- Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903
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The transient receptor potential cation channel 5 (TRPC5) has been previously shown to affect podocyte survival in the kidney. As such, inhibitors of TRPC5 are interesting candidates for the treatment of chronic kidney disease (CKD). Herein, we report the synthesis and biological characterization of a series of N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors. Work reported here evaluates the benzimidazole scaffold and substituents resulting in the discovery of AC1903, a TRPC5 inhibitor that is active in multiple animal models of CKD.
- Sharma, Swagat H.,Pablo, Juan Lorenzo,Montesinos, Monica Suarez,Greka, Anna,Hopkins, Corey R.
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supporting information
p. 155 - 159
(2018/12/11)
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- BENZIMIDAZOLES AND AZA-BENZIMIDAZOLES, AND METHODS OF USE THEREOF
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Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II). (Formulae (II), (III))
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Page/Page column 47; 48
(2019/02/15)
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- Heterocyclic Ring and Carbocyclic Derivative
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The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect, e.g. a compound of Formula (I): wherein R2 is a hydrogen atom or the like; ring A is five- to seven-cycloalkane or th
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Paragraph 0398-0399
(2016/02/18)
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- Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists
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Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.
- Sasmal, Pradip K.,Sasmal, Sanjita,Rao, P. Tirumala,Venkatesham,Roshaiah,Abbineni, Chandrasekhar,Khanna, Ish,Jadhav, Vikram P.,Suresh,Talwar, Rashmi,Muzeeb, Syed,Receveur, Jean-Marie,Frimurer, Thomas M.,Rist, ?ystein,Elster, Lisbeth,H?gberg, Thomas
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scheme or table
p. 5443 - 5448
(2011/01/03)
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- MEDICINAL USE OF RECEPTOR LIGANDS
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Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5-membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH3; X is =CH- or =N-; L, is -CH2- or -CH2CH2- ; L2 is a bond, -CH2- or -CO-; R2 is H or C,-C3 alkyl, or -N(R2) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.
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Page/Page column 48-49
(2008/06/13)
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- Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis
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A series of 2-substituted N-benzyl benzimidazole containing molecules has been synthesized and its structure-activity relationship for the human DP receptor has been evaluated. Selective DP antagonists with nanomolar potency for the DP receptor were identified in this novel series of benzimidazoles.
- Beaulieu, Christian,Wang, Zhaoyin,Denis, Danielle,Greig, Gillian,Lamontagne, Sonia,O'Neill, Gary,Slipetz, Deborah,Wang, Jennifer
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p. 3195 - 3199
(2007/10/03)
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- Synthesis and antimicrobial activity of some new piperidinyl benzimidazoles
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A series of 2-(4-methylpiperidin-1-yl)-1,5(6)-disubstituted-1H- benzimidazoles (1-18) were prepared through the reaction of 2-chloro (or 2- chloromethyl)-1H-benzimidazole derivatives with 4-methylpiperidine. For the preparation of the individual isomers,
- Kus,Goker,Ayhan,Ertan,Altanlar,Akin
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p. 413 - 417
(2007/10/03)
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