| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544278000 | Three ring hetero atoms in the bicyclo ring system | 37 |
| 20090326224 | THIENO PYRIMIDINE COMPOUNDS - A compound for treating cancer tumors, particularly ovarian cancer tumors, is described, where a fused cyclic pyrimidine having a cancer treating ability is effective to allow selective delivery to a cancerous tumor. | 12-31-2009 |
| 20100222585 | PREPARATION OF DIHYDROTHIENO [3, 2-D] PYRIMIDINES AND INTERMEDIATES USED THEREIN - The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO | 09-02-2010 |
| 20110130563 | SYNTHESIS IF DIHYDROTHIENO[3,2-D]PYRIMIDINE DIOLS - The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers. | 06-02-2011 |
| 20080234482 | 5,6-Dimethylthieno[2,3-Di] Pyrimidine Derivatives, the Preparation Method Thereof and the Pharmaceutical Composition Comprising the Same for Anti-Virus - Disclosed herein are 5,β-dimethylthieno[2,3-d]pyrimidine derivatives useful as antiviral agents. More particularly, disclosed are 5,β-dimethylthieno[2,3-djpyrimidine derivatives represented by Formula 1, having an excellent inhibitory effect on the proliferation of hepatitis C virus (HCV), pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the prevention and treatment of hepatitis C virus (HCV), containing, as active ingredients, these compounds. The 5,6-dimethylthieno[2,3-d]pyrimidine derivatives represented by Formula 1 have an excellent effect of inhibiting the proliferation of hepatitis C virus and also have low toxicity. Thus, these compounds are available as agents for the prevention and treatment of hepatitis C. | 09-25-2008 |
| 544279000 | Three ring nitrogens in the bicyclo ring system | 33 |
| 20100125138 | PROCESS FOR MAKING (R)-3-(2,3-DIHYDROXYPROPYL)-6-FLUORO-5-(2-FLOURO-4-IODOPHENYLAMINO)-8-MET- HYLPYRIDO[2,3-d]PYRIMIDINE-4,7(3H,8H)-DIONE AND INTERMEDIATES THEREOF - The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione. | 05-20-2010 |
| 20090281314 | METHOD FOR PRODUCING BICYCLIC GUANIDINES BY USE OF A CYCLIC UREA AND A DEHYDRATING AGENT - The present invention is directed to a method for producing bicyclic guanidines comprising heating a reaction mixture comprising cyclic urea and a dehydrating agent to a temperature ≧90° C. | 11-12-2009 |
| 20090209757 | Processes for the preparation and purification of paliperidone palmitate - The present invention encompasses processes for the preparation and purification of paliperidone palmitate. | 08-20-2009 |
| 20090281313 | METHOD FOR PRODUCING BICYCLIC GUANIDINES BY USE OF A CYCLIC UREA - The present invention is directed to a method for producing bicyclic guanidines comprising heating a cyclic urea to a temperature >200° C. to form the bicyclic guanidines. | 11-12-2009 |
| 20100069632 | SALTS OF PYRROLOPYRIMIDINONE DERIVATIVES AND PROCESS FOR PREPARING THE SAME - The present invention relates to salts of a pyrrolopyrimidinone derivative having superior PDE-5 inhibition activity and a process for preparing the same. More particularly, the present invention relates to a crystalline acid addition salt prepared by reacting a pyrrolopyrimidinone derivative with an acid selected from gentisic acid, maleic acid, citric acid, fumaric acid and tartaric acid. With no hygroscopic property and superior long-term storage stability, photostability and thermal stability, the salts of the pyrrolopyrimidinone derivative are appropriate to be prepared into medications and, with superior PDE-5 inhibition activity, are useful for the treatment and prevention of erectile dysfunction, pulmonary arterial hypertension, chronic obstructive pulmonary disease, benign prostatic hypertrophy and lower urinary tract diseases. | 03-18-2010 |
| 20120202999 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 08-09-2012 |
| 20100274013 | DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS ACTIVE AGENT - Disclosed herein are novel compounds of Formula (1) as defined in the specification having excellent inhibitory activity against dipeptidyl peptidase-IV (DPP-IV), methods of preparing the same and pharmaceutical compositions comprising the same as an active agent. | 10-28-2010 |
| 20120220770 | PREPARATION OF BICYCLIC GUANIDINE SALTS IN AN AQUEOUS MEDIA - Disclosed herein are bicyclic guanidine salts formed as the reaction product of reactants comprising (a) a compound having the general formula CX | 08-30-2012 |
| 20080221322 | CHEMICAL PROCESS - The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline. | 09-11-2008 |
| 544280000 | The other cyclo in the bicyclo ring system is five-membered | 24 |
| 20110196154 | AMORPHOUS PEMETREXED DISODIUM - Processes for the preparation of amorphous pemetrexed disodium, and removal of residual solvents from amorphous pemetrexed disodium. | 08-11-2011 |
| 20110196155 | CRYSTALLINE FORMS OF PEMETREXED DIACID AND PROCESSES FOR THE PREPARATION THEREOF - Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof. | 08-11-2011 |
| 20090124802 | Diaryl-purines, azapurines and -deazapurines as non-nucleoside reverse transcriptase inhibitor for treatment of hiv - This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment. | 05-14-2009 |
| 20120165526 | Useful Pharmaceutical Salts of 7- [(3R, 4R) - 3 - Hydroxy -4 - Hydroxymethyl - Pyrrolidin -1- Ylmethyl] -3, 5-Dihydro-Pyrrolo [3, 2-D] Pyrimidin -4-One - The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-d]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties. | 06-28-2012 |
| 20110282057 | AZA-INDOLES AND RELATED COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY - The present invention provides compounds are disclosed herein having the formula: | 11-17-2011 |
| 20090012294 | Highly pure pemetrexed Diacid and processes for the preparation thereof - Provided are highly pure pemetrexed diacid and pharmaceutically acceptable salts thereof, and processes for their preparation. | 01-08-2009 |
| 20110288297 | Pyrrolo[2,3-d]Pyrimidine Derivatives; Their Intermediates and Synthesis - This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin- | 11-24-2011 |
| 20100305319 | METHOD OF PURIFYING A SALT, SODIUM SALT AND DISODIUM SALT OF PEMETREXED - A method of purifying a salt of pemetrexed have a structure of formula (III) by salting-out, wherein if M | 12-02-2010 |
| 20110172424 | NEW CRYSTALLINE FORMS OF PEMETREXED DIACID, AND PREPARATIONS THEREOF - Three new crystalline forms of pemetrexed diacid, preparation methods and uses thereof are disclosed. These preparation processes are simple and have better practicality. | 07-14-2011 |
| 20090036678 | Process for the synthesis of E1 activating enzyme inhibitors - The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1S,2S,4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. | 02-05-2009 |
| 20090247750 | PROCESS FOR PREPARING NUCLEOSIDE ANALOGS - The invention provides an improved method for preparing a compound of formula 2: | 10-01-2009 |
| 20120245349 | Process for the production of a pemetrexed salt - A process of making a pemetrexed salt comprising:
| 09-27-2012 |
| 20110124862 | PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH A CYCLIC AMINO GROUP AS CRF ANTAGONISTS - [Problem to be Solved] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. | 05-26-2011 |
| 20110124861 | Process for Preparing Pemetrexed Disodium and Its Intermediate, 4-(4-Carbomethoxyphenyl) Butanal - The present invention provides a process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl)butanal. The process for preparing the intermediate comprises the following steps: condensing methyl 4-bromobenzoate with 3-buten-1-ol; extracting with an organic solvent during the work-up; adding silica gel to decolorize; and evaporating the organic solvent to give 4-(4-carbomethoxyphenyl)butanal. The product obtained by the present process, with a yield of higher than 80%, and a purity measured by GC of higher than 95%, may be directly used in the next bromination reaction for synthesizing pemetrexed disodium without purification. The present process is suitable for industrial production, as the operation is simple and the reagents used are cheap and readily available. | 05-26-2011 |
| 20100190981 | PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS - The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. | 07-29-2010 |
| 20110263851 | PROCESSES FOR PREPARING INTERMEDIATES OF PEMETREXED - Provided are processes for preparing intermediates of pemetrexed. | 10-27-2011 |
| 20120172595 | NOVEL PROCESS FOR THE SYNTHESIS OF PEMETREXED DISODIUM SALT - The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 | 07-05-2012 |
| 20120149902 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVE - Provided is a compound represented by the Formula (I) having a HER2 inhibitory action or a pharmacologically acceptable salt thereof, | 06-14-2012 |
| 20100094003 | Process for preparing inhibitors of nucleoside phosphorylases and nucleosidases - The present invention relates to a new process for the preparation of compounds of general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The present invention relates to a new process for the preparation of compounds of general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). | 04-15-2010 |
| 20120226037 | PYRROLO [2,3-D] PYRIMIDINES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS FOR TREATMENT OF HIV - This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment. | 09-06-2012 |
| 20120259115 | PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES: THEIR INTERMEDIATES AND SYNTHESIS - This invention relates to methods and intermediates useful for the synthesis of pyrrolo [2,3-d] pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed. | 10-11-2012 |
| 20110275808 | STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS - A process for stereoselective synthesis of a compound of Formula (I) | 11-10-2011 |
| 20120330013 | PREPARATION METHOD OF MLN4924 AS AN E1 ACTIVATING INHIBITOR - The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cyclopentenone with isopropylidene, regioselective cleavage of isopropylidene moiety, and synthesis of cyclic sulfate. | 12-27-2012 |
| 20080227980 | Preparation of a 7H-Pyrrolo [2,3-D] Pyrimidine Derivative - The present invention provides highly efficient methods for the preparation of {6-[4-(4-ethyl-piperazin-1-ylmethyl)-phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-((R)-1-phenyl-ethyl)-amine (I). | 09-18-2008 |
