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Drug delivery conjugates for treating resistant cancer and for use in combination therapy

A cancer and pharmaceutical technology, used in drug combinations, anti-tumor drugs, pharmaceutical formulations, etc., can solve problems such as adverse side effects, damage to host cells, non-pathogenic cells, etc.

Inactive Publication Date: 2017-02-22
ENDOCTYE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many currently available chemotherapeutic agents and radiation therapy regimens have undesirable side effects because they lack sufficient selectivity to preferentially destroy pathogenic cells and thus may also harm normal host cells (such as cells of the hematopoietic system) and other non-specific cells. pathogenic cells

Method used

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  • Drug delivery conjugates for treating resistant cancer and for use in combination therapy
  • Drug delivery conjugates for treating resistant cancer and for use in combination therapy
  • Drug delivery conjugates for treating resistant cancer and for use in combination therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0165] Compound Example

[0166] The compounds described herein can be prepared using the procedures and syntheses described herein and using general methods of organic synthesis. In particular, methods for preparing such compounds are described in US Patent Application Publication No. 2005 / 0002942, the disclosure of which is incorporated herein by reference.

[0167] Example. General formation of folate-peptides. Preparation of Folate-Containing Peptidyl Fragment Pte-Glu-(AA) by a Polymer-Supported Sequential Method Using Standard Methods n -NH(CHR 2 )CO 2 H (3), such as the Fmoc strategy on acid-sensitive Fmoc-AA-Wang resin (1), as shown in the scheme below:

[0168] plan

[0169]

[0170] (a) 20% piperidine / DMF; (b) Fmoc-AA-OH, PyBop, DIPEA, DMF; (c) Fmoc-Glu(O- t -Bu)-OH, PyBop, DIPEA, DMF; (d) 1. N 10 (TFA)-Pte-OH; PyBop, DIPEA, DMSO; (e) TFAA, (CH 2 SH) 2 , i -Pr 3 SiH; (f) NH 4 OH, pH 10.3.

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Abstract

Described herein are drug delivery conjugates for targeted therapy. In particular, described herein are drug delivery conjugates that include polyvalent linkers comprising one or more unnatural amino acids that are useful for treating cancers and inflammatory diseases. In some embodiments, the cancer is selected from the group consisting of a carcinoma, a sarcoma, a lymphoma, Hodgekin's disease, a melanoma, a mesothelioma, Burkitfs lymphoma, a nasopharyngeal carcinoma, a leukemia, and a myeloma.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. § 119(e) of U.S. Provisional Application Serial No. 61 / 979,344, filed April 14, 2014, and U.S. Provisional Application Serial No. 62 / 057,473, filed September 30, 2014, The disclosures of both of said applications are expressly incorporated herein by reference. technical field [0003] The invention described herein relates to drug delivery conjugates for the treatment of drug resistant cancers. Furthermore, the invention described herein pertains to drug delivery conjugates that enhance the efficacy of other anticancer agents. [0004] Background of the invention [0005] The mammalian immune system provides means for recognizing and eliminating pathogenic cells (eg, tumor cells) and other invading foreign pathogens. While the immune system usually provides a strong line of defense, there are many instances where pathogenic cells (eg, cancer cells) and other infectious ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K33/243
CPCA61K47/551A61K47/64A61K31/282A61K31/337A61K31/357A61K31/4745A61K31/704A61P35/00A61P35/02A61P43/00A61K33/243A61K39/3955A61K2039/505C07K16/22C07K2317/24
Inventor I.R.弗拉霍夫C.P.利蒙J.A.雷迪
Owner ENDOCTYE INC
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