33769-07-2Relevant articles and documents
Targeting GRP receptor: Design, synthesis and preliminary biological characterization of new non-peptide antagonists of bombesin
Palmioli, Alessandro,Nicolini, Gabriella,Tripodi, Farida,Orsato, Alexandre,Ceresa, Cecilia,Donzelli, Elisabetta,Arici, Martina,Coccetti, Paola,Rocchetti, Marcella,La Ferla, Barbara,Airoldi, Cristina
supporting information, (2021/02/27)
We report the rational design, synthesis, and in vitro preliminary evaluation of a new small library of non-peptide ligands of Gastrin Releasing Peptide Receptor (GRP-R), able to antagonize its natural ligand bombesin (BN) in the nanomolar range of concen
ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE
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Paragraph 0968; 0969, (2020/05/06)
The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.
HETEROARYL RHEB INHIBITORS AND USES THEREOF
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Paragraph 00401, (2018/11/10)
The present invention provides compounds, compositions thereof, and methods of using the same. Compositions comprising a compound of this invention or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in compositions of this invention is such that it is effective to measurably inhibit Rheb, in a biological sample or in a patient.
Synthesis and antiproliferatory activity of ruthenium complexes containing N-heterocyclic carboxylates
Kennedy, David C.,James, Brian R.
, p. 32 - 36 (2017/03/11)
Solvates of the complexes Ru2Cl(pic)4(EtOH) (2), Ru(Im-CO2)3 (3), and Ru(Im-CO2)(Im-CO2H)Cl2 (4), were synthesized from reaction of RuCl3·3H2O or K3[RuCl6] with the N-heterocyclic carboxylic acids pyridine-2-carboxylic acid (picolinic acid, Hpic), and imidazole-4-carboxylic acid (Im-CO2H). Crystals of 2–4 could not be grown and hence characterization was done by elemental analysis, NMR, IR, and conductivity data; 2 and 4 were tested for antiproliferatory activity in vitro against a human breast cancer cell line, but were less active than, for example, Ru complexes containing bis-imidazole or 4,4′-biimidazole that we studied previously [see Can. J. Chem. 89 (2011) 948]. Preliminary work with a third potential ligand, 3-nitro-1,2,4-triazole-5-carboxylic acid (abbreviated HCANT), and other nitro heterocyclic compounds is also presented.
BICYCLIC LACTAMS AND METHODS OF USE THEREOF
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Page/Page column 132, (2017/01/23)
The invention provides novel compounds having the general formula I: (I) wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
Synthesis method of calmodulin inhibitor for treating brain-derived diseases
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Paragraph 0033; 0034; 0035, (2017/08/29)
The invention discloses a synthesis method of a calmodulin inhibitor for treating brain-derived diseases and belongs to the technical field of synthesis of chemicals. The technical scheme is characterized in that a synthetic route of the synthesis method
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors
Papillon, Julien P. N.,Adams, Christopher M.,Hu, Qi-Ying,Lou, Changgang,Singh, Alok K.,Zhang, Chun,Carvalho, Jose,Rajan, Srinivan,Amaral, Adam,Beil, Michael E.,Fu, Fumin,Gangl, Eric,Hu, Chii-Whei,Jeng, Arco Y.,LaSala, Daniel,Liang, Guiqing,Logman, Michael,Maniara, Wieslawa M.,Rigel, Dean F.,Smith, Sherri A.,Ksander, Gary M.
, p. 4749 - 4770 (2015/06/25)
CYP11B2, the aldosterone synthase, and CYP11B1, the cortisol synthase, are two highly homologous enzymes implicated in a range of cardiovascular and metabolic diseases. We have previously reported the discovery of LCI699, a dual CYP11B2 and CYP11B1 inhibi
Substituted Diphenylethers, -Amines, -Sulfides and -Methanes for the Treatment of Respiratory Disease
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Page/Page column 21, (2009/01/20)
The invention relates to substituted diphenylethers, -amines, -sulfides, and -methanes as useful pharmaceutical compounds for treating respiratory-disorders, pharmaceutical compositions containing them, and processes for their preparation.
ORGANIC COMPOUNDS
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Page/Page column 68-69, (2008/06/13)
The present invention provides a compound of formula (I):said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential
Tanaka, Rieko,Rubio, Almudena,Harn, Nancy K.,Gernert, Douglas,Grese, Timothy A.,Eishima, Jun,Hara, Mitsunobu,Yoda, Nobuyuki,Ohashi, Rui,Kuwabara, Takashi,Soga, Shiro,Akinaga, Shiro,Nara, Shinji,Kanda, Yutaka
, p. 1363 - 1382 (2008/02/13)
The design and synthesis of a novel piperidine series of farnesyltransferase (FTase) inhibitors with reduced potential for metabolic glucuronidation are described. The various substitution and exchange of the phenyl group at the C-2 position of the previously described 2-(4-hydroxy)phenyl-3-nitropiperidine 1a (FTase IC50 = 5.4 nM) resulted in metabolically stable compounds with potent FTase inhibition (14a IC50 = 4.3 nM, 20a IC50 = 3.0 nM, and 50a IC50 = 16 nM). Molecular modeling studies of these compounds complexed with FTase and farnesyl pyrophosphate are also described.