University of California

Nereus Pharmaceuticals, Inc.

Amydis, Inc.

Other

University of Missouri

La Jolla Bioengineering Institute

Amydis Diagnostics, Inc.

Emmanuel A Theodorakis

Michael A Palladino

Jerry Yang

Stella Sarraf

Sheila Ann Grant

Venkat Rami Reddy Macherla

Marcos Intaglietta

Ta-Hsiang Chao

John A Frangos

Mark A Haidekker

Yogesh S Sanghvi

Young-Ger Suh

Young Ger Suh

Ke Wen

Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.

Amyloid targeting agents and methods of using the same

Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the methods for treating of diseases associated with an amyloid or amyloid like proteins.

There are provided compounds and methods for the detection of amyloids and treatment of diseases related to amyloids including Alzheimer's disease and other related amyloid-based neurodegenerative diseases.

Amyloid binding agents

Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection.

Interleukin-1 and tumor necrosis factor-&#x3b1; modulators; syntheses of such modulators and methods of using such modulators

A device and a method for measuring viscosity that includes attaching molecular rotors to a solid surface, exposing the solid surface to a fluid having a viscosity to be measured, and taking optical measurements to determine viscosity. The solid surface is preferably quartz, polystyrene or silicate glass, such as a fiber optic probe or a glass cuvette. The molecular rotors are of the type that includes an electron-donor group and electron-acceptor group that are linked by a single bond so that the groups may rotate with respect to one another, and that exhibit a fluorescence emission when rotation is hindered.

Supported molecular biofluid viscosity sensors for in vitro and in vivo use

Interleukin-1 and tumor necrosis factor-&#x3b1;modulators; syntheses of such modulators and methods of using such modulators

Novel compounds are disclosed that have the chemical structure of Formula (II), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-&#x3b1; modulators, and thus are useful in the treatment of various listed diseases. wherein the R groups are defined as provided in the specification. These compounds are useful, for example, as anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds are disclosed, as are methods of using these synthetic and semi-synthetic compounds in the treatment of the above-listed disease states.

Method of treating inflammation with acanthoic acid derivatives

Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&#x3b1; modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R-R, R, R, R-Ris not hydrogen, Ror Ror Ris not methyl, or Ris not CH, then Ris selected from the group consisting of hydrogen, a halogen, COOH, C-Ccarboxylic acids, C-Cacyl halides, C-Cacyl residues, C-Cesters, C-Csecondary amides, (C-C)(C-C) tertiary amides, (C-C)(C-C) cyclic amides, (C-C) amines, C-Calcohols, (C-C)(C-C) ethers, C-Calkyls, C-Csubstituted alkyls, C-Calkenyls, C-Csubstituted alkenyls, and C-Caryls. If all R-R, R, R, R-Rare hydrogen, R, R, and Rare each methyl, and Ris CH, then Ris selected from hydrogen, a halogen, C-Ccarboxylic acids, C-Cacyl halides, C-Cacyl residues, C-Cesters, C-Csecondary amides, (C-C)(C-C) tertiary amides, C-Calcohols, (C-C)(C-C) ethers other than methyl-acetyl ether, C-Calkyls, C-Csubstituted alkyls, C-Calkenyls, C-Csubstituted alkenyls, and C-Caryls. Rand Rare each separately selected from hydrogen, a halogen, C-Calkyl, C-Csubstituted alkyls, C-Calkenyl, C-Csubstituted alkenyl, C-Calkynyl, C-Cacyl, C-Calcohol, and C-Caryl. R-R, R, R, and R-Rare each separately selected from hydrogen, a halogen, C-Calkyl, C-Csubstituted alkyls, C-Calkenyl, C-Csubstituted alkenyl, C-Calkynyl, and C-Caryl. Ris selected from hydrogen, a halogen, C-Calkyl, C-Csubstituted alkyls, C-Calkenyl, C-Csubstituted alkenyl, and C-Calkynyl. Ris selected from hydrogen, a halogen, CH, C-Calkyl, C-Csubstituted alkyl, C-Calkenyl, C-Csubstituted alkenyl, C-Calcohol, and C-Caryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

Interleukin-1 and tumor necrosis factor-&#x3b1; modulators, synthesis of said modulators and their enantiomers and methods of using said modulators

Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&#x3b1; modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R&#x2013;R, R, R, R&#x2013;Ris not hydrogen, Ror Ror Ris not methyl, or Ris not CH, then Ris selected from the group consisting of hydrogen, a halogen, COOH, C&#x2013;Ccarboxylic acids, C&#x2013;Cacyl halides, C&#x2013;Cacyl residues, C&#x2013;Cesters, C&#x2013;Csecondary amides, (C&#x2013;C)(C&#x2013;C) tertiary amides, (C&#x2013;C)(C&#x2013;C) cyclic amides, (C&#x2013;C) amines, C&#x2013;Calcohols, (C&#x2013;C)(C&#x2013;C) ethers, C&#x2013;Calkyls, C&#x2013;Csubstituted alkyls, C&#x2013;Calkenyls, C&#x2013;Csubstituted alkenyls, and C&#x2013;Caryls. If all R&#x2013;R, R, R, R&#x2013;Rare hydrogen, R, R, and Rare each methyl, and Ris CH, then Ris selected from hydrogen, a halogen, C&#x2013;Ccarboxylic acids, C&#x2013;Cacyl halides, C&#x2013;Cacyl residues, C&#x2013;Cesters, C&#x2013;Csecondary amides, (C&#x2013;C)(C&#x2013;C) tertiary amides, C&#x2013;Calcohols, (C&#x2013;C)(C&#x2013;C) ethers other than methyl-acetyl ether, C&#x2013;Calkyls, C&#x2013;Csubstituted alkyls, C&#x2013;Calkenyls, C&#x2013;Csubstituted alkenyls, and C&#x2013;Caryls. Rand Rare each separately selected from hydrogen, a halogen, C&#x2013;Calkyl, C&#x2013;Csubstituted alkyls, C&#x2013;Calkenyl, C&#x2013;Csubstituted alkenyl, C&#x2013;Calkynyl, C&#x2013;Cacyl, C&#x2013;Calcohol, and C&#x2013;Caryl. R&#x2013;R, R, R, and R&#x2013;Rare each separately selected from hydrogen, a halogen, C&#x2013;Calkyl, C&#x2013;Csubstituted alkyls, C&#x2013;Calkenyl, C&#x2013;Csubstituted alkenyl, C&#x2013;Calkynyl, and C&#x2013;Caryl. Ris selected from hydrogen, a halogen, C&#x2013;Calkyl, C&#x2013;Csubstituted alkyls, C&#x2013;Calkenyl, C&#x2013;Csubstituted alkenyl, and C&#x2013;Calkynyl. Ris selected from hydrogen, a halogen, CH, C&#x2013;Calkyl, C&#x2013;Csubstituted alkyl, C&#x2013;Calkenyl, C&#x2013;Csubstituted alkenyl, C&#x2013;Calcohol, and C&#x2013;Caryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

Interleukin-1 and tumor necrosis factor-&#x3b1;  modulators, synthesis of said modulators and their enantiomers and methods of using said modulators

Disclosed herein are novel tricyclic diterpene compounds. These compounds, including their prodrug esters and acid-addition salts, are useful as Interleukin-1 and Tumor Necrosis Factor-&#x3b1; modulators, and thus are useful in the treatment of various diseases. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of the novel compounds that are useful as anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making the compounds and their analogs are also disclosed, as are methods of using these synthetic and semi-synthetic compounds in the treatment of the above-listed disease states.

Tricyclic diterpene derivatives

Silylating reagents having a group other than a divalent oxygen separating two silyl groups provide regioselective protection of reactive groups under robust conditions, such as basic conditions used in alkylation, acylation and deoxygenation. In particular, silylating reagents having a group other than oxygen separating two silyl groups are useful for protecting two hydroxy groups of a ribonucleic or deoxyribonucleic acid. Alkylation of a 2&prime;-hydroxy group of a ribonucleoside protected with the inventive silylating agents in the presence of an excess of a mild hindered base such as sodium HMDS may be carried out without protecting the exocyclic amine and oxo functionalities of nucleobases.

Growing community of inventors

San Diego, CA, United States of America

Emmanuel A Theodorakis