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Overview

Tags

Hemic and Lymphatic Diseases

Neoplasms

Other Diseases

Colony-stimulating factors

Biosimilar

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

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Targets

Most frequently developed targets

Disease Domain	Count

Hemic and Lymphatic Diseases	1
Neoplasms	1

Top 5 Drug Type	Count

Colony-stimulating factors	1
Biosimilar	1

Top 5 Target	Count

CSF-3R(Colony stimulating factor 3 receptor)	1

Analogs of the C-nucleoside pyrazofurin were prepared in 7-9 steps using a key Pd(0)-catalyzed coupling reaction between protected iodopyrazoles I (R = Et, X = CO₂Et; R = Me, X = Br) and glycal II to form the glycosyl bond.Conditions for this reaction were improved from those previously described for related reactions in order to maximize product yields and eliminate the need for triphenylarsine.

01 Mar 1997·European Journal of PharmacologyQ3 · MEDICINE

Cardioprotection with a novel adenosine regulating agent mediated by intravascular adenosine

Q3 · MEDICINE

Article

Author: David A. Bullough ; Kevin M. Mullane ; Michael A. Kurz ; Mark A. Young ; Christopher J.L. Buggé

Adenosine is cardioprotective in models of myocardial stunning and infarction, but the precise compartment within the heart in which adenosine elicits its cardioprotective effects has not been determined. The goals of the present study were to (i) investigate the effects of a novel adenosine regulating agent, GP531 (5-amino-1-beta-n-(5-benzylamino-5-deoxyribofuranosyl) imidazole-4-carboxamide), on post-ischemic myocardial function, and (ii) examine the contribution of endogenous adenosine in the intravascular and interstitial compartments in mediating the beneficial effects. Pigs were instrumented for measurement of myocardial segment shortening, and for sampling of coronary venous blood and myocardial interstitial fluid for determination of adenosine concentration. Myocardial dysfunction was induced by 4 x 8 min coronary occlusions, and recovery of regional function was monitored for 2 h. In control pigs, function recovered to 24 +/- 2% of baseline after 2 h. Treatment with GP531 improved functional recovery to 55 +/- 3%. GP531-mediated cardioprotection was prevented by adenosine receptor blockade with 8-sulfophenyltheophylline (23 +/- 2%). GP531 did not affect basal adenosine levels, but caused a 2-fold greater increase in vascular adenosine concentration with ischemia (54.6 +/- 10.6 vs. 28.1 +/- 8.0 microM in controls. P < 0.05). In contrast, the interstitial adenosine concentration was not significantly different in treated vs. untreated control pigs (9.4 +/- 3.9 vs. 15.0 +/- 1.8 microM in controls). These data indicate that (1) GP531 improves recovery of myocardial function following ischemia reperfusion injury via an adenosine receptor-dependent mechanism, and (2) the cardioprotection is associated with increased intravascular, but not interstitial, adenosine concentration during ischemia. Therefore, we conclude that cardioprotection elicited by GP531-enhanced endogenous adenosine is dependent on an intravascular site of action.

100 Deals associated with SICOR, Inc.

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100 Translational Medicine associated with SICOR, Inc.

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Pipeline

Pipeline Snapshot as of 17 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Approved

1

10

Other

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

TBO-Filgrastim ( CSF-3R )	Bone marrow depression More	Approved
AKI-2 ( ADK )	Inflammation More	Discontinued
UK-101 ( LMP2 )	Neoplasms More	Discontinued
AKI-1 ( ADK )	Inflammation More	Discontinued
GP-531 ( AMPK )	Myocardial Ischemia More	Discontinued