use disorders

The present invention provides a compound having the structure of the instant invention of a pharmaceutically acceptable salt or ester thereof, methods of preparing the same, and methods of treating a subject with compounds of the instant invention in combination therapies.

Carboxylic diarylthiazepineamines as mu-opioid receptor agonists

The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof.

Class of mu-opioid receptor agonists

This invention provides a compound having the structure   

Small molecule inducers of GDNF as potential new therapeutics for neuropsychiatric disorders

This invention relates to compounds having the following structure: wherein Y is O, X is O, bond &#x3b1; is absent and bond &#x3b2; is present, or Y is H, X is CH, bond &#x3b1; is present, and bond &#x3b2; is absent; atom Z is a carbon and bonds &#x3c7;, &#x3b4; and &#x3b3; are present, or atom Z is a nitrogen and bonds &#x3c7;, &#x3b4; and &#x3b3; are absent, or atom Z is a nitrogen and bonds &#x3c7; and &#x3b4; are present and &#x3b3; is absent. R, R, R, R, R, and Rare various substituents as described in the specification.

pH-responsive fluorescent false neurotransmitters and their use

The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I). 

Compounds, compositions and methods for reducing toxicity and treating or preventing diseases

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond &#x3b1; is absent and bond &#x3b2; is present, or Y is H, X is CH, bond &#x3b1; is present, and bond &#x3b2; is absent; atom Z is a carbon and bonds &#x3c7;, &#x3b4; and &#x3b3; are present, or is a nitrogen and bonds &#x3c7;, &#x3b4; and &#x3b3; are absent; Ris &#x2014;H, &#x2014;OH, &#x2014;O&#x2014;R, &#x2014;N(H)&#x2014;R, &#x2014;N(H)&#x2014;(CH)&#x2014;NH, &#x2014;N(R)(R), or a piperazine cation; Ris either covalently bound to R, or is &#x2014;H, or is covalently bound to Rso as to form a substituted or unsubstituted pyrrole or Ris covalently bound to Ror Ror R; or Rand Rare covalently joined to form an aromatic ring; Ris either covalently bound to Rso as to form a pyrrole, or is, inter alia, &#x2014;H, &#x2014;OH, alkyl, or when Z is nitrogen Ris &#x2550;O; Ris, inter alia, &#x2014;H, &#x2014;OH, or &#x2014;RNH; Ris, inter alia, &#x2014;H, &#x2014;OH, or &#x2014;RNH, and Ris either is covalently bound to Ror is &#x2014;H, or Ris covalently bound to Ror Ror R. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds. 

Fluorescent substrates for monoamine transporters as optical false neurotransmitters

The present invention provides novel glycoconjugates such as glycopeptides, as well as convergent methods for the synthesis thereof. An exemplary preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the glycoconjugates of the invention.

Glycopeptide conjugates and uses thereof

The present invention provides novel &#x3b1;-O-linked glycoconjugates such as &#x3b1;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &#x3b1;-O-linked glycoconjugates.

&#x3b1;-O-linked glycoconjugates, methods of preparation and uses thereof

The present invention provides novel &agr;-O-linked glycoconjugates such as &agr;-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the &agr;-O-linked glycoconjugates.

&agr;-O-linked glycoconjugates, methods of preparation and uses thereof

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New York, NY, United States of America

Dalibor Sames