Patent classifications
C07D243/12
Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action
The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action
The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
HETEROCYCLIC COMPOUNDS FOR TREATING OR PREVENTING DISORERS CAUSED BY REDUCED NEUROTRANSMISSION OF SEROTONIN, NOREPHNEPHRINE OR DOPAMINE
A heterocyclic compound represented by the general formula (1) or a salt thereof:
##STR00001## wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH.sub.2—; R.sup.1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R.sup.2 and R.sup.3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R.sub.2 and R.sub.3 are bonded to form a cyclo-C3-C8 alkyl group; and R.sup.4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
Metabotropic Glutamate Receptor Negative Allosteric Modulators (NAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
Metabotropic Glutamate Receptor Negative Allosteric Modulators (NAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
Haptens, hapten conjugates, compositions thereof preparation and method for their preparation and use
A method for performing a multiplexed diagnostic assay, such as for two or more different targets in a sample, is described. One embodiment comprised contacting the sample with two or more specific binding moieties that bind specifically to two or more different targets. The two or more specific binding moieties are conjugated to different haptens, and at least one of the haptens is an oxazole, a pyrazole, a thiazole, a nitroaryl compound other than dinitrophenyl, a benzofurazan, a triterpene, a urea, a thiourea, a rotenoid, a coumarin, a cyclolignan, a heterobiaryl, an azo aryl, or a benzodiazepine. The sample is contacted with two or more different anti-hapten antibodies that can be detected separately. The two or more different anti-hapten antibodies may be conjugated to different detectable labels.
Compositions and methods for modulating ciliogenesis
Disclosed herein are methods for modifying ciliogenesis in one or more cells of a subject, the method comprising administering to the subject an effective amount of a composition comprising a Notch signaling inhibitor, wherein the modification results in an increase in a number of cilia, an increase in a length of cilia, and/or an increase in a beat frequency of cilia as compared to a control. Also disclosed herein are methods for modifying ciliogenesis in one or more cells of a subject, the method comprising administering to the subject from 0.1 μg/kg to 100 g/kg of a Notch signaling inhibitor. In some embodiments, the methods can be used to treat Chronic Obstructive Pulmonary Disease (COPD), Emphysema, Asthma, Primary Ciliary Dyskinesia (PCD), Cystic Fibrosis (CF), or hydrocephalus.
Compositions and methods for modulating ciliogenesis
Disclosed herein are methods for modifying ciliogenesis in one or more cells of a subject, the method comprising administering to the subject an effective amount of a composition comprising a Notch signaling inhibitor, wherein the modification results in an increase in a number of cilia, an increase in a length of cilia, and/or an increase in a beat frequency of cilia as compared to a control. Also disclosed herein are methods for modifying ciliogenesis in one or more cells of a subject, the method comprising administering to the subject from 0.1 μg/kg to 100 g/kg of a Notch signaling inhibitor. In some embodiments, the methods can be used to treat Chronic Obstructive Pulmonary Disease (COPD), Emphysema, Asthma, Primary Ciliary Dyskinesia (PCD), Cystic Fibrosis (CF), or hydrocephalus.
Cholecystokinin B receptor targeting for imaging and therapy
Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.
Cholecystokinin B receptor targeting for imaging and therapy
Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.