913168-10-2Relevant academic research and scientific papers
CONJUGATION OF MCR1 LIGAND WITH CYTOTOXIC DRUGS FOR TREATING SKIN CANCER
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, (2021/01/29)
Ligand-drug conjugates for targeted melanoma therapies are disclosed herein. A ligand is conjugated to a cytotoxic cancer drug through a cleavage linker. The ligand can bind to an overexpressed receptor on a cancer cell, resulting in selectivity. This allows the drug to enter a cancer cell selectively and release the drug within that specific cancer cell. Such therapies provide selectivity to melanoma through a ligand that targets the MC1R receptor, which is highly expressed in 80% of malignant melanomas. The ligand-drug conjugates can be used to deliver a wide range of cytotoxic cancer drugs selective to melanoma cells which may solve the drug resistance problem of melanoma in current therapies.
Novel mTOR inhibitor compounds and the use thereof
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Paragraph 0085; 0090; 0118-0120, (2021/03/09)
The novel mTOR inhibitor compounds of the present invention are capable of selective drug delivery to bone and released slowly in bone for a long period of time. The present invention relates to a targeted compound linked to a mTOR inhibitory bone disease therapeutic agent.
Novel mTOR inhibitor compounds and the use thereof
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Paragraph 0113-0118; 0146-0148, (2021/03/16)
The novel mTOR inhibitor compounds of the present invention are capable of selective drug delivery to bone and released slowly in bone for a long period of time. The present invention relates to a targeted compound linked to a mTOR inhibitory bone disease therapeutic agent.
HSP90-TARGETING CONJUGATES AND FORMULATIONS THEREOF
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Paragraph 00378, (2018/07/05)
Conjugates of an active agent attached to a targeting moiety, such as an HSP90 binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.
A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors
Kraj?ovi?ová, Soňa,Gucky, Tomá?,Hendrychová, Denisa,Kry?tof, Vladimír,Soural, Miroslav
, p. 13530 - 13541 (2017/12/15)
Herein, we report an alternative synthetic approach for selected 2,6,9-trisubstituted purine CDK inhibitor conjugates with folic acid as a drug-delivery system targeting folate receptors. In contrast to the previously reported approaches, the desired conj
NEUROTENSIN RECEPTOR BINDING CONJUGATES AND FORMULATIONS THEREOF
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Paragraph 00335, (2017/11/10)
Conjugates of an active agent attached to a neurotensin receptor-binding targeting moiety via a linker have been designed. Nanoparticles and microparticles comprising such conjugates can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or other diseases.
PENICILLAMINE CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
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Paragraph 00385, (2018/01/17)
Conjugates of an active agent attached to a targeting moiety via a penicillamine linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide increased stability and improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.
TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
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Paragraph 00569, (2016/01/25)
Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designe
DUPA Conjugation of a Cytotoxic Indenoisoquinoline Topoisomerase i Inhibitor for Selective Prostate Cancer Cell Targeting
Roy, Jyoti,Nguyen, Trung Xuan,Kanduluru, Ananda Kumar,Venkatesh, Chelvam,Lv, Wei,Reddy, P. V. Narasimha,Low, Philip S.,Cushman, Mark
, p. 3094 - 3103 (2015/04/27)
(Figure Presented). Prostate-specific membrane antigen (PSMA) is overexpressed in most prostate cancer cells while being present at low or undetectable levels in normal cells. This difference provides an opportunity to selectively deliver cytotoxic drugs
PROCESSES FOR MAKING EPOTHILONE COMPOUNDS AND ANALOGS
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Page/Page column 50, (2009/01/20)
The present invention relates to processes for making epothilone compounds and analogs thereof, such as epi-epothilone A or epi-epothilone B, and aziridinyl-epothilone analogs.
