N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the α2δ subunit of voltage gated calcium channels
摘要:
A series of N-acridin-9-yl-butane-1,4-diamines were found to be high-affinity ligands of the alpha(2)deltasubunit of voltage gated calcium channels. The SAR studies of butane-1,4-diamine side chain resulted in the identification of compound 10 (IC50=9 nM), which is more potent than gabapentin (IC50=27 nM). Partial saturation of the acridine ring was also pursued and provided a compound with higher binding affinity than 1. (C) 2004 Elsevier Ltd. All rights reserved.
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the α2δ subunit of voltage gated calcium channels
摘要:
A series of N-acridin-9-yl-butane-1,4-diamines were found to be high-affinity ligands of the alpha(2)deltasubunit of voltage gated calcium channels. The SAR studies of butane-1,4-diamine side chain resulted in the identification of compound 10 (IC50=9 nM), which is more potent than gabapentin (IC50=27 nM). Partial saturation of the acridine ring was also pursued and provided a compound with higher binding affinity than 1. (C) 2004 Elsevier Ltd. All rights reserved.
The present invention provides a compound represented by the formula:
wherein Ar is an aryl group optionally having substituents, R is a C
1-6
alkyl group, R
1
is a hydrogen atom, a hydrocarbon group optionally having substituents, an acyl group or a heterocyclic group optionally having substituents, X is an oxygen atom or an imino group optionally having substituents, ring A is a piperidine ring optionally further having substituents, and ring B is a benzene ring having substituents, or a salt thereof, and an agent for the prophylaxis or treatment of lower urinary tract abnormality and the like, which contains the compound.
[EN] STAT DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION DE STAT ET LEURS UTILISATIONS
申请人:KYMERA THERAPEUTICS INC
公开号:WO2021188696A1
公开(公告)日:2021-09-23
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用相同的方法。
[EN] PYRIDIN-4-YLAMINE COMPOUNDS USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN<br/>[FR] COMPOSES DE PYRIDIN-4-YLAMINE CONVENANT POUR LE TRAITEMENT DE LA DOULEUR NEUROPATHIQUE
申请人:MERCK & CO INC
公开号:WO2005051915A1
公开(公告)日:2005-06-09
The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
NITROGENOUS COMPOUNDS AND ANTIVIRAL DRUGS CONTAINING THE SAME
申请人:Kureha Chemical Industry Co., Ltd.
公开号:EP1273571A1
公开(公告)日:2003-01-08
The present invention provides novel compounds having antiviral activities and antiviral drugs containing the compounds as the active ingredient. The compounds are shown by the following general formula (1),
wherein typically A1 and A2 are each guanidine or a group of the general fomula (ia) ; A3 is a mono- or poly-cyclic heteroaromatic ring contining 1 or 2 heteroatoms ; B1 is a single bond or alkylene group; R1 is hydrogen or alkyl group; W is an alkylene having 2-3 carbons, a cycloalkylene having 5-10 carbons, aromatic ring having 6-10 carbons, or a heteroaromatic ring having 5-10 carbons; y is C(=O)-; x is -C(=O)-NH-; n1 is an integer of 1-2; n2 is an integer of 2-3; D is a substituent selected from among various groups.