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Plural diazine rings

Subclass of:

544 - Organic compounds -- part of the class 532-570 series

544000000 - ORGANIC COMPOUNDS (CLASS 532, SUBCLASS 1)

544000000 - HETEROCYCLIC CARBON COMPOUNDS CONTAINING A HETERO RING HAVING CHALCOGEN (I.E., OXYGEN, SULFUR, SELENIUM, OR TELLURIUM) OR NITROGEN AS THE ONLY RING HETERO ATOMS (Class 540, subclass 1)

544001000 - Hetero ring is six-membered having two or more ring hetero atoms of which at least one is nitrogen (e.g., selenazines, etc.)

544224000 - The six-membered hetero ring consists of two nitrogens and four carbons (e.g., 1,2-diazines, etc.)

544242000 - 1,3-diazines

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
544295000 Plural diazine rings 68
20080242862Novel imidazo based heterocycles - The present invention is directed to novel imidazopyrazine compounds useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.10-02-2008
20080249305Novel imidazole based heterocycles - The present invention is directed to novel imidazopyrazine compounds useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.10-09-2008
20090012296Processes for the preparation of crystalline form beta of imatinib mesylate - Provided is a process for the preparation of crystalline form β of Imatinib mesylate.01-08-2009
20090030203PREPARATION OF 2-AMINO-THIAZOLE-5-CARBOXYLIC-ACID DERIVATIVES - A method for preparing a compound of the structure I,01-29-2009
20090149650PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula,06-11-2009
20090203906NOVEL AMINODICARBOXYLIC ACID DERIVATIVES HAVING PHARMACEUTICAL PROPERTIES - The invention relates to compounds of formulae (II), (IV), and (VI) as shown below,08-13-2009
20090299064METHODS AND INTERMEDIATES FOR THE PREPARATION OF OPTIONALLY RADIO-LABELED IMATINIB - The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I,12-03-2009
20090312546QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS - Disclosed are methods for the preparation of compounds of formula (I):12-17-2009
20100029939PREPARATION OF KETONE AMIDES - The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.02-04-2010
20100063280PROCESS FOR PREPARING CCR-5 RECEPTOR ANTAGONISTS UTILIZING 4-SUBSTITUTED 1-CYCLOPROPANE-SULFONYL-PIPERIDINYL COMPOUNDS - The present invention discloses a novel process to prepare 4-substituted 1-Cyclopropane-sulfonyl-Piperidinyl compounds, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine] compounds.03-11-2010
20100121057Process for the Preparation of Piperazine Benzothiazoles - The present invention discloses a process for the preparation of compounds of formula (I)05-13-2010
20100152445Inhibitors of Diacylglycerol Acyltransferase - Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.06-17-2010
20100317853NOVEL IMATINIB CAMSYLATE AND METHOD FOR PREPARING THEREOF - The present invention relates to a novel imatinib camsylate and a method for preparing the same. Imatinib camsylate according to the present invention has a faster absorption rate and higher absorption concentration in terms of pharmacokinetics, and further has excellent water solubility, as compared to commercially available imatinib mesylate.12-16-2010
20100317854NOVEL AMINODICARBOXYLIC ACID DERIVATIVES HAVING PHARMACEUTICAL PROPERTIES - The invention relates to compounds of formulae (II), (IV), and (VI) as shown below,12-16-2010
20110003991PIPERAZINE DERIVATIVES AND THEIR USE IN CONTROLLING PESTS - The use of a compound of formula I01-06-2011
20110275810CARBAMIC ACID COMPOUNDS COMPRISING A PIPERAZINE LINKAGE AS HDAC INHIBITORS - This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula:11-10-2011
20110306763PROCESS FOR THE PREPARATION OF IMATINIB AND SALTS THEREOF - Disclosed herein is a process for preparation of imatinib free base which comprises condensing 4-Methyl-N-(4-pyridin-3-yl-pyrimidin-2-yl)-benzene-1,3-diamine with 4-(4-Methyl-piperazin-1-ylmethyl)-benzoic acid ester in the presence of base including organic bases and inorganic bases in an organic solvent to form imatinib.12-15-2011
20120046463Process for the Preparation of Imatinib Base - Provided is an environmentally-friendly process for preparing imatinib base in high yield, without the use of an organic solvent.02-23-2012
20120149903PROCESS FOR PREPARING AND PURIFYING 3-AMINOPROPANOL - The present invention relates to a process for purifying a reaction output which comprises 3-aminopropanol and is obtained in the reaction of ethylene cyanohydrin with hydrogen in the presence of ammonia, which comprises distilling the reaction output comprising 3-aminopropanol in two or more stages, the ammonia content of the reaction output comprising 3-aminopropanol before introduction into the first distillation stage being 1% by weight or less and the temperature in the distillation stages being not more than 135° C.06-14-2012
20120226038 Crystal Form H of Imatinib Mesylate for Pharmaceutical Use - The invention relates to particular crystal forms of the methanesulfonic acid addition salt of 4-(4-methyl piperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide,09-06-2012
20120226039N-Phenyl-2-pyrimidine-amine Derivatives - The present invention relates to novel amides and a process for preparing these amides.09-06-2012
20120302750PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula,11-29-2012
20120309968POLYMORPHS OF DASATINIB, PREPARATION METHODS AND PHARMACEUTICAL COMPOSITIONS THEREOF - Polymorph I of dasatinib monohydrate and Polymorph II of dasatinib, their preparation methods and pharmaceutical compositions containing the same are provided. These polymorphs have better physicochemical properties, are more stable and are more suitable for industrial scale production.12-06-2012
20120316338Methods and Intermediates for the Preparation of Optionally Radio-Labeled Imatinib - The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I,12-13-2012
20120330014METHOD FOR PRODUCING IMATINIB BASE - The present invention relates to a novel method for preparing an imatinib base, and more particularly to a method for preparing an imatinib base, which comprises reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2′-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. In addition, the invention provides a novel thioester compound, which is used in the preparation of imatinib base, and a preparation method thereof. Ultimately, the invention provides a method of preparing the imatinib base in an economic manner and in high yield and purity and is expected to be used in the commercial production of large amounts of the imatinib base.12-27-2012
20130030177SYNTHESIS PROCESS OF DASATINIB AND INTERMEDIATE THEREOF - Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.01-31-2013
20130041149New Method for Synthesizing Imatinib - In the present invention, a synthesis method of Imatinib is disclosed, which comprises the following steps: the Imatinib, namely 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-[4-(3-pyridinyl)-pyrimidin-2-ylamino]-benzamide shown in formula (III), is formed by reacting 4-methyl-N-3-(4-pyridin-3-yl-pyrimidin-2-yl)-1,3-benzenediamine shown in formula (I) with 4-(4-methyl-piperazin-1-methyl)-benzoic ester shown in formula (II), under the action of a base and in a non-protonic organic solvent,02-14-2013
20130060030PROCESS FOR THE PREPARATION OF HIGHLY PURE CRYSTALLINE IMATINIB BASE - A process for the preparation of highly pure crystalline imatinib base form- N of Formula (I) is disclosed. Imatinib base of this invention is suitable for conversion to pharmaceutically acceptable salts.03-07-2013
20130144059USE OF PDGF-R INHIBITORS FOR THE TREATMENT OF LYMPH NODE METASTASIS OF GASTRIC CANCER - The present invention relates to the use of PDGF-R inhibitors for the treatment of lymph node metastasis of gastric cancers and to a method of treating mammals including humans suffering from gastric cancer.06-06-2013
20130203990PROCESS FOR THE PREPARATION OF IMATINIB MESYLATE - The present application relates to process for the preparation of imatinib mesylate. This application also relates to the processes for preparation of alpha crystalline form of imatinib mesylate.08-08-2013
20130245258Preparation Method of alpha-imatinib Mesylate - Disclosed is a preparation method of α-imatinib mesylate. The reaction temperature of the method is low and the yield of the crystal is improved. Furthermore, the method is applicable to the industrial production.09-19-2013
20130324725AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.12-05-2013
20130324726METHOD FOR PRODUCING IMATINIB BASE - A method for preparing an imatinib base includes reacting 4-(4-methyl-piperazinomethyl)-benzoic acid with a 2,2′-dibenzothiazolyl disulfide derivative in the presence of a phosphine derivative to prepare a novel thioester compound and preparing an imatinib base using the thioester compound as a reaction intermediate. With the method, imatinib base in higher yield and/or purity can be prepared cost-effectively.12-05-2013
20140051853Salt forms of 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-- 2-ylamino)phenyl]-benzamide - The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.02-20-2014
20140221652IMPROVED PROCESS FOR PREPARATION OF IMATINIB AND ITS MESYLATE SALT - Disclosed is a process for the preparation of imatinib of formula (I), or its mesylate salt with controlled level of genotoxic impurity of formula (II), a key intermediate for imatinib.08-07-2014
20140350249THERAPEUTIC AGENT FOR CEREBRAL INFARCTION - The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-α, IL-1β, IL-6 and MCP-1 and the like.11-27-2014
20140350250THERAPEUTIC AGENT FOR CEREBRAL INFARCTION - The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-α, IL-1β, IL-6 and MCP-1 and the like.11-27-2014
20150018552N-Phenyl-2-pyrimidine-amine Derivatives - The present invention relates to novel amides and a process for preparing these amides.01-15-2015
20150057446PROCESS FOR PREPARING DASATINIB MONOHYDRATE - The present invention provides an improved process for preparing N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole carboxamide monohydrate or Dasatinib monohydrate (Formula A).02-26-2015
20150299164PROCESS FOR PREPARING IMATINIB AND SALTS THEREOF, FREE OF GENOTOXIC IMPURITY F - The invention relates to an improved process for the preparation of Imatinib and salts thereof, in particular Imatinib Mesylate, having a content of a particular genotoxic impurity, named impurity F, within the pharmacopeia limits.10-22-2015
20150336913PROCESS FOR THE PREPARATION OF DASATINIB AND ITS INTERMEDIATES - The present invention relates to processes for the preparation of dasatinib and its intermediates.11-26-2015
20160074399Salts of an Epidermal Growth Factor Receptor Kinase Inhibitor - The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same. Examples include hydrobromide and bis-besylate salts of N-(3-(2-(4-(4-acerylpiperazin-1-yl)-2-methoxyphenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)phenyl)acrylamide). The salts and their polymorphs are evaluated for their properties such as stability, solubility, and pharmacokinetics.03-17-2016
544296000 Plural 1,3-diazine rings 26
20080293940Amide Derivative and Medicine - The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof.11-27-2008
20090156811Process for the Preparation of Bosentan - A process for the preparation of 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-[2,2′]bipyrimidinyl-4-yl]-benzenesulfonamide, bosentan, comprising the reaction of a compound of formula (II) or a salt thereof,06-18-2009
20100184978BIPYRIDINE COMPOUND, TRANSITION METAL COMPLEX, AND METHOD FOR PRODUCTION OF CONJUGATED AROMATIC COMPOUND USING THE TRANSITION METAL COMPLEX - A bipyridine compound represented by the formula (1):07-22-2010
20110015394Method of Synthesis of Bosentan, Its Polymorphic Forms and Its Salts - The present invention relates to alkaline earth metal salts of bosentan, anyhdrous bosentan, polymorphic forms thereof, amorphous bosentan and processes for preparing them. The present invention further relates to a process for the preparation of bosentan and its pharmaceutically acceptable salts.01-20-2011
20110263853HPLC METHOD FOR THE ANALYSIS OF BOSETAN AND RELATED SUBSTANCES AND USE OF THESE SUBSTANCES AS REFERENCE STANDARDS AND MARKERS - The present invention relates to a new HPLC method for the analysis of the drug substance bosentan and related substances and to the use of said substances as reference standards and markers.10-27-2011
20120041200PROCESS FOR THE PREPARATION OF BOSENTAN - The invention concerns a new process for the preparation of bosentan or bosentan monohydrate by reaction of compound of Formula II with ethylene glycol in the presence of potassium bases and the potassium salt of bosentan.02-16-2012
20120130073INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.05-24-2012
20120149904BISPYRIMIDINES FOR ELECTRONIC APPLICATIONS - The present invention relates to compounds of formula06-14-2012
20120165528CHIRAL BINAPHTHYL COMPOUNDS - The present invention relates to chiral binaphthyl compounds having good solubility and high helical twisting power. The chiral binaphthyl compounds as dopants in the liquid crystal compositions can help enhance the display quality of the liquid crystal panels.06-28-2012
20120232270HETEROAROMATIC PHTHALONITRILES - Disclosed are an oligomer and a phthalonitrile monomer having the formulas:09-13-2012
20120283440CRYSTALLINE FORMS OF BOSENTAN SALTS AND PROCESSES FOR THEIR PREPARATION - The present invention relates to crystalline forms of bosentan salts and processes for their preparation.(FORMULA)11-08-2012
20130079517Electroluminescent Device - Disclosed are electroluminescent devices that comprise organic layers that contain certain organic compounds containing one or more pyrimidine moieties. The organic compounds containing one or more pyrimidine moieties are suitable components of blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in for example mobile phones, televisions and personal computer screens.03-28-2013
20130245259PROCESS FOR THE PREPARATION OF BOSENTAN MONOHYDRATE - The invention relates to improved processes for the preparation of bosentan monohydrate which provide higher yield and purity.09-19-2013
20130253195PROCESS FOR PREPARING BOSENTAN MONOHYDRATE AND ITS INTERMEDIATED - The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.09-26-2013
20130296560Novel Process For Preparation Of Bosentan - A novel ammonium salt of Bosentan of formula (VIII); has been disclosed. The salt may be either crystalline or amorphous or mixture of Crystalline and amorphous form. A novel single pot process for the preparations of ammonium salt of Bosentan has been disclosed. The process comprises reacting the 4,6-dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine with 4-tert-butylbenzenesulfonamide in the presence of solvent and a base; adding ethylene glycol to the reaction mass and isolating the ammonium salt of Bosentan. The ammonium salt of Bosentan is converted into Bosentan and further into Bosentan Monohydrate which are substantially free from dimer impurity and 6-hydroxy impurity.11-07-2013
20130303762PROCESS FOR PREPARING BOSENTAN - The present invention relates to an improved process for preparing Bosentan of formula (I).11-14-2013
20130324727ANTI-FOLATE ANTIMALARIALS WITH DUAL-BINDING MODES AND THEIR PREPARATION - The present invention is anti-folate antimalarials with dual-binding modes of the general formula (I) [refer to structure in the abstract] wherein R12-05-2013
20140018536AROMATIC AMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME - An aromatic amine derivative represented by the following formula (1), wherein at least one of Ar01-16-2014
20140039187CXCR4 ANTAGONISTS FOR THE TREATMENT OF MEDICAL DISORDERS - The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis.02-06-2014
20140073788Preparation of Polymer Conjugates of Therapeutic, Agricultural, and Food Additive Compounds - Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions.03-13-2014
20140142308PHOTOELECTRIC MATERIALS AND PREPARATION THEREOF - Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials.05-22-2014
20140275535ACID ADDITION SALTS OF BOSENTAN - The present invention relates to the stable acid addition salts of Bosentan that are useful for the purification of Bosentan base. In particular, the Bosentan acid addition salt is selected from Bosentan citrate and Bosentan tartrate.09-18-2014
20160002174CXCR4 Antagonists for the Treatment of Medical Disorders - The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis.01-07-2016
20160009694CYCLOHEXANEDIAMINE COMPOUNDS AND METHODS FOR THEIR PREPARATION01-14-2016
20160052891PREPARATION OF PYRIMIDINE INTERMEDIATES USEFUL FOR THE MANUFACTURE OF MACITENTAN - The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 I or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare the compound of formula I-3 I which is an important synthetic intermediate used in the preparation of macitentan.02-25-2016
20160075693AVANAFIL PREPARATION METHOD - Disclosed is a method for preparing avanafil (I) by using cytosine as the starting material. The preparation steps comprise: using cytosine as the raw material, and enabling the cytosine to react with side chain 3-chlorine-4-methoxybenzyl halogen, N-(2-methylpyrimidine) methanamide and S-hydroxymethyl pyrrolidine, to prepare the target product avanafil (I). For the preparation method, the raw material is easily obtained, and the process is simple, economical, and environmentally friendly, so the method meets the requirement of industrial boost.03-17-2016

Patent applications in class Plural diazine rings

Patent applications in all subclasses Plural diazine rings

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