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Inhibitors of cxcr1/2 as adjuvants in the transplant of pancreatic islets

A technology of islet transplantation and inhibitors, applied in medical preparations containing active ingredients, active ingredients of anhydride/acid/halide, allergic diseases, etc.

Inactive Publication Date: 2015-09-16
DOMPE FARM SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Another disadvantage is that the Edmonton protocol requires the use of a combination of immunosuppressive drugs; sirolimus and tacrolimus must be taken for life or as long as the transplanted islets continue to function
However, these drugs have significant side effects, and reducing these side effects is desirable

Method used

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  • Inhibitors of cxcr1/2 as adjuvants in the transplant of pancreatic islets
  • Inhibitors of cxcr1/2 as adjuvants in the transplant of pancreatic islets
  • Inhibitors of cxcr1/2 as adjuvants in the transplant of pancreatic islets

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Embodiment Construction

[0047] As will be described below, the compound of formula I is effective in improving the survival and function of the implant after islet transplantation in animal models.

[0048] In detail, the data obtained in the experimental model of islet transplantation demonstrated that the above compounds (represented by R(-)-2-[(4-isobutylphenyl)propionyl]-methanesulfonamide) were β-cells from loss of activity and / or degeneration of the apparent role.

[0049] According to a preferred embodiment of the present invention, the compound of formula I is Reparixin. According to another preferred embodiment, the compound of formula I is maricin.

[0050] Compounds of the invention effectively support engraftment of transplanted islet cells in type 1 diabetes.

[0051] In fact, as will become clearer from the experimental section below, intravenous administration of Reparixin in animal models from -1 to +6 days of syngeneic or allogeneic islet transplantation elicited up to Median ti...

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Abstract

The invention relates to CXCR1 and CXCR2 inhibitors for the preparation of a medicament for use as an adjuvant in the transplant of pancreatic islets in Type 1 diabetes patients. In particular, the compounds thagt can be used according to the invention have the following formula (I) in which R and R' are as defined in the description.

Description

[0001] This application is a divisional application of the application number 201080045208.5 and the title of the invention is "CXCR1 / 2 inhibitor as an adjuvant in pancreatic islet transplantation". The parent application is the PCT application PCT / EP2010 / 064921 entered the Chinese national phase application. technical field [0002] The present invention relates to compounds useful as adjuvants in islet transplantation in patients with type 1 diabetes. Background technique [0003] Pancreatic tissue transplantation in the form of whole pancreas or isolated islets has become a clinical option for the treatment of type 1 insulin-dependent diabetes. [0004] Islet transplantation is particularly attractive because it is less invasive and associated with a lower risk of serious complications than whole pancreas transplantation; however, this approach is still limited by low efficiency. [0005] Early strategies for islet transplantation were based on protocols that had been s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/39A61P37/06
CPCA61K31/18A61P37/00A61P37/06A61P43/00A61P3/10A61K31/185C07C311/51
Inventor 洛伦佐·皮耶蒙蒂路易莎·达丰希奥马尔塞洛·阿莱格雷蒂
Owner DOMPE FARM SPA
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