39945-51-2Relevant articles and documents
New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study
Maccallini, Cristina,Gallorini, Marialucia,Sisto, Francesca,Akdemir, Atilla,Ammazzalorso, Alessandra,De Filippis, Barbara,Fantacuzzi, Marialuigia,Giampietro, Letizia,Carradori, Simone,Cataldi, Amelia,Amoroso, Rosa
, p. 1632 - 1645 (2021/07/28)
Nonsteroidal aromatase inhibitors (NSAIs) are well-established drugs for the therapy of breast cancer. However, they display some serious side effects, and their efficacy can be compromised by the development of chemoresistance. Previously, we have report
Method of fluorination using iodonium ylides
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Page/Page column 60-61, (2019/04/30)
A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
Carbazole inhibitors of histamine receptors for the treatment of disease
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, (2012/01/04)
The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
Potent inhibition of Norwalk virus by cyclic sulfamide derivatives
Dou, Dengfeng,Tiew, Kok-Chuan,He, Guijia,Mandadapu, Sivakoteswara Rao,Aravapalli, Sridhar,Alliston, Kevin R.,Kim, Yunjeong,Chang, Kyeong-Ok,Groutas, William C.
experimental part, p. 5975 - 5983 (2011/11/07)
A new class of compounds that exhibit anti-norovirus activity in a cell-based system and embody in their structure a cyclosulfamide scaffold has been identified. The structure of the initial hit (compound 2a, ED50 4 μM, TD50 50 μM) has been prospected by exploiting multiple points of diversity and generating appropriate structure-activity relationships.
A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
scheme or table, p. 3669 - 3674 (2011/12/16)
An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
10-Substituted Cytisine Derivatives and Methods of Use Thereof
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Page/Page column 32, (2010/03/31)
The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is subs
NOVEL CYCLIC AMINOBENZOIC ACID DERIVATIVE
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Page/Page column 51, (2010/11/27)
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or - (CH2)n- (n represents 0,1 or 2) ; X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and -COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity
Chellappan, Sheela K.,Xiao, Yingxian,Tueckmantel, Werner,Kellar, Kenneth J.,Kozikowski, Alan P.
, p. 2673 - 2676 (2007/10/03)
We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was foun
2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION
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Page/Page column 80, (2010/11/30)
A 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented by the generalformula (1): [Chemical formula 1] (1) or a pharmaceutically acceptable saltthereof. They are useful as a therapeutic/preventive agent for diabetes, diabeticnephropathy, or glomerulosclerosis.
LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, AND METHODS OF MAKING AND USING THEM
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Page 85, (2010/02/10)
One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.
