C07B59/00

Deuterium-enriched isoindolinonyl-piperidinonyl conjugates and oxoquinazolin-3(4H)-yl-piperidinonyl conjugates and methods of treating medical disorders using same
09809603 · 2017-11-07 · ·

The invention provides deuterium-enriched isoindolinonyl-piperidinonyl conjugates, deuterium-enriched oxoquinazolin-3(4H)-yl-piperidinonyl conjugates, pharmaceutical compositions, and methods of using such conjugates and pharmaceutical compositions to treat cancer, angiogenesis disorders, immune disorders, and other medical disorders.

PET Tracer Purification System

The present invention provides a new chemical process, a new cassette configuration, and new software for the automated production of multiple batches of an [.sup.18F]-labelled compound on a single cassette. The invention allows one synthesizer in one hot cell to produce sequentially a plurality of batches of [.sup.18F]-labelled PET tracer in the same day. In particular, the present invention provides a novel arrangement useful for purifying two consecutive batches of a reaction mixture comprising an .sup.18F-labelled compound.

PET Tracer Purification System

The present invention provides a new chemical process, a new cassette configuration, and new software for the automated production of multiple batches of an [.sup.18F]-labelled compound on a single cassette. The invention allows one synthesizer in one hot cell to produce sequentially a plurality of batches of [.sup.18F]-labelled PET tracer in the same day. In particular, the present invention provides a novel arrangement useful for purifying two consecutive batches of a reaction mixture comprising an .sup.18F-labelled compound.

2-Amino-3,5-Difluoro-3,6-Dimethyl-6-Phenyl-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treating Alzheimer's Disease
20170313658 · 2017-11-02 · ·

The present invention is directed to compounds according to Formula (I) which compounds are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for 5 which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.

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ISOINDOLINE DERIVATIVE, INTERMEDIATE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
20170313676 · 2017-11-02 ·

Provided are an isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereof. The isoindoline derivative and the pharmaceutical composition thereof can regulate the production or activity of immunological cytokines, thus effectively treating cancer and inflammatory disease.

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ORGANIC ELECTROLUMINESCENCE DEVICE

The present invention provides an organic EL device having at least an anode, a hole injection layer, a first hole transport layer, a second hole transport layer, a luminous layer, an electron transport layer, and a cathode in order of description. The second hole transport layer includes an arylamine compound having a specific structure, and the electron transport layer includes a pyrimidine derivative having a specific structure. The organic EL device of the present invention has a high efficiency, a low driving voltage, and a longer life.

ORGANIC ELECTROLUMINESCENCE DEVICE

The present invention provides an organic EL device having at least an anode, a hole injection layer, a first hole transport layer, a second hole transport layer, a luminous layer, an electron transport layer, and a cathode in order of description. The second hole transport layer includes an arylamine compound having a specific structure, and the electron transport layer includes a pyrimidine derivative having a specific structure. The organic EL device of the present invention has a high efficiency, a low driving voltage, and a longer life.

6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT

The present invention comprises compounds of Formula I.

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wherein: A.sup.1, A.sup.2, A.sup.3, A.sup.4, A.sup.5, R.sup.1, and R.sup.2 are defined in the specification.

The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPYL

Methods, and related compositions, for the improved synthesis of [.sup.18F]DCFPyL are disclosed. Also provided are methods, and related compositions, for the use of [.sup.18F]DCFPyL so produced.

RHO KINASE INHIBITOR BA-1049 (R) AND ACTIVE METABOLITES THEREOF

The disclosure provides rho kinase inhibitor BA-1049(R), an hydroxy metabolite of BA-1049(R), and adipate salts and deuterated forms thereof, useful for treating CNS disorders and injuries.