145133-11-5

Upstream product

• 4200-46-8 (1H-imidazol-4-yl)-acetic acid methyl ester 
• 76-83-5 trityl chloride 
• 596-43-0 bromo-triphenyl-methane 
• 3251-69-2 2-(1H-imidazol-5-yl)acetic acid hydrochloride 
• 51718-80-0 methyl 2-(1H-imidazol-4-yl)acetate hydrochloride 
• 3251-69-2 imidazole-4-acetic acid hydrochloride 

Downstream Products

• 199007-39-1 (±)-methyl 3-phenyl-2-(1-trityl-1H-imidazol-4-yl)propanoate 
• 574704-86-2 [3-(4-cyano-3-naphthalen-1-yl-benzyl)-3H-imidazol-4-yl]-acetic acid methyl ester 
• 179026-34-7 [1-(4-Cyanobenzyl)-1H-imidazol-5-yl]acetic acid methyl ester 
• 445434-57-1 methyl [1-(4-Cyano-3-fluorobenzyl)-1H-imidazol-5-yl]acetate 
• 179025-89-9 1-(4-nitrophenylmethyl)-1H-imidazol-5-ylacetic acid methyl ester 
• 497160-00-6 2-(1-trityl-1H-imidazol-4-yl)-malonic acid dimethyl ester 
• 731746-84-2 2-(1H-imidazol-4-yl)-2-methylpropanoic acid 

Relevant academic research and scientific papers

ACYCLIC CXCR4 INHIBITORS AND USES THEREOF

The present invention relates to compounds and methods useful for modulation, e.g. inhibition, of C-X-C receptor type 4 (CXCR4). The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the compositions in the treatment of various disorders.

α-Amino Acid-Isosteric α-Amino Tetrazoles

The synthesis of all 20 common natural proteinogenic and 4 otherα-amino acid-isosteric α-amino tetrazoles has been accomplished, whereby the carboxyl group is replaced by the isosteric 5-tetrazolyl group. The short process involves the use of the key Ugi tetrazole reaction followed by deprotection chemistries. The tetrazole group is bioisosteric to the carboxylic acid and is widely used in medicinal chemistry and drug design. Surprisingly, several of the common α-amino acid-isosteric α-amino tetrazoles are unknown up to now. Therefore a rapid synthetic access to this compound class and non-natural derivatives is of high interest to advance the field.

Discovery of α-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of ρ1γ-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone

The ρ-containing γ-aminobutyric acid type A receptors (GABAARs) play an important role in controlling visual signaling. Therefore, ligands that selectively target these GABAARs are of interest. In this study, we demonstrate that the partial GABAAR agonist imidazole-4-acetic acid (IAA) is able to penetrate the blood–brain barrier in vivo; we prepared a series of α- and N-alkylated, as well as bicyclic analogues of IAA to explore the structure–activity relationship of this scaffold focusing on the acetic acid side chain of IAA. The compounds were prepared via IAA from l-histidine by an efficient minimal-step synthesis, and their pharmacological properties were characterized at native rat GABAARs in a [3H]muscimol binding assay and at recombinant human α1β2γ2Sand ρ1GABAARs using the FLIPR membrane potential assay. The (+)-α-methyl- and α-cyclopropyl-substituted IAA analogues ((+)-6 a and 6 c, respectively) were identified as fairly potent antagonists of the ρ1GABAAR that also displayed significant selectivity for this receptor over the α1β2γ2SGABAAR. Both 6 a and 6 c were shown to inhibit GABA-induced relaxation of retinal arterioles from porcine eyes.

IMIDAZOLE DERIVATIVES USED AS TAFIA INHIBITORS

The invention relates to compounds of formula (I), which are inhibitors of the activated thrombin-activatable fibrinolysis inhibitor. The compounds of formula (I) are suited for producing medicaments for the prevention and treatment of diseases accompanied by thromboses, embolisms, hypercoagulability or fibrotic changes.

Prenyl transferase inhibitors

A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R23); and the remaining substituents are as defined in the disclosure.

Dihydro-2h-napthalene-1-one inhibitors of ras farnesyl transferase

The present invention provides dihydro-2H-napthalene-1-ones of formula (V), and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such a

Inhibitors of prenyl-protein transferase

The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Inhibitors of prenyl-protein transferase

The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds

Inhibitors of prenyl-protein transferase

The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors

PCT No. PCT/US97/06257 Sec. 371 Date Oct. 2, 1998 Sec. 102(e) Date Oct. 2, 1998 PCT Filed Apr. 1, 1997 PCT Pub. No. WO97/36876 PCT Pub. Date Oct. 9, 1997The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.