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41 results about "Anagrelide" patented technology
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Anagrelide is used to treat a certain blood disorder (thrombocythemia), which is caused by your bone marrow making too many platelets.
Controlled release compositions of agents that reduce circulating levels of platelets and methods therefor
InactiveUS20090324710A1Reducing circulating platelet numberReduce circulating platelet countOrganic active ingredientsBiocideControlled releaseNormal level
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.
Owner:BIOVASCULAR INC
Oral enteric preparation containing Grel drugs and aspirin
The invention relates to a novel oral enteric preparation which is composed of 0.1-1000mg of Grel drugs, or medically acceptable salts, ester or derivatives, 37.5-325mg of aspirin and at least one medically acceptable load, wherein the Grel drugs, or medically acceptable salts, esters or derivatives are clopidogrel, prasugrel, brilinta, sarpogrelate, ozagrel, anagrelide, pamicogrel, or medically acceptable salts, ester or derivatives, preferably, clopidogrel sulfate. The oral enteric preparation is used for curing acute coronary syndrome (ACS), angor pectoris, stroke, myocardial infarction or cardia cerebrovascular diseases of patients. According to the oral enteric preparation, adverse reactions such as functional gastrointestinal disorders, nausea, vomit, gastritis, concealed hemorrhage, ulcer exacerbation and gastrointestinal bleeding caused by strong stimulus of aspirin to stomach can be avoided.
Owner:王定豪
Substituted quinazolines
InactiveUS20110130413A1Promote absorptionImproved pharmacokinetic profileOrganic active ingredientsBiocideSide effectPatient compliance
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.
Owner:SHIRE PLC
Methods and compositions for treating platelet-related disorders
InactiveUS20080113024A1Inhibiting development and progression and propagationReduce morbidityBiocideSenses disorderNormal levelPharmaceutical formulation
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 to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.
Owner:BIOVASCULAR INC
Controlled release compositions of agents that reduce circulating levels of platelets and methods therefor
InactiveUS9040483B2Reduce interactionReduce the numberOrganic active ingredientsSenses disorderControl releaseNormal level
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.
Owner:BIOVASCULAR INC
Imidazoquinazoline derivatives as anagrelide analogues for the treatment of myeloprolific diseases and thrombotic diseases
InactiveUS20110071173A1Improve pharmacokineticsSide effect profileOrganic active ingredientsBiocideDiseaseSide effect
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.
Owner:SHIRE PLC
Substituted quinazolines
InactiveUS20110065735A1Good water solubilityReduce cardiotoxicityBiocideOrganic active ingredientsSide effectPatient compliance
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.
Owner:SHIRE PLC
Process for the preparation of ethyl-N-(2,3-dichloro-6-nitrobenzyl)glycine hydrochloride
InactiveUS8133996B2Shorten the counting processBiocideHydroxy compound active ingredientsHydrogenLeaving group
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.
Owner:CIPLA LTD
Substituted quinazolines
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.
Owner:SHIRE PLC
Substituted quinazolines
InactiveUS20110071174A1Improve pharmacokineticsSide effect profileBiocideOrganic chemistrySide effectPatient compliance
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.
Owner:SHIRE PLC
Imidazoquinazoline derivatives as anagrelide analogues for the treatment of myeloprolific diseases and thrombotic diseases
InactiveCN102076695AHas antimegakaryocyte activityOrganic active ingredientsOrganic chemistryDiseasePatient compliance
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.
Owner:SHIRE PLC
Substituted quinazolines and their uses for myeoloprolific and thrombotic diseases
InactiveUS20110086851A1Improve pharmacokineticsSide effect profileBiocideOrganic active ingredientsSide effectPatient compliance
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.
Owner:SHIRE PLC
Substituted quinazolines as blood platelet lowering agents
InactiveUS20110071172A1Improve pharmacokineticsSide effect profileOrganic active ingredientsBiocideSide effectMedicine
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 (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.
Owner:SHIRE PLC
2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents
InactiveUS20110071171A1Improve pharmacokineticsSide effect profileBiocideOrganic active ingredientsSide effectPatient compliance
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.
![2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9f8352e0-0781-4012-9992-4d2a782a3d08/US20110071171A1-20110324-C00001.png "2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents")
![2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9f8352e0-0781-4012-9992-4d2a782a3d08/US20110071171A1-20110324-C00002.png "2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents")
![2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9f8352e0-0781-4012-9992-4d2a782a3d08/US20110071171A1-20110324-C00003.png "2h- pyrimido [2, 1-b] quinazolin-2-one derivatives and their use as platelet Anti-aggregative agents")
Owner:SHIRE PLC
Substituted quinazolines
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 toimproved 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.
Owner:SHIRE PLC
Substituted quinazolines
InactiveUS20100137343A1Improve pharmacokineticsEnhance the imageOrganic active ingredientsBiocideSide effectPatient compliance
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.
Owner:SHIRE PLC
Preparation method of anagrelide derivative
InactiveCN107722017AImprove protectionReasonable process designOrganic chemistryThrombocytosisProcess design
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.
Owner:TLC NANJING PHARMA RANDD CO LTD
Substituted quinazolines
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.
Owner:SHIRE PLC
Substituted quinazolines for reducing platelet count
ActiveUS8304420B2Reduce cardiotoxicityOrganic active ingredientsBiocideReduced platelet countSide effect
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.
Owner:SHIRE PLC
Substituted quinazolines
ActiveUS20080176875A1Promote absorptionImproved pharmacokinetic profileOrganic active ingredientsBiocideSide effectPatient compliance
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.
Owner:SHIRE PLC
Substituted quinazolines as blood platelet lowering agents
InactiveCN102076687AHas antimegakaryocyte activityOrganic active ingredientsOrganic chemistrySide effectMedicine
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.
Owner:SHIRE PLC
Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents
InactiveCN102066379ADecreased platelet countOrganic active ingredientsOrganic chemistrySide effectPatient compliance
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.
![Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/d7a2d029-1aed-43a0-aa0d-e995e1beb30a/DPA00001278965800011.png "Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents")
![Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/d7a2d029-1aed-43a0-aa0d-e995e1beb30a/FPA00001278965900011.png "Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents")
![Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/d7a2d029-1aed-43a0-aa0d-e995e1beb30a/FPA00001278965900021.png "Imidazo [2,1-b] quinazolin-2-one derivatives and their use as platelet anti-aggregative agents")
Owner:SHIRE PLC
Use of anagrelide for treating cancer
ActiveUS20170360793A1Reducing any chemotactic responsePotential for metastasisOrganic active ingredientsDigestive systemDiseaseThrombocytosis
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.
Owner:AROVELLA THERAPEUTICS LTD
A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one
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.
![A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/19f29466-6a52-4d32-8b4d-1fc566486c27/BDA0000514525400000021.png "A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one")
![A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/19f29466-6a52-4d32-8b4d-1fc566486c27/BDA0000514525400000022.png "A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one")
![A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/19f29466-6a52-4d32-8b4d-1fc566486c27/BDA0000514525400000031.png "A method for preparing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-(3h)-one")
Owner:SHANGHAI TIANCI INT PHARMA
Anti-tumor use of anagrelide and derivatives thereof
InactiveUS20170143717A1Disturb proliferationGood effectOrganic active ingredientsCell culture active agentsCancer researchAnagrelide
The present invention provides an anti-tumor use of Anagrelide and derivatives thereof and, more specifically, the present invention provides the use of Anagrelide and derivatives thereof in the preparation of pharmaceuticals or pharmaceutical compositions for the treatment or inhibition of tumors.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Substituted quinazolines
Owner:SHIRE PLC
Applications of phosphodiesterase PDE3A in determination of tumor treatment effect of Anagrelide
InactiveCN107312824AMicrobiological testing/measurementDisease diagnosisPhosphodiesteraseTherapeutic effect
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.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Application of pde3a in judgment of tumor treatment effect of anagrelid
InactiveUS20190145978A1Microbiological testing/measurementDisease diagnosisPhosphodiesteraseTherapeutic effect
Application of a phosphodiesterase PDE3A and genes thereof in judgment of a tumor treatment effect of Anagrelide. Specifically provided is usage of a PDE3A gene sequence, protein, or anti-PDE3A protein specific antibody in preparation of a diagnostic reagent or a diagnostic kit. The diagnostic reagent or kit is used for (a) judging a tumor treatment effect of Anagrelide, and / or (b) judging whether Anagrelide is appropriate for treating a tumor patient. Also provided is a corresponding detection kit.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Use of anagrelide for treating cancer
ActiveUS11324746B2Prevent attractionReduced responseOrganic active ingredientsDigestive systemDiseaseThrombocytosis
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.
Owner:AROVELLA THERAPEUTICS LTD
A kind of synthetic method of anagrelide key intermediate, analog or its salt
ActiveCN103333078BFew reaction stepsEasy to operateOrganic compound preparationAmino-carboxyl compound preparationTiclopidineGlycine
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.
Owner:SHANGHAI PUKANG PHARMA
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