Patent classifications
C07D221/16
Ligands for Alpha-7 Nicotinic Acetylcholine Receptors and Methods of Treating Neurological and Inflammatory Conditions
Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.
Compositions and methods for decreasing, or preventing or reversing gain of, skin pigmentation in a mammalian subject
The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR).
Compositions and methods for decreasing, or preventing or reversing gain of, skin pigmentation in a mammalian subject
The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR).
Process for the preparation of cycloheptapyridine CGRP receptor antagonists
The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process. ##STR00001##
Compounds comprising a hetero-fluorene group
The present invention relates to a compound, and to an organic semiconductor layer comprising this compound, suitable for use as an organic semiconductor layer for electronic devices, and a method of manufacturing the same, wherein the compound comprises a hetero-fluorene group and is represented by formula 1.
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NOVEL SUBSTITUTED TRICYCLIC COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Organic molecules having two non-conjugated bridges between a donor and an acceptor for effective thermally activated delayed fluorescence for use in optoelectronic devices
The invention relates to purely organic emitter molecules of a new type according to formula I and to the use thereof in optoelectronic devices, in particular in organic light-emitting diodes (OLEDs), comprising donor D: an aromatic or heteraromatic chemical group on which the HOMO is located and which optionally has at least one substitution; acceptor A: an aromatic or heteromatic chemical group on which the LUMO is located and which optionally has at least one substitution; bridge B1, bridge B2: organic groups that link the donor D and the acceptor A in a non-conjugated manner; wherein in particular the energy difference ΔE(S.sub.1−T.sub.1) between the lowest excited singlet (S1) state of the organic emitter molecule and the triplet (T1) state of the organic emitter molecule lying thereunder is less than 2000 cm.sup.−1.
Organic molecules having two non-conjugated bridges between a donor and an acceptor for effective thermally activated delayed fluorescence for use in optoelectronic devices
The invention relates to purely organic emitter molecules of a new type according to formula I and to the use thereof in optoelectronic devices, in particular in organic light-emitting diodes (OLEDs), comprising donor D: an aromatic or heteraromatic chemical group on which the HOMO is located and which optionally has at least one substitution; acceptor A: an aromatic or heteromatic chemical group on which the LUMO is located and which optionally has at least one substitution; bridge B1, bridge B2: organic groups that link the donor D and the acceptor A in a non-conjugated manner; wherein in particular the energy difference ΔE(S.sub.1−T.sub.1) between the lowest excited singlet (S1) state of the organic emitter molecule and the triplet (T1) state of the organic emitter molecule lying thereunder is less than 2000 cm.sup.−1.
Compounds, compositions and methods for prevention and/or treatment of cancer
The present invention includes compounds, compositions and methods that are useful for preventing or treating melanoma or any other cancer in a subject, such as a GPCR-expressing cancer. In certain embodiments, the compounds comprise estrogen (including estrogen derivatives or analogues), a selective GPER agonist and/or another G-protein coupled receptor (GPCR) agonist that increases cancer cell differentiation.
Mutant KRAS inhibitors
Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.