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排名前五的药物类型	数量

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5

项与 Therabel Research S.A. 相关的药物

THE-320

靶点-

作用机制-

在研机构

Therabel Research S.A.

原研机构

Therabel Research S.A.

在研适应症

前列腺增生症

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区-

首次获批日期-

THE-1869

靶点-

作用机制-

在研机构-

原研机构

Therabel Research S.A.

在研适应症-

非在研适应症

心绞痛

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

THE/DL-302

靶点

NCX1

作用机制

NCX1抑制剂

在研机构-

原研机构

Therabel Research S.A.

在研适应症-

非在研适应症

心脏衰竭

最高研发阶段终止

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100 项与 Therabel Research S.A. 相关的临床结果

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0 项与 Therabel Research S.A. 相关的专利（医药）

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7

项与 Therabel Research S.A. 相关的文献（医药）

2001-03-01·Journal of Medicinal Chemistry1区 · 医学

Electrooxidation Potential as a Tool in the Early Screening for New Safer Clozapine-like Analogues

1区 · 医学

Article

作者: Wikström, Håkan ; Deby-Dupont, Ginette ; Bruhwyler, Jacques ; Delarge, Jacques ; Mouithys-Mickalad, Ange ; Kauffmann, Jean-Michel ; Géczy, Joseph ; Damas, Jacques ; Liégeois, Jean-François ; Liao, Yi ; Petit, Christine

The chemical modification of clozapine (1) has permitted the finding of new analogues, e.g., olanzapine (2), quetiapine (3), 5-(4-methylpiperazin-1-yl)-8-chloropyrido[2,3-b][1,5]benzoxazepine fumarate (9), with a clinical or psychopharmacological profile similar to that of clozapine. However, when developing new derivatives, the designers are discouraged by the development of clozapine-induced agranulocytosis. Different researchers have raised the role played by the oxidizability of the molecule in such a deleterious effect. In the present paper, we examined the oxidation profile (direct scavenging abilities, efficacy in inhibiting lipid peroxidation, and electrooxidation potential) of newly developed methoxy and trifluoromethylsulfonyloxy analogues related to clozapine, some of them being described as putative antipsychotic. The oxazepine derivative 7, unlike the other diazepine derivatives (6, 10--12), was not readily oxidized. Using a statistical predictive model for hematotoxicity previously described, 7 was found in the cluster of potentially nontoxic compounds while diazepine derivatives 6 and 10-12 were classified as potentially toxic compounds. Among these original compounds, 7, which presents a preclinical clozapine-like profile and a low sensitivity to oxidation, could be a promising antipsychotic candidate with low side effects. Considering the tricyclic derivatives examined so far, some elements of structure-oxidation relationship (SOR) might be pointed out. Regarding the nature of the tricyclic ring substituent, from the most to the least sensitive to oxidation, the sequence was as follows: HO > Cl > CH(3)O > CF(3)SO(2)O. The nature of the tricyclic ring influenced also the sensitivity to oxidation; the diazepine moiety appeared to be the most reactive ring compared to oxa- and thiazepine congeners. These parameters could be advantageously integrated in the early design of new safer clozapine-like analogues.

1998-12-01·Behavioural Pharmacology4区 · 心理学

Comparative study of pirlindole, a selective RIMA, and its two enantiomers using biochemical and behavioural techniques

4区 · 心理学

Article

作者: Delarge, J. ; Dresse, A. ; Lejeune, C. ; Damas, J. ; De Tullio, P. ; Gerardy, J. ; Liegeois, J. F. ; Geczy, J. ; Bruhwyler, J. ; Decamp, E. ; Chleide, E.

The interaction with monoamine oxidase A (MAO-A) and B has been shown to be sensitive to the absolute configuration of molecules. Therefore, the aim of this study was to compare the effects of the racemic pirlindole (a selective and reversible MAO-A inhibitor) and its two enantiomers using biochemical techniques (in vitro and ex vivo determination of rat brain MAO-A and MAO-B activity) and behavioural models (forced swimming test and reserpine-induced hypothermia and palpebral ptosis test). In vitro, the MAO-A IC50 of (+/-)-pirlindole, R-(-)-pirlindole and S-(+)-pirlindole were 0.24, 0.43 and 0.18 microM, respectively. Ex vivo, their ID50 were 24.4, 37.8 and 18.7 mg/kg i.p. The differences between the three compounds were not significant, with a ratio between the two enantiomers [R-(-)/S-(+)] of 2.2 in vitro and 2.0 ex vivo. MAO-B was only slightly inhibited. In the forced swimming test and the reserpine-induced hypothermia and ptosis model, the three compounds had an antidepressant profile. In the forced swimming test, the minimal effective dose ratio between the R-(-) and the S-(+) was again around 2.0. The behavioural observations were thus clearly in accordance with the biochemical data.

1998-04-01·Current Medicinal Chemistry2区 · 医学

Dopamine D4 Receptors: A New Opportunity for Research on Schizophrenia

2区 · 医学

Review

作者: Liegeois, Jean-Francois ; Delarge, Jacques ; Eyrolles, Laurence ; Bruhwyler, Jacques

Classically, the D2 receptors formed the core of the dopamine hypothesis for schizophrenia. Recently, the dopamine D4 receptors have received particular attention in this context. This is due to the atypical antipsychotic, clozapine, which is effective in treating refractory schizophrenics without the side-effect profile of typical neuroleptics, and displays a ten-fold higher affinity for D4 compared to D2 or D3 receptors. Following various . reports presenting the interest of D4 receptors in treating schizophrenia, multiple chemical developments were made. During the last five years, various structures were described with a high selectivity for D4 receptor subtype. Currently, although the first clinical report was very disappointing, the observation which support the idea that D4 might serve as a target for clozapine have significantly modified and extended the understanding of mechanism underlying atypical antipsychotic treatment of schizophrenia.

100 项与 Therabel Research S.A. 相关的药物交易

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100 项与 Therabel Research S.A. 相关的转化医学

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药物(靶点)	适应症	全球最高研发状态

THE-320	前列腺增生症更多	批准上市
THE/DL-302 ( NCX1 )	心脏衰竭更多	终止
THE-1869	心绞痛更多	终止
JL-13 ( 5-HT2A receptor x D2 receptor x D4 receptor )	抑郁症更多	无进展
CYL-358	心绞痛更多	无进展