University of Nebraska

University of Pennsylvania

Ikaria Inc.

University of California

Sdg LLC

Stephen Gregory DiMagno

Michael J Therien

Bao Hu

Haoran Sun

Kevan M Shokat

Chao Zhang

Alma L Burlingame

Masahiro Tanaka

Kirk Hansen

Ronald Cerny

Raynard L Bateman

Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods.

Functionally modified polypeptides and radiobiosynthesis

The present invention relates to HPMA-CBz copolymers and methods for treating certain diseases comprising administering the copolymers to a subject in need thereof.

Drug delivery system for treating disease

The present application provides, inter alia, chemical compounds useful as synthesis intermediates, said compounds comprising one or more guanidinium moieties and a hypervalent iodine atom. Methods for making these compounds are also provided.

Guanidinium compounds

This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Radioiodinated compounds

This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation ofF labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Fluorination of aromatic ring systems

This invention relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated and radiofluorinated aromatic compounds.

Processes and reagents for making diaryliodonium salts

This disclosure relates to compounds, reagents, and methods useful in the synthesis of aryl fluorides, for example, in the preparation ofF labeled radiotracers. For example, this disclosure provides universal 'locked' aryl substituents that result in StereoElectronic Control of Unidirectional Reductive Elimination (SECURE) from diaryliodonium salts. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Iodonium Cyclophanes for SECURE arene functionalization

Provided herein are methods of detecting anions in solution. In particular, the methods can be used to detect trace anions in solution. For example, the anions can be present in an amount of between about 500 femtomoles to about 10 millimoles.

Detection and quantification of anions

The present invention is directed to a method for preparing an anhydrousF-radiolabeled fluorinating agent by a nucleophilic reaction of a hydratedF-radiolabeled fluoride ion source with an unsaturated carrier compound; treating theF-radiolabeled carrier compound to produce a non-aqueous mixture of theF-radiolabeled carrier compound in a solvent; and reacting theF-radiolabeled carrier compound with a nucleophilic composition in a nucleophilic reaction to produce an anhydrousF-radiolabeled fluorinating agent. The present invention is also directed to an anhydrousF-radiolabeled fluorinating agent comprising the formula [QM](F). Additionally, the present invention is directed to anF-radiolabeled fluorinated radiopharmaceutical or anF-radiolabeled fluorinated radiotracer prepared by reacting the anhydrousF-radiolabeled fluorinating agent with a drug intermediate. The present invention is further directed to methods for treating a disease or imaging a subject using anF-radiolabeled fluorinated radiopharmaceutical or anF-radiolabeled fluorinated radiotracer.

[object Object]

Anhydrous organic fluoride salts and reagents prepared by a method comprising the nucleophilic substitution of a fluorinated aromatic or fluorinated unsaturated organic compound with a salt having the formula:[QM]Ain an inert polar, aprotic solvent; wherein M is an atom capable of supporting a formal positive charge, the n groups Q are independently varied organic moieties, n is an integer such that the [QM] carries at least one formal positive charge, x is an integer defining the number of formal positive charge(s), +, carried by the [QM], Ais an anionic nucleophile capable of substituting for F in the fluorinated compound and F represents fluorine or a radioisotope thereof.

Anhydrous fluoride salts and reagents and methods for their production

This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventing or treating disease withH-Pyrrolo[2.3-d]pyrimidine derivatives. More specifically, the invention relates to a 1H-Pyrrolo[2.3-d]pyrimidine which is a compound of Formula I or II: or a pharmaceutically-acceptable salt or prodrug thereof;wherein:

1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof

Heavily fluorinated sugar analogs

The novel compounds of the present invention are .beta.-octafluoro-meso-tetraarylporphyrins of formula (I) and their metallic complexes of formula (II): ##STR1## .beta.-octafluoro-meso-tetraaryl porphyrins are synthesized by reacting 3,4-difluoropyrrole with an aromatic aldehyde in the presence of boron trifluoride etherate, followed by oxidation. The difluoropyrrole used in this reaction is produced by reacting 3,3,4,4-tetrafluoropyrroline or its corresponding salt, 3,3,4,4-tetrafluoropyrrolidinium salt, with a base such as potassium tert-butoxide. The metalloporphyrins of the present invention are synthesized by deprontonating .beta.-octafluoro-meso-tetraarylporphyrin ligands and treating said ligands with metal ions.

Octafluoro-meso-tetraarylporphyrins and methods for making these

Electron-deficient porphyrins are provided, as well as processes and intermediates for their preparation. In preferred embodiments, the electron-deficient porphyrins are prepared by condensing pyrrole derivatives and removing water thus formed from the resulting reaction mixture.

Growing community of inventors

Lincoln, NE, United States of America

Stephen Gregory DiMagno