41 results about "Anagrelide" patented technology

Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V):where R constitutes a suitable leaving group, which may not be hydrogen. The R group may be selected from: (i) —SiR13, (ii) —CH2Ar, (iii) —COOR2, and (iv) sulfonates such as —SO2R3.

This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.

This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1, and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

The invention discloses a preparation method of an anagrelide derivative, and belongs to the field of pharmaceutical synthesis. The method is reasonable in process design, high in operability, relatively mild in reaction condition and high in yield, and can realize industrial production. According to the preparation method of the anagrelide derivative, synthesis of the anagrelide derivative is realized by taking 1,2,3,4-tetrachlorobenzene as a raw material through six-step reaction. The anagrelide derivative prepared through the preparation method provides an important basis for scientific evaluation of the quality, the safety and the efficacy of anagrelide; furthermore, the anagrelide derivative is high in pharmacological activity, can be prepared into drugs for treating thrombocytosis caused by various reasons, and has an important application value.

This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets. An example of a compound of the present invention is methyl 2-(2-amino-5,6- dichloroquinazolin-3 (4H)-yl)-2-methylpropanoate or the 3,3-demethyl anagrelide open-ringed analog.

This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below where the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

The invention provides a novel method for preparing 6,7-dichloro-1,5-imidazolinyl [2,1-b] quinazoline-2-(3H)-one. The method comprises the following steps: preparing a compound with the structure shown as the formula (IV), and then preparing anagrelide by taking the compound shown as the formula (IV) as an intermediate. The method has the advantages of being simple to operate, moderate in reaction condition, low in overall cost, high in yield, high in anagrelide purity and the like. Thus, the method is suitable for industrial production.

The present invention relates to 3- and 5-substituted analogs of the selective platelet lowering agent anagrelide, which have the potential to reduce cardiovascular side effects and lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More particularly, the present invention relates to certain imidazoquinazoline derivatives that have utility as platelet lowering agents in humans. The compounds of the present invention act by inhibiting megakaryocytopoiesis and thereby inhibiting platelet formation.

The present invention relates to applications of phosphodiesterase PDE3A and a gene thereof in determination of the tumor treatment effect of Anagrelide, and specifically provides use of a PDE3A gene sequence, a protein, or a specific antibody against PDE3A protein in preparation of a diagnostic reagent or a diagnostic kit, wherein the diagnostic reagent or kit is used for (a) determining the tumor treatment effect of anagrelide, and / or (b) determine whether tumor patients can be treated with anagrelide. The invention further provides a corresponding test kit.

The present invention relates to the use of the anti-megakaryocytic agent anagrelide, or a therapeutically active metabolite thereof, in the prevention or treatment of metastatic disease in cancer patients displaying paraneoplastic thrombocytosis.

The invention provides a synthesis method for a key intermediate, analogue or salt of ticlopidine. The synthesis method comprises the following steps of: (1) adding 6-nitro-2,3-dichlorobenzaldehyde and glycine or corresponding substituted glycine into a solution and adding a reducing agent to completely react to obtain N-(6-nitro-2,3-dichlorobenzyl) glycine and an analogue thereof; and (2) completely reacting the N-(6-nitro-2,3-dichlorobenzyl) glycine and the analogue thereof under the action of a catalyst to obtain the key intermediate, analogue or salt of the ticlopidine, wherein the solution in the step (1) is a mixed solution of a protic solvent and an inorganic base, and the reducing agent is one or a mixture of sodium borohydride, potassium borohydride, lithium borohydride, sodium cyanoborohydride and acetic sodium borohydride. The method is simple in operation, mild and easily-controlled in condition, convenient for aftertreatment, environment-friendly and higher in yield, and is a brand new efficient industrial synthesis method for the key intermediate, analogue or salt of the ticlopidine.