156079-00-4Relevant academic research and scientific papers
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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Page/Page column 416; 417, (2021/01/29)
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
METHODS FOR PREPARING PSMA CONJUGATES
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Paragraph 0259-0260, (2020/12/07)
This disclosure relates to processes for preparing compounds that are useful in the treatment of disease, such as cancer, in mammals. In particular, the invention described herein pertains to processes for preparing compounds capable of targeting PSMA exp
1,3,4-OXADIAZOLE AND THIADIAZOLE COMPOUNDS AS IMMUNOMODULATORS
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Paragraph 57, (2016/09/26)
The present invention relates to 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by
Water-soluble and cleavable quercetin-amino acid conjugates as safe modulators for P-glycoprotein-based multidrug resistance
Kim, Mi Kyoung,Choo, Hyunah,Chong, Youhoon
, p. 7216 - 7233 (2015/01/08)
Quercetin-amino acid conjugates with alanine or glutamic acid moiety attached at 7-O and/or 3-O position of quercetin were prepared, and their multidrug resistance (MDR)-modulatory effects were evaluated. A quercetin-glutamic acid conjugate, 7-O-Glu-Q (3a
CONJUGATES FOR TREATING DISEASES CAUSED BY PSMA EXPRESSING CELLS
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Page/Page column 67-68, (2014/06/11)
The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.
In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates
Kim, Mi Kyoung,Park, Kwang-su,Yeo, Woon-seok,Choo, Hyunah,Chong, Youhoon
experimental part, p. 1164 - 1171 (2009/07/11)
In order to discover a quercetin prodrug with improved bioavailability, we synthesized nine quercetin-amion acid conjugates and estimated their pharmacokinetic properties including water solubility, stability against chemical or enzymatic hydrolysis, and
Novel inhibitors of carboxypeptidase G2 (CPG2): Potential use in antibody-directed enzyme prodrug therapy
Khan, Tariq H.,Eno-Amooquaye, Ebun A.,Searle, Frances,Browne, Pat J.,Osborn, Helen M. I.,Burke, Philip J.
, p. 951 - 956 (2007/10/03)
The design and synthesis of potent thiocarbamate inhibitors for carboxypeptidase G2 are described. The best thiocarbamate inhibitor N-(p- methoxybenzenethiocarbonyl)amino-L-glutamic acid 6d, chosen for preliminary investigations of in vitro ant
High purity N-(4-[N,N-bis(2-iodoethyl)amino]phenoscycarbonyl)-L-glutamic acid
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, (2008/06/13)
A new salt of a prodrug useful in antibody directed enzyme prodrug therapy (ADEPT) is disclosed. A hydrogen iodide salt of the prodrug N-(4-[N,N-bis(2-iodoethyl)amino]phenoxycarbonyl)-L-glutamic acid is prepared which can be obtained in crystalline form. Preparation of the crystalline form of the prodrug enables preparation of the prodrug in highly pure form.
Optimization of Alkylating Agent Prodrugs Derived from Phenol and Aniline Mustards: A New Clinical Candidate Prodrug (ZD2767) for Antibody-Directed Enzyme Prodrug Therapy (ADEPT)
Springer, Caroline J.,Dowell, Robert,Burke, Philip J.,Hadley, Elma,Davies, D. Huw,et al.
, p. 5051 - 5065 (2007/10/03)
Sixteen novel potential prodrugs derived from phenol or aniline mustards and their 16 corresponding drugs with ring substitution and/or different alkylating functionalities were designed.The 4-bis(2-bromoethyl)-(1a), 4-bis(2-iodoethyl)-(1b), and
