676477-10-4Relevant academic research and scientific papers
Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach
Ratni, Hasane,Rogers-Evans, Mark,Bissantz, Caterina,Grundschober, Christophe,Moreau, Jean-Luc,Schuler, Franz,Fischer, Holger,Alvarez Sanchez, Ruben,Schnider, Patrick
, p. 2275 - 2289 (2015)
From a micromolar high throughput screening hit 7, the successful complementary application of a chemogenomic approach and of a scaffold hopping exercise rapidly led to a low single digit nanomolar human vasopressin 1a (hV1a) receptor antagonist 38. Initial optimization of the mouse V1a activities delivered suitable tool compounds which demonstrated a V1a mediated central in vivo effect. This novel series was further optimized through parallel synthesis with a focus on balancing lipophilicity to achieve robust aqueous solubility while avoiding P-gp mediated efflux. These efforts led to the discovery of the highly potent and selective brain-penetrant hV1a antagonist RO5028442 (8) suitable for human clinical studies in people with autism.
Novel indole derivative and medicine containing the same (by machine translation)
-
Paragraph 0133; 0134, (2018/06/30)
[A] formation of Amyloid fibrils can be compounds, including therapeutic or prophylactic agent for neurodegenerative disease Amyloid fibrils formation inhibitor compound and of. (I) or its pharmaceutically acceptable compound represented by the formula [a] or a salt or solvate thereof includes the, Amyloid fibrils formation inhibitor. [R1 And R2 Each independently is H, an alkyl group, a cyano group or the like; R3 And R4 Each independently is H, or an alkyl group; R3 And R4 The, joint may form a ring; Ar1 And Ar2 The substituted or unsubstituted heteroaryl group are independently substituted/unsubstituted aryl groups /; X and Y are each independently a single bond, - (=O) - C etc., Z is O or CH2 ; N is an integer of 1 - 3][Drawing] no (by machine translation)
AROMATIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS
-
Paragraph 00416; 00420, (2015/07/07)
Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.
NOVEL BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
-
Paragraph 0153; 0154, (2013/03/26)
The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
-
Page/Page column 26; 28; 29, (2013/03/26)
The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
AZASPIRO DERIVATIVES
-
Page/Page column 17, (2008/12/06)
The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorder
INDOLE COMPOUNDS
-
Page/Page column 22, (2008/06/13)
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof; (formula I) wherein X, R1,R2, and R3are as defined in the specification, a process for the preparation of such compounds, pharmaceutical composi
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping
Hall, Adrian,Billinton, Andy,Brown, Susan H.,Chowdhury, Anita,Giblin, Gerard M.P.,Goldsmith, Paul,Hurst, David N.,Naylor, Alan,Patel, Sadhana,Scoccitti, Tiziana,Theobald, Pamela J.
, p. 2684 - 2690 (2008/12/21)
We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy i
Indol-3-y-carbonyl-piperidin and piperazin-derivatives
-
Page/Page column 21, (2010/11/25)
The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention
