| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544295000 | Plural diazine rings | 68 |
| 20080242862 | Novel 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 |
| 20080249305 | Novel 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 |
| 20090012296 | Processes 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 |
| 20090030203 | PREPARATION OF 2-AMINO-THIAZOLE-5-CARBOXYLIC-ACID DERIVATIVES - A method for preparing a compound of the structure I, | 01-29-2009 |
| 20090149650 | PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula, | 06-11-2009 |
| 20090203906 | NOVEL AMINODICARBOXYLIC ACID DERIVATIVES HAVING PHARMACEUTICAL PROPERTIES - The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, | 08-13-2009 |
| 20090299064 | METHODS 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 |
| 20090312546 | QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS - Disclosed are methods for the preparation of compounds of formula (I): | 12-17-2009 |
| 20100029939 | PREPARATION 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 |
| 20100063280 | PROCESS 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 |
| 20100121057 | Process for the Preparation of Piperazine Benzothiazoles - The present invention discloses a process for the preparation of compounds of formula (I) | 05-13-2010 |
| 20100152445 | Inhibitors 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 |
| 20100317853 | NOVEL 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 |
| 20100317854 | NOVEL AMINODICARBOXYLIC ACID DERIVATIVES HAVING PHARMACEUTICAL PROPERTIES - The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, | 12-16-2010 |
| 20110003991 | PIPERAZINE DERIVATIVES AND THEIR USE IN CONTROLLING PESTS - The use of a compound of formula I | 01-06-2011 |
| 20110275810 | CARBAMIC 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 |
| 20110306763 | PROCESS 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 |
| 20120046463 | Process 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 |
| 20120149903 | PROCESS 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 |
| 20120226039 | N-Phenyl-2-pyrimidine-amine Derivatives - The present invention relates to novel amides and a process for preparing these amides. | 09-06-2012 |
| 20120302750 | PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS - The invention relates to processes for preparing compounds having the formula, | 11-29-2012 |
| 20120309968 | POLYMORPHS 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 |
| 20120316338 | Methods 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 |
| 20120330014 | METHOD 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 |
| 20130030177 | SYNTHESIS 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 |
| 20130041149 | New 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 |
| 20130060030 | PROCESS 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 |
| 20130144059 | USE 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 |
| 20130203990 | PROCESS 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 |
| 20130245258 | Preparation 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 |
| 20130324725 | AMINOPYRIMIDINES 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 |
| 20130324726 | METHOD 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 |
| 20140051853 | Salt 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 |
| 20140221652 | IMPROVED 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 |
| 20140350249 | THERAPEUTIC 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 |
| 20140350250 | THERAPEUTIC 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 |
| 20150018552 | N-Phenyl-2-pyrimidine-amine Derivatives - The present invention relates to novel amides and a process for preparing these amides. | 01-15-2015 |
| 20150057446 | PROCESS 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 |
| 20150299164 | PROCESS 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 |
| 20150336913 | PROCESS 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 |
| 20160074399 | Salts 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 |
| 20080293940 | Amide 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 |
| 20090156811 | Process 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 |
| 20100184978 | BIPYRIDINE 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 |
| 20110015394 | Method 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 |
| 20110263853 | HPLC 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 |
| 20120041200 | PROCESS 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 |
| 20120130073 | INHIBITORS 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 |
| 20120149904 | BISPYRIMIDINES FOR ELECTRONIC APPLICATIONS - The present invention relates to compounds of formula | 06-14-2012 |
| 20120165528 | CHIRAL 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 |
| 20120232270 | HETEROAROMATIC PHTHALONITRILES - Disclosed are an oligomer and a phthalonitrile monomer having the formulas: | 09-13-2012 |
| 20120283440 | CRYSTALLINE 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 |
| 20130079517 | Electroluminescent 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 |
| 20130245259 | PROCESS 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 |
| 20130253195 | PROCESS 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 |
| 20130296560 | Novel 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 |
| 20130303762 | PROCESS FOR PREPARING BOSENTAN - The present invention relates to an improved process for preparing Bosentan of formula (I). | 11-14-2013 |
| 20130324727 | ANTI-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 R | 12-05-2013 |
| 20140018536 | AROMATIC AMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME - An aromatic amine derivative represented by the following formula (1), wherein at least one of Ar | 01-16-2014 |
| 20140039187 | CXCR4 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 |
| 20140073788 | Preparation 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 |
| 20140142308 | PHOTOELECTRIC MATERIALS AND PREPARATION THEREOF - Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials. | 05-22-2014 |
| 20140275535 | ACID 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 |
| 20160002174 | CXCR4 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 |
| 20160009694 | CYCLOHEXANEDIAMINE COMPOUNDS AND METHODS FOR THEIR PREPARATION | 01-14-2016 |
| 20160052891 | PREPARATION 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 |
| 20160075693 | AVANAFIL 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 |
