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概览

疾病领域	数量

免疫系统疾病	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

5-LOX(5-脂氧合酶)	1

关联

4

项与 The Janssen Research Foundation 相关的药物

R-85355

靶点

5-LOX

作用机制

5-LOX抑制剂

在研机构

The Janssen Research Foundation

原研机构

The Janssen Research Foundation

在研适应症

银屑病

非在研适应症-

最高研发阶段临床阶段不明

首次获批国家/地区-

首次获批日期-

R-59949

靶点

DGK

作用机制

DGK抑制剂

在研机构-

原研机构

The Janssen Research Foundation

在研适应症-

非在研适应症-

最高研发阶段无进展

首次获批国家/地区-

首次获批日期-

R-90324

靶点

VEGFR x bFGF

作用机制

VEGFR拮抗剂 [+1]

在研机构-

原研机构

The Janssen Research Foundation

在研适应症-

非在研适应症

肿瘤

最高研发阶段无进展

首次获批国家/地区-

首次获批日期-

100 项与 The Janssen Research Foundation 相关的临床结果

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0 项与 The Janssen Research Foundation 相关的专利（医药）

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642

项与 The Janssen Research Foundation 相关的文献（医药）

2014-07-01·Behavioural Brain Research3区 · 心理学

Genetic deletion of PDE10A selectively impairs incentive salience attribution and decreases medium spiny neuron excitability

3区 · 心理学

Article

作者: De Backer, Jean-François ; Raes, Adam ; Gall, David ; D'Hooge, Rudi ; Schiffmann, Serge ; Lambot, Laurie ; Piccart, Elisabeth ; Vanhoof, Greet

The striatum is the main input structure to the basal ganglia and consists mainly out of medium spiny neurons. The numerous spines on their dendrites render them capable of integrating cortical glutamatergic inputs with a motivational dopaminergic signal that originates in the midbrain. This integrative function is thought to underly attribution of incentive salience, a process that is severely disrupted in schizophrenic patients. Phosphodiesterase 10A (PDE10A) is located mainly to the striatal medium spiny neurons and hydrolyses cAMP and cGMP, key determinants of MSN signaling. We show here that genetic depletion of PDE10A critically mediates attribution of salience to reward-predicting cues, evident in impaired performance in PDE10A knockout mice in an instrumentally conditioned reinforcement task. We furthermore report modest impairment of latent inhibition in PDE10A knockout mice, and unaltered prepulse inhibition. We suggest that the lack of effect on PPI is due to the pre-attentional nature of this task. Finally, we performed whole-cell patch clamp recordings and confirm suggested changes in intrinsic membrane excitability. A decrease in spontaneous firing in striatal medium spiny neurons was found. These data show that PDE10A plays a pivotal role in striatal signaling and striatum-mediated salience attribution.

2011-11-01·Synthetic Communications

Novel Procedure for the Coupling of Sterically Hindered Electron-Deficient Anilines to the 6-Position of the Purine Core

作者: Vandenput, Dirk ; Guillemont, Jérôme ; Lewi, Paul ; Leenders, Ruben ; Heeres, Jan

Sterically hindered electron-deficient anilines are coupled to the 6-position of the purine core only when activated as their corresponding TFA-amide.The free anilines did not react under all conditions tested.After aqueous work-up, the TFA-group is lost.This procedure provides a new tool in the construction of purines functionalized with a sterically hindered electron-deficient aniline in the 6-position.

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Lipid-itraconazole Interaction in Lipid Model Membranes

3区 · 医学

Article

作者: Ruysschaert, J-M ; Bossche, H Vanden ; Marichal, P ; Duquenoy, P H ; Brasseur, R ; Goormaghtigh, E

AbstractItraconazole, a lipophilic, fungal sterol-biosynthesis inhibitor, does not disturb membrane organization parameters measured by differential scanning calorimetry and infrared spectroscopy. Conformational analysis studies suggest that the molecular volume and the position of itraconazole in the lipid membrane is similar to that of dipalmitoyl phosphatidylcholine. The mean energy of interaction between itraconazole and the phospholipid is-60.6 kJ mol−1 whereas this energy in the pure lipid matrix is-54.3 kJ mol−1. The mean molecular area of itraconazole calculated by projecting the molecule on the lipid-water interface is equal to that occupied by the pure lipid (60 Å2/molecule).

100 项与 The Janssen Research Foundation 相关的药物交易

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100 项与 The Janssen Research Foundation 相关的转化医学

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其他

4

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当前项目

药物(靶点)	适应症	全球最高研发状态

R-85355 ( 5-LOX )	银屑病更多	临床阶段不明
R-59949 ( DGK )	-	无进展
R-173262	免疫系统疾病更多	无进展
R-90324 ( VEGFR x bFGF )	肿瘤更多	无进展